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抗疟药物青蒿素及其衍生物治疗呼吸系统疾病。

Anti-malarial drug, artemisinin and its derivatives for the treatment of respiratory diseases.

机构信息

Department of Physiology, Yong Loo Lin School of Medicine, National University of Singapore, 117593, Singapore.

Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, 117600, Singapore.

出版信息

Pharmacol Res. 2020 Aug;158:104901. doi: 10.1016/j.phrs.2020.104901. Epub 2020 May 13.

Abstract

Artemisinins are sesquiterpene lactones with a peroxide moiety that are isolated from the herb Artemisia annua. It has been used for centuries for the treatment of fever and chills, and has been recently approved for the treatment of malaria due to its endoperoxidase properties. Progressively, research has found that artemisinins displayed multiple pharmacological actions against inflammation, viral infections, and cell and tumour proliferation, making it effective against diseases. Moreover, it has displayed a relatively safe toxicity profile. The use of artemisinins against different respiratory diseases has been investigated in lung cancer models and inflammatory-driven respiratory disorders. These studies revealed the ability of artemisinins in attenuating proliferation, inflammation, invasion, and metastasis, and in inducing apoptosis. Artemisinins can regulate the expression of pro-inflammatory cytokines, nuclear factor-kappa B (NF-κB), matrix metalloproteinases (MMPs), vascular endothelial growth factor (VEGF), promote cell cycle arrest, drive reactive oxygen species (ROS) production and induce Bak or Bax-dependent or independent apoptosis. In this review, we aim to provide a comprehensive update of the current knowledge of the effects of artemisinins in relation to respiratory diseases to identify gaps that need to be filled in the course of repurposing artemisinins for the treatment of respiratory diseases. In addition, we postulate whether artemisinins can also be repurposed for the treatment of COVID-19 given its anti-viral and anti-inflammatory properties.

摘要

青蒿素是一种倍半萜内酯化合物,具有过氧基团,从青蒿(Artemisia annua)中分离得到。几个世纪以来,青蒿素一直被用于治疗发热和寒战,最近由于其过氧化物酶特性被批准用于治疗疟疾。随着研究的深入,发现青蒿素对炎症、病毒感染、细胞和肿瘤增殖具有多种药理作用,对多种疾病具有疗效。此外,青蒿素的毒性谱相对安全。人们研究了青蒿素对不同呼吸道疾病的作用,包括肺癌模型和炎症驱动的呼吸障碍。这些研究揭示了青蒿素在减弱增殖、炎症、侵袭和转移以及诱导细胞凋亡方面的能力。青蒿素可以调节促炎细胞因子、核因子-κB(NF-κB)、基质金属蛋白酶(MMPs)、血管内皮生长因子(VEGF)的表达,促进细胞周期停滞,驱动活性氧(ROS)的产生,并诱导 Bak 或 Bax 依赖性或非依赖性凋亡。在这篇综述中,我们旨在提供有关青蒿素与呼吸疾病关系的最新知识的综合更新,以确定在重新利用青蒿素治疗呼吸疾病的过程中需要填补的空白。此外,鉴于其抗病毒和抗炎特性,我们还推测青蒿素是否也可以重新用于治疗 COVID-19。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a9c3/7217791/ca560a83b7aa/ga1_lrg.jpg

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