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采用硅胶、Sephadex LH-20等柱色谱方法对广藿香进行抗补体活性导向分离与鉴定,从乙酸乙酯部位和正丁醇部位共分离鉴定了15个黄酮、1个三萜和2个酚酸类成分,包括5-羟基-3,7,3’,4’-四甲氧基黄酮(1)、5-羟基-7,3’,4’-三甲氧基-二氢黄酮(2)、5,4’-二羟基-3,7,3’-三甲氧基黄酮(3)、5-羟基-3,7,4’-三甲氧基黄酮(4)、5,4’-二羟基-7,3’-二甲氧基黄酮(5)、木犀草素(6)、槲皮素-7,3’,4’-三甲醚(7)、岳桦素(8)、3,5,7-三羟基-3’,4’-二甲氧基黄酮(9)、槲皮素(10)、芹菜素(11)、山柰酚(12)、5-羟基-7,3’,4’-三甲氧基黄酮(13)、山柰酚-7-O-β-D-葡萄糖苷(14)、山柰酚-3-O-β-D-葡萄糖苷-7-O-α-L-鼠李糖苷(15)、齐墩果酸(16)、香草酸(17)、对甲基苄醇(18),其中化合物5,7,8,12～15,18均为首次从唇形科刺蕊草属植物中分离得到。对所得单体化合物进行经典和旁路途径的体外抗补体活性测定,并利用补体缺失血清鉴定活性最强化合物的抗补体作用靶点,结果表明,化合物3,7,10,12,16对经典和旁路途径的补体激活均有抑制作用(CH500.072～1.08 g.L-1,AP500.39～0.49 g.L-1),而化合物5,6仅对经典途径有抑制活性;活性最强的槲皮素-7,3’,4’-三甲醚(7)作用于补体系统的C1q,C2,C5和C9组分,值得深入研究。
The anti-complement activity of patchouli was isolated and identified by silica gel and Sephadex LH-20 column chromatography. Fifteen flavonoids, one triterpenoid and two phenolic acids were isolated and identified from ethyl acetate and n-butanol. Class components include 5-hydroxy-3,7,3 ’, 4’-tetramethoxyflavone (1), 5-hydroxy-7,3’, 4’-trimethoxy-flavanone 5,4’-dihydroxy-3,7,3’-trimethoxyflavone (3), 5-hydroxy-3,7,4’-trimethoxyflavone (4), 5,4’-dihydroxy- (5), luteolin (6), quercetin-7,3 ’, 4’-trimethylether (7), beryllium (8), 3,5-dimethoxyflavone 7-trihydroxy-3 ’, 4’-dimethoxyflavone (9), quercetin (10), apigenin (11), kaempferol (12), 5- hydroxy-7,3’, 4 -trimethoxyflavone (13), kaempferol -7-O-β-D-glucoside (14), kaempferol-3-O-β-D-glucoside-7-O-α-L (15), oleanolic acid (16), vanillic acid (17) and p-methylbenzyl alcohol (18). Among them, compounds 5,7,8,12 ~ Isolated from the plants of the kaempfer In vitro and in vivo anti-complement activity assays of the obtained monomeric compounds were performed, and the complement -activated sera were used to identify the anti-complement targets of the most active compounds. The results showed that compounds 3, 7, 10, (CH500.072 ~ 1.08 gL-1, AP500.39 ~ 0.49 gL-1), while compounds 5 and 6 only inhibited the classical pathway. The most active quercetin 7,3 ’, 4’-trimethylether (7) acts on the C1q, C2, C5 and C9 components of the complement system and deserves further study.