摘要
目的:研究香椿果抗补体活性成分。方法:采用溶血法进行抗补体活性筛选,然后利用溶剂萃取和多种色谱技术分离纯化,以1H-NMR,13C-NMR波谱方法,结合文献数据,鉴定化合物结构。结果:香椿果提取物具有显著抗补体活性,经溶剂萃取,其中乙酸乙酯部位为活性部位,从中分离得到14个化合物,分别鉴定为没食子酸(1),没食子酸甲酯(2),6-O-没食子酰基-葡萄糖(3),1,2,3-三-O-没食子酰基-β-D-葡萄糖(4),1,2,6-三-O-没食子酰基-β-D-葡萄糖(5),1,2,3,6-四-O-没食子酰基-β-D-葡萄糖(6),1,2,3,4,6-五-O-没食子酰基-β-D-葡萄糖(7),槲皮素-3-O-α-L-鼠李糖苷(8),芦丁(9),异鼠李素-3-O-β-半乳糖苷(10),槲皮素-3-O-β-半乳糖苷(11),山柰酚-3-O-β-D-葡萄糖苷(12),山柰酚-3-O-α-L-鼠李糖苷(13),槲皮素(14)。其中化合物3~14为首次从香椿果中分离得到,化合物5,10,11为首次从香椿中分离得到。化合物4~7有显著抗补体活性,半数抑制浓度(IC_(50))分别为88.3,76.2,13.9,9.6μmol·L^(-1)。结论:香椿果活性部位为乙酸乙酯萃取部位,活性成分为其中没食子酰基葡萄糖苷衍生物和黄酮苷,前者抗补体活性显著强于后者,并且其抗补体活性随着与葡萄糖羟基相连接的没食子酰基数目的增加而增强。
Objective： To investigate the anti-complement constituents from the fruits of Toona sinensis. Method： The anti-complement constituents were screened by hemolysis method, then isolated and purified with different chromatographic techniques. Their structures were elucidated with the methods of 1H-NMR, 13 C-NMR and together with the comparison of reported data. Result： The methanol extracts of the fruits of T. sinensis showed apparent anti-complement activity, and fourteen polypenols were isolated from the active EtOAc fraction. The structures of the compounds were identified as gallic acid （1）, methyl gallate （2）, 6-O-galloyl-D-glucpyranose （3）, 1, 2, 3-tri-O-galloyl-β-D-glucopyranose （4）, 1, 2, 6-tri-O-galloyl-β-D-glucopyranose （5）, 1, 2, 3, 6-tetra-O-galloyl-β-D-glucopyranose （6）, 1, 2, 3, 4, 6-penta-O-galloyl-β-D-glucopyranose （7）, quercetin-3-O- α-L-rhamnopyanoside （ 8 ）, rutin （ 9 ）, isorhamnetin-3-O-/3-galactopyranoside （ 10 ）, quercetin-3-O-β- galactopyranoside （ 11 ） , kaempferol-3-O-β-D-glucopyranoside （ 12 ） , kaempferol-3-O-α-L-rhamnopyranoside （13）, and quercetin （14） . Compounds 3-14 were isolated from the fruits of T. sinensis for the first time, and compounds 5, 10 and 11 were isolated for the first time from the plant. Compounds 4-7 showed apparent anti- complement activity, with the IC50 of 88.3, 76.2, 13.9 and 9.6 μmmol · L-1 respectively. Conclusion： The methanol extracts of the fruits of T. sinensis showed apparent anti-complement activity, and the EtOAc fraction was the active fraction. Epigallocatechin glucoside derivatives and flavonoids were the active components, and the former ones showed more potent anti-complement activity than the flavonoids; in addition, the activity was increased with the increasing of numbers of galloyl moieties.
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2017年第21期52-58,共7页
Chinese Journal of Experimental Traditional Medical Formulae
基金
国家"十三五"重点研发计划项目(2016YFC0502607-01)
贵州省科技创新人才团队项目[黔科合平台人才(2016)5625号]
贵州省高层次创新型人才培养项目[黔科合人才(2016)4018号]
关键词
香椿
抗补体活性
多酚
黄酮
Toona sinensis
anti-complement
polyphenols
flavonoids
