番荔枝内酯结构类型及作用机制研究进展  

Progress in the studies on structure types and action mechanism of Annonaceous acetogenins

作　　者：张帅[1] 曾鑫年[1] 黄田福[1] 黎卓莹[1] 

机构地区：[1]华南农业大学教育部农药与化学生物学重点实验室,广东广州510642

出　　处：《西北农林科技大学学报（自然科学版）》2005年第12期21-26,共6页Journal of Northwest A&F University(Natural Science Edition)

基　　金：广东省自然科学基金项目(32253)

摘　　要：简述了邻双四氢呋喃环(THF)型、非邻双THF型、单THF型和无THF型番荔枝内酯的结构特 点,分析了其活性基因THF环、γ-内酯环、环间碳链和环上侧碳链的构效关系,指出环间碳链是比γ-内酯环和THF 更重要的结构因子,最后综述了番荔枝内酯的作用机制。结果认为,结构因子对番荔枝内酯生物活性的影响以及番 荔枝内酯在细胞中的溶解性、膜的构象和运载特性将成为今后主要的研究方向。This paper reviews the structural characterization of adjacent bis-THF, non-adjacent bisTHF,mono-THF,non-THF acetogenins,analyzes the structural activity relationship of active groups of tetrahydrofuran （THF）,γ-lactone rings,alkyl spacer moiety linking the THF and γ-lactone ring moieties and the alkyl side chain,indicating that alkyl spacer moiety is a more improtant structural factor for the potent activity,and finally summarizes the action mechanism of Annonaceous acetogenins. As a result,effect on the Annonaceous acetogenins bioactivity by structural factors,solubility in the cell of Annonaceous acetogenins,and conformation and delivery of membrane will become the major study directions in the future.

关 键 词：番荔枝内酯 结构类型 构效关系 作用机制 

分 类 号：R979.19[医药卫生—药品]