| 氧杂蒽酮对脂肪酸合酶的抑制作用及构效分析 |
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| 作者姓名： | 权小芳 马晓丰 |
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| 作者单位： | 中国科学院研究生院生命科学学院, 北京 100049 |
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| 基金项目： | 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 |
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| 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.
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| 关 键 词： | 脂肪酸合酶 氧杂蒽酮 抑制剂 构效分析 |
| 收稿时间： | 2011-10-10 |
| 修稿时间： | 2011-11-15 |
Structure-activity relationship study on inhibition of fatty acid synthase by xanthones |
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| Authors: | QUAN Xiao-Fang MA Xiao-Feng |
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| Institution: | College of Life Sciences, Graduate University, Chinese Academy of Sciences, Beijing 100049, China |
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| 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. |
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| Keywords: | fatty acid synthase xanthones inhibitors structure-activity analysis |
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