Berberine: New Insights from Pharmacological Aspects to Clinical Evidences in the Management of Metabolic Disorders
Berberine: New Insights from Pharmacological Aspects to Clinical Evidences in the Management of Metabolic Disorders
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DOI：
10.2174/0929867323666160411143314
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发表时间：
2016-01-01
影响因子：
4.1
通讯作者：
Cicero, Arrigo F. G.
中科院分区：
文献类型：
--
作者：
Caliceti, Cristiana;Franco, Placido;Cicero, Arrigo F. G.
黄连素是一种季铵盐，来自异喹啉生物碱中的原小檗碱族，存在于性别黄连科等植物中。黄连素被认为可以改善糖脂代谢紊乱，初步的临床证据表明，黄连素能够减少内皮炎症，改善血管健康，即使在已经受到心血管疾病影响的患者中也是如此，这表明小黄碱及其代谢物在临床实践中可能具有有趣的作用。然而，黄连素的理化性质、药代动力学和代谢还没有完全阐明，报道了相互矛盾的数据。本文综述了黄连素的药理和生物学特性，重点介绍了黄连素及其药理活性代谢物及其活性的不同机制，以阐明黄连素单独或与其他营养食品联合应用于治疗与心血管疾病风险增加相关的代谢紊乱的正确使用。还特别注意评估其在各种情况下的短期和中期使用耐受性、安全性和有效性的现有临床试验，如血脂异常、空腹血糖受损、代谢综合征和2型糖尿病。
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.