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 Source | ID |
---|---|
PubMed CID | 12305198 |
CHEMBL ID | 4086974 |
CHEBI ID | 197067 |
SCHEMBL ID | 21578402 |
MeSH ID | M0155969 |
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.
Toxicity
Excerpt | Reference | Relevance |
---|---|---|
" 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
Excerpt | Reference | Relevance |
---|---|---|
" 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
Excerpt | Reference | Relevance |
---|---|---|
"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)
Class | Description |
---|---|
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 ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1456919 | Antiproliferative activity against wild type human MDA-MB-435 cells expressing FAP-alpha incubated for 48 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456921 | Antiproliferative activity against FAP-alpha deficient human MDA-MB-231 cells incubated for 48 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456934 | Cardiotoxicity 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 echocardiography | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456931 | Antitumor 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1420577 | Cytotoxic activity against human AC16 cells assessed as cell swelling at 1 uM after 24 hrs by phase contrast microscopic method | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1420581 | Toxicity in ip dosed Kunming mouse assessed as mortality | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1420575 | Antiproliferative activity against human HepG2/ADM cells by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1456935 | Cardiotoxicity 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 echocardiography | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1420576 | Selectivity index, ratio of IC50 for human AC16 cells to IC50 for human HepG2 cells | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1456893 | Cytotoxicity in BMSC (unknown origin) assessed as cell viability at 1000 nmol/L after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456920 | Antiproliferative activity against FAP-alpha deficient human MCF7 cells incubated for 48 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1420572 | Antiproliferative activity against human HepG2 cells by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1456943 | Acute toxicity in iv dosed Kunming mouse measured less than 4 hrs post dose | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1420578 | Cytotoxic activity against human AC16 cells assessed as cell detachment from substratum at 1 uM after 24 hrs by phase contrast microscopic method | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1456933 | Cardiotoxicity 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 echocardiography | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456932 | Cardiotoxicity 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 echocardiography | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456940 | Cardiotoxicity 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456929 | Antitumor 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 control | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456926 | Antiproliferative 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 assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1420573 | Antiproliferative activity against human AC16 cells by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1420574 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20 | Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin. |
AID1456945 | Acute toxicity in Kunming mouse assessed as mortality at 4 umol/kg, iv after 8 hrs post dose | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Fibroblast Activation Protein α Activated Tripeptide Bufadienolide Antitumor Prodrug with Reduced Cardiotoxicity. |
AID1456942 | Cardiotoxicity 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 22 | 2017 | Journal 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)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 2 (6.45) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 20 (64.52) | 24.3611 |
2020's | 9 (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.
| This Compound (21.47) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 32 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |