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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >A comprehensive review on beta-lapachone: Mechanisms, structural modifications, and therapeutic potentials
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A comprehensive review on beta-lapachone: Mechanisms, structural modifications, and therapeutic potentials

机译:关于β-乙酰酮的全面审查:机制,结构修改和治疗潜力

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摘要

beta-Lapachone (beta-lap, 1), an ortho-naphthoquinone natural product isolated from the lapacho tree (Tabebuia avellanedae) in many regions of South America, has received extensive attention due to various pharmacological activities, such as antitumor, anti-Trypanosoma cruzi, anti-Mycobacterium tuberculosis, antibacterial, and antimalarial activities. Related mechanisms of beta-lap have been widely investigated for a full understanding of its therapeutic potentials. Numerous derivatives of beta-lap have been reported with aims to generate new chemical entities, improve the corresponding biological potency, and overcome disadvantages of its physical and chemical properties and safety profiles. This review will give insight into the pharmacological mechanisms of beta-lap and provide a comprehensive understanding of its structural modifications with regard to different therapeutic potentials. The available clinical trials related to beta-lap and its derivatives are also summarized. (C) 2020 Elsevier Masson SAS. All rights reserved.
机译:beta-Lapachone(beta-lap,1)是从南美许多地区的拉帕乔树(Tabebuia avellanedae)中分离出来的一种邻萘醌天然产物,由于具有多种药理活性,例如抗肿瘤、抗克鲁兹锥虫、抗结核分枝杆菌、抗菌和抗疟疾活性,已受到广泛关注。β-lap的相关机制已被广泛研究,以充分了解其治疗潜力。β-lap的许多衍生物已被报道,其目的是生成新的化学实体,提高相应的生物效力,并克服其物理和化学性质及安全性方面的缺点。本综述将深入了解β-lap的药理机制,并全面了解其结构修饰对不同治疗潜力的影响。还总结了与β-lap及其衍生物相关的现有临床试验。(C) 2020年爱思唯尔马森SAS。版权所有。

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