摘要
小檗碱是在像小檗这样的植物中发现的异喹啉类生物碱中原小檗碱中的季铵盐。小檗碱被公认能改善糖和脂代谢紊乱,初步临床证据表明小檗碱有减少血管内皮细胞的炎症改善血管健康的能力,甚至在患者已经受心血管疾病的影响后,这表明小檗碱及其代谢产物在临床实践中可能起有趣的作用。然而,其理化性质,药代动力学和代谢并没有被完全阐明,也已被报道了矛盾的数据。 本文提供了一个关于小檗碱的总结,以集中于小檗碱及其药理活性代谢物及相关活动下不同的机制来代替它的药理和生物特征,以明确黄连素食品补充剂使用,单独使用或与其他保健品协同使用的正确,为了与心血管疾病风险增加相关的代谢性疾病的管理。我们特别关注了可供临床试验评估其短期和中长期使用的耐受性,在各种条件下的安全性和有效性,如血脂异常、空腹血糖受损、代谢综合征和2型糖尿病。
关键词: 小檗碱、理化性质、代谢、生物利用度、安全性、hyperglicemia、血脂紊乱、心血管疾病。
Current Medicinal Chemistry
Title:Berberine: New Insights from Pharmacological Aspects to Clinical Evidences in the Management of Metabolic Disorders
Volume: 23 Issue: 14
Author(s): Cristiana Caliceti, Placido Franco, Silvia Spinozzi, Aldo Roda, Arrigo F.G. Cicero
Affiliation:
关键词: 小檗碱、理化性质、代谢、生物利用度、安全性、hyperglicemia、血脂紊乱、心血管疾病。
摘要: 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.
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Cristiana Caliceti, Placido Franco, Silvia Spinozzi, Aldo Roda, Arrigo F.G. Cicero , Berberine: New Insights from Pharmacological Aspects to Clinical Evidences in the Management of Metabolic Disorders, Current Medicinal Chemistry 2016; 23 (14) . https://dx.doi.org/10.2174/0929867323666160411143314
DOI https://dx.doi.org/10.2174/0929867323666160411143314 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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