Update on the Benefits and Mechanisms of Action of the Bioactive Vegetal Alkaloid Berberine on Lipid Metabolism and Homeostasis

Abstract

Elevation of circulating levels of blood cholesterol, especially LDL cholesterol, and/or the decrease of HDL cholesterol levels have long been recognized as primary risk factors for developing atherosclerosis that leads to cardiovascular and cerebrovascular disease. Hypertriglyceridemia is an independent risk factor that is known to contribute to the development of atherosclerosis. Thus, various interventional efforts aimed at reducing hypercholesterolemia and hypertriglyceridemia have been practiced clinically for decades to reduce morbidity and mortality risk associated with deleterious cardiovascular and cerebrovascular events. As such, many drugs have been developed and clinically used to treat hypocholesteremia and/or hypertriglyceridemia; however, dietary approaches including supplements along with changes in nutrition and lifestyle have become increasingly attractive and acceptable methods used to control borderline or moderately increased levels of blood cholesterol and triacylglycerols. In this regard, the use of a plant/herbal bioactive compound, berberine (BBR), has recently been studied extensively in terms of its efficacy as well as its mechanisms of action and safety as an alternative intervention that beneficially modulates blood lipids. The aim of this review is to provide a comprehensive update on BBR research, new concepts and directions in terms of product development and current challenges, and future prospects of using BBR to manage diseases and complications associated with dyslipidemia.

Dietary berberine regulates lipid metabolism in muscle and liver of black sea bream (Acanthopagrus schlegelii) fed normal or high-lipid diets

“…Notably, numerous studies have demonstrated that BBR can reduce lipogenesis by down-regulating pparγ expression in different tissues (11,29,45,61,62) . Hence, the lipid-lowering effect of BBR was mainly attributed to the fact that it can mitigate lipid accumulation in liver through down-regulating lipogenesis and up-regulating lipolysis pathways, similar to mechanisms reported in mammals (14,42,61) .…”

“…Several studies reported that some feed additives could reduce liver lipid deposition and alleviate the adverse effects caused by HL diets, such as bile acids (8,9) , L-carnitine (10) , fenofibrate (11) , choline, betaine (12) and xylooligosaccharides (13) . Berberine (BBR) (18,5,6-dyhydro-9,10-dimethoxybenzo(g)-1,3benzodioxolo(5,6-a) quinolizinium) is an isoquinoline alkaloid isolated from Coptis chinensis (Chinese goldthread), Hydrastis canadensis (goldenseal), Berberis vulgaris (barberry) and other herbs (14) or manufactured by chemical synthesis. It has been commonly used in Chinese medicine for its antiinflammatory, antibacterial, antioxidant and antiapoptotic Abbreviations: accα, acetyl-CoA carboxylase α; ALT, alanine aminotransferase; AST, aspartate aminotransferase; BBR, berberine; Con, control; ConB, control diet with berberine supplementation; cpt1a, carnitine palmitoyltransferase 1a; fas, fatty acid synthase; FI, feed intake; g6pd, glucose 6-phosphate dehydrogenase; HL, high lipid; HLB, high-lipid diet with berberine supplementation; hsl, hormone-sensitive lipase; lpl, lipoprotein lipase; LPS, lipase; srebp-1, sterol regulatory element binding protein-1; VSI, viscerosomatic index; 6pgd, 6-phosphogluconate dehydrogenase.…”

Antiviral activity of berberine

“…It is present in several medicinal plants, such as Berberis vulgaris, Coptis chinensis, Hydrastis canadensis, Coptidis rhizoma, Xanthoriza simplicissima, Phellodendron amurense, and Chelidonium majus. Berberine exhibits unusual biochemical and pharmacological activities, including antidiabetic [1], hypolipidemic [2], antihypertensive [3], anti-inflammatory [4], antidiarrheal [5], hepatoprotective [6], antidepressant [7], anticancer [8], antibacterial [9], and antiviral [10] properties. BBR is capable of penetrating all cell lines, but the cumulative concentration is the highest in Hep G-2 cells [11].…”

Efficacy of Hwangryunhaedok-tang (Huang-lian-jie-du-tang, Oren-gedoku-to) for patients with hyperlipidemia: a study protocol for a randomized, double-blind, placebo-controlled, parallel, investigator-initiated clinical trial

“…In addition, in the high-cholesterol animal model, the administration of HHT for 8 weeks significantly prevented the progression of thoracic aortic plaque with an anti-oxidative effect [ 13 ]. In particular, Berberine , a component of HHT, has been reported to reduce TC and LDL-C levels and increase high-density lipoprotein cholesterol (HDL-C) levels in animals and humans through mechanisms such as absorption of cholesterol in the intestine, removal of LDL receptor-mediated LDL-C, and conversion of cholesterol into bile [ 14 ]. In a randomized controlled trial (RCT) comparing HHT and statins in patients with hyperlipidemia, both groups exhibited significantly decreased TC, TG, and LDL-C and significantly increased HDL-C after treatment, compared to the levels before treatment.…”