Berberine is an
alkaloid from several medicinal plants originally used to treat
diarrhea and
dysentery as a traditional Chinese herbal medicine. In recent years,
berberine has been discovered to exhibit a wide spectrum of biological activities in the treatment of diverse diseases ranging from
cancer and neurological dysfunctions to metabolic disorders and
heart diseases. This review article summarizes the clinical practice and laboratory exploration of
berberine for the treatment of cardiometabolic and
heart diseases, with a focus on the novel insights and recent advances of the underlying mechanisms recognized in the past decade.
Berberine was found to display pleiotropic
therapeutic effects against
dyslipidemia,
hyperglycemia,
hypertension,
arrhythmia, and
heart failure. The mechanisms of
berberine for the treatment of cardiometabolic disease involve combating
inflammation and oxidative stress such as inhibiting
proprotein convertase subtilisin/kexin 9 (PCSK9) activation, regulating electrical signals and
ionic channels such as targeting human
ether-a-go-go related gene (hERG) currents, promoting energy metabolism such as activating
adenosine monophosphate-activated
protein kinase (AMPK) signaling pathway, modifying gut microbiota to promote transforming of
berberine into its intestine-absorbable form, and interacting with non-coding RNAs via targeting multiple signaling pathways such as AMPK, mechanistic target of
rapamycin (mTOR), etc. Collectively,
berberine appears to be safe and well-tolerated in clinical practice, especially for those who are intolerant to
statins. Knowledge from this field may pave the way for future development of more effective pharmaceutical approaches for managing cardiometabolic risk factors and preventing
heart diseases.