- Application of acetyl bufalin in preparation of antitumor drugs
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The invention discloses an application of acetyl bufalin in preparation of antitumor drugs. A structure of the acetyl bufalin is shown as a formula (I), the acetyl bufalin can increase the antineoplastic curative effect, and has good inhibition effect for lung cancer cells.
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Paragraph 0024-0027
(2018/09/08)
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- Microbial transformation of three bufadienolides by Nocardia sp. and some insight for the cytotoxic structure-activity relationship (SAR)
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Resibufogenin, cinobufagin, and bufalin are cytotoxic steroids isolated from the Chinese drug Chan'su. Biotransformation of these three bufadienolides by Nocardia sp. NRRL 5646 was investigated. Notably, resibufogenin was converted to 3-acetyl 15β-hydroxyl bufotalin, via an unprecedented 14β,15β-epoxy ring cleavage and a regio-selective acetoxylation. This product showed significantly increased cytotoxic activity. The regio-selective acetylation of the 3-OH was also involved in the other reactions. The structures of metabolites were established by ESI-LC/MS and 2D NMR techniques. The in vitro cytotoxic activities against human cancer cell lines of the substrates and the transformed products were determined by the MTT method and their structure-activity relationship (SAR) was discussed. This investigation provided a useful approach to prepare new bufadienolides and the SAR research.
- Zhang, Jian,Sun, Yang,Liu, Ji-Hua,Yu, Bo-Yang,Xu, Qiang
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p. 6062 - 6065
(2008/09/16)
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