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天然产物作为 PCSK9 调节剂的作用:综述。

The role of natural products as PCSK9 modulators: A review.

机构信息

Department of Toxicology & Pharmacology, Faculty of Pharmacy, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran.

GI Pharmacology Interest Group (GPIG), Universal Scientific Education and Research Network (USERN), Tehran, Iran.

出版信息

Phytother Res. 2024 Aug;38(8):4081-4098. doi: 10.1002/ptr.8260. Epub 2024 Jun 20.

Abstract

A variety of mechanisms and drugs have been shown to attenuate cardiovascular disease (CVD) onset and/or progression. Recent researchers have identified a potential role of proprotein convertase subtilisin/kexin type 9 (PCSK9) in modulating lipid metabolism and reducing plasma low density lipoprotein (LDL) levels. PCSK9 is the central protein in the metabolism of LDL cholesterol (LDL-C) owing to its major function in LDL receptor (LDLR) degradation. Due to the close correlation of cardiovascular disease with lipid levels, many in vivo and in vitro investigations are currently underway studying the physiological role of PCSK9. Furthermore, many studies are actively investigating the mechanisms of various compounds that influence lipid associated-disorders and their associated cardiovascular diseases. PCSK9 inhibitors have been shown to have significant impact in the prevention of emerging cardiovascular diseases. Natural products can effectively be used as PCSK9 inhibitors to control lipid levels through various mechanisms. In this review, we evaluate the role of phytochemicals and natural products in the regulation of PCSK9, and their ability to prevent cardiovascular diseases. Moreover, we describe their mechanisms of action, which have not to date been delineated.

摘要

多种机制和药物已被证明可减轻心血管疾病(CVD)的发生和/或进展。最近的研究人员已经确定了前蛋白转化酶枯草溶菌素/ kexin 9 型(PCSK9)在调节脂质代谢和降低血浆低密度脂蛋白(LDL)水平方面的潜在作用。由于其在 LDL 受体(LDLR)降解中的主要功能,PCSK9 是 LDL 胆固醇(LDL-C)代谢的核心蛋白。由于心血管疾病与血脂水平密切相关,目前正在进行许多体内和体外研究,以研究 PCSK9 的生理作用。此外,许多研究正在积极研究影响与脂质相关的疾病及其相关心血管疾病的各种化合物的机制。PCSK9 抑制剂已被证明在预防新出现的心血管疾病方面具有重要作用。天然产物可有效用作 PCSK9 抑制剂,通过多种机制控制脂质水平。在这篇综述中,我们评估了植物化学物质和天然产物在调节 PCSK9 中的作用,以及它们预防心血管疾病的能力。此外,我们描述了它们的作用机制,这些机制迄今尚未确定。

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