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J Enzyme Inhib Med Chem. 2013 Dec;28(6):1162-70. doi: 10.3109/14756366.2012.719503. Epub 2012 Sep 26.

Structure-activity relationships of bergenin derivatives effect on α-glucosidase inhibition.

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Department of Applied Chemistry, Faculty of Science and Engineering, Kinki University , Kowakae, Higashiosaka-shi, Osaka , Japan.


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.

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