Cinobufotalin - CAS 1108-68-5
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Not Intended for Therapeutic Use. For research use only.
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Cinobufotalin is one of the bufadienolides prepared from toad venom. It has anticancer activity.
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1.Studies on cytotoxic constituents from the skin of the toad Bufo bufo gargarizans.
Zhao HY1, Wu FK, Qiu YK, Wu Z, Jiang YT, Chen JY. J Asian Nat Prod Res. 2010 Sep;12(9):793-800. doi: 10.1080/10286020.2010.505187.
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.
2.Venenum Bufonis induces rat neuroinflammation by activiating NF-κB pathway and attenuation of BDNF.
Bi QR1, Hou JJ2, Qi P3, Ma CH4, Shen Y5, Feng RH6, Yan BP7, Wang JW8, Shi XJ9, Zheng YY10, Wu WY11, Guo D12. J Ethnopharmacol. 2016 Mar 21. pii: S0378-8741(16)30161-1. doi: 10.1016/j.jep.2016.03.049. [Epub ahead of print]
ETHNOPHARMACOLOGICAL RELEVANCE: Venenum Bufonis (VB), also called toad venom, has been widely used in clinic as a cardiotonic, anohyne and antineoplastic agents both in China and other Asian countries. However, its neurotoxicity and cardiotoxicity limit its wide clinical application. Compared with extensive attention attracted with cardiotoxicity, the toxic effect of VB on Central Nervous System (CNS) is much less studied.
3.[Inhibitory effect of total bufadienolides from toad venom against H22 tumor in mice and their metabolites].
Li Z1, Gao H, Wang J, Qu T, Chen L, Wang Z, Zhang Q. Zhongguo Zhong Yao Za Zhi. 2011 Nov;36(21):2987-93.
OBJECTIVE: To evaluate the inhibitory effect of total bufadienolides from toad venom against H22 tumor in mice and preliminarily analyze the structures of the metabolites in tissues.
4.Pre-clinical evaluation of cinobufotalin as a potential anti-lung cancer agent.
Kai S1, Lu JH1, Hui PP1, Zhao H2. Biochem Biophys Res Commun. 2014 Sep 26;452(3):768-74. doi: 10.1016/j.bbrc.2014.08.147. Epub 2014 Sep 6.
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 anti-lung cancer activity of cinobufotalin in vivo and in vitro, and studied the underlying mechanisms. We demonstrated that cinobufotalin displayed considerable cytotoxicity against lung cancer cells (A549, H460 and HTB-58 lines) without inducing significant cell apoptosis. Our data suggest that mitochondrial protein cyclophilin D (Cyp-D)-dependent mitochondrial permeability transition pore (mPTP) opening mediates cinobufotalin-induced non-apoptotic death of lung cancer cells. The Cyp-D inhibitor cyclosporine A (CsA), the mPTP blocker sanglifehrin A (SfA), and Cyp-D shRNA-silencing significantly inhibited cinobufotalin-induced mitochondrial membrane potential (MMP) reduction and A549 cell death (but not apoptosis).
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CAS 1108-68-5 Cinobufotalin

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