Red Yeast Rice Plus Berberine: Practical Strategy for Promoting Vascular and Metabolic Health

Lovastatin, the progenitor of the statin family, is in fact a naturally occurring compound produced by the yeast Monascus purpureus. Red yeast rice (RYR), a traditional Chinese food made by fermenting rice with M purpureus, is an herbal medicine that has been used for 1200 y as a therapy for problems related to circulation and digestion. RYR contains a range of compounds known as monacolins, of which monacolin K-renamed lovastatin by pharmaceutical researchers-was found to be the most potent inhibitor of cholesterol synthesis. Standardized extracts of RYR, providing 10 mg of monacolins daily, have been shown to lower elevated low-density lipoprotein (LDL) cholesterol by approximately 20%. In a large secondary prevention trial in China, RYR was found to be markedly protective with respect to cardiovascular events and total mortality. Yet RYR very rarely induces the myopathy and hepatic damage commonly seen with prescription statin therapy. The Chinese herbal compound berberine, used to treat diabetes and congestive heart failure in China, has been shown to increase hepatic expression of LDL receptors and, hence, to lower LDL cholesterol, by extending the half-life of LDL receptor messenger ribonucleic acid (mRNA). This effect is complementary to the increased transcription of this mRNA promoted by statin therapy. Because berberine is well tolerated aside from transient gastrointestinal (GI) upset in some people and, in particular, has not been reported to cause myopathy or hepatic damage, the combination of RYR and berberine may have the potential to achieve reductions in LDL cholesterol comparable with those achieved with prescription statin therapy, but without the associated risks such as muscle damage and diabetes. Moreover, berberine, via its ability to activate adenosine monophosphate-activated kinase (AMPK), which it shares with the drug metformin, can lower triglycerides, improve metabolic syndrome, aid glycemic control in diabetics, and act directly on the vasculature to promote vascular health. It may also have the potential to reduce risk for various cancers, osteoporosis, osteoarthritis, nonalcoholic fatty-liver disease, and neurodegenerative disorders, although such predictions are highly speculative. Whereas statin therapy modestly increases risk for type 2 diabetes, berberine likely has the opposite effect. These considerations suggest that combined administration of RYR and berberine may provide a broader range of health protection than is afforded by prescription statin therapy, with lower risks for serious adverse effects compared with statins. Randomized, controlled trials (RCTs) assessing the effect of optimal intakes of RYR and berberine on serum lipids and other vascular risk factors are needed.