New cytotoxic bufadienolides from the biotransformation of resibufogenin by Mucor polymorphosporus |
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Authors: | Min Ye Dongge An Dean Guo |
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Institution: | a The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, Beijing 100083, China b Beijing Institute of Microchemistry, Beijing 100091, China |
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Abstract: | Resibufogenin is a cytotoxic steroid isolated from the Chinese drug ChanSu. The biotransformation of resibufogenin by Mucor polymorphosporus afforded 22 products, and 15 of them were new. The transformation reactions involved hydroxylations at C-1β, C-5, C-7α, C-7β, C-12α, C-12β and C-16α, as well as epimerization or dehydrogenation of 3-OH. Hydroxylations at C-12α, C-12β and C-16α were the major reactions, each giving products in >5% yields, whereas the other products were obtained in fairly low yields. Some of the products showed decreased but still potent cytotoxicities. This investigation provided a useful approach to prepare new bufadienolides and most of them were difficult to obtain by chemical means. |
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Keywords: | Biotransformation Bufadienolide Cytotoxicity Mucor polymorphosporus Resibufogenin |
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