目的 研究芫花Daphne genkwa枝叶中三萜类成分及其α-葡萄糖苷酶抑制活性。方法 运用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、半制备高效液相色谱及重结晶等多种分离方法进行分离纯化,根据理化性质以及波谱数据对分离的单体化合物进行结构鉴定,对获得的化合物测定α-葡萄糖苷酶抑制活性。结果 从芫花95%乙醇提取物中共分离得到20个三萜类化合物,分别鉴定为山楂酸(1)、常春藤皂苷元(2)、齐墩果酸(3)、3β,13β-dihydroxyolean-11-en-28-oic acid(4)、11-oxoerythrodiol(5)、3β-hydroxy-11-oxo-olean-12-en-28-oic acid(6)、坡模酸(7)、3β-hydroxyolean-12-en-28-aldehyde(8)、3β-hydroxyolean-12-en-11-one(9)、3-羰基齐墩果酸(10)、古柯二醇(11)、oleanolic acid 2-oxopropyl ester(12)、熊果酸(13)、ilelatifol A(14)、3β-hydroxy-11-oxours-12-en-28-oic acid(15)、2α,3β-dihydroxyurs-12-en-28-oic acid(16)、3β-hydroxy-11-oxo-ursan-12-ene(17)、2-oxopropyl (3β)-3-hydroxyurs-12-en-28-oate(18)、熊果醛(19)和11α-methoxyurs-12-ene-3β,12-diol(20)。其中化合物1、3、4、13、15和16对α-葡萄糖苷酶具有较明显的抑制活性。结论 化合物6为首次从芫花中分离得到。化合物1~5、7~20为瑞香属内首次分离得到。化合物1、3、4、13、15和16表现出高于阳性对照阿卡波糖的α-葡萄糖苷酶的抑制活性,这表明芫花的枝叶中含具有降糖作用的天然活性分子。

Objective To investigate the triterpenoid constituents and their inhibitory effect on α-glucosidase found in the branches and leaves of Yuanhua (Daphne genkwa Sieb. et Zucc). Methods The 95% ethanol extract of D. genkwa was separated and purified by silica gel, Sephadex LH-20, semi-preparative HPLC and other separation methods, and the structures of the isolates were identified according to the physical and chemical properties as well as spectral data. The inhibitory effect on α-glucosidase of the obtained compounds was examined. Results A total of 20 triterpenoids were elucidated as maslinic acid (1), hederagenin (2), oleanolic acid (3), 3β,13β-dihydroxyolean-11-en-28-oic acid (4), 11-oxoerythrodiol (5), 3β-hydroxy-11-oxo-olean-12-en-28-oic acid (6), pomolic acid (7), 3β-hydroxyolean-12-en-28-aldehyde (8), 3β-hydroxyolean-12-en-11-one (9), 3-oxo-oleanolic acid (10), erythrodiol (11), oleanolic acid 2-oxopropyl ester (12), ursolic acid (13), ilelatifol A (14), 3β-hydroxy-11-oxours-12-en-28-oic acid (15), 2α,3β-dihydroxyurs-12-en-28-oic acid (16), 3β-hydroxy-11-oxo-ursan-12-ene (17), 2-oxopropyl(3β)-3-hydroxyurs-12-en-28-oate (18), ursolic aldehyde (19) and 11α-methoxyurs-12-ene-3β,12-diol (20). Amongst, compounds 1, 3, 4, 13, 15 and 16 were observed with good inhibitory activity against α-glucosidase. Conclusion Compound 6 was reported from Daphne genkwa Sieb. et Zucc for the first time. Compounds 1-5 and 7-20 were reported from Daphne genus for the first time. Compounds 1, 3, 4, 13, 15 and 16 displayed superior inhibitory activity compared to the positive control acarbose against α-glucosidase. This suggests the presence of bioactive constituents with hypoglycemic activity in the branches and leaves of D. genkwa.

国家自然科学基金资助项目（22177016）；山东省中医药科技发展计划项目（2020M037）；2019年医疗服务与保障能力提升补助资金“全国中药资源普查项目”（财社［2019］39号）