没食子酰基 Bergenin 衍生物抑制 α-葡萄糖苷酶的构效关系研究。
Structure-activity relationships of bergenin derivatives effect on α-glucosidase inhibition.
机构信息
Department of Applied Chemistry, Faculty of Science and Engineering, Kinki University , Kowakae, Higashiosaka-shi, Osaka , Japan.
出版信息
J Enzyme Inhib Med Chem. 2013 Dec;28(6):1162-70. doi: 10.3109/14756366.2012.719503. Epub 2012 Sep 26.
The α-glucosidase inhibitory activities of bergenin derivatives were evaluated. Bergenin derivatives were synthesized from bergenin which is a characteristic compound of B. ligulata. A new bergenin derivative, 11-O-(3',4'-dimethoxybenzoyl)-bergenin showed the highest potent inhibitory activity among those of bergenin derivatives. The presence of substituents at 3',4'-position in bergenin derivatives altered the α-glucosidase inhibitory activity. 11-O-(3',4'-dimethoxybenzoyl)-bergenin was noncompetitive inhibitor for α-glucosidase. The present study reveals that bergenin derivatives could be classified as a new group of α-glucosidase inhibitors.
本研究评价了岩白菜素衍生物的α-葡萄糖苷酶抑制活性。岩白菜素衍生物是从岩白菜素中合成的，岩白菜素是岩白菜属植物的特征化合物。在岩白菜素衍生物中，11-O-(3',4'-二甲氧基苯甲酰基)-岩白菜素表现出最高的α-葡萄糖苷酶抑制活性。岩白菜素衍生物在 3'，4'-位取代基的存在改变了α-葡萄糖苷酶抑制活性。11-O-(3',4'-二甲氧基苯甲酰基)-岩白菜素是非竞争性α-葡萄糖苷酶抑制剂。本研究表明，岩白菜素衍生物可归类为新型α-葡萄糖苷酶抑制剂。
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