An insight into the medicinal attributes of berberine derivatives: A review

In the last few decades, traditional natural products have been the center of attention for the scientific community and exploration of their therapeutic abilities is proceeding perpetually. Berberine, with remarkable therapeutic diversity, is a plant derived isoquinoline alkaloid which is widely used as a traditional medicine in China. Berberine has been tackled as a fascinating pharmacophore to make great contributions to the discovery and development of new therapeutic agents against variegated diseases. Despite its tremendous therapeutic potential, clinical utility of this alkaloid was significantly compromised due to undesirable pharmacokinetic properties. To overcome this limitation, several structural modifications were performed on this scaffold to improve its therapeutic efficacy. The collective efforts of the community have achieved the tremendous advancements, bringing berberine to clinical use and discovering new therapeutic opportunities by structural modifications on the berberine scaffold. In this review, recent advancements in the medicinal chemistry of berberine and its derivatives in the last few years (2016?2020) have been compiled to represent inclusive data associated with various biological activities of this alkaloid. The comprehensive structure?activity relationship studies along with molecular modelling and mechanistic studies have also been summarized. This article would be highly helpful for the scientific community to get better insight into medicinal research of berberine and become a compelling guide for the rational design of berberine based compounds.

Automated summary

Berberine, a plant-derived isoquinoline alkaloid, has shown remarkable therapeutic diversity and potential for the discovery of new therapeutic agents. Despite its clinical utility being compromised by undesirable pharmacokinetic properties, structural modifications have been made to improve its therapeutic efficacy, leading to significant advancements in its medicinal chemistry. This review provides a comprehensive overview of recent advancements in the field and serves as a valuable guide for the rational design of berberine-based compounds.