Page last updated: 2024-11-12

arenobufagin

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

Description

arenobufagin: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID12305198
CHEMBL ID4086974
CHEBI ID197067
SCHEMBL ID21578402
MeSH IDM0155969

Synonyms (24)

Synonym
464-74-4
bufa-20,22-dienolide, 3,11,14-trihydroxy-12-oxo- (3-beta,5-beta,11-alpha)-
5-beta-bufa-20,22-dienolide, 12-oxo-3-beta,11-alpha,14-trihydroxy-
12-oxo-3-beta,11-alpha,14-trihydroxy-5-beta-bufa-20,22-dienolide
arenobufagin
CHEBI:197067
5-[(3s,5r,8r,9s,10s,11s,13r,14s,17r)-3,11,14-trihydroxy-10,13-dimethyl-12-oxo-2,3,4,5,6,7,8,9,11,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl]pyran-2-one
unii-27r42qlm25
3,11,14-trihydroxy-12-oxo-bufa-20,22-dienolide
27r42qlm25 ,
C20035
CS-3693
AC-34734
HY-N0876
SCHEMBL21578402
AKOS030526814
NCGC00485924-01
arenobufogenin
DTXSID00963565
CHEMBL4086974
5-((3s,5r,8r,9s,10s,11s,13r,14s,17r)-3,11,14-trihydroxy-10,13-dimethyl-12-oxohexadecahydro-1h-cyclopenta[a]phenanthren-17-yl)-2h-pyran-2-one
AS-76734
(3.beta.,5.beta.,11.alpha.)-3,11,14-trihydroxy-12-oxobufa-20,22-dienolide
GLXC-13270

Research Excerpts

Overview

Arenobufagin (ArBu) is a natural anticancer drug with good anti-tumor effects, but its clinical applications and drug development potential are limited due to its toxicity. It is a major active component of toad venom, a traditional Chinese medicine used for cancer therapy.

ExcerptReferenceRelevance
"Arenobufagin is a naturally occurring bufadienolide showing promising antitumor activity accompanied however with apparent cardiac toxicity. "( Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
Chang, YQ; Chen, WM; Hou, W; Huang, ZX; Lin, H; Lin, J; Peng, QL; Sun, PH; Wang, LH; Xu, HG; Yao, Z; Zhang, DM, 2018
)
2.31
"Arenobufagin (ArBu) is a natural anticancer drug with good anti-tumor effects, but its clinical applications and drug development potential are limited due to its toxicity. "( Arenobufagin-loaded PEG-PLA nanoparticles for reducing toxicity and enhancing cancer therapy.
Bo, G; Bo, S; Chuan, L; Haiyu, Z; Hongjie, W; Jiaying, Y; Keke, L; Linna, W; Nan, S; Qinghe, Z; Shan, J; Wenya, G; Xiaolu, W; Yan, Z; Yanyan, Z; Yu, Z, 2023
)
3.8
"Arenobufagin (ArBu) is an important anti-tumor ingredient of Chan'su which has long been used as traditional Chinese medicine in clinic for tumor therapy in China."( The lipid homeostasis regulation study of arenobufagin in zebrafish HepG2 xenograft model and HepG2 cells using integrated lipidomics-proteomics approach.
Bian, BL; Guo, FF; Si, N; Wang, HJ; Wei, JY; Wei, XL; Yang, J; Yang, ZG; Zhao, HY; Zhao, LJ, 2020
)
2.27
"Arenobufagin (ABG) is a major active component of toad venom, a traditional Chinese medicine used for cancer therapy. "( Systemic delivery of the anticancer agent arenobufagin using polymeric nanomicelles.
Dong, D; Li, Z; Su, K; Wu, B; Xie, Q; Yuan, X, 2017
)
2.16

Toxicity

ExcerptReferenceRelevance
" The purpose of this study is to reduce the toxic side effects of ArBu and improve the efficacy of tumor treatment by incorporating it into poly(ethylene glycol)-b-poly (lactide) co-polymer (PEG-PLA)."( Arenobufagin-loaded PEG-PLA nanoparticles for reducing toxicity and enhancing cancer therapy.
Bo, G; Bo, S; Chuan, L; Haiyu, Z; Hongjie, W; Jiaying, Y; Keke, L; Linna, W; Nan, S; Qinghe, Z; Shan, J; Wenya, G; Xiaolu, W; Yan, Z; Yanyan, Z; Yu, Z, 2023
)
2.35

Pharmacokinetics

ExcerptReferenceRelevance
" The method was successfully applied to the determination and pharmacokinetic study of arenobufagin in rat plasma following intraperitoneal administration."( Quantitative determination of arenobufagin in rat plasma by ultra fast liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study.
Chen, X; Han, W; Jiang, W; Li, G; Ma, A; Ye, W; Zhang, D, 2013
)
0.9

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
steroid lactone
[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]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1456919Antiproliferative activity against wild type human MDA-MB-435 cells expressing FAP-alpha incubated for 48 hrs by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456921Antiproliferative activity against FAP-alpha deficient human MDA-MB-231 cells incubated for 48 hrs by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456934Cardiotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as decrease in left ventricular internal systole dimension at 4 umol/kg, iv administered starting on day 5 measured after day 22 by echocardiography2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456931Antitumor activity against human MDA-MB-231 cells xenografted in BALB/C nude mouse assessed as tumor regression at 4 umol/kg, iv administered starting on day 5 measured after day 22 by Ki67 staining-based assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1420577Cytotoxic activity against human AC16 cells assessed as cell swelling at 1 uM after 24 hrs by phase contrast microscopic method2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1420581Toxicity in ip dosed Kunming mouse assessed as mortality2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1420575Antiproliferative activity against human HepG2/ADM cells by MTT assay2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1456935Cardiotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as decrease in left ventricular internal diastole dimension at 4 umol/kg, iv administered starting on day 5 measured after day 22 by echocardiography2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1420576Selectivity index, ratio of IC50 for human AC16 cells to IC50 for human HepG2 cells2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1456893Cytotoxicity in BMSC (unknown origin) assessed as cell viability at 1000 nmol/L after 72 hrs by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456920Antiproliferative activity against FAP-alpha deficient human MCF7 cells incubated for 48 hrs by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1420572Antiproliferative activity against human HepG2 cells by MTT assay2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1456943Acute toxicity in iv dosed Kunming mouse measured less than 4 hrs post dose2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1420578Cytotoxic activity against human AC16 cells assessed as cell detachment from substratum at 1 uM after 24 hrs by phase contrast microscopic method2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1456933Cardiotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as increase in interventricular septal diastole dimension at 4 umol/kg, iv administered starting on day 5 measured after day 22 by echocardiography2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456932Cardiotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as increase in interventricular septal systole dimension at 4 umol/kg, iv administered starting on day 5 measured after day 22 by echocardiography2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456940Cardiotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as cytoplasmic vacuolization at 4 umol/kg, iv administered starting on day 5 measured after day 22 by hematoxylin-eosin staining-based assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456929Antitumor activity against human MDA-MB-231 cells xenografted in BALB/C nude mouse at 4 umol/kg, iv administered starting on day 5 measured after day 22 by Ki67 staining-based assay relative to control2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456926Antiproliferative activity against human MDA-MB-231 cells assessed as decrease in cell viability at 62.5 to 500 nmol/L after 72 hrs by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1420573Antiproliferative activity against human AC16 cells by MTT assay2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1420574Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin.
AID1456945Acute toxicity in Kunming mouse assessed as mortality at 4 umol/kg, iv after 8 hrs post dose2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
AID1456942Cardiotoxicity in BALB/C nude mouse xenografted with human MDA-MB-231 cells assessed as increase in LDH level at 4 umol/kg, iv administered starting on day 5 measured after day 222017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (6.45)18.2507
2000's0 (0.00)29.6817
2010's20 (64.52)24.3611
2020's9 (29.03)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.47

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 Index21.47 (24.57)
Research Supply Index3.50 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.47)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other32 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]