苦瓜中葫芦烷型三萜成分及其抗肝纤维化活性的研究  

Cucurbitane triterpenoids from Momordica charantia L.and their anti-hepatic fibrosis activity

作　　者：岳佳音 徐静 张晓书 赵余庆 YUE Jiayin;XU Jing;ZHANG Xiaoshu;ZHAO Yuqing(School of Pharmacy,Shenyang Medical College,Shenyang 110034,China;School of Functional Food and Wine,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳医学院药学院,沈阳110034 [2]沈阳药科大学功能食品与葡萄酒学院,沈阳110016

出　　处：《西北药学杂志》2024年第1期26-31,共6页Northwest Pharmaceutical Journal

基　　金：沈阳医学院科技基金项目(编号:20195074)。

摘　　要：目的研究苦瓜酸水解产物的化学成分及其抗肝纤维化活性。方法用正、反相柱层析等色谱手段进行分离纯化,用波谱技术与文献数据对照鉴定其结构;并用四甲基偶氮唑盐(methylthiazolyl tetrazolium,MTT)法测定部分化合物体外对大鼠肝星状细胞(t-HSC/Cl-6)增殖的抑制作用。结果共分离出10个葫芦烷型三萜类化合物,分别鉴定为:5β,19-epoxy-3β-hydroxy-19(R)-methoxy-27-norcucurbita-6,23(E)-dien-25-one(1);5β,19-epoxy-3β-hydroxy-19(S)-methoxy-27-norcucurbita-6,23(E)-dien-25-one(2);5β,19-epoxy-25-methoxycucurbita-6,23(E)-dien-3β-ol(3);karavilagenin A(4);(23E)-5β,19-epoxycucurbita-6,23,25-triene-3β-ol(5);23E-5β,19-epoxy-cucurbita-6,23-dien-3β,25-diol(6);25-O-methylkaravilagein D(7);(23E)-3β-hydroxy-7β,25-dimethoxycucurbita-5,23-dien-19-al(8);karavilagenin B(9);(19S,23E)-5β,19-epoxy-19-methoxycucurbita-6,23-diene-3β,25-diol(10)。体外活性筛选发现化合物1和化合物2对t-HSC/Cl-6有一定的抑制细胞增殖作用,IC50分别为(25.92±2.63)、(26.22±2.77)μmol·L^(-1)。结论化合物1和化合物2为首次从该植物中分离得到,其对肝纤维化细胞增殖有一定的抑制作用。Objective To investigate the chemical constituents from acid hydrolyzed ethanol extract of Momordica charantia L.and their anti-hepatic fibrosis activity.Methods The compounds were isolated and purified by various chromatographic techniques,and their structures were identified by spectroscopic analysis and spectral data.Methylthiazolyl tetrazolium(MTT)assay was used to determine the cytotoxic activity of some compounds against activated rat hepatic stellate cells(t-HSC/Cl-6)in vitro.Results 10 cucurbitane triterpenoids were isolated from the acid hydrolyzed ethanol extract of M.charantia.Their structures were identified as 5β,19-epoxy-3β-hydroxy-19(R)-methoxy-27-norcucurbita-6,23(E)-dien-25-one(1);5β,19-epoxy-3β-hydroxy-19(S)-methoxy-27-norcucurbita-6,23(E)-dien-25-one(2);5β,19-epoxy-25-methoxycucurbita-6,23(E)-dien-3β-ol(3);karavilagenin A(4);(23E)-5β,19-epoxycucurbita-6,23,25-triene-3β-ol(5);23E-5β,19-epoxy-cucurbita-6,23-dien-3β,25-diol(6);25-O-methylkaravilagein D(7);(23E)-3β-hydroxy-7β,25-dimethoxycucurbita-5,23-dien-19-al(8);karavilagenin B(9);and(19S,23E)-5β,19-epoxy-19-methoxycucurbita-6,23-diene-3β,25-diol(10),respectively.Compounds 1 and 2 showed moderate cytotoxicity against the hepatic stellate cells tested in vitro with IC50 values of(25.92±2.63)and(26.22±2.77)μmol·L^(-1) respectively.Conclusion Compounds 1 and 2 were isolated from the fruit of M.charantia for the first time,and they can inhibit the proliferation of hepatic fibrotic cells.

关 键 词：苦瓜 葫芦烷型三萜化合物 抗肝纤维化活性 

分 类 号：R284.1[医药卫生—中药学]