Caliceti Cristiana, Franco Placido, Spinozzi Silvia, Roda Aldo, Cicero Arrigo F G
Atherosclerosis Research Unit, Poliambulatorio Pad. 2, Via Albertoni, 15, 40138 Bologna, Italy.
Curr Med Chem. 2016;23(14):1460-76. doi: 10.2174/0929867323666160411143314.
Berberine is a quaternary ammonium salt from the protoberberine group of isoquinoline alkaloids found in such plants as gender Berberis. Berberine is recognised to improve glucose and lipid metabolism disorders and preliminary clinical evidences suggest the ability of berberine to reduce endothelial inflammation improving vascular health, even in patients already affected by cardiovascular diseases, suggesting a possible interesting role of berberine and its metabolites in clinical practice. However, its physicochemical properties, pharmacokinetic, and metabolism are not fully elucidated and contradictory data have been reported. This review provides a summary regarding the pharmacological and biological features of berberine, with a focus on berberine as well as their pharmacologically active metabolites and the different mechanisms underlying their activities in order to clarify the correct use of berberine supplementation, alone or in association with other nutraceuticals, for the management of metabolic disorders associated to increased cardiovascular disease risk. A particular attention has also been given to the available clinical trials assessing its short- and middle- term use tolerability, safety and efficacy in various conditions, such as dyslipidaemia, impaired fasting glucose, metabolic syndrome and type 2 diabetes.
小檗碱是一种来自原小檗碱类异喹啉生物碱的季铵盐，存在于如小檗属植物等植物中。小檗碱被认为可改善葡萄糖和脂质代谢紊乱，初步临床证据表明，即使在已患有心血管疾病的患者中，小檗碱也有降低内皮炎症、改善血管健康的能力，这表明小檗碱及其代谢产物在临床实践中可能具有有趣的作用。然而，其理化性质、药代动力学和代谢尚未完全阐明，且已报道了相互矛盾的数据。本综述总结了小檗碱的药理和生物学特性，重点关注小檗碱及其药理活性代谢产物，以及其活性背后的不同机制，以阐明单独或与其他营养保健品联合使用小檗碱补充剂治疗与心血管疾病风险增加相关的代谢紊乱的正确用法。还特别关注了评估其在血脂异常、空腹血糖受损、代谢综合征和2型糖尿病等各种情况下短期和中期使用耐受性、安全性和有效性的现有临床试验。
