MICROBIAL TRANSFORMATIONS OF NATURAL ANTI-TUMOR AGENTS .23. CONVERSION OF WITHAFERIN-A TO 12-BETA-HYDROXY AND 15-BETA-HYDROXY DERIVATIVES OF WITHAFERIN-A
MICROBIAL TRANSFORMATIONS OF NATURAL ANTI-TUMOR AGENTS .23. CONVERSION OF WITHAFERIN-A TO 12-BETA-HYDROXY AND 15-BETA-HYDROXY DERIVATIVES OF WITHAFERIN-A
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DOI：
10.1016/0039-128x(82)90030-7
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发表时间：
1982-01-01
期刊：
影响因子：
2.7
通讯作者：
BUDESINSKY, M
中科院分区：
文献类型：
--
作者：
FUSKA, J;PROUSEK, J;BUDESINSKY, M
用抗肿瘤内酯withaferin-A进行微生物转化实验。线虫NRRL 1393在干扰素a下转化为15 β。-hydroxywithaferin-A （2a）和12 - β。-hydroxywithaferin-A(3)。采用溶剂萃取法分离羟基化代谢物，采用柱层析和薄层色谱法纯化。羟基化代谢物的结构通过1H- NMR和13C NMR， IR和质谱分析以及酰化衍生物的制备来确定。化合物2a和3a抑制体外培养的P-388小鼠淋巴细胞白血病细胞的生长和生化功能。
Microbial transformation experiments were conducted with the antitumor lactone withaferin-A. Cunninghamella elegans NRRL 1393 transformed withaferin-A to 15.beta.-hydroxywithaferin-A (2a) and 12.beta.-hydroxywithaferin-A (3a). The hydroxylated metabolites were isolated by solvent extraction and were purified by column chromatography and TLC. Structures of the hydroxylated metabolites were determined by 1H- and 13C NMR, IR and mass spectral analyses, and by the preparation of acylated derivatives. Compounds 2a and 3a inhibited the growth and biochemical functions of in vitro grown P-388 murine lymphocytic leukemic cells.