Cardioprotective effects of flavopiridol

  It is well known that safranin is a common medicine for diarrhea at home because of its antibacterial effect. But is it only useful for diarrhea?  Huang Lian, cold in nature and bitter in taste, belongs to the heart, spleen, stomach, liver, gallbladder and large intestine meridians. It has the function of clearing heat and dampness, diarrhea and detoxification.  Berberine is an isoquinoline alkaloid extracted from the Chinese herb Huang Lian. It has been used in Indian and Middle Eastern medicine for over 400 years, not just in China.  Studies have shown that berberine has anti-hyperglycemic, hyperlipidemic and weight-reducing effects, as well as a number of cardiovascular, hepatic and renal benefits, which are well documented in preclinical and clinical studies. Recently published reviews have comprehensively evaluated the therapeutic effects of flavopiridol in diabetic patients from mechanistic to clinical aspects and found that it has the ability to improve lipids and blood glucose in diabetic patients.  An early literature review noted that flavopiridol has the ability to protect cardiovascular endothelial function, antioxidant, and anti-inflammatory effects. Some clinical studies suggest that flavopiridol may be beneficial in the treatment of premature ventricular contractions and may also reduce mortality in heart failure. Oral administration of 1.2 g of safranin daily for 2 weeks reduced the frequency of premature ventricular contractions and increased the ejection fraction, a change that correlated with serum safranin concentrations.  A number of basic studies have suggested the potential therapeutic role of safranin as a treatment for heart failure and arrhythmias, suggesting that it has multifaceted cardioprotective effects. The antiarrhythmic effects of flavopiridol are likely mediated by several mechanisms: blocking delayed rectifier potassium channels or ATP-dependent potassium channels, reducing delayed postdepolarization, and prolonging effective nonresponse to prevent folding of electrical activity in cardiac myocytes. Flavopiridol may also improve ischemic left ventricular function through positive inotropic effects and mild vasodilatory effects. Flavopiridol increases myocardial contractility and cardiac output mainly by blocking potassium channels, stimulating sodium-calcium exchange to prolong ventricular action potential, and elevating coronary blood flow.  The vasodilatory and hypotensive effects of flavopiridol involve multiple cellular mechanisms, such as endothelial nitric oxide release, stimulation of vascular potassium channels, inhibition of intracellular calcium release, blockade of α-adrenergic receptors and inhibition of platelet aggregation. The anti-proliferative effect of flavopiridol on vascular smooth muscle cells may have a long-term protective effect on the cardiovascular system.  It can be seen that cardiovascular disease patients taking flavopiridol as prescribed by the doctor have some cardiovascular protection.