Berberine and its derivatives represent as the promising therapeutic agents for inflammatory disorders.

Berberine, with the skeleton of quaternary ammonium, has been considered as the well-defined natural product in treating multiple diseases, including inflammation, acute and chronic infection, autoimmune diseases, and diabetes. However, due to the low bioavailability and systemic exposure, broad clinical applications of berberine have been largely impeded. Numerous studies have been conducted to further explore the therapeutic capacities of berberine in preclinical and clinical trials. Over the past, berberine and its derivatives have been shown to possess numerous pharmacological activities, as evidenced in intestinal, pulmonary, skin, and bone inflammatory disorders. In the present review, the pharmacological impact of berberine on inflammatory diseases are fully discussed, with indication that berberine and its potential derivatives represent promising natural therapeutic agents with anti-inflammatory properties.