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去氢表雄酮的生物转化、衍生物合成及细胞毒活性研究

Biotransformation of Dihydroepiandrosterone and the Synthesis and Cytotoxic Activities of the16-Benzylidene Derivatives
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摘要 去氢表雄酮是一种重要的生物活性物质,也是甾体药物的重要中间体.研究了卷枝毛霉对去氢表雄酮的生物转化,从其发酵液中分离得到两种产物,7α-和7β-羟基去氢表雄酮.并利用Claison-Schim-idt缩合反应制备了7α-羟基去氢表雄酮的16-苯亚甲基衍生物,活性测试表明,在16位引入带有不同取代基的苯亚甲基结构可增强此类化合物的细胞毒活性. Dihydroepiandrosterone （DHEA） is one important bioactivity compound and one important interme-diate of steroid drugs. It is for the first time to report the biotransformation of DHEA by Mucor circinelloides and two products was obtained. Furthermore, the 16-benzylidene derivatives were synthesized by Claison-Schimidt reaction. The cytotoxie evaluation showed that these derivatives had better activity than the parent compound.
作者 单丽红 乔星 李央 张璐珈 焦凯 刘宏民
机构地区 郑州大学药学院 郑州大学新药研发中心
出处 《郑州大学学报（工学版）》 CAS 北大核心 2013年第1期62-65,69,共5页 Journal of Zhengzhou University（Engineering Science）
基金 国家自然科学基金资助项目(81172937)
关键词 去氢表雄酮 卷枝毛霉 7-羟基化 16-苯亚甲基衍生物 细胞毒活性 dihydroepiandrosterone Mucor circinelloides 7-hydroxylation 16-benzylidene derivatives cyto- toxic activity
分类号 R914.5 [医药卫生—药物化学]
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郑州大学学报（工学版）
2013年 第1期

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