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

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.