Page last updated: 2024-12-11

icariin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators
FloraRankFlora DefinitionFamilyFamily Definition
EpimediumgenusA plant genus of the family BERBERIDACEAE which is used in DRUGS, CHINESE HERBAL. Members contain flavonol glycosides including epimedins, icariin and noricariin.[MeSH]BerberidaceaeThe Barberry plant family of the order Ranunculales, subclass Magnoliidae, class Magnoliopsida. The shrubs have spiny leaves.[MeSH]

Cross-References

ID SourceID
PubMed CID5318997
CHEMBL ID553204
CHEBI ID78420
SCHEMBL ID312615
MeSH IDM0158708

Synonyms (69)

Synonym
BRD-K65639003-001-02-5
icariin ,
SDCCGMLS-0066754.P001
SPECTRUM4_001975
SPECTRUM5_000933
NCGC00178583-01
BSPBIO_002599
icariine
489-32-7
MLS001424083
MLS000759413
smr000466309
4h-1-benzopyran-4-one, 3-((6-deoxy-alpha-l-mannopyranosyl)oxy)-7-(beta-d-glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-
3-((6-deoxymannopyranosyl)oxy)-7-(glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-4h-1-benzopyran-4-one
KBIOGR_002475
KBIO3_002099
SPBIO_001650
SPECTRUM3_001130
SPECTRUM2_001695
SPECTRUM1505257
HMS2051J13
C17555
CHEMBL553204
epimedii herba icariin
3-[(6-deoxy-alpha-l-mannopyranosyl)oxy]-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-4-oxo-4h-chromen-7-yl beta-d-glucopyranoside
STK801622
bdbm50027363
chebi:78420 ,
5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)-7-[(2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxychromen-4-one
AKOS005614005
A827628
5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-7-(((2s,4s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yl)oxy)-3-(((3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl)oxy)-4h-chromen-4-one
BBL010487
HMS2235I20
CCG-38780
CCG-100955
unii-vnm47r2qsq
vnm47r2qsq ,
ieariline
AB00639912-06
SCHEMBL312615
NC00205
epimedii herba icariin [mi]
4h-1-benzopyran-4-one, 3-((6-deoxy-.alpha.-l-mannopyranosyl)oxy)-7-(.beta.-d-glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-buten-1-yl)-
CS-3675
MLS006011789
AM85785
Q-100549
HY-N0014
mfcd00210516
SR-01000759346-4
sr-01000759346
5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-7-(((2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yl)oxy)-3-(((2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl)oxy)-4h-chromen-4-one
icariin, analytical standard
icariin, >=94% (hplc)
3-[(6-deoxy-alpha-l-mannopyranosyl)oxy]-7-(beta-d-glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-buten-1-yl)-4h-1-benzopyran-4-one
DB12052
5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)-7-((2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yloxy)-3-((2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yloxy)-4h-chromen-4-one
BCP18807
Q5985057
VS-02526
5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-7-{[(2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-3-{[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy}-4h-chromen-4-one
TZJALUIVHRYQQB-XLRXWWTNSA-N
BRD-K65639003-001-05-8
BRD-K65639003-001-09-0
DTXSID00964133
-anhydroicaritin
EX-A6783
5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-7-{[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-3-[(3,4,5-trihydroxy-6-methyloxan-2-yl)oxy]-4h-chromen-4-one

Research Excerpts

Overview

Icariin is a prenylated flavonol glycoside extracted from the medical plant Epimedium. It can inhibit the proliferation and migration of FLSs. Icariin (ICA) is an effective agent to delay bone loss by regulating the bone homeostasis.

ExcerptReferenceRelevance
"Icariin is a prenylated flavonol glycoside extracted from the medical plant Epimedium, which can inhibit the proliferation and migration of FLSs."( Icariin arrests cell cycle progression and induces cell apoptosis through the mitochondrial pathway in human fibroblast-like synoviocytes.
Li, F; Li, S; Liu, B; Meng, Q; Pu, L, 2021
)
2.79
"Icariin (ICA) is a flavonol glycoside that exerts a plethora of pharmacological effects."( Icariin ameliorates metabolic syndrome-induced benign prostatic hyperplasia in rats.
Abdel-Naim, AB; Albadr, NA; Aljehani, AA; Eid, BG; Nasrullah, MZ; Neamatallah, T, 2022
)
2.89
"Icariin (Ica) is a flavonoid isolated from Epimedii Herba (Berberidaceae)."( Icariin Protects H9c2 Rat Cardiomyoblasts from Doxorubicin-Induced Cardiotoxicity: Role of Caveolin-1 Upregulation and Enhanced Autophagic Response.
Bava, I; Bosco, F; Cardamone, A; Cariati, L; Carresi, C; Coppoletta, AR; Foti, DP; Gliozzi, M; Greco, M; Guarnieri, L; Macrì, R; Maiuolo, J; Mollace, R; Mollace, V; Musolino, V; Nucera, S; Palma, E; Ruga, S; Scarano, F; Scicchitano, M; Zito, MC, 2021
)
2.79
"Icariin (ICA) is a traditional Chinese medicine that has been proven to have outstanding protective effects on the vascular system and to regulate cellular autophagy effectively."( Icariin activates autophagy to trigger TGFβ1 upregulation and promote angiogenesis in EA.hy926 human vascular endothelial cells.
Guo, R; Li, X; Shao, L; Sheng, L; Wen, Y; Zhang, Y, 2022
)
2.89
"Icariin is an effective ingredient of the traditional Chinese medicine, Epimedium."( Research progress on icariin, a traditional Chinese medicine extract, in the treatment of asthma.
Dong, YC; Shang, Y; Tong, ZY; Yuan, JY; Zhao, JY, 2022
)
1.76
"Icariin (ICA) is a flavonoid derived from the genus Epimedium, a traditional Chinese herb and a potential therapeutic drug for TBI."( Protective Effects of Icariin on Traumatic Brain Injury.
Cai, R; Du, A; Shi, J; Wu, Q, 2021
)
1.66
"Icariin (ICA) is an effective agent to delay bone loss by regulating the bone homeostasis."( Effects of Icariin on Modulating Gut Microbiota and Regulating Metabolite Alterations to Prevent Bone Loss in Ovariectomized Rat Model.
Han, Y; Li, X; Liu, L; Wang, L; Wang, S; Wang, X; Xu, Y; Yan, H; Ye, H; Zhang, X, 2022
)
1.83
"Icariin (ICA) is a flavonoid extracted from the traditional Chinese medicine Epimedium."( Icariin attenuates ischaemic stroke through suppressing inflammation mediated by endoplasmic reticulum stress signalling pathway in rats.
Liao, Y; Mo, Z; Xu, Y; Zheng, J, 2022
)
2.89
"Icariin is a major bioactive pharmaceutical compound derived from Epimedium plants, which is known due to its anti-inflammatory and antioxidant effects."( Potential effects of icariin, the Epimedium-derived bioactive compound in the treatment of COVID-19: a hypothesis.
Ghasemnejad-Berenji, M; Khezri, MR; Mohammadi, T; Moloodsouri, D; Nazari-Khanamiri, F, 2022
)
1.76
"Icariin is a prenylated flavonol glycoside isolated from Epimedium brevicornum, serving as the main active pharmaceutical constituent to treat bone loss."( Autocrine Activity of Extracellular Vesicles Induced by Icariin and Its Effectiveness in Glucocorticoid-Induced Injury of Bone Microvascular Endothelial Cells.
Gao, F; Li, T; Li, Z; Lu, J; Sun, W; Wu, X; Zhang, Q, 2022
)
1.69
"Icariin is a principal active component from traditional Chinese medicine Herba Epimedii and has been demonstrated to exert potential antiarrhythmic effect."( Icariin attenuates excessive alcohol consumption-induced susceptibility to atrial fibrillation through SIRT3 signaling.
Dong, X; Huang, YT; Jiang, H; Liu, T; Wang, HS; Xu, DY; Xu, YL; Xue, XD; Yin, ZT; Yu, LM; Zhao, JK; Zhao, QS; Zhou, ZJ, 2022
)
2.89
"Icariin is a primary active component of the traditional Chinese medicinal plant Epimedium grandiflorum. "( Molecular mechanisms regulating the pharmacological actions of icariin with special focus on PI3K-AKT and Nrf-2 signaling pathways.
Aggarwal, K; Agrawal, R; Goyal, A; Pradhan, K; Verma, A, 2022
)
2.4
"Icariin is a phytomolecule from herbal Epimedium, a traditional Chinese medicine widely used to treat musculoskeletal disorders for thousands of years."( A Phytomolecule Icariin Protects from Sarcopenia Partially by Suppressing Myosin Heavy Chain Degradation in Orchiectomized Rats.
Cao, HJ; Huang, CS; Li, L; Qin, L; Shi, KD; Sun, AR; Wang, XL; Yang, WY, 2022
)
1.79
"Icariin (ICA) is a naturally occurring phytochemical agent primarily extracted from Epimedium Brevicornum Maxim (Family Berberidaceae) with a broad spectrum of bioactivities. "( Icariin Alleviates
Aleem, MT; Chen, C; Hanif, S; Huang, S; Li, K; Li, Q; Lv, H; Rajput, SA; Shaukat, A; Shaukat, I; Shukat, R; Yang, L; Yao, Z; Zhang, X, 2022
)
3.61
"Icariin is a main active component of Epimedium, possessing therapeutic effects on various neurodegenerative diseases."( Effects of icariin on alleviating schizophrenia-like symptoms by regulating the miR-144-3p/ATP1B2/mTOR signalling pathway.
Han, B; Ji, H; Liu, Y; Pan, B; Wang, Y; Weng, J; Xu, L; Zhu, X, 2022
)
1.83
"Icariin (ICA) is a flavonoid glycoside purified from the natural product Epimedium, which is reported to exert an inhibitory effect on a variety of cancers."( Icariin Induces Triple-Negative Breast Cancer Cell Apoptosis and Suppresses Invasion by Inhibiting the JNK/c-Jun Signaling Pathway.
Gao, S; Han, X; Ji, F; Liu, J; Lv, Y; Meng, Q; Shi, W; Wu, H; Yin, Y; Zhang, Q; Zhang, X; Zhang, Z, 2023
)
3.07
"Icariin (ICA) is a marker compound isolated from the total flavonoids of Epimedium brevicornu Maxim."( Icariin improves learning and memory function in Aβ
Di, X; Li, Y; Lu, F; Sun, S; Wan, M; Zhang, Z; Zhao, M, 2024
)
3.61
"Icariin is a flavonoid extracted from epimedium brevicornu maxim, and has been shown to improve nephropathy disease."( AR/RKIP pathway mediates the inhibitory effects of icariin on renal fibrosis and endothelial-to-mesenchymal transition in type 2 diabetic nephropathy.
Chen, ZS; Ding, X; Tao, R; Wan, L; Xu, Y; Yao, W, 2024
)
2.42
"Icariin is a type of flavonoid derived from the Chinese herbal plant Epimedium sagittatum Maxim. "( Neuroprotective role of icariin in experimental spinal cord injury via its antioxidant, anti‑neuroinflammatory and anti‑apoptotic properties.
Dai, H; Jia, G; Li, W; Zhang, Y, 2019
)
2.26
"Icariin is a prenylated flavonol glycoside isolated from Epimedium herb, and has been shown to be its main bioactive component. "( PI3K-AKT Signaling Activation and Icariin: The Potential Effects on the Perimenopausal Depression-Like Rat Model.
Cao, LH; Fang, XY; Huang, HY; Li, XM; Miao, MS; Qiao, JY; Zhang, R, 2019
)
2.24
"Icariin (ICA) is a principal active component from traditional Chinese medicine Epimedium grandiflorum. "( Pharmacological effects of icariin.
He, C; Shi, J; Wang, Z, 2020
)
2.3
"Icariin (ICA) is a major flavonoid isolated from the traditional oriental herbal medicine Epimedium that has been recently proved to show potential therapeutic efficacy on T2DM."( Icariin Attenuates Diabetic Cardiomyopathy and Downregulates Extracellular Matrix Proteins in Heart Tissue of Type 2 Diabetic Rats.
Aa, J; Ding, X; Ding, Y; Qiao, C; Song, Z; Tao, J; Wang, H, 2020
)
2.72
"Icariin (ICA), which is an active component of Epimedii (a Chinese medicinal herb), has been verified to demonstrate a wide range of therapeutic effects, such as alleviating various kinds of brain injury."( Neuroprotective effects of icariin in neonatal hypoxia-ischemic brain damage via its anti-apoptotic property.
Luo, L; Rong, Y; Wang, M, 2021
)
1.64
"Icariin (ICA) is a typical flavonoid compound extracted from Epimedii Folium with anti-inflammatory and bone-protective effects."( Icariin inhibits the inflammation through down-regulating NF-κB/HIF-2α signal pathways in chondrocytes.
Li, A; Liu, Z; Meng, Q; Qin, S; Wang, P; Wang, W; Xiong, X; Zhang, J; Zhang, S, 2020
)
2.72
"Icariin (ICA) is a flavonoid extracted from the leaves and stems of Herba epimedii with a wide range of pharmacological effects, such as anti-osteoporosis, anti-fibrosis, anti-aging, anti-inflammation and antioxidation."( Icariin ameliorates streptozocin-induced diabetic nephropathy through suppressing the TLR4/NF-κB signal pathway.
Cheng, Y; Fang, Q; Hao, JQ; He, YH; Ma, RY; Qi, MY; Zhou, SJ, 2021
)
2.79
"Icariin (ICA) is a bioactive compound isolated from epimedium-derived flavonoids that modulates bone mesenchymal stem cell osteogenesis and adipogenesis. "( Icariin stimulates osteogenesis and suppresses adipogenesis of human bone mesenchymal stem cells via miR-23a-mediated activation of the Wnt/β-catenin signaling pathway.
Jia, B; Jiang, Y; Li, T; Wang, Y; Xu, Y, 2021
)
3.51
"Icariin (ICA) is a bioactive flavonoid extracted from Epimedium brevicornum Maxim and exhibits a variety of pharmacological activities including antiinflammatory and antioxidant effects. "( Icariin attenuates renal fibrosis in chronic kidney disease by inhibiting interleukin-1β/transforming growth factor-β-mediated activation of renal fibroblasts.
Feng, X; Wang, C; Wang, L; Wang, M; Ye, C; Zhou, Y, 2021
)
3.51
"Icariin is a biologically active substance in "( Icariin, an Up-and-Coming Bioactive Compound Against Neurological Diseases: Network Pharmacology-Based Study and Literature Review.
Ma, J; Sun, X; Wang, S; Wang, Y; Wu, M; Zeng, Y; Zhou, G; Zhou, W, 2021
)
3.51
"Icariin is a potent stimulator of osteogenic differentiation; however, the mechanism underlying its osteogenic effect remains unclear. "( Glucocorticoid-induced leucine zipper may play an important role in icariin by suppressing osteogenesis inhibition induced by glucocorticoids in osteoblasts.
Chen, DY; Chen, LH; Chen, SZ; Jiang, ZL; Jin, H; Lin, Z; Sun, Y; Xia, AX; Zhou, P; Zhu, YW, 2017
)
2.13
"Icariin is a promising therapeutic strategy for asthma, and PGD2 might be a new target for asthma therapy in OVA-induced and RSV-infected asthma model."( Effects of icariin on asthma mouse model are associated with regulation of prostaglandin D2 level.
Qiao, J; Sun, S; Wang, J; Yuan, L,
)
1.96
"Icariin is a prenylated flavonol glycoside with low cost."( Synthesis of prenylated flavonols and their potents as estrogen receptor modulator.
Gong, L; Jiang, Y; Liu, J; Tao, Z; Yang, B, 2017
)
1.18
"Icariin is a prenylated flavonol glycoside isolated from Epimedium herb, and has been shown to be the main bioactive component."( The effect of icariin on bone metabolism and its potential clinical application.
Peng, S; Wang, D; Wang, Z; Yang, D; Zhang, J; Zhen, W, 2018
)
1.56
"Icariin (ICA) is a flavonoid isolated from certain plant species in the genus Epimedium, especially Epimedium brevicornum. "( Icariin inhibits LPS-induced cell inflammatory response by promoting GRα nuclear translocation and upregulating GRα expression.
Cai, W; Deng, X; Huang, J; Jiang, T; Li, W; Shen, Z; Sun, X, 2018
)
3.37
"Icariin (ICA) is a flavonoid glucoside derived from the Epimedium plant genus, which has potent regenerative properties and is used in western medicine to treat impotence. "( Icariin improves Fanconi anemia hematopoietic stem cell function through SIRT6-mediated NF-kappa B inhibition.
Cole, A; Du, W; Li, X; Li, Y; McLaughlin, S, 2018
)
3.37
"Icariin is a traditional Chinese drug that has long been used to treat various diseases. "( Icariin promotes wound healing by enhancing the migration and proliferation of keratinocytes via the AKT and ERK signaling pathway.
Hu, L; Liu, G; Liu, J; Liu, Y; Mi, B; Wu, Y; Xiong, L; Ye, S; Zhou, W, 2018
)
3.37
"Icariin is an active flavonoid that is reported to inhibit autophagy."( Icariin inhibits autophagy and promotes apoptosis in SKVCR cells through mTOR signal pathway.
Chang, H; Deng, S; Fan, D; Jiang, S, 2018
)
2.64
"Icariin (ICA) is a major active ingredient in Herba epimedii, which is commonly used as a Chinese herbal medicine for the treatment of osteoporosis. "( Icariin stimulates osteogenic differentiation and suppresses adipogenic differentiation of rBMSCs via estrogen receptor signaling.
He, H; Lei, X; Li, X; Liu, X; Mo, S; Ou, L; Pan, Y; Peng, B; Peng, X; Sun, K; Tian, Y; Wang, H; Wang, P; Wu, Z; Yang, L; Zhang, R; Zhu, X, 2018
)
3.37
"Icariin (ICA) is a bioactive flavonoid with renal protective actions. "( Icariin Improves Sepsis-Induced Mortality and Acute Kidney Injury.
Feng, G; Feng, Y; Liu, L; Shang, W; Suo, J; Wang, M; Wang, Z; Xie, C; Xie, H, 2018
)
3.37
"Icariin is a pharmacologically active flavonoid glycoside, which shows potential application in treatment of osteoporosis."( Bone-targeting drug delivery system of biomineral-binding liposomes loaded with icariin enhances the treatment for osteoporosis.
Bian, T; Huang, J; Li, C; Liu, Z; Lyu, J; Pi, F; Sun, X; Wei, J; Zhong, Z, 2019
)
1.46
"Icariin (ICA) is a prenylated flavonol glycoside derived from Herba Epimedii, a medicinal plant with a variety of pharmacological activities, including anticancer, antidiabetic and anti‑obesity effects."( Icariin suppresses cell cycle transition and cell migration in ovarian cancer cells.
Cao, W; Dai, L; Li, A; Liu, Z; Qin, S; Wang, P; Xie, F; Xiong, X; Yuan, W; Zhang, J, 2019
)
2.68
"Icariin is a flavonoid derived from Epimedium sagittatum, and has a wide range of biological and pharmacological effects; however, little is known regarding its effect on drug‑resistant ovarian cancer and the signal transduction pathways underlying the regulation of apoptosis and autophagy. "( Icariin enhances the chemosensitivity of cisplatin‑resistant ovarian cancer cells by suppressing autophagy via activation of the AKT/mTOR/ATG5 pathway.
Chang, H; Deng, S; Fan, D; Jiang, S, 2019
)
3.4
"Icariin is a major component isolated from Epimedium brevicornum Maxim and has been reported to exhibit anti-tumor activity. "( Icariin induces apoptosis by suppressing autophagy in tamoxifen-resistant breast cancer cell line MCF-7/TAM.
Cheng, X; Deng, G; Duan, F; Li, Q; Tan, S; Yuan, Q, 2019
)
3.4
"Icariin (ICA) is a flavonoid used in traditional Chinese medicine."( Icariin protects mouse Leydig cell testosterone synthesis from the adverse effects of di(2-ethylhexyl) phthalate.
Lian, X; Lin, J; Liu, Y; Lv, R; Mo, K; Sun, J; Wang, D; Wang, S; Xie, M; Xu, L; Xu, S, 2019
)
2.68
"Icariin (ICA) is a naturally occurring furanocoumarin and exhibits many pharmacological properties, including potent improvement on learning and memory."( Icariin ameliorates learning and memory impairments through ERK/CaMKIIα/CREB signaling and HPA axis in prenatally stressed female offspring.
Cao, YJ; Chen, YW; Deng, HH; He, J; Li, Y; Li, YC; Xia, SZ; Yue, YS; Zheng, XX, 2019
)
2.68
"Icariin is a flavonoid from plant belonging to the genus Epimedium, commonly known as Horny goat weed or Yin Yang Huo. "( Angiogenic and MMPs modulatory effects of icariin improved cutaneous wound healing in rats.
Appukuttan, AV; Devi, HS; Kumar, D; Kumawat, S; Lingaraju, MC; Patel, MR; Sadam, A; Singh, TU; Singh, WR, 2019
)
2.22
"Icariin is a major active component isolated from the traditional Chinese herb Epimedium brevicornum, with a wide range of pharmacological and biological activities. "( Icariin attenuates the enhanced prothrombotic state in atherosclerotic rabbits independently of its lipid-lowering effects.
Bai, XJ; Xie, XL; Yuan, ZY; Zhang, WP; Zheng, XP, 2013
)
3.28
"Icariin is a natural compound which inhibits tumour cell growth and induces apoptotic cell death in a variety of cancer cells."( Icariin synergizes with arsenic trioxide to suppress human hepatocellular carcinoma.
Ji, S; Li, W; Wang, L; Wang, M; Zhang, C; Zhang, J, 2014
)
2.57
"Icariin is a flavonol widely present in many herbal preparations, which is used to improve sexual function and prevent osteogenesis."( Interaction of the bioactive flavonol, icariin, with the essential human solute carrier transporters.
Chan, T; Cheung, FS; Li, Z; Zheng, J; Zhou, F; Zhu, L, 2014
)
1.39
"Icariin appears to be a promising drug to treat major age-related diseases, like neurodegeneration, memory and depressive disorders, chronic inflammation, diabetes, and osteoporosis."( Plant polyphenols in the treatment of age-associated diseases: revealing the pleiotropic effects of icariin by network analysis.
Schluesener, H; Schluesener, JK, 2014
)
1.34
"Icariin is a natural compound that is conventionally reported to have activity against a variety of cancers."( Icariin-mediated inhibition of NF-κB activity enhances the in vitro and in vivo antitumour effect of 5-fluorouracil in colorectal cancer.
Cai, GX; Cai, SJ; Gu, WL; Guan, ZQ; Li, DW; Li, XX; Peng, JJ; Shi, DB; Xu, Y; Zheng, HT, 2014
)
2.57
"Icariin is a flavonol glycoside isolated from Epimedium genus and has been used in the treatment of sexual dysfunction and osteoporosis. "( Effect of icariin on UDP-glucuronosyltransferases in mouse liver.
Jin, T; Li, LS; Liu, J; Lu, YF; Shi, JS; Xu, SF, 2014
)
2.25
"Icariin is a natural compound with anti-cancer activity against a variety of cancers."( Synergistic Anti-Cancer Effects of Icariin and Temozolomide in Glioblastoma.
Guo, H; Guo, M; Wang, Y; Yang, L, 2015
)
1.42
"Icariin is an important pharmacologically active flavonol diglycoside that can inhibit inflammation in lipopolysaccharide (LPS)-stimulated macrophages. "( Icariin inhibits foam cell formation by down-regulating the expression of CD36 and up-regulating the expression of SR-BI.
Duan, H; Li, B; Qian, P; Wang, S; Wu, J; Yan, L; Yang, H, 2015
)
3.3
"Icariin which is a flavonoid glucoside isolated from Epimedium brevicornu Maxim, has been reported to have anti-osteoporotic, anti-inflammatory and anti-depressant-like activities. "( Regulation of Th17/Treg function contributes to the attenuation of chronic airway inflammation by icariin in ovalbumin-induced murine asthma model.
Dong, J; Liu, B; Liu, F; Luo, Q; Lv, Y; Sun, J; Wei, Y, 2015
)
2.08
"Icariin is a flavonol glycoside with a wide range of pharmacological and biological activities. "( Resonance energy transfer, pH-induced folded states and the molecular interaction of human serum albumin and icariin.
Cheng, XX; Fan, XY; Jiang, FL; Lei, KL; Liu, Y, 2015
)
2.07
"Icariin is a natural compound with activity against a variety of cancers."( Arsenic Trioxide and Icariin Show Synergistic Anti-leukemic Activity.
Dai, L; Li, P; Liu, Y; Song, T; Wang, L; Wang, Z; Zhang, H, 2015
)
1.46
"Icariin is a flavonol isolated from medicinal herbal tonics."( Icariin, a natural flavonol glycoside, extends healthspan in mice.
Cai, WJ; Chen, XL; Huang, JH; Shen, ZY; Wu, B; Xia, SJ; Zhang, SQ; Zhang, XM, 2015
)
2.58
"Icariin is a flavonoid isolated from the traditional Chinese herbal medicine Epimedium brevicornum Maxim and has been reported to be effective for the treatment of a variety of cardiovascular diseases. "( Icariin Attenuates High-cholesterol Diet Induced Atherosclerosis in Rats by Inhibition of Inflammatory Response and p38 MAPK Signaling Pathway.
Hu, Y; Liu, K; Miao, C; Ren, L; Sun, B; Yan, M; Zhang, Y, 2016
)
3.32
"Icariin (ICA) is an active compound extracted from Epimedium brevicornum Maxim. "( Icariin Prevents Cartilage and Bone Degradation in Experimental Models of Arthritis.
Ping, DQ; Qiang, CY; Tao, C; Wei, CC; You, FT, 2016
)
3.32
"Icariin (ICA), which is an essential bioactive component extracted from the herb Epimedium, possesses neuroprotective properties. "( Icariin promotes cell proliferation and regulates gene expression in human neural stem cells in vitro.
Guan, YQ; Li, L; Li, YL; Yang, P; Zhang, L, 2016
)
3.32
"Icariin is a flavonoid component of a traditional Chinese medicine reported to possess a broad spectrum of pharmacological effects."( Icariin, a major constituent from Epimedium brevicornum, attenuates ibotenic acid-induced excitotoxicity in rat hippocampus.
Deng, Y; Gong, Q; Jin, F; Li, F; Shi, J; Zong, N, 2016
)
2.6
"Icariin is a major bioactive compound of Epimedii Herba, a traditional oriental medicine exhibiting anti-cancer, anti-inflammatory and anti-osteoporosis activities. "( Icariin Metabolism by Human Intestinal Microflora.
Han, J; Kim, M; Wu, H, 2016
)
3.32
"Icariin is a major flavonoid isolated from Epimedium spp. "( Icariin promotes mouse hair follicle growth by increasing insulin-like growth factor 1 expression in dermal papillary cells.
Fan, ZX; Hu, ZQ; Lin, BJ; Liu, H; Miao, Y; Su, YS; Xiao, SE, 2017
)
3.34
"1. Icariin is a major constituent of flavonoids derived from the Chinese medicinal herb Epimedium revicornum Maxim. "( Protective effects of icariin on cognitive deficits induced by chronic cerebral hypoperfusion in rats.
Gong, QH; Huang, XN; Luo, Y; Shi, JS; Sun, AS; Wu, Q; Xu, RX; Yu, LM, 2009
)
1.29
"Icariin is a safe and effective natural anti-inflammatory drug, its partial mechanism is possible the multiple links intervention on pro-inflammatory cytokines (TNF-alpha, IL-6), inflammatory mediators (NO) and adhesion molecules (CD11b)."( [Effects of icariin on inflammation model stimulated by lipopolysaccharide in vitro and in vivo].
Dong, JC; Wu, JF; Xu, CQ, 2009
)
2.17
"Icariin is a bioactive herbal ingredient isolated from Epimedii Herba. "( Analysis of biliary excretion of icariin in rats.
Chen, KK; Chiu, AW; Lin, CW; Lin, LC; Tsai, TH; Wu, YT, 2010
)
2.08
"Icariin is a flavonoid extracted from the traditional Chinese herb Epimedium brevicornum Maxim."( Icariin inhibits hydrogen peroxide-induced toxicity through inhibition of phosphorylation of JNK/p38 MAPK and p53 activity.
Gao, XM; Guo, H; Li, WW; Wang, XM; Zhang, BL, 2011
)
2.53
"Icariin is a major constituent of flavonoids isolated from the herb Epimedium. "( Icariin attenuates social defeat-induced down-regulation of glucocorticoid receptor in mice.
Dong, J; Du, J; Le, J; Liu, B; Wu, J; Xu, C; Xu, Y, 2011
)
3.25
"Icariin is a major constituent of flavonoid isolated from the plant Herba epimedii, which is used as a traditional Chinese medicine to nourish the kidney and reinforce yang. "( Protective effect of Icariin on the early stage of experimental diabetic nephropathy induced by streptozotocin via modulating transforming growth factor β1 and type IV collagen expression in rats.
Liu, HR; Qi, MY; Su, YH; Yu, SQ, 2011
)
2.13
"Icariin (ICA) is an active component of Herba Epimedium effective in preventing osteoporosis. "( Different molecular targets of Icariin on bMSCs in CORT and OVX -rats.
Bian, Q; Huang, JH; Liu, SF; Ning, Y; Shen, ZY; Wang, YJ; Yang, Z; Zhao, YJ, 2012
)
2.11
"Icariin is a flavonol extracted from several plant species of the Epimedium family."( Icariin and its derivative icariside II extend healthspan via insulin/IGF-1 pathway in C. elegans.
Cai, WJ; Huang, JH; Kapahi, P; Shen, ZY; Wu, B; Zhang, SQ; Zhang, XM, 2011
)
2.53
"Icariin is a bioactive herbal ingredient isolated from Herba epimedii, which has been widely used for the treatment of osteoporosis and male sexual dysfunction in traditional Chinese medicine. "( Changes in the intestinal absorption mechanism of icariin in the nanocavities of cyclodextrins.
Cui, YL; Lin, KM; Meng, FC; Wang, QS; Zhang, Y, 2012
)
2.07
"Icariin (ICA) is a kind of new biological respone modifier(BRM) and differentiational agent. "( [Experimental studies of icariin on anticancer mechanism].
Li, X; Mao, H; Wang, Y; Zhang, L, 2000
)
2.05
"Icariin is a cGMP-specific PDE5 inhibitor that may be developed into an oral effective agent for the treatment of ED."( Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities.
Fu, J; Kim, EK; Lin, CS; Liu, WJ; Tian, L; Xin, ZC; Yuan, YM, 2003
)
2.15
"Icariin is a flavonoid isolated from Epimedium and is considered to be the major pharmacological active component of Epimedii Herba. "( Protective effects of icariin on human umbilical vein endothelial cell injury induced by H2O2 in vitro.
Huang, ZQ; Wang, YK, 2005
)
2.09
"Icariine is a flavonoid isolated from a traditional Chinese medicine Epimedium pubescens and is the main active compound of it. "( Icariine stimulates proliferation and differentiation of human osteoblasts by increasing production of bone morphogenetic protein 2.
Chen, ZQ; Dang, GT; Liu, ZJ; Ma, QJ; Yin, XX, 2007
)
3.23
"Icariin is a prenylated flavonol glycoside contained in the herb Epimedium, which has long been used to improve bone fracture healing or prevent osteoporosis because of the belief that the herb has bone-strengthening action. "( Icariin inhibits the osteoclast formation induced by RANKL and macrophage-colony stimulating factor in mouse bone marrow culture.
Bai, MH; Chen, KM; Ge, BF; Liu, XY; Lu, MB; Ma, PH; Wang, Y, 2007
)
3.23
"Icariin is an monomer purified from Epimedium Koreanum Nakai. "( [Effects of icariin on the differentiation of HL-60 cells].
Cui, Z; Zhang, L; Zhao, Y, 1997
)
2.12

Effects

Icariin has a number of pharmacological actions, including anti‑inflammatory, anti‑oxidative and anti‑apoptotic effects. It has a significant anti-osteoporotic activity, but its clinical application is limited due to a poor oral bioavailability.

Icariin (ICA) has been implicated in certain biological and pathological processes, including myocardial ischemia/reperfusion (I/R) injury. Icariin has shown great potential in improving cell activity and VEGF, BDNF secretion in vitro.

ExcerptReferenceRelevance
"Icariin has a variety of biological activities, such as lipid-lowering effects, and has attracted widespread attention in recent years. "( Icariin and its metabolites regulate lipid metabolism: From effects to molecular mechanisms.
Gao, H; Li, W; Wang, M; Wu, B, 2020
)
3.44
"Icariin has a significant anti-osteoporotic activity, but its clinical application is limited due to a poor oral bioavailability especially under pathological conditions like osteoporosis. "( Icariin combined with snailase shows improved intestinal hydrolysis and absorption in osteoporosis rats.
Chen, Y; Gao, X; Huang, M; Liu, C; Liu, Y; Qu, D, 2017
)
3.34
"Icariin has a regulatory effect on steroidogenesis in HaCaT cells, which may provide a promising therapeutic target for the treatment of inflammatory skin disorders."( Icariin inhibits inflammation via immunomodulation of the cutaneous hypothalamus-pituitary-adrenal axis in vitro.
Dong, J; Kong, L; Liang, X; Liu, A; Luo, Q; Lv, Y; Yang, X, 2019
)
3.4
"Icariine has a direct stimulatory function on the differentiation of MC3T3-E1 osteoblastic cells in vitro, which may be mediated by increasing the production of Smad1 and Smad5 in osteoblasts."( Regulation of the levels of Smad1 and Smad5 in MC3T3-E1 cells by Icariine in vitro.
Shi, N; Wang, S; Xue, Y; Zhou, H, 2014
)
1.36
"Icariin has a number of pharmacological actions, including anti‑inflammatory, anti‑oxidative and anti‑apoptotic effects."( Icariin protects H9c2 cardiomyocytes from lipopolysaccharide‑induced injury via inhibition of the reactive oxygen species‑dependent c‑Jun N‑terminal kinases/nuclear factor-κB pathway.
Bian, ZY; Dai, J; Deng, W; Liu, Y; Ni, J; Tang, QZ; Yuan, Y; Zhou, H, 2015
)
2.58
"Icariine has a direct stimulatory effect on the proliferation and differentiation of cultured human osteoblast cells in vitro, which may be mediated by increasing production of BMP-2 in osteoblasts."( Icariine stimulates proliferation and differentiation of human osteoblasts by increasing production of bone morphogenetic protein 2.
Chen, ZQ; Dang, GT; Liu, ZJ; Ma, QJ; Yin, XX, 2007
)
3.23
"Icariin has attracted increasing attention because of its wide variety of pharmacological effects."( Effects of icariin on the fracture healing in young and old rats and its mechanism.
Chen, F; Chen, Y; Han, J; Song, S; Xia, T; Xu, C; Zhang, C; Zhang, X, 2021
)
2.45
"Icariin (ICA) has been found to exhibit protective effects on multiple chronic diseases like diabetes, liver, heart, and renal fibrosis."( Icariin attenuates bleomycin-induced pulmonary fibrosis by targeting Hippo/YAP pathway.
Dong, J; Du, W; Liu, X; Tang, Z; Yang, F, 2021
)
2.79
"Icariin has the characteristics of multitargeted intervention in the treatment of asthma."( Research progress on icariin, a traditional Chinese medicine extract, in the treatment of asthma.
Dong, YC; Shang, Y; Tong, ZY; Yuan, JY; Zhao, JY, 2022
)
1.76
"Icariin has been utilized to treat various ailments as a natural chemical extract."( Immunomodulatory effects of icariin in a myocardial infarction mouse model.
Deng, G; Li, Z; Liu, C; Nasser, MI; Sai, X; Wang, L; Xiaowu, W; Zhu, P, 2022
)
1.74
"Icariin (ICA) has proven to exert neuroprotective function through anti-inflammatory function."( Icariin alleviates autistic-like behavior, hippocampal inflammation and vGlut1 expression in adult BTBR mice.
Du, Z; Fan, X; Fei, X; Jiang, P; Li, D; Li, S; Liao, H; Tang, Y; Wang, L; Yang, H; Zhao, L; Zhou, L, 2023
)
3.07
"Icariin has been shown to regulate endocrine and metabolic imbalances."( Therapeutic potential of icariin in rats with letrozole and high-fat diet-induced polycystic ovary syndrome.
Hai, Y; Huang, X; Ke, X; Li, P; Li, X; Ren, L; Tian, J; Wang, J; Wang, M; Zhang, R; Zuo, B; Zuo, L, 2023
)
1.93
"Icariin (ICA) has wide applications in nutraceuticals and medicine with strong anticancer activities. "( De novo biosynthesis of anticarcinogenic icariin in engineered yeast.
An, T; Feng, X; Li, C; Lin, G; Liu, Y; Qin, L; Xu, Y, 2023
)
2.62
"Icariin has been identified that it could cross the blood-brain barrier and enter the hippocampus to exhibit therapeutic effects."( Anti-inflammatory effects of icariin in the acute and chronic phases of the mouse pilocarpine model of epilepsy.
Feng, L; Liu, Y; Wang, J; Wu, Y; Yan, L; Yang, K, 2023
)
1.92
"Icariin has been reported to exert multiple effects on BMSCs, including its proliferation, osteogenic, and chondrogenic differentiation."( Icariin protects rabbit BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated autophagy via MAPK signaling pathway.
Huang, H; Jiao, F; Liu, D; Tang, D; Tang, W; Zhang, H; Zhang, Z, 2020
)
2.72
"Icariin has been shown to enhance bone formation."( Icariin Accelerates Fracture Healing
Chen, YP; Han, J; Song, SL; Xia, T; Xu, CH; Yang, N; Zhang, C; Zhang, X; Zhang, XY, 2020
)
3.44
"Icariin liposome has excellent therapeutic effects on acute blunt muscle injury in rats by improving immunity, repairing cytoskeleton and cellular integrity, anti-inflammation, anti-fibrosis and antioxidant stress."( An injectable liposome for sustained release of icariin to the treatment of acute blunt muscle injury.
Cai, J; Cai, L; Chen, H; Feng, Y; Guo, Q; Wang, J; Wang, X; Xie, L; Zheng, W; Zhu, G, 2020
)
2.26
"Icariin has a variety of biological activities, such as lipid-lowering effects, and has attracted widespread attention in recent years. "( Icariin and its metabolites regulate lipid metabolism: From effects to molecular mechanisms.
Gao, H; Li, W; Wang, M; Wu, B, 2020
)
3.44
"Icariin (ICA) has been used as a promising anti‑aging drug; however, its underlying molecular mechanism is yet to be elucidated. "( Icariin modulates the sirtuin/NF‑κB pathway and exerts anti‑aging effects in human lung fibroblasts.
Feng, X; Huang, X; Jiang, Y; Tong, Y; Wang, C; Wang, Y; Xu, C, 2020
)
3.44
"Icariin has the potentials to be developed as a medicine for the wellness of the aged adults."( Icariin enhances youth-like features by attenuating the declined gut microbiota in the aged mice.
Guo, X; Han, R; Hsiao, WLW; Huang, G; Khan, I; Law, BYK; Leong, W; Li, X; Liao, W; Liu, L; Wong, VKW; Xia, C; Xia, W; Yin, L, 2021
)
2.79
"Icariin has a significant anti-osteoporotic activity, but its clinical application is limited due to a poor oral bioavailability especially under pathological conditions like osteoporosis. "( Icariin combined with snailase shows improved intestinal hydrolysis and absorption in osteoporosis rats.
Chen, Y; Gao, X; Huang, M; Liu, C; Liu, Y; Qu, D, 2017
)
3.34
"Icariin (Ic) has been demonstrated as a potent osteoinductive compound for bone tissue engineering. "( A Novel Approach to Utilize Icariin as Icariin-Derived ECM on Small Intestinal Submucosa Scaffold for Bone Repair.
Li, M; Zhang, C; Zhao, J; Zhong, Y, 2017
)
2.19
"Icariin has previously been demonstrated to attenuate hyperglycemia‑induced renal injury, however the renoprotective effects of icariin in a rat model of pregnancy‑induced hypertension (PIH) remain to be elucidated. "( Icariin improves acute kidney injury and proteinuria in a rat model of pregnancy‑induced hypertension.
Chang, W; Li, J; Xu, N; Yuan, W; Zhang, W, 2017
)
3.34
"Icariin (ICA) has been implicated in certain biological and pathological processes, including myocardial ischemia/reperfusion (I/R) injury. "( Icariin protects against ischemia‑reperfusion injury in H9C2 cells by upregulating heat shock protein 20.
Ke, ZP; Luo, M; Ren, ZH; Shi, Y, 2018
)
3.37
"Icariin has been demonstrated to aid in the maintenance of the articular cartilage phenotype in a rat model of post‑traumatic osteoarthritis (PTOA)."( Role of IFT88 in icariin‑regulated maintenance of the chondrocyte phenotype.
Dong, Y; Guo, F; Wang, L; Wang, R; Wang, S; Wu, Y; Xiang, W; Xu, T; Zhang, J, 2018
)
1.54
"Icariin (ICA) has been suggested to restore osteogenic function. "( Icariin promotes the proliferation and differentiation of osteoblasts from the rat mandible by the Wnt/β‑catenin signalling pathway.
Wang, R; Wang, Y; Zhang, F, 2018
)
3.37
"Icariin has been reported to possess high anticancer activity. "( Icariin reduces human colon carcinoma cell growth and metastasis by enhancing p53 activities.
Tian, M; Yan, X; Yang, S, 2018
)
3.37
"Icariin has a regulatory effect on steroidogenesis in HaCaT cells, which may provide a promising therapeutic target for the treatment of inflammatory skin disorders."( Icariin inhibits inflammation via immunomodulation of the cutaneous hypothalamus-pituitary-adrenal axis in vitro.
Dong, J; Kong, L; Liang, X; Liu, A; Luo, Q; Lv, Y; Yang, X, 2019
)
3.4
"Icariin (ICA) has shown great potential in improving cell activity and VEGF, BDNF secretion in vitro."( Icariin and mesenchymal stem cells synergistically promote angiogenesis and neurogenesis after cerebral ischemia via PI3K and ERK1/2 pathways.
Liu, D; Xu, L; Ye, Y; Yuan, W; Zhang, Q, 2018
)
2.64
"Icariin (ICA) has shown potential osteoprotective effects."( Icariin promotes osteogenic differentiation of bone marrow stromal cells and prevents bone loss in OVX mice via activating autophagy.
Cai, L; Hou, Z; Li, S; Liang, X; Xie, Y; Yan, F; Zhu, X, 2019
)
2.68
"Icariin (ICA) has been reported to facilitate cardiac differentiation of mouse embryonic stem (ES) cells; however, the mechanism by which ICA induced cardiomyogenesis has not been fully elucidated yet. "( mGluR5 stimulating Homer-PIKE formation initiates icariin induced cardiomyogenesis of mouse embryonic stem cells by activating reactive oxygen species.
Huang, Y; Lou, Y; Zhang, Y; Zhao, Q; Zheng, B; Zhou, L; Zhu, D, 2013
)
2.09
"Icariin has been shown to attenuate diabetic nephropathy in rats by decreasing transforming growth factor-β (TGF-β) and type IV collagen expression, but its mode of action in glomerular mesangial cells is uncertain. "( Icariin attenuates high glucose-induced type IV collagen and fibronectin accumulation in glomerular mesangial cells by inhibiting transforming growth factor-β production and signalling through G protein-coupled oestrogen receptor 1.
Ding, XS; Li, HM; Li, YC; Zhang, C, 2013
)
3.28
"Icariine has a direct stimulatory function on the differentiation of MC3T3-E1 osteoblastic cells in vitro, which may be mediated by increasing the production of Smad1 and Smad5 in osteoblasts."( Regulation of the levels of Smad1 and Smad5 in MC3T3-E1 cells by Icariine in vitro.
Shi, N; Wang, S; Xue, Y; Zhou, H, 2014
)
1.36
"Icariin (ICA) has demonstrated to induce cardiomyocyte differentiation from murine embryonic stem (ES) cells in vitro, however, the mechanisms have not been fully elucidated. "( Involvement of PIKE in icariin induced cardiomyocyte differentiation from murine embryonic stem cells.
Huang, Y; Tang, L; Zheng, B; Zhou, L; Zhu, D, 2014
)
2.16
"Icariin has a number of pharmacological actions, including anti‑inflammatory, anti‑oxidative and anti‑apoptotic effects."( Icariin protects H9c2 cardiomyocytes from lipopolysaccharide‑induced injury via inhibition of the reactive oxygen species‑dependent c‑Jun N‑terminal kinases/nuclear factor-κB pathway.
Bian, ZY; Dai, J; Deng, W; Liu, Y; Ni, J; Tang, QZ; Yuan, Y; Zhou, H, 2015
)
2.58
"Icariin has been found to possess effective aphrodisiac, antioxidant, immunomodulatory, hepatoprotective, cardioprotective, vasodilatory, antidepressant and anti-osteoporosis activities."( Evaluation of medicinal value of Epimedium elatum on the basis of pharmacologically active constituents, Icariin and Icariside-II.
Arief, ZM; Munshi, AH; Shawl, AS, 2015
)
1.35
"Icariine has been reported to facilitate the bone healing and reduce the occurrence of osteoporosis in clinical, moreover, laboratory studies which have proved that Icariine promotes the proliferation and differentiation of osteoblasts in vitro."( Icariine Restores LPS-Induced Bone Loss by Downregulating miR-34c Level.
Chen, A; Li, D; Liu, J; Sun, X; Wang, Y; Xiao, Q, 2016
)
2.6
"Icariin has also been shown to regulate the proliferation and osteogenic differentiation of rat bone marrow stromal cells (rBMSCs)."( Icariin promotes proliferation and osteogenic differentiation of rat adipose-derived stem cells by activating the RhoA-TAZ signaling pathway.
Jing, X; Li, B; Li, N; Wu, Y; Xu, T; Ye, Y, 2017
)
2.62
"Icariin (ICA) has neuroprotection in oxygen-glucose deprivation (OGD) neurons by increasing Sirtuin1 (SIRT1). "( Icariin protects against brain injury by enhancing SIRT1-dependent PGC-1alpha expression in experimental stroke.
Li, EG; Wang, ZY; Wu, XX; Xu, Y; Zhu, HR; Zhu, XL,
)
3.02
"Icariin has been reported to enhance bone healing and treat osteoporosis. "( Icariin inhibits osteoclast differentiation and bone resorption by suppression of MAPKs/NF-κB regulated HIF-1α and PGE(2) synthesis.
Chen, MH; Hsieh, TP; Sheu, SY; Sun, JS, 2011
)
3.25
"Icariin (ICA) has previously been shown to induce cardiomyocyte (CM) differentiation of murine embryonic stem cells in vitro, but its effect on ADSCs remains unclear."( Icariin-mediated differentiation of mouse adipose-derived stem cells into cardiomyocytes.
Jin, MS; Liu, HW; Liu, W; Shi, S; Sun, XD; Yan, Y; Zhang, Y, 2010
)
2.52
"Icariin has been shown to significantly facilitate the differentiation of embryonic stem (ES) cells into cardiomyocytes in vitro. "( Involvement of ubiquitin-proteasome system in icariin-induced cardiomyocyte differentiation of embryonic stem cells using two-dimensional gel electrophoresis.
Cui, R; Li, H; Lou, YJ; Zhang, YY; Zhou, LM; Zhu, DY, 2011
)
2.07
"Icariin has been shown to improve penile hemodynamics in animal models of erectile dysfunction from cavernous nerve injury and castration. "( Effects of icariin on improving erectile function in streptozotocin-induced diabetic rats.
Cui, WS; Gao, ZZ; Gong, YQ; Li, GY; Li, WR; Liu, T; Qin, XC; Shindel, AW; Xin, H; Xin, ZC; Zhou, F, 2011
)
2.2
"Icariin has been reported to enhance bone healing and treat osteoporosis. "( Icariin enhances the healing of rapid palatal expansion induced root resorption in rats.
Lin, S; Liu, Z; Lu, H; Wang, F; Xu, J, 2012
)
3.26
"Icariin has protective effects on cerebral ischemia/reperfusion injured neurons. "( Protective effects of icariin on neurons injured by cerebral ischemia/reperfusion.
Li, L; Shi, JS; Zhou, QX, 2005
)
2.09
"Icariin has testosterone mimetic properties and has therapeutic potential in the management of hypoandrogenism."( The testosterone mimetic properties of icariin.
Yang, QT; Zhang, ZB, 2006
)
2.05
"Icariine has a direct stimulatory effect on the proliferation and differentiation of cultured human osteoblast cells in vitro, which may be mediated by increasing production of BMP-2 in osteoblasts."( Icariine stimulates proliferation and differentiation of human osteoblasts by increasing production of bone morphogenetic protein 2.
Chen, ZQ; Dang, GT; Liu, ZJ; Ma, QJ; Yin, XX, 2007
)
3.23
"Icariin has been reported to facilitate the differentiation of mouse embryonic stem (ES) cells into cardiomyocytes; however, the mechanism on cardiomyogenic cell lineage differentiation has not been fully elucidated yet. "( Involvement of NF-kappaB and AP-1 activation in icariin promoted cardiac differentiation of mouse embryonic stem cells.
Lou, Y; Wo, Y; Yu, Y; Zhu, D, 2008
)
2.04

Actions

Icariin promotes bone formation and inhibits bone loss, and effectively restores bone structure and strength in chronic high-dose alcohol-induced osteopenic rats. Icariin can inhibit inflammation, lipid peroxidation and apoptosis after spinal cord injury.

ExcerptReferenceRelevance
"Icariin (ICA) plays a therapeutic role in many autoimmune diseases."( The effect of icariin on autoimmune premature ovarian insufficiency via modulation of Nrf2/HO-1/Sirt1 pathway in mice.
Chen, H; Han, Z; Liang, X; Liu, C; Peng, F; Song, L; Xu, X; Zhang, Q, 2022
)
1.8
"Icariin (IC) promotes osteogenic differentiation, and it may be a potential small molecule drug for local application in bone regeneration. "( Icariin-loaded porous scaffolds for bone regeneration through the regulation of the coupling process of osteogenesis and osteoclastic activity.
Cai, L; Deng, Z; Liu, H; Sun, W; Xie, Y; Yan, F, 2019
)
3.4
"Icariin promotes apoptosis and suppresses SKOV3 cell activities through the PI3K-Akt signalling pathway. "( Study on the regulatory mechanism and experimental verification of icariin for the treatment of ovarian cancer based on network pharmacology.
Fu, Y; Gao, J; Li, Q; Ming, W; Qin, J; Song, L; Wang, S, 2020
)
2.24
"Icariin treatment may suppress the expression of cathepsin K in the tibia of GIOP mice."( Icariin ameliorates dexamethasone‑induced bone deterioration in an experimental mouse model via activation of microRNA‑186 inhibition of cathepsin K.
Huang, J; Ma, Y; Yang, H, 2018
)
2.64
"Icariin promotes bone formation and inhibits bone loss, and effectively restores bone structure and strength in chronic high-dose alcohol-induced osteopenic rats."( Icariin Restores Bone Structure and Strength in a Rat Model of Chronic High-Dose Alcohol-Induced Osteopenia.
Cai, M; Liu, PC; Liu, R; Wu, JZ, 2018
)
2.64
"Icariin can inhibit autophagy and promote apoptosis in SKVCR cells by activating mTOR signal pathway."( Icariin inhibits autophagy and promotes apoptosis in SKVCR cells through mTOR signal pathway.
Chang, H; Deng, S; Fan, D; Jiang, S, 2018
)
2.64
"Icariin can inhibit inflammation, lipid peroxidation and apoptosis after spinal cord injury, reduce histopathological damage of spinal cord, improve the motor function, effectively protect spinal cord tissue, and has an obvious neuroprotective effect."( [Neuroprotective effect of icariin on spinal cord injury in rats].
Ding, W; Ren, XS; Yang, XY, 2018
)
2.22
"Icariin can inhibit fibroblast further osteogenic differentiation through inhibiting the effect of cytokines on the fibroblast osteogenesis type markers and osteogenic gene expression and osteogenic differentiation."( Effects of icariin on cytokine-induced ankylosing spondylitis with fibroblastic osteogenesis and its molecular mechanism.
Feng, X; Jia, C; Li, M; Liu, H; Wu, Z, 2014
)
1.51
"Icariin can enhance the expression of osteogenic markers of ROB in collagen hydrogel three-dimensional culture significantly."( [Icariin enhances differentiation and maturation of rat calvarial osteoblasts in collagen hydrogel three-dimensional culture].
Chen, KM; Gao, YH; Shi, WG; Wang, MG; Xie, YF; Zhou, J, 2015
)
2.77
"Icariin could inhibit adipogenic differentiation of BMSCs in the osteoblast-osteoclast co-culture, promoting osteogenic differentiation and inhibiting osteoclast differentiation."( Icariin influences adipogenic differentiation of stem cells affected by osteoblast-osteoclast co-culture and clinical research adipogenic.
Feng, P; Li, D; Li, Y; Mo, G; Mo, L; Yang, Z; Zhang, S, 2017
)
2.62
"Icariin did not activate ERE-luciferase activity in UMR 106 cells, via the ERalpha or the ERbeta-mediated pathway, but it did increase ERalpha phosphorylation at Ser118."( Icariin protects against bone loss induced by oestrogen deficiency and activates oestrogen receptor-dependent osteoblastic functions in UMR 106 cells.
Chen, WF; Lai, WP; Leung, PC; Mok, SK; Wang, XL; Wong, MS; Yao, XS, 2010
)
2.52
"Icariin could inhibit the activation of NF-κB p65 protein in asthmatic rat pulmonary tissue."( Molecular mechanism of icariin on rat asthmatic model.
Cao, YX; Dong, JC; DU, WJ; Duan, XH; LE, JJ; Liu, BJ; Wu, JF; Xu, CQ, 2011
)
1.4
"Icariin promotes differentiation of the mesenchymal stem cells C3H10T1/2 into osteoblasts, and its effect is related to the restraining of ERK expression and activation of p38 expression in the MAPK signaling pathway."( [Analysis of the osteogenetic effects exerted on mesenchymal stem cell strain C3H10T1/2 by icariin via MAPK signaling pathway in vitro].
Bian, Q; Mao, XY; Shen, ZY, 2012
)
2.04
"Icariin was able to enhance cGMP levels in SNP-treated cavernous smooth muscle cells."( Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells.
Banie, L; Lin, CS; Lin, G; Lue, TF; Ning, H; Xin, ZC, 2006
)
1.45

Treatment

Icariin treatment significantly suppressed PCa growth, bone metastasis and destruction as well as osteoclastogenesis in vivo. Icariin-treated rats had lower weight gain and reduced triglycerides, fasting insulin, HOMA-IR, TNF-α, and interleukin-6.

ExcerptReferenceRelevance
"Both icariin treatment and TRIB1 overexpression inhibited proliferation and inflammatory responses but promoted the apoptosis of TNF-α-treated RA-FLSs. "( Icariin represses the inflammatory responses and survival of rheumatoid arthritis fibroblast-like synoviocytes by regulating the TRIB1/TLR2/NF-kB pathway.
Chen, S; Guo, J; Shi, XD; Wan, X; Wu, ZM; Xiang, YR; Zhu, XB, 2022
)
2.68
"Icariin treatment inhibited ethanol-induced atrial ferroptosis by reducing atrial mitochondrial damage, ROS accumulation and iron overload."( Inhibition of ferroptosis by icariin treatment attenuates excessive ethanol consumption-induced atrial remodeling and susceptibility to atrial fibrillation, role of SIRT1.
Dong, X; Huang, T; Huang, YT; Jiang, H; Wang, HS; Wang, ZS; Xu, YL; Yin, ZT; Yu, LM; Zhao, JK; Zhao, QS; Zhou, ZJ, 2023
)
1.92
"Icariin-treated rats had lower weight gain and reduced triglycerides, fasting insulin, HOMA-IR, TNF-α, and interleukin-6 with higher high-density lipoprotein cholesterol levels than PCOS rats."( Therapeutic potential of icariin in rats with letrozole and high-fat diet-induced polycystic ovary syndrome.
Hai, Y; Huang, X; Ke, X; Li, P; Li, X; Ren, L; Tian, J; Wang, J; Wang, M; Zhang, R; Zuo, B; Zuo, L, 2023
)
1.93
"Icariin treatment significantly suppressed PCa growth, bone metastasis and destruction as well as osteoclastogenesis in vivo. "( Icariin inhibits prostate cancer bone metastasis and destruction via suppressing TAM/CCL5-mediated osteoclastogenesis.
Chen, C; Chen, Z; Hong, M; Wang, N; Wang, S; Wang, Z; Xiang, S; Zheng, Y; Zhou, J, 2023
)
3.8
"Icariin treatment increased ALP activity and induced the expression of Cbfα1, BMP-2 and BMP-4 in rBMSCs in a dose-dependent manner. "( Icariin Accelerates Fracture Healing
Chen, YP; Han, J; Song, SL; Xia, T; Xu, CH; Yang, N; Zhang, C; Zhang, X; Zhang, XY, 2020
)
3.44
"Icariin treatment improved motor coordination and learning skills while lowered oxidative stress biomarkers in the serum, brain, kidney, and liver of the aged mice."( Icariin enhances youth-like features by attenuating the declined gut microbiota in the aged mice.
Guo, X; Han, R; Hsiao, WLW; Huang, G; Khan, I; Law, BYK; Leong, W; Li, X; Liao, W; Liu, L; Wong, VKW; Xia, C; Xia, W; Yin, L, 2021
)
2.79
"Icariin treatment reversed the dexamethasone (DXM)‑induced disequilibrium of calcium homeostasis and bone resorption, and increased serum alkaline phosphatase, tartrate resistant acid phosphatase, osteocalcin and deoxypyridinoline."( Icariin ameliorates dexamethasone‑induced bone deterioration in an experimental mouse model via activation of microRNA‑186 inhibition of cathepsin K.
Huang, J; Ma, Y; Yang, H, 2018
)
2.64
"Icariin‑treated ATDC5 cells and primary chondrocytes expressed IFT88."( Role of IFT88 in icariin‑regulated maintenance of the chondrocyte phenotype.
Dong, Y; Guo, F; Wang, L; Wang, R; Wang, S; Wu, Y; Xiang, W; Xu, T; Zhang, J, 2018
)
1.54
"Icariin treatment also induced DNA damage in HCT116 cells."( Icariin reduces human colon carcinoma cell growth and metastasis by enhancing p53 activities.
Tian, M; Yan, X; Yang, S, 2018
)
2.64
"Icariin-treated mice showed significantly reduced serum anti-dsDNA antibody level and immune complex deposition."( Icariin alleviates murine lupus nephritis via inhibiting NF-κB activation pathway and NLRP3 inflammasome.
Chen, X; Li, L; Ni, H; Su, B; Ye, H; You, X, 2018
)
2.64
"The icariin 30 mg/kg-treated group regained body weight at 7 and 8 d post TBI."( Icariin Improves Functional Behavior in a Mouse Model of Traumatic Brain Injury and Promotes Synaptic Plasticity Markers.
Bae, J; Bang, Y; Bu, Y; Cho, JH; Joo, H; Lee, BJ; Lee, JS; Lee, K; Park, JW, 2019
)
2.44
"Icariin treatment also significantly inhibited the increased Smad2/3 and decreased E-cadherin protein expressions in the kidneys of UUO mice."( The antifibrotic and anti-inflammatory effects of icariin on the kidney in a unilateral ureteral obstruction mouse model.
Chen, CM; Chen, HA; Chiang, CK; Guan, SS; Liu, SH; Wu, CT, 2019
)
1.49
"Icariin treatment protects against CKD-associated renal fibrosis via its antifibrotic and anti-inflammatory properties. "( The antifibrotic and anti-inflammatory effects of icariin on the kidney in a unilateral ureteral obstruction mouse model.
Chen, CM; Chen, HA; Chiang, CK; Guan, SS; Liu, SH; Wu, CT, 2019
)
2.21
"Icariin treatment can effectively prevent both bone loss in osteoporosis and alveolar bone resorption induced by periodontitis."( [Effect of oral administration of icariin on periodontitis associated alveolar bone resorption in an osteoporosis mouse model].
Luo, Y; Tao, ML; Yang, W; Zhao, P, 2019
)
2.24
"Icariin treatment rapidly induced extracellular signal-regulated kinase (ERK) and c-Jun N terminal kinase (JNK) activation but showed no effect on activation of p38 kinase."( Icariin induces osteoblast proliferation, differentiation and mineralization through estrogen receptor-mediated ERK and JNK signal activation.
Li, H; Song, L; Zhang, X; Zhao, J; Zhou, Y, 2013
)
2.55
"Icariin treatment significantly increased the blastocyst cell numbers (47.02 ± 4.93 vs."( The regulatory role of icariin on apoptosis in mouse preimplantation embryos with reduced microRNA-21.
Cao, YC; Gao, JM; Jia, ZY; Liu, FH; Liu, XR; Shi, YR; Tian, JL; Zhang, C; Zhen, D, 2014
)
1.43
"Icariin treatment in mice with CIA also resulted in less number of Th17 cells and decreased ratio of CD4(+)IL-17(+) cells."( A natural flavonoid glucoside, icariin, regulates Th17 and alleviates rheumatoid arthritis in a murine model.
Chi, L; Gao, W; Lu, X; Shu, X, 2014
)
1.41
"Icariin-treated mice also show lower frequency of Th17 cells in CNS mononuclear cells."( A natural flavonoid glucoside icariin inhibits Th1 and Th17 cell differentiation and ameliorates experimental autoimmune encephalomyelitis.
Deng, W; Li, C; Shen, R; Zeng, G, 2015
)
1.43
"Icariin treatment resulted in a reduced expression of p-P38 and p-ERK signal activation induced by TNF-α/IFN-γ; however, only SB203580, the p38 alpha/beta inhibitor, inhibited the secretion of inflammatory cytokines induced by TNF-α/IFN-γ in cultured HaCaT cells."( Icariin inhibits TNF-α/IFN-γ induced inflammatory response via inhibition of the substance P and p38-MAPK signaling pathway in human keratinocytes.
Dong, J; Kong, L; Liu, B; Liu, J; Liu, Y; Luo, Q; Pang, Q; Wang, J; Xu, F; Zhang, H, 2015
)
2.58
"Icariin treatment also decreased the levels of extracellular and intracellular Aβ1-42 in 3 × Tg-AD primary neurons, modulated the distribution of Aβ along the neurites, and protected against mitochondrial fragmentation in 3 × Tg-AD neurons."( Neuroprotective Effects of Icariin on Brain Metabolism, Mitochondrial Functions, and Cognition in Triple-Transgenic Alzheimer's Disease Mice.
Chen, YJ; Han, SX; He, XY; Huang, XX; Ni, JZ; Zhang, DS; Zheng, HY, 2016
)
1.45
"Icariin pretreatment could ameliorate the decreased striatum DA content and the loss of TH-IR neurons in the SNpc induced by MPTP. "( Neuroprotective properties of icariin in MPTP-induced mouse model of Parkinson's disease: Involvement of PI3K/Akt and MEK/ERK signaling pathways.
Chen, L; Chen, WF; Chen, XH; Du, ZR; Teng, JJ; Wong, MS; Wu, L; Xu, AL, 2017
)
2.19
"Icariin treatment also ameliorated chronic cerebral hypoperfusion-induced oxidative stress in the brain, as evidenced by reduced malondialdehyde formation and maintained superoxide dismutase activity."( Protective effects of icariin on cognitive deficits induced by chronic cerebral hypoperfusion in rats.
Gong, QH; Huang, XN; Luo, Y; Shi, JS; Sun, AS; Wu, Q; Xu, RX; Yu, LM, 2009
)
1.39
"With icariin treatment, the BMP-2, SMAD4, Cbfa1/Runx2, and OPG gene expressions were up-regulated; the RANKL gene expression was however down-regulated."( Icariin isolated from Epimedium pubescens regulates osteoblasts anabolism through BMP-2, SMAD4, and Cbfa1 expression.
Chen, MH; Hsieh, TP; Liu, MH; Sheu, SY; Sun, JS, 2010
)
2.26
"Icariin pretreatment can partially reverse these effects."( Icariin protects murine chondrocytes from lipopolysaccharide-induced inflammatory responses and extracellular matrix degradation.
Chen, MH; Liu, MH; Sheu, SY; Sun, JS; Tsai, SW, 2010
)
2.52
"Icariin-treated animals also had a significantly greater expression of nicotinamide adenine dinucleotide phosphate-positive nerves and the endothelial cell markers, von Willebrand factor (vWF), and platelet endothelial cell adhesion molecule-1 (PECAM)."( Effects of icariin on improving erectile function in streptozotocin-induced diabetic rats.
Cui, WS; Gao, ZZ; Gong, YQ; Li, GY; Li, WR; Liu, T; Qin, XC; Shindel, AW; Xin, H; Xin, ZC; Zhou, F, 2011
)
1.48
"Icariin treatment preserved penile hemodynamics, smooth muscle and endothelial integrity, and neuronal nitric oxide synthase expression in the penis of diabetic rats. "( Effects of icariin on improving erectile function in streptozotocin-induced diabetic rats.
Cui, WS; Gao, ZZ; Gong, YQ; Li, GY; Li, WR; Liu, T; Qin, XC; Shindel, AW; Xin, H; Xin, ZC; Zhou, F, 2011
)
2.2
"Icariin treatment led to greater trabecular bone volume and trabecular number compared with vehicle treatment in WT mice. "( The beneficial effect of Icariin on bone is diminished in osteoprotegerin-deficient mice.
Feng, Y; Peng, S; Shao, ZW; Wu, W; Yang, C; Yang, SH; Zhen, WX; Zheng, D, 2012
)
2.13
"The Icariin-treated groups displayed decreased RRI values, decreased osteoclast numbers and activity levels, and increased OPG/RANKL expression ratios."( Icariin enhances the healing of rapid palatal expansion induced root resorption in rats.
Lin, S; Liu, Z; Lu, H; Wang, F; Xu, J, 2012
)
2.3
"(2) Icariin treatment also improved the steady-state serum BGP and might have promoted bone formation."( The testosterone mimetic properties of icariin.
Yang, QT; Zhang, ZB, 2006
)
1.08
"Icariin treatment (60 and 120 mg/kg, by gavage for 3 months) dose-dependently protected against the development of aluminium-induced spatial learning and memory deficits."( Protective effects of icariin against learning and memory deficits induced by aluminium in rats.
Gong, QH; Lu, YF; Luo, Y; Nie, J; Shi, JS; Wu, Q, 2007
)
1.38
"Treatment with icariin relieved the elevated protein and mRNA levels of group I mGluR receptors as well as the diminished protein and mRNA levels of EAAT2 in the PRS male offspring."( Antidepressant-like activity of icariin mediated by group I mGluRs in prenatally stressed offspring.
Dang, S; Lin, T; Su, Q; Sun, H; Zhang, H; Zhang, J; Zhang, X; Zhu, Z, 2017
)
1.08
"Pretreatment with icariin protected cardiomyocytes from I/R-induced oxidative stress through activation of sirtuin-1 /FOXO1 signalling."( Icariin protects cardiomyocytes against ischaemia/reperfusion injury by attenuating sirtuin 1-dependent mitochondrial oxidative damage.
Chen, YQ; Di, SY; Fan, CX; Feng, JY; Feng, X; Ha, XQ; Han, JS; Ma, ZQ; Wang, YC; Wei, Y; Wu, B; Yu, LM; Zhang, Y, 2018
)
2.26
"Treatment with icariin obviously induced de novo P-gp expression, decreased oxidative stress, and promoted osteogenesis."( Icariin may benefit the mesenchymal stem cells of patients with steroid-associated osteonecrosis by ABCB1-promoter demethylation: a preliminary study.
Hu, S; Kan, WS; Mo, FB; Sun, ZB; Wang, JW; Xiao, H; Ye, SN; Zhang, QS, 2015
)
2.2
"Treatment with icariin promoted hair shaft elongation, prolonged the hair cycle growth phase (anagen) in cultured VHFs, and accelerated transition of hair cycle from telogen to anagen phase in the dorsal skin of mice. "( Icariin promotes mouse hair follicle growth by increasing insulin-like growth factor 1 expression in dermal papillary cells.
Fan, ZX; Hu, ZQ; Lin, BJ; Liu, H; Miao, Y; Su, YS; Xiao, SE, 2017
)
2.25
"Treatment of icariin promotes osteoblast MC3T3-E1 proliferation and differentiation in vitro, potentially owing to its role in increasing BMP-2 protein expression."( Icariin stimulates MC3T3-E1 cell proliferation and differentiation through up-regulation of bone morphogenetic protein-2.
Cao, H; Ke, Y; Qian, W; Zhang, CJ; Zhang, GL; Zhang, Y, 2012
)
2.17
"Treatment with icariin reduced the losing of body weight in diabetic rats. "( [Icariin reduces mitochondrial oxidative stress injury in diabetic rat hearts].
Bao, H; Chen, L, 2011
)
1.63
"Treatment with icariin for 8 weeks markedly improved the cardiac function, which may be related to reducing mitochondrial oxidative stress injuries in diabetic rats."( [Icariin reduces mitochondrial oxidative stress injury in diabetic rat hearts].
Bao, H; Chen, L, 2011
)
1.63
"Treatment with icariin (final concentration 0.25, 0.5, and 1 mg/L) during ischemia/reperfusion-mimetic incubation in vitro concentration-dependently attenuated neuronal damage with characteristics of increasing injured neuronal absorbance of MTT, decreasing LDH release, decreasing cell apoptosis, and blunting elevation of intracellular calcium concentration. "( Protective effects of icariin on neurons injured by cerebral ischemia/reperfusion.
Li, L; Shi, JS; Zhou, QX, 2005
)
1
"Oral treatment with icariin ( 98.6 % purity) for 4 weeks potentially improves erectile function. "( Effects of icariin on erectile function and expression of nitric oxide synthase isoforms in castrated rats.
Guo, YL; Liu, WJ; Tian, L; Xin, H; Xin, ZC; Yuan, YM, 2005
)
1.04
"Treatment of icariin for 21 consecutive days mainly reversed the above effects in the mouse FST."( Antidepressant-like effect of icariin and its possible mechanism in mice.
Jiang, F; Kong, L; Pan, Y; Xia, X; Xia, Z; Zhang, W, 2005
)
0.97
"Treatment of icariin could significantly produce a relaxation of precontracted coronary arterial rings with intact endothelium in a concentration-dependent manner."( Vasorelaxant effects of icariin on isolated canine coronary artery.
Huang, ZQ; Xu, HB, 2007
)
1

Toxicity

ExcerptReferenceRelevance
" Our results showed that ICA reversed the adverse effect of DEHP on Leydig cell proliferation, and decreased ROS levels and elevated Δψm levels."( Icariin protects mouse Leydig cell testosterone synthesis from the adverse effects of di(2-ethylhexyl) phthalate.
Lian, X; Lin, J; Liu, Y; Lv, R; Mo, K; Sun, J; Wang, D; Wang, S; Xie, M; Xu, L; Xu, S, 2019
)
1.96

Pharmacokinetics

ICA-PG-liposomes changed the pharmacokinetic behaviour of epimedin A, B, C and icariin after intermuscular administration of Chuankezhi injection to rat.

ExcerptReferenceRelevance
" Calculated parameters confirmed usefulness of the method in rat pharmacokinetic studies on ICA."( Determination of icariin and metabolites in rat serum by capillary zone electrophoresis: rat pharmacokinetic studies after administration of icariin.
Liu, J; Lou, YJ, 2004
)
0.66
"As a prerequisite to the determination of pharmacokinetic parameters of icariin in rats, an HPLC method using UV detection was developed and validated."( HPLC analysis and pharmacokinetics of icariin in rats.
Cheng, S; He, J; Qiu, F; Wang, S, 2007
)
0.84
"In this research, pharmacokinetic comparisons of icariin, emodin and psoralen from the extracts of herba Epimedii, Nepal dock root and Ficus hirta yahl, and GKG were conducted."( In vivo pharmacokinetics comparisons of icariin, emodin and psoralen from gan-kang granules and extracts of herba Epimedii, Nepal dock root, Ficus hirta yahl.
Chen, Y; Duan, J; Guo, T; Li, B; Li, Y; Xie, W; Yan, S; Zhou, Y, 2009
)
0.87
"5, 2, 4, 6, 8, 12 and 24 h) after administration, the concentrations of icariin, emodin and psoralen in rat plasma were determined by HPLC-UV, and main pharmacokinetic parameters were estimated."( In vivo pharmacokinetics comparisons of icariin, emodin and psoralen from gan-kang granules and extracts of herba Epimedii, Nepal dock root, Ficus hirta yahl.
Chen, Y; Duan, J; Guo, T; Li, B; Li, Y; Xie, W; Yan, S; Zhou, Y, 2009
)
0.85
"The pharmacokinetic parameters of icariin, emodin and psoralen in GKG were elevated comparing with those of herb extracts."( In vivo pharmacokinetics comparisons of icariin, emodin and psoralen from gan-kang granules and extracts of herba Epimedii, Nepal dock root, Ficus hirta yahl.
Chen, Y; Duan, J; Guo, T; Li, B; Li, Y; Xie, W; Yan, S; Zhou, Y, 2009
)
0.9
"ICA-PG-liposomes changed the pharmacokinetic behaviour and enhanced icariin distribution in tissues."( Pharmacokinetics and tissue distribution profile of icariin propylene glycol-liposome intraperitoneal injection in mice.
Chen, XY; Lu, CT; Yang, W; Yu, XC; Zhang, L; Zhao, YZ, 2012
)
0.86
" The pharmacokinetic properties of bioactive ingredients in Herba Epimedii have also been discussed."( Pharmacological effects and pharmacokinetic properties of icariin, the major bioactive component in Herba Epimedii.
Li, C; Li, Q; Lu, T; Mei, Q, 2015
)
0.66
" The sensitive and selective method was applied to a pharmacokinetic study of icarrin, naringin and osthole in rats after oral administration of Gushudan capsule."( Simultaneous determination of icariin, naringin and osthole in rat plasma by UPLC-MS/MS and its application for pharmacokinetic study after oral administration of Gushudan capsules.
Deng, Y; Guo, X; Li, F; Li, N; Lu, Y; Xiong, Z; Zhao, L, 2015
)
0.71
"To study pharmacokinetic characteristics of epimedin A, B, C and icariin after intermuscular administration of Chuankezhi injection to rat."( [Pharmacokinetics of epimedin A, B, C and icariin of Chuankezhi injection in rat].
Sun, S; Xu, SJ; Xu, YJ; Yang, L; Yu, JJ; Zhu, YL, 2016
)
0.94
" The method was successfully applied to plasma pharmacokinetic and tissue distribution studies of icariin in rat."( Pharmacokinetics, Tissue Distribution, and Metabolism Study of Icariin in Rat.
Guo, L; Xu, S; Xu, Y; Yang, L; Yu, J; Zhan, J, 2017
)
0.91

Compound-Compound Interactions

Icariin combined with breviscapine has synergistic effects on erectile function of SHR. The aim of this study was to assess the efficacy and mechanisms of icariin in combination with daily sildenafil.

ExcerptReferenceRelevance
"Previous studies suggest that treatment with icariin (ICA) combined with Panax notoginseng saponins (PNS) improved behavior and cholinergic system disorders followed by amyloid beta-peptide(25-35) lateral ventricle injection in rats."( Effects of icariin combined with Panax notoginseng saponins on ischemia reperfusion-induced cognitive impairments related with oxidative stress and CA1 of hippocampal neurons in rat.
Lou, Y; Qu, L; Zheng, M, 2008
)
1
"To investigate the effect and mechanism of icariin combined with breviscapine on the erectile function of SHR."( Icariin combined with breviscapine improves the erectile function of spontaneously hypertensive rats.
Cheng, Y; Fan, Z; He, Y; Jiang, J; Jiang, R; Li, Y; Liu, J, 2014
)
2.11
"Icariin combined with breviscapine has synergistic effects on erectile function of SHR through different signal pathways."( Icariin combined with breviscapine improves the erectile function of spontaneously hypertensive rats.
Cheng, Y; Fan, Z; He, Y; Jiang, J; Jiang, R; Li, Y; Liu, J, 2014
)
3.29
"To optimize the process of Icraiin be hydrolyzed to Baohuoside I by cellulase by Plackett-Burman design combined with Central Composite Design (CCD) response surface methodology."( [Optimization of process of icraiin be hydrolyzed to Baohuoside I by cellulase based on Plackett-Burman design combined with CCD response surface methodology].
Chen, HM; Dai, Y; Deng, Y; Hu, J; Kang, M; Song, CX, 2014
)
0.4
"The optimum process of Icraiin be hydrolyzed to Baohuoside I by cellulase is determined by Plackett-Burman design combined with CCD response surface methodology."( [Optimization of process of icraiin be hydrolyzed to Baohuoside I by cellulase based on Plackett-Burman design combined with CCD response surface methodology].
Chen, HM; Dai, Y; Deng, Y; Hu, J; Kang, M; Song, CX, 2014
)
0.4
" The aim of this study was to assess the efficacy and mechanisms of icariin in combination with daily sildenafil on neurogenic erectile dysfunction and penile atrophy in a rat model of bilateral cavernous nerves injury."( Effect of icariin in combination with daily sildenafil on penile atrophy and erectile dysfunction in a rat model of bilateral cavernous nerves injury.
Fu, X; Guan, R; Lei, H; Wu, Y; Xin, H; Xin, Z; Xu, Y; Yang, Y, 2017
)
1.09
" This study aimed to investigate the therapeutic effects of icariin combined with adipose-derived stem cells on osteoporosis in a postmenopausal osteoporosis model after ovariectomy in rats."( Therapeutic effect of icariin combined with stem cells on postmenopausal osteoporosis in rats.
Ju, C; Liu, Y; Tang, D; Wang, D; Wang, Z; Xu, F, 2018
)
1.04
" The aforementioned results suggested that such a strategy of icariin combined with the snailase held a great potential in promoting the intestinal hydrolysis and absorption of icariin in the osteoporosis status, providing new research ideas for the active ingredients of traditional Chinese medicine with similar properties."( Icariin combined with snailase shows improved intestinal hydrolysis and absorption in osteoporosis rats.
Chen, Y; Gao, X; Huang, M; Liu, C; Liu, Y; Qu, D, 2017
)
2.14
"ICS combined with CSSH could promote the repair of osteochondral defect in rabbit knees."( Repair of osteochondral defect using icariin-conditioned serum combined with chitosan in rabbit knees.
Ji, Q; Jiao, J; Liu, A; Ming, D; Shang, M; Zhang, C; Zhang, J, 2020
)
0.83
"ICS combined with CSSH attenuated cartilage injury and abnormal subchondral remodeling in rabbits with KOA."( Icariin-conditioned serum combined with chitosan attenuates cartilage injury in rabbit knees with osteochondral defect.
Fan, F; Liu, A; Meng, L; Shang, M; Zhang, C; Zhang, J, 2023
)
2.35
"ICS combined with CSSH could promote the repair of osteochondral defect and stabilize subchondral bone remodeling in rabbit knees."( Icariin-conditioned serum combined with chitosan attenuates cartilage injury in rabbit knees with osteochondral defect.
Fan, F; Liu, A; Meng, L; Shang, M; Zhang, C; Zhang, J, 2023
)
2.35

Bioavailability

Icariin has a significant anti-osteoporotic activity, but its clinical application is limited due to a poor oral bioavailability. Some ingredients in GKG may increase the dissolution and absorption of icariin, emodin and psoralen in rats.

ExcerptReferenceRelevance
"Poor bioavailability of prenylated flavonoids results from their poor intrinsic permeation and transporter-mediated efflux."( Intestinal absorption mechanisms of prenylated flavonoids present in the heat-processed Epimedium koreanum Nakai (Yin Yanghuo).
Chen, Y; Hu, M; Jia, XB; Zhao, YH, 2008
)
0.35
" Some ingredients in GKG may increase the dissolution and absorption, and improve bioavailability of icariin, emodin and psoralen in rats."( In vivo pharmacokinetics comparisons of icariin, emodin and psoralen from gan-kang granules and extracts of herba Epimedii, Nepal dock root, Ficus hirta yahl.
Chen, Y; Duan, J; Guo, T; Li, B; Li, Y; Xie, W; Yan, S; Zhou, Y, 2009
)
0.84
" Icariin with the poor solubility and low bioavailability limited the treatment of many diseases in clinic."( Colon targeted oral drug delivery system based on alginate-chitosan microspheres loaded with icariin in the treatment of ulcerative colitis.
Cui, YL; Gao, LN; Wang, GF; Wang, QS; Zhou, J, 2016
)
1.56
"Icariin has a significant anti-osteoporotic activity, but its clinical application is limited due to a poor oral bioavailability especially under pathological conditions like osteoporosis."( Icariin combined with snailase shows improved intestinal hydrolysis and absorption in osteoporosis rats.
Chen, Y; Gao, X; Huang, M; Liu, C; Liu, Y; Qu, D, 2017
)
3.34
" Furthermore, Preliminary pharmacokinetics evaluation also indicated an excellent oral bioavailability of 29."( Synthesis and biological evaluation of methylpyrimidine-fused tricyclic diterpene analogs as novel oral anti-late-onset hypogonadism agents.
Bai, J; Liu, M; Liu, T; Qiu, WW; Tang, J; Wang, LT; Xie, J; Xing, Y; Yang, F; Yi, Z, 2019
)
0.51
" Typical osteoporosis fracture treatments, such as bisphosphonates and hormone replacement, present important challenges because of their low bioavailability on the site of action."( In vitro effects of the co-release of icariin and strontium from bioactive glass submicron spheres on the reduced osteogenic potential of rat osteoporotic bone marrow mesenchymal stem cells.
Barrioni, BR; Martins, T; Mosqueira, L; Ocarino, NM; Pereira, MM; Serakides, R, 2020
)
0.83
"Although icariin has been reported to have antidepressant-like effects in different animal models, its poor oral bioavailability and low efficiency of delivery to the brain limit its application."( Intranasal delivery of icariin via a nanogel-thermoresponsive hydrogel compound system to improve its antidepressant-like activity.
Cui, YL; Hu, MJ; Kou, N; Lu, YR; Wang, QS; Xu, D, 2020
)
1.29
" All these strategies manage to improve the bioavailability of the above-mentioned flavonoids, thus increasing their concentration in the desired places."( Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review.
Dulf, FV; Rácz, CP; Szabó, R, 2022
)
0.98
" However, pharmacokinetic studies have shown that its poor bioavailability limited its application."( Nanotherapy for bone repair: milk-derived small extracellular vesicles delivery of icariin.
Dong, J; Dong, M; Han, W; Kong, Y; Liu, T; Niu, W; Wang, L; Yang, Q; Yu, X, 2023
)
1.14

Dosage Studied

Icariin at 10(-6)M (a physiologically achievable concentration in vivo) activated this signal pathway. Ten participants with bipolar I or bipolar II disorders, currently depressed, and with active alcohol abuse or dependence were given open-label icariin of up to 300 mg/day for 8 weeks.

ExcerptRelevanceReference
" Icarrin also exerted a stimulatory effect on corticosterone production at the highest dosage (1000 micrograms/L)."( [Effects of icarrin on secretive function of cultured granulosa and adrenal cortical cells of rats].
Li, E; Li, F; Lu, Z; Song, S; Tong, X; Wang, X, 1997
)
0.3
"Female Wistar rats were ovariectomized and administered different dosage of Icariin and 17beta-estradiol for eight weeks."( [Effects of Icariin on ovariectomized osteoporotic rats].
Bao, JR; Li, SF; Yan, Y; Yang, JW; Zhang, Q; Zhao, W, 2005
)
0.94
"The epididymis impair was induced by injection of streptozocin at dosage of 60 mg/kg ip in SD rats."( [Amelioration of icariin for the epididymis impairment induced by streptozocin (STZ) in rats].
Gong, Y; Liu, HR; Qi, MY; Shi, J; Xie, GY, 2013
)
0.73
" Furthermore, dosage response studies showed that icariin at 10(-6)M (a physiologically achievable concentration in vivo) also activated this signal pathway."( Icariin stimulates the osteogenic differentiation of rat bone marrow stromal cells via activating the PI3K-AKT-eNOS-NO-cGMP-PKG.
Chen, KM; Ge, BF; Guo, XY; Ma, HP; Ma, XN; Xian, CJ; Zhai, YK; Zhen, P; Zhou, J, 2014
)
2.1
"In vivo, BALB/c mice were exposed to smoke of 15 cigarettes for 1 h/day, 6 days/week for 3 months and dosed with icariin (25, 50 and 100 mg/kg) or dexamethasone (1 mg/kg)."( Icariin ameliorates cigarette smoke induced inflammatory responses via suppression of NF-κB and modulation of GR in vivo and in vitro.
Dong, J; Li, L; Liu, B; Sun, J; Wu, J; Xu, C; Zhang, H, 2014
)
2.06
"Ten participants with bipolar I or bipolar II disorders, currently depressed, and with active alcohol abuse or dependence were given open-label icariin of up to 300 mg/day for 8 weeks using a flexible dosing strategy."( An open-label pilot study of icariin for co-morbid bipolar and alcohol use disorder.
Brown, ES; Wignall, N; Xiao, H, 2016
)
0.93
"The findings of the present study demonstrated that low dosage of icariin could promote BMSCs proliferation."( [Wnt/β-catenin signaling is involved in the Icariin induced proliferation of bone marrow mesenchymal stem cells].
Fu, S; Hong, H; Yang, L; Zhang, R, 2016
)
0.93
" BLIN stimulated total anti-DHAV-1 antibody secretion in ducklings at the dosage of 4 mg per duckling, but did not stimulate IL-2 and IFN-γ secretion significantly."( Anti-DHAV-1 reproduction and immuno-regulatory effects of a flavonoid prescription on duck virus hepatitis.
Chen, Y; Hu, Y; Liu, J; Wang, D; Wang, Y; Wu, Y; Yang, J; Yao, F; Zeng, L, 2017
)
0.46
"In a puncture-induced LBP rat model, the severity of LBP was quantified using the paw/foot withdrawal threshold method after intragastric administration of ICA at a dosage of 50 mg/kg/d or 100 mg/kg/d."( Icariin Ameliorates Lower Back Pain in Rats via Suppressing the Secretion of Cytokine-Induced Neutrophil Chemoatractant-1.
Guo, Z; Han, Z; Jin, G; Li, J; Luo, M; Ma, Y; Tang, G; Wang, S, 2020
)
2
"ICA treatment resulted in a significant amelioration of mechanical allodynia in a dose-response manner, and the analgesic effect could last for two weeks even during the washout period."( Icariin Ameliorates Lower Back Pain in Rats via Suppressing the Secretion of Cytokine-Induced Neutrophil Chemoatractant-1.
Guo, Z; Han, Z; Jin, G; Li, J; Luo, M; Ma, Y; Tang, G; Wang, S, 2020
)
2
"Icariin at the dosage of 100 mg/kg/d and 200 mg/kg/d markedly ameliorated rat renal function in a dose-dependent manner."( Icariin, the main prenylflavonoid of Epimedii Folium, ameliorated chronic kidney disease by modulating energy metabolism via AMPK activation.
Lu, J; Lv, C; Yang, W; Zhang, X; Zhao, Y, 2023
)
3.8
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
bone density conservation agentAn agent that inhibits bone resorption and/or favor bone mineralization and bone regeneration. Used to heal bone fractures and to treat bone diseases such as osteopenia and osteoporosis.
phytoestrogenAny compound produced by a plant that happens to have estrogenic activity.
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitorAn EC 3.1.4.* (phosphoric diester hydrolase) inhibitor that blocks the action of 3',5'-cyclic-GMP phosphodiesterase (EC 3.1.4.35).
antioxidantA substance that opposes oxidation or inhibits reactions brought about by dioxygen or peroxides.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
glycosyloxyflavoneA member of the class of flavones having one or more glycosyl residues attached at unspecified positions.
flavonolsAny hydroxyflavone in which is the ring hydrogen at position 3 of the heterocyclic ring is replaced by a hydroxy group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency11.22020.003245.467312,589.2998AID2517
Chain A, Beta-lactamaseEscherichia coli K-12Potency12.58930.044717.8581100.0000AID485341
DNA polymerase betaHomo sapiens (human)Potency63.09570.022421.010289.1251AID485314
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Lysine-specific histone demethylase 1AHomo sapiens (human)IC50 (µMol)26.44000.00312.16029.6000AID1515260
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)5.90000.00001.18439.6140AID362785
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
regulation of double-strand break repair via homologous recombinationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of protein ubiquitinationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of protein localizationLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to UVLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to gamma radiationLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair-dependent chromatin remodelingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuroblast proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
protein demethylationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of epithelial to mesenchymal transitionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuron projection developmentLysine-specific histone demethylase 1AHomo sapiens (human)
cerebral cortex developmentLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
neuron maturationLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cell sizeLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-templated transcriptionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
guanine metabolic processLysine-specific histone demethylase 1AHomo sapiens (human)
muscle cell developmentLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of androgen receptor signaling pathwayLysine-specific histone demethylase 1AHomo sapiens (human)
response to fungicideLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to cAMPLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cold-induced thermogenesisLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neural precursor cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of stem cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin remodelingLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
telomeric DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
p53 bindingLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
oxidoreductase activityLysine-specific histone demethylase 1AHomo sapiens (human)
enzyme bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear receptor coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K4 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
identical protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
MRF bindingLysine-specific histone demethylase 1AHomo sapiens (human)
flavin adenine dinucleotide bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear androgen receptor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
telomeric repeat-containing RNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
FAD-dependent H3K4me/H3K4me3 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
promoter-specific chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
chromatinLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
chromosome, telomeric regionLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
nucleoplasmLysine-specific histone demethylase 1AHomo sapiens (human)
transcription regulator complexLysine-specific histone demethylase 1AHomo sapiens (human)
protein-containing complexLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair complexLysine-specific histone demethylase 1AHomo sapiens (human)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (17)

Assay IDTitleYearJournalArticle
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID428313Reversal of P-gp-mediated multidrug resistance in human MCF7 cells assessed as assessed as increase in intracellular adriamycin accumulation at 5 uM incubated 2 hrs before adriamycin challenge by spectrophotometry2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis and antimultidrug resistance evaluation of icariin and its derivatives.
AID1515260Inhibition of LSD1 (unknown origin) by fluorescence assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Flavone-based natural product agents as new lysine-specific demethylase 1 inhibitors exhibiting cytotoxicity against breast cancer cells in vitro.
AID671761Inhibition of SARS coronavirus nsP13 helicase activity expressed in Escherichia coli Rosetta assessed inhibition of DNA unwinding activity at 10 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of myricetin and scutellarein as novel chemical inhibitors of the SARS coronavirus helicase, nsP13.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1555262Cytotoxicity against mouse TM3 cells assessed as reduction in cell viability measured after 24 hrs by sulforhodamine B assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of methylpyrimidine-fused tricyclic diterpene analogs as novel oral anti-late-onset hypogonadism agents.
AID671764Inhibition of HCV NS3 helicase ATP hydrolysis activity overexpressed in Escherichia coli BL21(DE3) assessed as inhibition of inorganic phosphate release by AM/MG-based colometric analysis in the presence of M13 ssDNA2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of myricetin and scutellarein as novel chemical inhibitors of the SARS coronavirus helicase, nsP13.
AID1555261Induction of testosterone production in mouse TM3 cells assessed as increase in testosterone level at 20 uM measured after 24 hrs by ELISA relative to control2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of methylpyrimidine-fused tricyclic diterpene analogs as novel oral anti-late-onset hypogonadism agents.
AID1256912Inhibition of human IDH1 R132H mutant expressed in IPTG-induced Escherichia coli BL21 cells assessed as oxidation of NADPH to NADP+ after 5 mins by spectrophotometry2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Discovery of α-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1.
AID1256913Inhibition of human IDH1 expressed in IPTG-induced Escherichia coli BL21 cells assessed as reduction of NADP+ to NADPH after 5 mins by spectrophotometry2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Discovery of α-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1.
AID362788Inhibition of human PDE6C at 10 uM2008Journal of natural products, Sep, Volume: 71, Issue:9
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
AID362785Inhibition of human recombinant PDE5A1 expressed in COS7 cells2008Journal of natural products, Sep, Volume: 71, Issue:9
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID671762Inhibition of HCV NS3 helicase overexpressed in Escherichia coli BL21(DE3) assessed as inhibition of DNA unwinding activity at 10 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of myricetin and scutellarein as novel chemical inhibitors of the SARS coronavirus helicase, nsP13.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (766)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (0.26)18.7374
1990's19 (2.48)18.2507
2000's90 (11.75)29.6817
2010's453 (59.14)24.3611
2020's202 (26.37)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.78

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index42.78 (24.57)
Research Supply Index6.66 (2.92)
Research Growth Index5.95 (4.65)
Search Engine Demand Index125.13 (26.88)
Search Engine Supply Index3.81 (0.95)

This Compound (42.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (0.64%)5.53%
Reviews38 (4.89%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other734 (94.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]