1108-68-5

Usage

Uses

Used in Pharmaceutical Industry:
Cinobufotalin is used as a cardiotonic agent for its ability to strengthen the heart muscle and improve cardiac function, particularly in conditions such as heart failure and arrhythmias.
Used in Oncology:
Cinobufotalin is used as an anticancer agent for its potential to inhibit the growth and proliferation of cancer cells, especially in liver, lung, and colon cancers. It is being studied for its ability to target and destroy cancer cells while minimizing damage to healthy cells.
Used in Drug Development:
Cinobufotalin is used as a lead compound in the development of new pharmaceuticals targeting various diseases, including cancer and cardiovascular conditions. Its unique properties and mechanisms of action make it a promising candidate for further research and potential drug discovery.
Used in Traditional Chinese Medicine:
Cinobufotalin is used as a traditional medicine for its various therapeutic effects, including its anti-inflammatory and anti-tumor properties. It is often combined with other herbs and compounds to create formulations that target specific health conditions and promote overall well-being.

InChI:InChI=1/C26H34O7/c1-14(27)32-21-20(15-4-5-19(29)31-13-15)24(3)10-7-17-18(26(24)22(21)33-26)8-11-25(30)12-16(28)6-9-23(17,25)2/h4-5,13,16-18,20-22,28,30H,6-12H2,1-3H3/t16-,17-,18+,20-,21+,22+,23+,24+,25-,26+/m0/s1

Upstream product

• 1030609-22-3 cinobufotalin 3-nonanedioylarginine ester 
• 470-37-1 cinobufagin 

Related news

Neutralization of cardiac toxins oleandrin, oleandrigenin, bufalin, and Cinobufotalin (cas 1108-68-5) by digibind: Monitoring the effect by measuring free digitoxin concentrations08/15/2019

Oleandrin plant poisoning is common in children and the plant extract is used in Chinese medicines. The toxicity is due to oleandrin and the deglycosylated metabolite oleandrigenin. Bufalin and cinobufotalin (toad cardiac toxins) are also widely used in Chinese medicines like Chan SU, and Lu-She...detailed

Microbial transformation of Cinobufotalin (cas 1108-68-5) by Alternaria alternate AS 3.4578 and Aspergillus niger AS 3.73908/13/2019

Cinobufotalin (1), a major bioactive bufadienolide, has the potential anti-cancer activity. In the present paper, a scaled-up biotransformation of 1 by Aspergillus niger AS 3.739 and Alternaria alternate AS 3.4578 was performed for improving its biological activities and water-solubility. Seven ...detailed

Pre-clinical evaluation of Cinobufotalin (cas 1108-68-5) as a potential anti-lung cancer agent08/12/2019

Lung cancer is a major cause of cancer-related mortality in the United States and around the world. Due to the pre-existing or acquired chemo-resistance, the current standard chemotherapy regimens only show moderate activity against lung cancer. In the current study, we explored the potential an...detailed

Relevant academic research and scientific papers

Studies on cytotoxic constituents from the skin of the toad Bufo bufo gargarizans

To study the chemical composition of the skin of Bufo bufo gargarizans, many kinds of chromatography methods were used in the isolation procedures, while the structures of isolated compounds were determined on the basis of their NMR and MS spectral analysis. As a result, two new compounds were isolated from its ethanolic extract and characterized as cinobufotalin 3-nonanedioylarginine ester (8) and bufotalin 3-pimeloylarginine ester (14). Furthermore, 13 known compounds were obtained. Isolated bufadienolides showed significant inhibition effect against SMMC-7721 cell lines in vitro.

Comparative metabolism of cinobufagin in liver microsomes from mouse, rat, dog, minipig, monkey, and human

Cinobufagin (CB), a major bioactive component of the traditional Chinese medicine Chansu, has been reported to have potent antitumor activity. In this study, in vitro metabolism of CB among species was compared with respect to metabolic profiles, enzymes involved, and catalytic efficiency by using liver microsomes from human (HLM), mouse (MLM), rat (RLM), dog (DLM), minipig (PLM), and monkey (CyLM). Significant species differences in CB metabolism were revealed. In particular, species-specific deacetylation and epimerization combined with hydroxylation existed in RLM, whereas hydroxylation was a major pathway in HLM, MLM, DLM, PLM, and CyLM. Two monohydroxylated metabolites of CB in human and animal species were identified as 1α-hydroxylcinobufagin and 5β-hydroxylcinobufagin by using liquid chromatography-mass spectrometry and two-dimensional NMR techniques. CYP3A4 was identified as the main isoform involved in CB hydroxylation in HLM on the basis of the chemical inhibition studies and screen assays with recombinant human cytochrome P450s. Furthermore, ketoconazole, a specific inhibitor of CYP3A, strongly inhibited CB hydroxylation in MLM, DLM, PLM, and CyLM, indicating that CYP3A was responsible for CB hydroxylation in these animal species. The apparent substrate affinity and catalytic efficiency for 1α- and 5β-hydroxylation of CB in liver microsomes from various species were also determined. PLM appears to have K m and total intrinsic clearance value (Vmax/Km) similar to those for HLM, and the total microsomal intrinsic clearance values for CB obeyed the following order: mouse > dog > monkey > human > minipig. These findings provide vital information to better understand the metabolic behaviors of CB among various species. Copyright