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[摘要]
目的 研究茯苓Poria cocos非多糖类化学成分的抗补体活性。方法 通过溶血实验方法进行抗补体活性成分的导向分离,对所得化合物进行经典途径的体外抗补体活性测定,采用现代波谱技术ESI-MS、1H-NMR、13C-NMR进行结构鉴定。结果 从茯苓醋酸乙酯部位分离得到11个化合物,分别鉴定为豆甾醇(1)、羽扇豆醇(2)、齐墩果酸(3)、乌苏酸(4)、猪苓酸C(5)、土莫酸(6)、去氢土莫酸(7)、3-表-去氢土莫酸(8)、茯苓酸(9)、去氢茯苓酸(10)、松苓新酸(11)。化合物1~4为首次从茯苓中分离得到。抗补体实验表明化合物3~11对经典的补体激活具有不同程度的抑制作用。结论 三萜酸类化合物是茯苓非多糖类化学成分中主要的抗补体活性成分[CH50为(0.10~0.27)g/L]。
[Key word]
[Abstract]
Objective To investigate the non-polysaccharide chemical constituents of Poria cocos and their anti-complementary activity. Methods The anti-complementary bioassay-guided isolation was carried out with the hemolysis test as guide. All isolates were evaluated for their in vitro anti-complementary activities on the classical pathway. The structures were identified by various spectroscopic data including ESI-MS, 1H-NMR, and 13C-NMR data. Results Eleven compounds were isolated from the EtOAc fraction of P. cocos extracts, including stigmasterol (1), lupeol (2), oleanolic acid (3), ursolic acid (4), polyporenic acid C (5), tumulosic acid (6), dehydrotumulosic acid (7), 3-epi-dehydrotumulosic acid (8), pachymic acid (9), dehydropachymic acid (10), and dehydrotrametenolic acid (11). Compounds 1-4 were obtained from this plant for the first time, and compounds 3-11 showed the anti-complementary activity in different degrees. Conclusion Triterpenoid acids are the main anti-complementary constituents in the chemical constituents of P. cocos non-polysaccharides (CH50 0.10-0.27 g/L).
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[基金项目]
国家“重大新药创制”科技重大专项(2013ZX09402203)