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黄连碱:药理学、毒理学和药代动力学研究综述。

Palmatine: A review of its pharmacology, toxicity and pharmacokinetics.

机构信息

School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, PR China.

School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, PR China.

出版信息

Biochimie. 2019 Jul;162:176-184. doi: 10.1016/j.biochi.2019.04.008. Epub 2019 Apr 30.

Abstract

Palmatine is a natural isoquinoline alkaloid and has been widely used in pharmaceutical field. The purpose of this review is to provide the latest and comprehensive information on the pharmacology, toxicity and pharmacokinetics of palmatine in the past, to explore the therapeutic potential of this compound and look for ways to reduce toxicity. Information on palmatine was collected from the internet database PubMed, Elsevier, ResearchGate, Web of Science, Wiley Online Library and Europe PMC using a combination of keywords including "pharmacology", "toxicology", "pharmacokinetics". All studies of this genus were included in this review until March 2019. Palmatine has a wide spectrum of pharmacological effects, including anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, anti-bacterial, anti-viral and regulating blood lipids. However, palmatine has obvious DNA toxicity, and has a complex effect on metabolic enzymes in the liver. Pharmacokinetic studies have demonstrated that glucuronidation and sulfation are the main metabolic pathways of palmatine. Palmatine can be used in many diseases. Future research directions include: how the concentration of palmatine affects pharmacological effects and toxicity; the mechanism of synergy between palmatine and other protoberberine alkaloid; Structural modification of palmatine is one of the key methods to enhance pharmacological activity and reduce activity.

摘要

黄连碱是一种天然异喹啉生物碱,已广泛应用于制药领域。本综述的目的是提供过去关于黄连碱的药理学、毒性和药代动力学的最新和全面的信息,探索该化合物的治疗潜力,并寻找降低毒性的方法。通过组合使用“药理学”、“毒理学”、“药代动力学”等关键词,从互联网数据库 PubMed、Elsevier、ResearchGate、Web of Science、Wiley Online Library 和 Europe PMC 中收集了有关黄连碱的信息。本综述纳入了该属的所有研究,截至 2019 年 3 月。黄连碱具有广泛的药理作用,包括抗癌、抗氧化、抗炎、神经保护、抗菌、抗病毒和调节血脂。然而,黄连碱具有明显的 DNA 毒性,对肝脏中的代谢酶有复杂的影响。药代动力学研究表明,葡萄糖醛酸化和硫酸化是黄连碱的主要代谢途径。黄连碱可用于多种疾病。未来的研究方向包括:黄连碱的浓度如何影响药理作用和毒性;黄连碱与其他原小檗碱类生物碱协同作用的机制;黄连碱的结构修饰是增强药理活性和降低活性的关键方法之一。

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