| 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。 |
| 关键词: 番荔枝内酯 结构类型 构效关系 作用机制 |
| DOI： |
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| 基金项目:广东省自然科学基金项目（32253） |
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| Progress in the studies on structure types and action mechanism of Annonaceous acetogenins |
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| Abstract: |
| This paper reviews the structural characterization of adjacent bis-THF,non-adjacent bis-THF,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. |
| Key words: Annonaceous acetogenins structure type structural activity relationships mechanism of action |
