[关键词]
[摘要]
目的 探讨单四氢呋喃型番荔枝内酯类（单THF型ACGs）化合物对大鼠肝线粒体复合酶I活性的影响。方法 选用6个结构不同的单THF型ACGs，通过测定其对大鼠肝线粒体复合酶I的抑制活性，明确这些化合物结构中四氢呋喃环与内酯环之间碳数、取代羟基个数以及四氢呋喃环的核心构型对大鼠肝线粒体复合酶I活性的影响。 结果 6个单THF型ACGs对大鼠肝线粒体复合酶I均有一定的抑制活性，构效关系分析可见，在单THF型ACGs中，四氢呋喃环与内酯环间碳链越短，化合物活性越强，取代羟基个数并非是影响活性的决定性因素。结论 四氢呋喃环的核心构型为苏式/反式/赤式时比苏式/反式/苏式构型的抑制线粒体复合酶I的活性强。
[Key word]
[Abstract]
Objective To investigate the activity of mono-tetrahydrofuran (THF) annonaceous acetogenins (ACGs) against mitochondrial complex I of rats. Methods The inhibitory activity of mono-THF ACGs with six different chemical structures against mitochondrial complex I of rats was investigated to clarify the carbon number and substituted hydroxyl number between THF ring and lactone ring as well as the effect of the core configuration in THF ring on mitochondrial complex I of rats. Results The results show that mono-THF ACGs can inhibit the mitochondrial complex I of rats. With analysis of the results from the structure-activity relationship between antitumoral activity and their chemical structure of mono-THF ACGs, the less the carbon number between the two rings is, the better their inhibitory activities are; The number of substituted hydroxyl groups is not the decisive factor for influencing its activity in mono-THF ACGs. Conclusion The inhibitory activity of compound’s configurations with th/t/er is better than that of the compound’s configurations with th/t/th in mono-THF ACGs.
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[基金项目]
国家自然科学基金资助项目（81274057）；国家教育部博士点专项基金资助项目（20113237110009）；2江苏省高校优势学科建设工程资助项目（ysxk-2010）；江苏省科技厅项目（BK2012853）； 011年江苏省普通高校研究生科研创新计划项目（790）；2012年江苏省普通高校研究生科研创新计划项目（588）
