Compounds > triptonide
Page last updated: 2024-12-06

triptonide

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Triptonide is a natural product isolated from the marine sponge Halichondria okadai. It is a potent antimitotic agent that inhibits microtubule assembly and induces apoptosis in cancer cells. Triptonide is a promising anticancer drug candidate, and several studies are investigating its mechanism of action and its potential therapeutic applications. Triptonide's unique structural features and its potent biological activity have attracted significant interest from researchers in the field of drug discovery. Its synthesis is a complex process that involves multiple steps and requires specialized expertise. Studies on Triptonide are important to understand its potential use in treating cancer and other diseases.'

triptonide: extracted from Tripterygium wilfordii; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

triptonide : A diterpene triepoxide that is triptobenzene K in which the acylhydroquinone moiety has undergone oxidation to the corresponding triepoxyketone derivative. It has been isolated from the roots of Tripterygium wilfordii. [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]

FloraRankFlora DefinitionFamilyFamily Definition
TripterygiumgenusA plant genus of the family CELASTRACEAE that is a source of triterpenoids and diterpene epoxides such as triptolide.[MeSH]CelastraceaeA plant family of the order Celastrales, subclass Rosidae, class Magnoliopsida.[MeSH]

Cross-References

ID SourceID
PubMed CID65411
CHEMBL ID205190
CHEBI ID132267
SCHEMBL ID4884926
MeSH IDM0223519

Synonyms (39)

Synonym
HY-32736
DIVK1C_006664
SPECTRUM_001724
SPECTRUM5_001806
38647-11-9
triptonide
nsc-165677
nsc165677
NCI60_001273
KBIO2_002204
KBIO2_007340
KBIO1_001608
KBIO2_004772
KBIOSS_002204
SPECTRUM2_000477
SPBIO_000614
SPECPLUS_000568
(3bs,4as,5as,6as,7as,7bs,8as,8bs)-6a-isopropyl-8b-methyl-3b,4,4a,7a,7b,8b,9,10-octahydrotrisoxireno[6,7:8a,9:4b,5]phenanthro[1,2-c]furan-1,6(3h,6ah)-dione
(-)-triptonide
CHEBI:132267
CHEMBL205190
S9416
CCG-38708
triptolide, 14-deoxy-14-oxo-
nsc 165677
CS-0318
AKOS015896754
SCHEMBL4884926
Q-100449
triptonide, >=98% (hplc)
BCP26007
(5bs,6as,7as,8as,9as,9bs,10as,10bs)-8a-isopropyl-10b-methyl-1,5b,6,6a,8a,9a,9b,10b-octahydrotris(oxireno)[2',3':4b,5;2'',3'':6,7;2''',3''':8a,9]phenanthro[1,2-c]furan-3,8(2h,5h)-dione
(5bs,6as,7as,8as,9as,9bs,10as,10bs)-8a-isopropyl-10b-methyl-2,5,5b,6,6a,9a,9b,10b-octahydrotris(oxireno)[2',3':4b,5;2'',3'':6,7;2''',3''':8a,9]phenanthro[1,2-c]furan-3,8(1h,8ah)-dione
triptolide,14-deoxy-14-oxo
trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1,6(3h,6ah)-dione,3b,4,4a,7a,7b,8b,9,10-octahydro-8b-methyl-6a-(1-methylethyl)-,(3bs,4as,5as,6as,7as,7bs,8as,8bs)-
pg 492
(1s,2s,4s,5s,7s,9s,11s,13s)-1-methyl-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-ene-8,17-dione
DTXSID801317412
EX-A7744

Research Excerpts

Overview

Triptonide is a key bioactive small molecule identified in a traditional Chinese medicine named Tripterygium wilfordii Hook F. It has a broad spectrum of biological functions.

ExcerptReferenceRelevance
"Triptonide ("TN") is a small molecule monomer extract from the ancient Chinese herb Tripterygium wilfordii Hook."( Triptonide inhibits human nasopharyngeal carcinoma cell growth via disrupting Lnc-RNA THOR-IGF2BP1 signaling.
Chen, MB; Lu, PH; Lv, Y; Song, Y; Wang, SS; Wu, GP; Xu, XC; Zhang, ZQ; Zuo, Y, 2019)		2.68
"Triptonide is a key bioactive small molecule identified in a traditional Chinese medicine named Tripterygium wilfordii Hook F., and it has a broad spectrum of biological functions."( Triptonide Effectively Inhibits Wnt/β-Catenin Signaling via C-terminal Transactivation Domain of β-catenin.
Aguilar, JS; Avalos, A; Cameron, DJ; Chinison, J; Hao, J; Huang, Y; Wang, Z, 2016)		2.6

Effects

Triptonide has been reported to have a strong inhibition activity in cancers through screening of Chinese herbal medicine.

ExcerptReferenceRelevance
"Triptonide reportedly has strong antitumor and anti-inflammatory activities. "( lncRNA involved in triptonide-induced cytotoxicity in mouse germ cells.
Chen, C; Zeng, X; Zhang, X; Zhong, Y, 2020)		2.33
"Triptonide has been reported to have a strong inhibition activity in cancers through screening of Chinese herbal medicine."( Triptonide acts as a novel antiprostate cancer agent mainly through inhibition of mTOR signaling pathway.
Chen, L; Chen, M; Dong, F; Jiang, M; Sun, W; Wang, A; Wang, R; Yang, P; Zhang, C; Zhang, Y, 2019)		2.68

Treatment

ExcerptReferenceRelevance
"Triptonide treatment strongly inhibited the colony formation-, migration-, and invasion-promoting capacities of GCAFs."( Triptonide inhibits the pathological functions of gastric cancer-associated fibroblasts.
Chen, Y; Gao, Y; Jia, Y; Liu, X; Ma, D; Wang, C; Wang, Z; Yang, Y; Yuan, J; Zeng, F; Zhu, Z, 2017)		2.62

Toxicity

ExcerptReferenceRelevance
" The goal of this study is to explore powerful and low toxic Lyn-targeted anti-lymphoma agent."( Triptonide acts as a novel potent anti-lymphoma agent with low toxicity mainly through inhibition of proto-oncogene Lyn transcription and suppression of Lyn signal pathway.
Dong, F; Yang, P; Zhou, Q, 2017)		1.9
" However, celastrol, triptolide and triptonide have certain toxic effects on the liver, kidney, cholangiocyte heart, ear and reproductive system."( A comprehensive review on celastrol, triptolide and triptonide: Insights on their pharmacological activity, toxicity, combination therapy, new dosage form and novel drug delivery routes.
Dai, L; He, GN; Song, J, 2023)		1.44

Compound-Compound Interactions

ExcerptReferenceRelevance
" by micellar electrokinetic capillary chromatography combined with cloud point extraction."( Determination of triptonide by cloud point extraction combined with MEKC.
Jiang, YY; Wu, YW; Xiao, TX; Zhang, HL, 2008)		0.69

Dosage Studied

ExcerptRelevanceReference
"The dosage of triptonide was 200 micrograms/(kg."( [Male contraception of triptonide and its function mechanism].
Guo, Y; Hui, L; Liu, X; Wang, L; Ye, W, 2000)		0.98
" Suitable combination therapy, new dosage forms and new routes of administration can effectively reduce toxicity and increase the effect."( A comprehensive review on celastrol, triptolide and triptonide: Insights on their pharmacological activity, toxicity, combination therapy, new dosage form and novel drug delivery routes.
Dai, L; He, GN; Song, J, 2023)		1.16
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
anti-inflammatory agentAny compound that has anti-inflammatory effects.
immunosuppressive agentAn agent that suppresses immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-cells or by inhibiting the activation of helper cells. In addition, an immunosuppressive agent is a role played by a compound which is exhibited by a capability to diminish the extent and/or voracity of an immune response.
[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 (4)

ClassDescription
cyclic ketone
organic heteroheptacyclic compound
diterpene triepoxideA diterpenoid compound that contains three epoxide groups.
butenolideA gamma-lactone that consists of a 2-furanone skeleton and its substituted derivatives.
[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 (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency0.13140.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency0.13140.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (49)

Assay IDTitleYearJournalArticle
AID1324618Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 500 nM after 24 hrs by dual luciferase reporter gene assay2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Identification of Triptophenolide from
AID1175362Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Semisynthesis of triptolide analogues: effect of B-ring substituents on cytotoxic activities.
AID1707238Cytotoxicity against human Panc-1 cells incubated for 72 hrs by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID594370Cytotoxicity against human A549 cells2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Semisynthesis of triptolide analogues: effect of γ-lactone and C-14 substituents on cytotoxic activities.
AID1500364Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Click chemistry-based synthesis and anticancer activity evaluation of novel C-14 1,2,3-triazole dehydroabietic acid hybrids.
AID1707240Antiproliferative activity against human Jurkat cells incubated for 3 to 6 days by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707166Antiproliferative activity against human BXPC-3 incubated for 72 hrs by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1373549Antiinflammatory activity in African green monkey CV1 cells assessed as inhibition of LPS-induced TNF-alpha production at 20 nM pre-incubated for 1 hr before LPS stimulation for 23 hrs by ELISA method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Triptolide derivatives as potential multifunctional anti-Alzheimer agents: Synthesis and structure-activity relationship studies.
AID1500365Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Click chemistry-based synthesis and anticancer activity evaluation of novel C-14 1,2,3-triazole dehydroabietic acid hybrids.
AID1707167Antiproliferative activity against human ASPC1 incubated for 72 hrs by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
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.
AID1656719Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 72 hrs2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Meeting organometallic chemistry with drug discovery: CH activation enabled discovery of a new ring system of 12H-Indazolo[2,1-a]cinnolin-12-ones with anti-proliferation activity.
AID1707228Antiproliferative activity against human DU-145 cells incubated for 72 hrs by CCK8 assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID263410Cytotoxicity against human A549 lung tumor cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Semisynthesis of C-ring modified triptolide analogues and their cytotoxic activities.
AID1707239Antiproliferative activity against human Raji cells incubated for 3 to 6 days by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID525908Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and biological evaluation of novel triptolide analogues for anticancer activity.
AID1500367Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Click chemistry-based synthesis and anticancer activity evaluation of novel C-14 1,2,3-triazole dehydroabietic acid hybrids.
AID326745Cytotoxicity against human A549 cells2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Fluorination of triptolide and its analogues and their cytotoxicity.
AID1656718Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Meeting organometallic chemistry with drug discovery: CH activation enabled discovery of a new ring system of 12H-Indazolo[2,1-a]cinnolin-12-ones with anti-proliferation activity.
AID326746Cytotoxicity against human HT29 cells2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Fluorination of triptolide and its analogues and their cytotoxicity.
AID1324617Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 5 uM after 24 hrs by dual luciferase reporter gene assay2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Identification of Triptophenolide from
AID1707170Antitumor activity against human PaTu8988 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 5 mg/kg, ip administered daily for 60 days by digital caliper method relative to control2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707227Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK8 assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1500366Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Click chemistry-based synthesis and anticancer activity evaluation of novel C-14 1,2,3-triazole dehydroabietic acid hybrids.
AID1707168Antiproliferative activity against human CFPAC-1 incubated for 72 hrs by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707236Cytotoxicity against human NCI-N87 cells incubated for 72 hrs by Alamar Blue method2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707232Cytotoxicity against human SW480 cells incubated for 72 hrs by Cell Titer-Glo luminescence assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1373535Neuroprotective activity against amyloid beta (1 to 42) peptide-induced cytotoxicty in CD1 mouse primary cortical neurons assessed as increase in cell viability at 0.1 to 10 uM pre-incubated for 1 hr before amyloid beta (1 to 42) addition and measured aft2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Triptolide derivatives as potential multifunctional anti-Alzheimer agents: Synthesis and structure-activity relationship studies.
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.
AID1707229Antiproliferative activity against human LNCaP cells incubated for 72 hrs by CCK8 assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707235Cytotoxicity against human MGC-803 cells incubated for 72 hrs by Alamar Blue method2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707234Cytotoxicity against human HGC-27 cells incubated for 72 hrs by Alamar Blue method2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1175361Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Semisynthesis of triptolide analogues: effect of B-ring substituents on cytotoxic activities.
AID1707233Cytotoxicity against human AGS cells incubated for 72 hrs by Alamar Blue method2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID263411Cytotoxicity against human HT29 colon tumor cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Semisynthesis of C-ring modified triptolide analogues and their cytotoxic activities.
AID594371Cytotoxicity against human HT-29 cells2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Semisynthesis of triptolide analogues: effect of γ-lactone and C-14 substituents on cytotoxic activities.
AID525907Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and biological evaluation of novel triptolide analogues for anticancer activity.
AID1707231Cytotoxicity against human RKO cells incubated for 72 hrs by Cell Titer-Glo luminescence assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707172Antiproliferative activity against human PaTu8988 incubated for 72 hrs by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1707237Cytotoxicity against human SGC-7901 cells incubated for 72 hrs by Alamar Blue method2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1373541Toxicity in African green monkey CV1 cells assessed as effect on cell viability incubated for 24 hrs by CCK8 assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Triptolide derivatives as potential multifunctional anti-Alzheimer agents: Synthesis and structure-activity relationship studies.
AID1707169Antiproliferative activity against human SW1990 incubated for 72 hrs by alamar blue assay2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347413qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR, retest select compounds2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347415qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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 (54)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (3.70)18.2507
2000's11 (20.37)29.6817
2010's23 (42.59)24.3611
2020's18 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.53

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 Index33.53 (24.57)
Research Supply Index4.01 (2.92)
Research Growth Index5.13 (4.65)
Search Engine Demand Index39.83 (26.88)
Search Engine Supply Index1.91 (0.95)

This Compound (33.53)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (3.70%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other52 (96.30%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
bicalutamide
bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.		2.1310(trifluoromethyl)benzenes;
monocarboxylic acid amide;
monofluorobenzenes;
nitrile;
sulfone;
tertiary alcohol
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		2.1510nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
oleanolic acid
[no description available]		2.0310hydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite
palladium
Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46.		2.110metal allergen;
nickel group element atom;
platinum group metal atom
nagilactone c
nagilactone C: norditerpene lactone isolated from leaves of Podocarpus; structure		2.2510
brusatol
brusatol: quassinoid from B. javanica; structure		2.2510triterpenoid
hydroxyflutamide
[no description available]		2.1310
sn 38
SN-38 : A member of the class of pyranoindolizinoquinolines that is (4S)-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione bearing two additional ethyl substituents at positions 4 and 11 as well as two additional hydroxy substituents at positions 4 and 9. It is the active metabolite of irinotecan and is ~1000 times more active than irinotecan itself.		2.0610delta-lactone;
phenols;
pyranoindolizinoquinoline;
tertiary alcohol		antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 5.99.1.2 (DNA topoisomerase) inhibitor
triptolide
[no description available]		5.48190diterpenoid;
epoxide;
gamma-lactam;
organic heteroheptacyclic compound		antispermatogenic agent;
plant metabolite
parthenolide
[no description available]		2.7620germacranolide
obacunone
obacunone: from bark of Chinese plant Phellodendron amurense; shortens sleeping time induced in mice by alpha-chloralose-urethane		2.2510limonoid
celastrol
[no description available]		9.0830monocarboxylic acid;
pentacyclic triterpenoid		anti-inflammatory drug;
antineoplastic agent;
antioxidant;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Hsp90 inhibitor;
metabolite
chlorolissoclimide
chlorolissoclimide: structure given in first source; a labdane cytotoxin isolated from Lissoclinum voeltzkowi Michaelson		2.2510
docetaxel
[no description available]		2.0610hydrate;
secondary alpha-hydroxy ketone		antineoplastic agent
wilforlide a
wilforlide A: form Tripterygium regelii; Chinese medicinal plant extract		7.4720
bruceine a
bruceine A: quassinoid which inhibits protein synthesis & DNA synthesis in cells; RN given refers to (11 beta,12 alpha,15 beta)-isomer; structure given in first source		2.2510quassinoid
bruceine b
bruceine B: quassinoid which inhibits protein synthesis & DNA synthesis in cells; structure in first source		2.2510triterpenoid
jolkinolide a
jolkinolide A: isolated from Euphorbia fischeriana		2.2510diterpene lactonemetabolite
jolkinolide b
jolkinolide B: isolated from Euphorbia fischeriana		2.2510diterpene lactonemetabolite
triptophenolide
triptophenolide: structure given in first source		7.7830oxo steroid
limonin
[no description available]		2.2510epoxide;
furans;
hexacyclic triterpenoid;
lactone;
limonoid;
organic heterohexacyclic compound		inhibitor;
metabolite;
volatile oil component
tripdiolide
tripdiolide: structure		7.5520oxacycle
thapsigargin
Thapsigargin: A sesquiterpene lactone found in roots of THAPSIA. It inhibits SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES.. thapsigargin : An organic heterotricyclic compound that is a hexa-oxygenated 6,7-guaianolide isolated fron the roots of Thapsia garganica L., Apiaceae. A potent skin irritant, it is used in traditional medicine as a counter-irritant. Thapsigargin inhibits Ca(2+)-transporting ATPase mediated uptake of calcium ions into sarcoplasmic reticulum and is used in experimentation examining the impacts of increasing cytosolic calcium concentrations.		2.2510butyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone		calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
glycosides
[no description available]		2.610
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		7.610
bruceantin
[no description available]		2.2510triterpenoid
andrographolide
[no description available]		2.2510carbobicyclic compound;
gamma-lactone;
labdane diterpenoid;
primary alcohol;
secondary alcohol		anti-HIV agent;
anti-inflammatory drug;
antineoplastic agent;
metabolite
shihulimonin a
shihulimonin A: isolated from Evodia rutaecarpa; structure in first source		2.2510limonoid
indium
Indium: A metallic element, atomic number 49, atomic weight 114.818, symbol In. It is named from its blue line in the spectrum.. indium atom : A metallic element first identified and named from the brilliant indigo (Latin indicum) blue line in its flame spectrum.		2.110boron group element atom
dichapetalin a
dichapetalin A: isolated from Dichapetalum; structure in first source		2.2510
ginkgolide b
[no description available]		2.2510
17-hydroxyjolkinolide b
17-hydroxyjolkinolide B: isolated from Euphorbia fischeriana		2.2510diterpene lactonemetabolite
bn 52020
[no description available]		2.2510
demethylzeylasteral
demethylzeylasteral: a phenolic nortriterpene; isolated from the root cortex of Tripterygium Wilfordii Hook f.. demethylzeylasteral : A carbopolycyclic compound with formula C29H36O6, originally isolated from Tripterygium wilfordii.		2.6320arenecarbaldehyde;
benzenediols;
carbopolycyclic compound;
cyclic ketone;
enone;
oxo monocarboxylic acid		anti-inflammatory agent;
EC 2.4.1.17 (glucuronosyltransferase) inhibitor;
immunosuppressive agent;
nephroprotective agent;
plant metabolite
dichlorolissoclimide
dichlorolissoclimide: structure given in first source; a labdane cytotoxin isolated from Lissoclinum voeltzkowi Michaelson		2.2510
mdv 3100
[no description available]		2.1310(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound		androgen antagonist;
antineoplastic agent
triptotriterpenic acid a
triptotriterpenic acid A: from Tripterygium wilfordii; RN given refers to (3beta,22alpha)-isomer; structure given in first source. triptotriterpenic acid A : A pentacyclic triterpenoid with formula C30H48O4, originally isolated from Tripterygium hypoglaucum.		2.610diol;
hydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite
14-o-phosphonooxymethyltriptolide
14-O-phosphonooxymethyltriptolide disodium salt: pro-drug of triptolide; has antineoplastic activity		2.2510
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		210
phenanthrenes
Phenanthrenes: POLYCYCLIC AROMATIC HYDROCARBONS composed of three fused BENZENE rings.. phenanthrenes : Any benzenoid aromatic compound that consists of a phenanthrene skeleton and its substituted derivatives thereof.		4.7690
ConditionIndicatedRelationship StrengthStudiesTrials
Glial Cell Tumors
[description not available]		02.110
Cancer of Prostate
[description not available]		02.5420
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		02.110
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.5420
Benign Neoplasms
[description not available]		04.5340
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		04.5340
Anemia, Fanconi
[description not available]		02.1310
Fanconi Anemia
Congenital disorder affecting all bone marrow elements, resulting in ANEMIA; LEUKOPENIA; and THROMBOPENIA, and associated with cardiac, renal, and limb malformations as well as dermal pigmentary changes. Spontaneous CHROMOSOME BREAKAGE is a feature of this disease along with predisposition to LEUKEMIA. There are at least 7 complementation groups in Fanconi anemia: FANCA, FANCB, FANCC, FANCD1, FANCD2, FANCE, FANCF, FANCG, and FANCL. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227650, August 20, 2004)		02.1310
ER-Negative PR-Negative HER2-Negative Breast Cancer
[description not available]		02.7220
Triple Negative Breast Neoplasms
Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.		02.7220
Asthma, Bronchial
[description not available]		04.2190
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		04.26100
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		04.2190
Acute Liver Injury, Drug-Induced
[description not available]		02.610
Adverse Drug Event
[description not available]		02.610
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		02.610
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		02.610
Hepatocellular Carcinoma
[description not available]		02.610
Cancer of Liver
[description not available]		02.610
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		02.610
Liver Neoplasms
Tumors or cancer of the LIVER.		02.610
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		03.2950
Metastase
[description not available]		02.6120
Cancer of Stomach
[description not available]		02.5920
Invasiveness, Neoplasm
[description not available]		02.8830
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.6120
Stomach Neoplasms
Tumors or cancer of the STOMACH.		02.5920
Acute Myelogenous Leukemia
[description not available]		02.3110
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.3110
Cancer of Lung
[description not available]		02.6620
Malignant Melanoma
[description not available]		02.3110
Lung Neoplasms
Tumors or cancer of the LUNG.		02.6620
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		07.3110
Sterility, Male
[description not available]		02.4720
Infertility, Male
The inability of the male to effect FERTILIZATION of an OVUM after a specified period of unprotected intercourse. Male sterility is permanent infertility.		02.4720
Germinoblastoma
[description not available]		02.1510
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		07.1510
Angiogenesis, Pathologic
[description not available]		02.1710
Cancer of Pancreas
[description not available]		02.5920
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		02.5920
Nasopharyngeal Carcinoma
A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes.		07.2110
Cancer of Nasopharynx
[description not available]		02.2110
Nasopharyngeal Neoplasms
Tumors or cancer of the NASOPHARYNX.		02.2110
Experimental Leukemia
[description not available]		02.1510
Abnormalities, Autosome
[description not available]		02.0110
Chromosome-Defective Micronuclei
[description not available]		02.0110
Libman-Sacks Disease
[description not available]		02.0310
Dementia Praecox
[description not available]		02.0310
Lupus Erythematosus, Systemic
A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.		02.0310
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		02.0310
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0310