Acacetin is a Promising Drug Candidate for Cardiovascular Diseases.

AUTOIMMUNE disease prevention; CHINESE medicine; ANTICOAGULANTS; CARDIOVASCULAR diseases; CARDIOMYOPATHIES; FLAVONOIDS; HERBAL medicine; BRUGADA syndrome; PHYTOCHEMICALS; HEART failure; PLANT extracts; PHARMACY information services; MYOCARDIAL injury; MOLECULAR structure; MEDICINAL plants; ATRIAL fibrillation; MYOCARDIUM; VENTRICULAR arrhythmia; CARDIOTOXICITY; DIABETIC cardiomyopathy; BIOAVAILABILITY; CEREBRAL infarction; CARDIOVASCULAR agents; MYOCARDIAL depressants; HEART cells; PHARMACODYNAMICS

Phytochemical flavonoids have been proven to be effective in treating various disorders, including cardiovascular diseases. Acacetin is a natural flavone with diverse pharmacological effects, uniquely including atrial-selective anti-atrial fibrillation (AF) via the inhibition of the atrial specific potassium channel currents I Kur (ultra-rapidly delayed rectifier potassium current), I KACh (acetylcholine-activated potassium current), I sKCa (calcium-activated small conductance potassium current), and I to (transient outward potassium current). I to inhibition by acacetin, notably, suppresses experimental J-wave syndromes. In addition, acacetin provides extensive cardiovascular protection against ischemia/reperfusion injury, cardiomyopathies/heart failure, autoimmune myocarditis, pulmonary artery hypertension, vascular remodeling, and atherosclerosis by restoring the downregulated intracellular signaling pathway of Sirt1/AMPK/PGC-1α followed by increasing Nrf2/HO-1/SOD thereby inhibiting oxidation, inflammation, and apoptosis. This review provides an integrated insight into the capabilities of acacetin as a drug candidate for treating cardiovascular diseases, especially atrial fibrillation and cardiomyopathies/heart failure. [ABSTRACT FROM AUTHOR]

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