灵芝羊毛甾烷型三萜抗肿瘤构效关系初探A preliminary investigation on anti-tumor structure-activity relationship of lanostane triterpenes from Ganoderma spp.
杨梅;岳亚文;张劲松;唐庆九;冯娜;韩伟;
摘要(Abstract)：
多篇文献报道灵芝三萜具有良好的抗肿瘤活性，但其构效关系和作用靶点尚未系统比较。本研究以45种灵芝三萜为研究对象，通过对小鼠白血病细胞L1210的增殖抑制测定，来评价化合物抗肿瘤的能力。结果表明，灵芝菌丝体三萜和子实体中性三萜的活性较强。进一步采用DiscoveryStudio分子对接技术探讨了12种活性较强的灵芝三萜与5种抗肿瘤作用相关蛋白p53、Bcl-xl、EGFR、IL-2和VEGFR2之间可能的作用靶点，推测三萜化合物抗肿瘤能力与其结构上的乙酰氧基和母环上的共轭双键有关。其中，具有这一特征的含有3个乙酰氧基的ganoderic acid T，其抗肿瘤活性最强。本研究为灵芝三萜活性位点的寻找和结构改造提供了参考。
关键词(KeyWords)： 灵芝三萜;抗肿瘤活性;构效关系;分子对接;LibDock
基金项目(Foundation): 上海市科技兴农重点攻关项目[沪农科创字(2018)第1-1号];; 上海市农业科学院卓越团队[沪农科卓(2022)003]~~
作者(Authors): 杨梅;岳亚文;张劲松;唐庆九;冯娜;韩伟;
DOI: 10.13346/j.mycosystema.220007
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