链格孢菌AS 3.4578对蟾毒灵的微生物转化

Microbial transformation of bufotalin by Alternaria alternata AS 3.4578.

作者信息

Xin Xiu-Lan, Zhan Li-Bin, Li Feng-Yun, Ma Xiao-Chi, Liu Ke-Xin, Han Jian, Guo De-An

机构信息

The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.

出版信息

J Asian Nat Prod Res. 2009;11(1):7-11. doi: 10.1080/10286020802413197.

DOI:10.1080/10286020802413197

PMID:19180348

Abstract

The microbial transformation of a cytotoxic bufadienolide, bufotalin (1), was carried out. Three transformed products from 1 by Alternaria alternata were isolated. Their structures were characterized as 3-keto-bufotalin (2), 12 beta-hydroxyl-bufotalin (3), and 3-keto-12 beta-hydroxyl-bufotalin (4) based on the extensive NMR studies. Among them, 3 and 4 were new compounds with strong in vitro cytotoxic activities against HeLa cells.

摘要

对一种具有细胞毒性的蟾蜍二烯羟酸内酯——蟾毒灵（1）进行了微生物转化实验。从链格孢菌对1的转化产物中分离出三种化合物。基于广泛的核磁共振研究，确定它们的结构分别为3-酮基-蟾毒灵（2）、12β-羟基-蟾毒灵（3）和3-酮基-12β-羟基-蟾毒灵（4）。其中，3和4是新化合物，对人宫颈癌HeLa细胞具有很强的体外细胞毒性活性。