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天然PCSK9抑制剂在心血管疾病中的研究进展

Progress of natural PCSK9 inhibitors in cardiovascular diseases

中文摘要英文摘要

心血管疾病(cardiovascular disease,CVD)仍然是世界范围内死亡的主要原因,迫切需要寻找新的防治策略。前蛋白转化酶枯草溶菌素9(proprotein convertase subtilisin Keratin Type 9,PCSK9)作为低密度脂蛋白胆固醇(low-density lipoprotein cholesterol,LDL-C)的重要调节剂,在CVD的进展中起着关键作用。2015年,针对PCSK9的单克隆抗体依洛尤单抗(Evolocumab)和阿利西尤单抗(Alirocumab)被批准用于临床,但它们成本效益低和给药不方便等缺点限制了临床应用,因此需要开发可口服和成本低的PCSK9小分子抑制剂。天然化合物来源丰富,结构多样,有很大的药物开发潜力,是发展PCSK9小分子抑制剂的重要来源。本综述我们结合了最新文献探讨了PCSK9在心血管疾病中的作用以及天然产物作为PCSK9抑制剂的研究进展。

ardiovascular disease (CVD) is still the leading cause of death worldwide, and new prevention and treatment strategies are urgently needed. Proprotein convertase subtilisin Keratin Type 9 (PCSK9), as a vital modulator of low-density lipoprotein cholesterol (LDL-C), plays a key role in the progression of CVD. In 2015, monoclonal antibodies Evolocumab and Alirocumab targeting PCSK9 were approved for clinical use, but their low cost-effectiveness and inconvenient administration have limited clinical use, thus there is a need for the development of orally available and low-cost small-molecule inhibitors of PCSK9. Natural compounds have rich sources and diverse structures, which have great drug development potential and are an important source for the development of small molecule inhibitors of PCSK9. In this review, we combined the latest literature to explore the role of PCSK9 in cardiovascular diseases and the research progress of natural products as PCSK9 inhibitors.

佟晓永、杨珍

医药卫生理论医学研究方法基础医学

心血管疾病PCSK9天然PCSK9抑制剂

ardiovascular diseasePCSK9Natural PCSK9 inhibitors

佟晓永,杨珍.天然PCSK9抑制剂在心血管疾病中的研究进展[EB/OL].(2023-03-28)[2025-08-05].http://www.paper.edu.cn/releasepaper/content/202303-306.点此复制

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