海滨木巴戟中化学成分及其体外抑制滑膜细胞增殖活性研究  

Chemical constituents from Morinda citrifolia and their inhibitory activities on proliferation of synoviocytes in vitro

作　　者：赵莹莹 于绡梅 乔泽华 李娟[2,3] 唐浩轩 陈光英 付艳辉[1,2,3] ZHAO Ying-ying;YU Qiao-mei;QIAO Ze-hua;LI Juan;TANG Hao-xuan;CHEN Guang-ying;FU Yan-hui(China School of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou 350122,China;Engineering Research Center for Industrialization of Southern Medicinal Plants Resources of Hainan Province,Hainan Normal University,Haikou 571158,China;Laboratory of Tropical Medicinal Plant Chemistry of Ministry of Education,Hainan Normal University,Haikou 571158,China)

机构地区：[1]福建中医药大学药学院,福建福州350122 [2]海南师范大学南药资源产业化关键技术研究海南省工程研究中心,海南海口571158 [3]海南师范大学热带药用资源化学教育部重点实验室,海南海口571158

出　　处：《中国中药杂志》2021年第10期2519-2526,共8页China Journal of Chinese Materia Medica

基　　金：海南省重点研发计划项目(ZDYF2019116);国家自然科学基金项目(22067005);国家级大学生创新创业训练计划项目(202011658012,202011658003S);海南省级大学生创新创业训练计划项目(S202011658029,S202011658009);海口市科技计划项目创新平台建设项目(2020054)。

摘　　要：综合运用硅胶柱色谱、ODS柱色谱、Sephadex LH-20凝胶柱色谱以及制备型HPLC等现代色谱分离技术对茜草科巴戟天属植物海滨木巴戟Morinda citrifolia枝叶中的化学成分进行系统研究。根据化合物的理化性质和波谱数据,并通过与文献中相应化合物数据进行对照,鉴定了从海滨木巴戟枝叶的90%乙醇提取物中分离得到了17个化合物,分别鉴定为9,10-dihydroxy-4, 7-megastigmadien-3-one (1)、5,12-epoxy-6,9-hydroxy-7-megastigmen-3-one (2)、fukinone (3)、β-eudesmol (4)、sarmentol F (5)、4,5-dihydroblumenol A (6)、3-hydroxy-β-ionone (7)、aristol-8-en-1-one (8)、ergosta-7-en-3β-ol (9)、ergosta-7-ene-3β,5α,6β-triol (10)、(22E)-5α,8α-epidioxyergosta-6,22-dien-3β-ol (11)、橄榄脂素(12)、4-epi-larreatricin (13)、chushizisin I (14)、rabdosia acid A (15)、glycerol monolinoleate (16)和(9Z,12Z,15Z)-2,3-二羟丙基十八碳三烯酸酯(17)。其中化合物1~8为倍半萜类化合物,9~11为甾体类化合物,12~14为木脂素类化合物,15~17为脂肪酸类化合物,所有化合物均为首次从海滨木巴戟中分离得到。采用MTS法通过评价分离得到的化合物的体外抑制滑膜细胞增殖的活性来评价分离得到的单体化合物的抗类风湿性关节炎活性。活性评价结果表明化合物1~11具有较为显著的抗类风湿性关节炎活性,它们对MH7A滑膜成纤维细胞增殖抑制活性的IC50为(38.69±0.86)~(203.45±1.03)μmol·L-1。The chemical constituents from the stems and leaves of Morinda citrifolia were isolated and purified by column chromatography methods with silica gel, ODS, Sephadex LH-20 and preparative high performance liquid chromatography(HPLC). The structures of the isolated compounds were identified by physicochemical properties and spectroscopic analysis, as well as comparisons with the data reported in literature. 17 compounds were isolated from the 90% ethanol extract of the stems and leaves of M. citrifolia, and were identified as 9,10-dihydroxy-4, 7-megastigmadien-3-one(1), 5,12-epoxy-6,9-hydroxy-7-megastigmen-3-one(2), fukinone(3), β-eudesmol(4), sarmentol F(5), 4, 5-dihydroblumenol A(6), 3-hydroxy-β-ionone(7), aristol-8-en-1-one(8), ergosta-7-en-3β-ol(9), ergosta-7-ene-3β,5α,6β-triol(10),(22E)-5α,8α-epidioxyergosta-6,22-dien-3β-ol(11), olivil(12), 4-epi-larreatricin(13), chushizisin Ⅰ(14), rabdosia acid A(15), glycerol monolinoleate(16) and(9Z,12Z,15Z)-2,3-dihydroxypropyl octadeca-trienoate(17). All compounds were isolated from M. citrifolia for the first time. All isolated compounds were evaluated for their anti-rheumatoid arthritis activities via examining their inhibitory activities on the proliferation of synoviocytes in vitro using MTS met-hod. Compounds 1-11 showed significant anti-rheumatoid arthritis activities, displaying the inhibitory effects on the proliferation of MH7 A synovial fibroblast cell with the IC50 values ranging from(38.69±0.86) to(203.45±1.03) μmol·L-1.

关 键 词：海滨木巴戟 倍半萜 甾体 木脂素 脂肪酸 滑膜细胞增殖抑制活性 

分 类 号：R284.1[医药卫生—中药学]