The antioxidant, anti-α-glucosidase and anticholinesterase activity of the leaves and rhizomatous extract of Bergenia cordifolia were investigated. The rhizomes extract that showed a higher degree of 1,1-diphenyl-2-picrylhydrazyl radical scavenging and anti-α-glucosidase activity than reference compounds (rutin and acarbose respectively) were subjected to phytochemical analysis. The study revealed that previously unknown minor constituents from the plant, (+)-catechin 3-O-gallate, (+)-catechin 3,5-di-O-gallate and 1,2,4,6-tetra-O-galloyl-β- d-glucopyranoside, were the radical scavenging and anti-α-glucosidase principles. These compounds as well as the crude extracts were weak acetylcholienesterase inhibitors, suggesting a higher degree of selectivity against α-glucosidase enzyme. In comparison with the minor constituents, the previously known major constituents of the plant, bergenin and arbutin, were poor radical scavengers and enzyme inhibitors. Copyright © 2011 John Wiley & Sons, Ltd.