Synthesis and antiglycation potentials of bergenin derivatives

Bergenin (1), major bioactive compound isolated from methanolic extract of Mallotus philippinensis, displayed moderate AGE inhibition activity (IC50 = 186.73 μM). A series of derivatives of bergenin (3a–k) containing variety of aromatic acids were synthesized under mild conditions by modification of sugar part. Selective esterification of hydroxyl groups on the sugar part enhanced antiglycation potential of bergenin. Compounds 3j and 3k exhibited potent antiglycation activity with the IC50 values of 60.75 and 12.28 μM, respectively.

Graphical abstractA series of bergenin derivatives have been prepared and tested for their antiglycation properties.Figure optionsDownload full-size imageDownload as PowerPoint slide