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手性黄皮酰胺的研究进展
  • 期刊名称:通讯作者
  • 时间:0
  • 分类:R971[医药卫生—药品;医药卫生—药学] R282.71[医药卫生—中药学;医药卫生—中医学]
  • 作者机构:[1]中国医学科学院北京协和医学院药物研究所,北京100050
  • 相关基金:国家自然科学基金资助课题(30572342);长江学者和创新团队发展计划项目(IRT051)
  • 相关项目:用图象可视化技术对黄皮酰胺16个异构体生物学活性及机理研究
中文摘要:

黄皮酰胺是从中药黄皮叶中提取到的天然成分,现已完成其16个光学活性异构体的合成和拆分。通过对其中一对对映体(-)黄皮酰胺和(+)黄皮酰胺的深入研究发现,其代谢转化、药理作用等均具有立体选择性,即其中(-)黄皮酰胺是有效对映体,具有显著的保肝、促智、抗神经细胞凋亡等作用,而(+)黄皮酰胺为劣映体。现对手性黄皮酰胺的代谢转化、药动学和对神经系统的作用及机制研究进展进行综述。

英文摘要:

Clausenamide is a component isolated from Clausena lansium (lour) Skeel, which was synthesized and resolved into sixteen isomers. Clausenamide was found to possess stereoselectivity in its metabolic conversion and pharmacological effects through the study of one couple of enantiomer-(-) clausenamide and ( + ) clausenamide. (-) Clausenamide was found to be an active enantiomer in liver protection, nootropic potency, and inhibitory of neural apoptosis,while ( + ) clausenamide showed no such effects. The progress in the study of pharmacokinetics,pharmacodynamics,and the effects on nervous system of chiral clausenamide were reviewed in this article.

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