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

Abstract

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.

Keywords::

• Bergenin
• bergenin derivatives
• α-glucosidase inhibitor
• diabetes
• structure-activity relationship

Acknowledgments

I am grateful to Professor I. Horibe for number of valuable suggestions and discussions on this study. The author is grateful to assistant Professor T. Minemastsu (School of Pharmaceutical Sciences, Kinki University) for the NMR spectrometry experiments on this study.

Declaration of interest

The authors report no conflicts of interest.