氧杂蒽酮对脂肪酸合酶的抑制作用及构效分析

doi:10.7523/j.issn.2095-6134.2012.6.018

中国科学院大学学报 ›› 2012, Vol. ›› Issue (6): 841-846.DOI: 10.7523/j.issn.2095-6134.2012.6.018

氧杂蒽酮对脂肪酸合酶的抑制作用及构效分析

权小芳, 马晓丰

中国科学院研究生院生命科学学院, 北京 100049

收稿日期:2011-10-10 修回日期:2011-11-15 发布日期:2012-11-15
通讯作者: 马晓丰
基金资助:
中国科学院生命科学领域优秀青年科技专项基金(KSCX2-EW-Q-19);生命科学领域"十二五"基础前沿专项(KSCX2-EW-J-21);王宽诚教育基金和中国科学院研究生院院长基金(O95101PY00)资助

Structure-activity relationship study on inhibition of fatty acid synthase by xanthones

QUAN Xiao-Fang, MA Xiao-Feng

College of Life Sciences, Graduate University, Chinese Academy of Sciences, Beijing 100049, China

Received:2011-10-10 Revised:2011-11-15 Published:2012-11-15

摘要/Abstract

摘要： 研究山竹壳中存在的氧杂蒽酮类化合物对脂肪酸合酶(FAS)全反应的抑制作用,发现具有不同官能团和取代基的化合物抑制FAS的能力不同,其IC₅₀从1.24 μmol/L至1000 μmol/L以上不等.分析这些化合物抑制FAS能力和其结构之间的关系,发现了一系列的构效关系规律.

关键词: 脂肪酸合酶, 氧杂蒽酮, 抑制剂, 构效分析

Abstract: Fatty acid synthase (FAS), an important enzyme catalyzing the synthesis of long-chain fatty acid in vivo, has been reported to be a potential target for treatment of obesity. We found that xanthones with different functional groups and substituents have different inhibition activities on FAS, and the IC₅₀ values range from 1.24 μmol/L to 1000 μmol/L and above. Structure-activity relationships for these compounds were then analyzed, and some structure-activity rules were established.

Key words: fatty acid synthase, xanthones, inhibitors, structure-activity analysis

中图分类号:

R285.5

权小芳, 马晓丰. 氧杂蒽酮对脂肪酸合酶的抑制作用及构效分析[J]. 中国科学院大学学报, 2012, (6): 841-846.

QUAN Xiao-Fang, MA Xiao-Feng. Structure-activity relationship study on inhibition of fatty acid synthase by xanthones[J]. , 2012, (6): 841-846.

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氧杂蒽酮对脂肪酸合酶的抑制作用及构效分析

Structure-activity relationship study on inhibition of fatty acid synthase by xanthones

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