蓝萼香茶菜的抗补体活性成分研究

Chemical constituents of Rabdosia japonica var. glaucocalyx and their anti-complementary activity

目的:在前期研究基础上,深入研究蓝萼香茶菜的化学成分及其抗补体活性。方法:通过溶血试验,对蓝萼香茶菜各部位进行抗补体活性测试,以抗补体活性作为导向分离手段,运用多种色谱方法分离纯化蓝萼香茶菜中的化学成分,采用现代谱学技术进行结构鉴定,确定抗补体活性成分。结果:蓝萼香茶菜的正丁醇部位活性较强,从蓝萼香茶菜中分离得到11个化合物,分别为豆甾醇(1),豆甾醇-9(11)-烯-3-醇(2),蓝萼丁素(3),尾叶香茶菜丙素(4),山楂酸(5),科罗索酸(6),minheryinsⅠ(7),香叶木素(8),咖啡酸乙烯酯(9),咖啡酸(10),牡荆苷(11)。抗补体活性实验表明,化合物9,10以及前期分离得到的异槲皮苷、芦丁、槲皮素、槲皮素-3-甲醚、木犀草素、木犀草素-7-甲醚和芹菜素对经典途径的补体激活具有不同程度的抑制作用。结论:化合物2,4,6～9,11为首次从该植物中获得,咖啡酸的抗补体活性最强,CH50为0.041 g·L-1。

To study the chemical constituents of Rabdosia japonica var. glaucocalyx and their anti-complementary activity on the basis of preliminary studies. Target isolation guided by anti-complementary activity test, compounds in the chloroform and n-butanol fractious were isolated and purified by silica gel and Sephadex LH-20 column chromatographies, and preparative ttPLC. The structures were identified by various spectroscopic data including ESI-MS, 1H-NMR and 13 C-NMR data. The compounds were evaluated for anti- complementary activity in vitro. Eleven compounds were isolated from the chloroform and n-butanol soluble fractions and identified as stigmasterol （ 1 ）, stigmas-9 （ 11 ） -en-3-ol （ 2 ）, glaucocalyxin D （ 3 ）, kamebakaurin （ 4 ）, maslinic acid （ 5 ）, corosolic acid （ 6）, minheryins I （7） , diosmetin （8） , caffeic acid ethylene ester （9） , caffeic acid （10） and vitexin （11）. Isoquereetrin, rntin, querce- tin, 3-methylquercetin, luteolin, 7-methylluteolin, and apigenin which were isolated from the preliminary studies together with com- pounds 9 and 10 showed inhibition of the complement system by the classical pathway. Compounds 2, 4, 6-9 and 11 were obtained from this plant for the first time： Caffeic acid （10） showed the strongest activity in vitro with a CH50 value of 0. 041 g ·L^-1.