[关键词]
[摘要]
目的 研究白木香Aquilaria sinensis果皮的化学成分及其细胞毒性与抗菌活性。方法 采用正、反相硅胶柱、凝胶柱和薄层制备等色谱技术和重结晶进行分离纯化,通过波谱分析进行结构鉴定;以神经胶质瘤细胞SF-268、乳腺癌细胞MCF-7、大细胞肺癌细胞NCI-H460、肝癌细胞HepG-2为供试细胞株,采用SRB染色法对化合物进行体外细胞毒活性研究;以金黄色葡萄球菌和大肠杆菌为供试菌株,采用刃天青染色法对化合物进行体外抗菌活性研究。结果 从白木香果皮中分离到10个化合物,经波谱数据分析分别鉴定为isorhamnetin 3-O-(6″-O-(Z)-p-coumaroyl)-β-D-glucopyranoside(1)、buddlenoid A(2)、7-甲氧基-4′-羟基异黄酮(3)、木犀草素(4)、反式对香豆酸乙酯(5)、木香烃内酯(6)、表木栓醇(7)、豆甾醇(8)、对羟基苯甲酸甲酯(9)、邻苯二酚(10)。结论 化合物1~3、5、6、9、10为首次从该植物中分离得到,化合物1~3、5、6为首次从沉香属植物中分离得到;其中化合物6对上述4种肿瘤细胞株表现出较好的抑制作用,化合物1、4对金黄色葡萄球菌和大肠杆菌具有一定的抗菌活性。
[Key word]
[Abstract]
Objective To study the chemical constituents from the pericarps of Aquilaria sinensis and their cytotoxic and antibacterial activities. Methods The compounds were isolated by various chromatographic methods (silica gel, reverse silica gel, Sephadex LH-20, preparative TLC, and so on) and recrystallization. Their structures were identified by extensive analysis of the spectroscopic data. The cytotoxic effects of these compounds on neuroglioma SF-268, breast cancer MCF-7, large cell lung cancer NCI-H460, and hepatoma carcinoma HepG-2 cell lines were observed in vitro by SRB staining, and the antibacterial effects of these compounds on Staphyloccocus aureus and Escherichia coli were observed in vitro by Resazurin staining method. Results Ten compounds were isolated from the pericarps of A. sinensis and identified as isorhamnetin 3-O-(6″-O-(Z)-p-coumaroyl)-β-D-glucopyranoside (1), buddlenoid A (2), 7-methoxy-4′-hydroxyisoflavone (3), luteolin (4), trans-p-coumaric acid ethyl eater (5), costunolide (6), epifriedelanol (7), stigmasterol (8), p-hydroxybenzoate (9), and pyrocatechol (10). Conclusion Compounds 1—3, 5, 6, 9, and 10 are first isolated from the plant and compounds 1—3, 5, and 6 are isolated from the plants of genus Aquilaria Lam. for the first time. Compound 6 exhibits the significant cytotoxic activities against the above four cell lines and compounds 1 and 4 show some antibacterial activities against S. aureus and E. coli.
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[基金项目]
国家自然科学基金项目(81203006);广东省中国科学院全面战略合作项目(2011B090300078);广东省科技计划项目(2012A030100014)