Page last updated: 2024-11-12

glaucocalyxin a

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Description

glaucocalyxin A: chemical constituent of Rabdosia japonica var. glaucocalyx [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
Rabdosiagenus[no description available]LamiaceaeThe mint plant family. They are characteristically aromatic, and many of them are cultivated for their oils. Most have square stems, opposite leaves, and two-lipped, open-mouthed, tubular corollas (united petals), with five-lobed, bell-like calyxes (united sepals).[MeSH]
Rabdosia japonicaspecies[no description available]LamiaceaeThe mint plant family. They are characteristically aromatic, and many of them are cultivated for their oils. Most have square stems, opposite leaves, and two-lipped, open-mouthed, tubular corollas (united petals), with five-lobed, bell-like calyxes (united sepals).[MeSH]

Cross-References

ID SourceID
PubMed CID10471963
CHEMBL ID549359
MeSH IDM0155336

Synonyms (13)

Synonym
glaucocalyxin a
CHEMBL549359
79498-31-0
AC-34443
7alpha,14beta-dihydroxy-ent-kaur-16-ene-3,5-dione
CS-0018634
HY-N2112
AKOS037514678
(1r,2r,4s,9r,10s,13s,16r)-2,16-dihydroxy-5,5,9-trimethyl-14-methylidenetetracyclo[11.2.1.01,10.04,9]hexadecane-6,15-dione
wangzaozin b
leukamenin f
MS-25010
bdbm50552053

Research Excerpts

Overview

Glaucocalyxin A (GLA) is an alkaloid derived from a Chinese medicinal plant that exhibits anti-inflammatory, anti-tumor and neuroprotective properties. The compound has been found to ameliorate myocardial I/R injury in mice.

ExcerptReferenceRelevance
"Glaucocalyxin A (GLA) is a bioactive natural compound with anti-inflammatory activity. "( Glaucocalyxin A Attenuates IL-1
Li, Y; Wu, H; Zhang, Y; Zhu, W, 2022
)
3.61
"Glaucocalyxin A (GLA) is a bioactive ent-kauranoid diterpenoid derived from the herbal medicine, Rabdosia japonica var. "( Glaucocalyxin A alleviates LPS-mediated septic shock and inflammation via inhibiting NLRP3 inflammasome activation.
Ai, Y; Bai, Z; Chen, Y; Hou, X; Li, H; Li, R; Shi, W; Wang, C; Wang, Z; Xiao, X; Xu, G; Zhan, X, 2020
)
3.44
"Glaucocalyxin A (GLA) is a biologically active ent-kauranoid diterpenoid that has been found to ameliorate myocardial I/R injury in mice."( Glaucocalyxin A Protects H9c2 Cells Against Hypoxia/Reoxygenation-Induced Injury Through the Activation of Akt/Nrf2/HO-1 Pathway.
Dang, X; Lv, J; Niu, Z; Pan, L; Pei, H; Peng, Z; Wang, H; Zhang, R,
)
2.3
"Glaucocalyxin A (GLA) is an alkaloid derived from a Chinese medicinal plant that exhibits anti-inflammatory, anti-tumor and neuroprotective properties."( Glaucocalyxin A suppresses inflammatory responses and induces apoptosis in TNF-a-induced human rheumatoid arthritis via modulation of the STAT3 pathway.
Li, W; Ma, K; Wang, F; Yang, Y; Zhang, C, 2021
)
2.79
"Glaucocalyxin A (GLA) is a diterpenoid component isolated from Rabdosia japonica var."( Glaucocalyxin A induces apoptosis and autophagy in tongue squamous cell carcinoma cells by regulating ROS.
Jiang, Q; Qiu, J; Shi, F; Xue, D, 2021
)
2.79
"Glaucocalyxin A (GLA) is a biologically active ent-kauranoid diterpenoid isolated from Rabdosia japonica var. "( Glaucocalyxin A Attenuates the Activation of Hepatic Stellate Cells Through the TGF-β1/Smad Signaling Pathway.
Dong, Z; Gao, Q; Guo, H, 2018
)
3.37
"Glaucocalyxin A (GLA) is a natural ent-Kaurane diterpenoid that possesses cardioprotective effect. "( Glaucocalyxin A attenuates angiotensin II-induced cardiac fibrosis in cardiac fibroblasts.
Su, Q; Zhang, Y, 2018
)
3.37
"Glaucocalyxin A (GLA), is a diterpenoid extracted from Hara and has been studied for decades for its diverse bioactivities. "( Preparation, optimization of the inclusion complex of glaucocalyxin A with sulfobutylether-β-cyclodextrin and antitumor study.
Chen, G; Ren, L; Wang, J, 2019
)
2.21
"Glaucocalyxin A is a natural ent-Kaurane diterpenoid. "( Glaucocalyxin A: a review.
Jin, Y; Liu, X; Wu, X; Xiang, Z, 2014
)
3.29
"Glaucocalyxin A (GLA) is a biologically active ent-kauranoid diterpenoid isolated from Rabdosia japonica var. "( Glaucocalyxin A induces apoptosis in human leukemia HL-60 cells through mitochondria-mediated death pathway.
Gao, LW; Wang, B; Wang, JW; Yang, WH; Zhang, J, 2011
)
3.25
"Glaucocalyxin A (Gla A) is a new diterpenoid isolated from ethereal extract of the leaves of Rabdosia japonica (Burm f) Hara var glaucocalyx (Maxim) Hara (Labiatae) collected in Northeastern China. "( Effects of glaucocalyxin A on aggregation and cAMP levels of rabbit platelets in vitro.
Long, K; Zhang, B, 1993
)
2.12
"Glaucocalyxin A is a new diterpenoid isolated from the ethereal extract of the leaves of Rabdosia japonica (Burm f) Hara var glaucocalyx (Maxim) Hara (Labiatae) collected in the northeastern China. "( Inhibition by glaucocalyxin A of aggregation of rabbit platelets induced by ADP, arachidonic acid and platelet-activating factor, and inhibition of [3H]-PAF binding.
Bin, Z; Kun, L, 1992
)
2.09

Pharmacokinetics

ExcerptReferenceRelevance
" A pharmacokinetic analysis of glaucocalyxin A after intravenous administration in rats revealed that glaucocalyxin A followed a two-compartment open model."( Pharmacokinetic analysis of glaucocalyxin A in rat plasma by liquid-liquid extraction and HPLC.
Cao, L; Chen, Z; Li, Y; Shen Li, Y; Sun, J, 2009
)
0.93

Bioavailability

ExcerptReferenceRelevance
"The purpose of this study was to develop a new formulation to enhance the bioavailability simultaneously with controlled release of glaucocalyxin A (GLA)."( Controlled release of glaucocalyxin - a self-nanoemulsifying system from osmotic pump tablets with enhanced bioavailability.
Guoguang, C; Lili, R; Pingkai, O; Yanfei, M, 2017
)
0.66
"In this study, controlled release of GLA was achieved by the osmotic release strategy taking advantage of the bioavailability enhancing capacity of self-nanoemulsifying drug delivery systems (SNEDDS)."( Controlled release of glaucocalyxin - a self-nanoemulsifying system from osmotic pump tablets with enhanced bioavailability.
Guoguang, C; Lili, R; Pingkai, O; Yanfei, M, 2017
)
0.46
"It was concluded that simultaneous controlling on GLA release and enhanced bioavailability had been achieved by a combination of osmotic pump tablet and SNEDDS."( Controlled release of glaucocalyxin - a self-nanoemulsifying system from osmotic pump tablets with enhanced bioavailability.
Guoguang, C; Lili, R; Pingkai, O; Yanfei, M, 2017
)
0.46
" However, GLA presents poor solubility in water and low bioavailability through oral administration which has hindered its application in the clinic."( Preparation, optimization of the inclusion complex of glaucocalyxin A with sulfobutylether-β-cyclodextrin and antitumor study.
Chen, G; Ren, L; Wang, J, 2019
)
0.76
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Platelet glycoprotein VIHomo sapiens (human)IC50 (µMol)0.01150.00201.55884.0000AID1692274; AID1692275
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (7)

Processvia Protein(s)Taxonomy
positive regulation of platelet aggregationPlatelet glycoprotein VIHomo sapiens (human)
enzyme-linked receptor protein signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
platelet activationPlatelet glycoprotein VIHomo sapiens (human)
collagen-activated tyrosine kinase receptor signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
collagen-activated signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
platelet aggregationPlatelet glycoprotein VIHomo sapiens (human)
immune response-regulating signaling pathwayPlatelet glycoprotein VIHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
transmembrane signaling receptor activityPlatelet glycoprotein VIHomo sapiens (human)
protein bindingPlatelet glycoprotein VIHomo sapiens (human)
collagen bindingPlatelet glycoprotein VIHomo sapiens (human)
signaling receptor activityPlatelet glycoprotein VIHomo sapiens (human)
collagen receptor activityPlatelet glycoprotein VIHomo sapiens (human)
protein tyrosine kinase bindingPlatelet glycoprotein VIHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
membrane raftPlatelet glycoprotein VIHomo sapiens (human)
plasma membranePlatelet glycoprotein VIHomo sapiens (human)
cell surfacePlatelet glycoprotein VIHomo sapiens (human)
extracellular exosomePlatelet glycoprotein VIHomo sapiens (human)
tetraspanin-enriched microdomainPlatelet glycoprotein VIHomo sapiens (human)
plasma membranePlatelet glycoprotein VIHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID1161858Induction of apoptosis in human KB cells assessed as early apoptotic cells level at 10 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 7.08%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161839Antiproliferative activity against human HL7702 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID426932Cytotoxicity against human SH-SY5Y cells after 48 hrs by SRB method2009Journal of natural products, Jun, Volume: 72, Issue:6
ent-Kaurane diterpenoids from Isodon pharicus.
AID1692275Antagonist activity at GP6 in human platelet assessed as reduction in CRP-induced platelet-aggregation preincubated for 10 mins followed by collagen stimulation by aggregometry2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
AID426933Cytotoxicity against human PC3 cells after 48 hrs by SRB method2009Journal of natural products, Jun, Volume: 72, Issue:6
ent-Kaurane diterpenoids from Isodon pharicus.
AID1161837Antiproliferative activity against human KB cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161860Induction of apoptosis in human KB cells assessed as necrotic cells level at 10 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 3.23%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID426931Cytotoxicity against human A549 cells after 48 hrs by SRB method2009Journal of natural products, Jun, Volume: 72, Issue:6
ent-Kaurane diterpenoids from Isodon pharicus.
AID1161865Chemical stability in 10 mM pH 7.4 PBS buffer assessed as parent compound remaining at 1 uM at 37 degC after 24 hrs by HPLC method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161864Induction of apoptosis in human KB cells assessed as necrotic cells level at 20 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 3.23%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID426934Cytotoxicity against human MCF7 cells after 48 hrs by SRB method2009Journal of natural products, Jun, Volume: 72, Issue:6
ent-Kaurane diterpenoids from Isodon pharicus.
AID1161855Induction of apoptosis in human KB cells assessed as late apoptotic cells level at 5 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 2.26%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161861Induction of apoptosis in human KB cells assessed as viable cells level at 20 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 87.4%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161840Induction of apoptosis in human KB cells after 48 hrs by Annexin V and propidium iodide staining based flow cytometry2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161867Prodrug conversion in human KB cells lysates assessed as formation of cysteine conjugates at 500 uM in presence of 10 mM cysteine by LC-HRMS method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161854Induction of apoptosis in human KB cells assessed as early apoptotic cells level at 5 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 7.08%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161838Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161866Stability in 80% rat plasma assessed as parent compound remaining at 1 uM at 37 degC after 24 hrs by HPLC method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161835Antiproliferative activity against human SGC7901 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID426930Cytotoxicity against human NB4 cells after 48 hrs by SRB method2009Journal of natural products, Jun, Volume: 72, Issue:6
ent-Kaurane diterpenoids from Isodon pharicus.
AID1692271Inhibition of ADP-induced platelet aggregation in rabbit platelet suspension preincubated for 10 mins followed by ADP stimulation by turbidimetric method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
AID1161863Induction of apoptosis in human KB cells assessed as late apoptotic cells level at 20 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 2.26%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161859Induction of apoptosis in human KB cells assessed as late apoptotic cells level at 10 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 2.26%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161834Antiproliferative activity against mouse B16 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1692273Inhibition of PAF-induced platelet aggregation in rabbit platelet suspension preincubated for 10 mins followed by PAF stimulation by turbidimetric method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
AID1161857Induction of apoptosis in human KB cells assessed as viable cells level at 10 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 87.4%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1692274Antagonist activity at GP6 in human platelet assessed as reduction in collagen-induced platelet-aggregation preincubated for 10 mins followed by collagen stimulation by aggregometry2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
AID1692272Inhibition of arachidonic acid-induced platelet aggregation in rabbit platelet suspension preincubated for 10 mins followed by AA stimulation by turbidimetric method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
AID1161869Retention time of the compound in human KB cells lysates treated with 500 uM oridonin in presence of 10 mM cysteine by LC-HRMS method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161856Induction of apoptosis in human KB cells assessed as necrotic cells level at 5 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 3.23%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161862Induction of apoptosis in human KB cells assessed as early apoptotic cells level at 20 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 7.08%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161836Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161853Induction of apoptosis in human KB cells assessed as viable cells level at 5 uM after 48 hrs by Annexin V and propidium iodide staining based flow cytometry (Rvb = 87.4%)2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
AID1161833Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and biological evaluation of glaucocalyxin A derivatives as potential anticancer agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (49)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (2.04)18.7374
1990's3 (6.12)18.2507
2000's4 (8.16)29.6817
2010's24 (48.98)24.3611
2020's17 (34.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.35

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.35 (24.57)
Research Supply Index3.95 (2.92)
Research Growth Index5.66 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (2.00%)5.53%
Reviews1 (2.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other48 (96.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]