目的研究桔梗细胞悬浮培养体系对抗癌天然活性成分斑蝥素的生物转化,以获得具有新颖结构的斑蝥素衍生物。方法往桔梗悬浮培养体系中加入斑蝥素并培养6d,培养液经萃取后采用色谱方法进行分离纯化,产物的结构根据光谱数据予以鉴定。结果分离得到了以2∶1比例混合存在的两个转化产物。经光谱分析,两个产物鉴定为羰基还原为羟基的一对差向异构体1β-羟基斑蝥素(a)及1α-羟基斑蝥素(b)。结论a和b均为未见报道的新化合物。桔梗细胞培养体系对斑蝥素具有较强的选择性还原作用,此转化反应可用于斑蝥素衍生物的制备。

Object To investigate the biotransformation of cantharidin by cell suspension cultures of Platycodon grandiflorus (Jacq ) A DC Methods Cantharidin was added into cell suspension cultures of P·grandiflorus and incubated for another six days The culture supernatant was extracted with EtOAc and then subjected to silica gel chromatography.Results Two products were isolated as a mixture in a molar ratio of about 2∶1 Their structures were identified on the basis of spectroscopic data as 1β-OH cantharidin (Ⅱa) and 1α-OH cantharidin (Ⅱb) The relative configuration was elucidated according to NOESY spectrum.Conclusion The two products were new cantharidin derivatives.

国家杰出青年基金(39925040)；教育部跨世纪优秀人才基金