Berberine: A Bitter Phytochemical With Diversely Sweet Therapeutic Properties

Phytochemicals are bioactive secondary plant metabolites that can exert various biological effects in humans and animals. To date, hundreds of different phytochemicals have been identified along with their health-promoting effects. These substances are extracted from various parts of plants, purified, and processed as the main compounds in dietary supplements or nutraceuticals. Among them, berberine has been recognized for its diverse metabolic and therapeutic properties against cardiovascular disorders, type 2 diabetes, hypercholesterolemia, acute and chronic renal disorders, fatty liver disease, various forms of cancer, periodontitis, and others. The best-described mechanisms of action for its health-promoting effects are proposed to be through enhancing the endogenous antioxidant system, inhibiting the secretion of inflammatory cytokines, upregulating hepatic LDL receptors, enhancing insulin secretion, inhibiting hepatic gluconeogenesis, and regulating blood pressure and heart rate among others. In this article, we critically reviewed and summarized well-designed in vitro and in vivo studies, including recent clinical trials investigating the metabolic and therapeutic properties of berberine and its derivatives. Among the many health-promoting effects of berberine and its derivatives, their efficacy in managing type 2 diabetes is particularly promising. Indeed, available evidence suggests that further investigations may reveal that berberine ursodeoxycholate offers comparable efficacy to metformin, with fewer side effects. The superior efficacy and safety profile make this agent suitable for patients with type 2 diabetes with kidney and liver complications.