目的 研究茜草科虎刺属植物海南虎刺Damnacanthus hainanensis枝叶中的化学成分及其抗类风湿性关节炎活性。方法 综合运用硅胶柱色谱、反相硅胶柱色谱、Sephadex LH-20凝胶柱色谱以及制备型HPLC等色谱技术进行系统分离和纯化，根据分离得到化合物的理化性质及其波谱数据，并通过与文献中报道的波谱数据进行比对，鉴定化合物的结构；采用MTS法通过对分离得到化合物的体外抑制滑膜细胞增殖的活性进行测试以评价其抗类风湿性关节炎活性。结果 从海南虎刺枝叶的甲醇提取物中分离得到了18个化合物，分别鉴定为naucleidinal（1）、1,2,3,4-tetrahydronorharman-1-one（2）、19-O-methyl-3,14-dihydroangustoline（3）、latifoliamide B（4）、latifoliamide D（5）、bacilsubteramide A（6）、vinmajine I（7）、naucleofficine D（8）、1-甲氧甲酰-β-咔巴啉（9）、naphthisoxazol A（10）、1,6-dihydroxy-2-methyl-9,10-anthraquinone（11）、rubiadin-1-methyl ether（12）、1,3,6-trihydroxy-2-methoxymethyl-9,10-anthraquinone（13）、3,6-dihydroxy-2-hydroxymethyl-9,10-anthra quinone（14）、7-羟基色原酮（15）、5,7-二羟基色原酮（16）、6,4'-dihydroxy-3'-methoxyaurone（17）和farnisin（18）。抗类风湿性关节炎活性评价结果表明，化合物11～14、17和18对滑膜成纤维MH7A细胞增殖抑制活性的半数抑制浓度（median inhibition concentration，IC₅₀）值为（8.93±0.09）～（152.58±0.32）μmol/L。结论 所有化合物均为首次从虎刺属植物中分离得到。化合物11～14、17和18表现出了较为显著的抗类风湿性关节炎活性。

Objective To study the chemical constituents in the stems and leaves of Hainanhuci (Damnacanthus hainanensis) and their anti-rheumatoid arthritis activities. Methods The chemical constituents in the stems and leaves of D.hainanensis were isolated and purified by silica gel, ODS, Sephadex LH-20 gel column chromatographies and preparative HPLC. The chemical structures of all isolates were identified using physicochemical properties, spectroscopic analyses, as well as the comparisons with the reported data in literature. In addition, all isolates were evaluated for their anti-rheumatoid arthritis activities using MTS method, via measuring their anti-proliferative effects on synoviocytes in vitro. Results A total of 18 compounds were isolated from the methanol extract of the stems of D.hainanensis, which were identified as naucleidinal (1), 1,2,3,4-tetrahydronorharman-1-one (2), 19-O-methyl-3,14-dihydro angustoline (3), latifoliamide B (4), latifoliamide D (5), bacilsubteramide A (6), vinmajine I (7), naucleofficine D (8), 1-carbomethoxy-β-carboline (9), naphthisoxazol A (10), 1,6-dihydroxy-2-methyl-9,10-anthraquinone (11), rubiadin-1-methyl ether (12), 1,3,6-trihydroxy-2-methoxymethyl-9,10-anthraquinone (13), 3,6-dihydroxy-2-hydroxy methyl-9,10-anthraquinone (14), 7-hydroxychromone (15), 5,7-dihydroxychromone (16), 6,4'-dihydroxy-3'-methoxyaurone (17), and farnisin (18). Compounds 11-14, 17 and 18 displayed the inhibitory effects on the proliferation of MH7A synovial fibroblast cells with the IC₅₀ values in range of (8.93 ±0.09) to (152.58 ±0.32) μmol/L. Conclusion All compounds are isolated from the genus Damnacanthus for the first time, and compounds 11-14, 17 and 18 exhibited remarkable anti-rheumatoid arthritis activities.

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海南省自然科学基金项目(220RC596,222RC655,2019RC198);国家自然科学基金项目(21967008);国家自然科学基金项目(32070390);国家自然科学基金项目(22067005);海南省重点研发专项(ZDYF2022SHFZ028);海口市重点研发计划项目(2020054,2017050);海南省省级大学生创新训练项目(S202211658025,S202211658028);海南师范大学校级大学生创业实践项目(HSRS21-037)