Bergenin, a natural secondary metabolite, has been isolated from different parts of a number of plants. It is one of active ingredients in herbal and Ayurvedic formulations. It exhibits antiviral, antifungal, antitussive, antiplasmodial, antiinflammatory, antihepatotoxic, antiarrhythmic, antitumor, antiulcerogenic, antidiabetic and wound healing properties. It has been analyzed and estimated in different plant extracts, blood and drug samples using chromatographic techniques, and pharmacokinetic studies have been made. Several bergenin derivatives were isolated and/or synthesized and were found to possess pharmacological activities. Total synthesis of bergenin and its derivatives were reported. This review article covers literature on bergenin and its derivatives until 2013. Ethnomedicinal value of bergenin containing plant materials is also highlighted. This comprehensive review provides information on the potentiality of bergenin and its derivatives for therapeutic usages.
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