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水飞蓟宾的植物药理学视角:基于其有前景的免疫调节、抗凝和抗病毒特性,作为 COVID-19 的潜在预防或治疗剂。

Phyto-pharmacological perspective of Silymarin: A potential prophylactic or therapeutic agent for COVID-19, based on its promising immunomodulatory, anti-coagulant and anti-viral property.

机构信息

Department of Pharmaceutical Sciences, Drug Discovery Research Laboratory, Assam University, Silchar, India.

Department of Life Sciences, Presidency University, Kolkata, India.

出版信息

Phytother Res. 2021 Aug;35(8):4246-4257. doi: 10.1002/ptr.7084. Epub 2021 Apr 4.

Abstract

Coronavirus disease 2019 (COVID-19) triggered by a new viral pathogen, named severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), is now a global health emergency. This debilitating viral pandemic not only paralyzed the normal daily life of the global community but also spread rapidly via global travel. To date there are no effective vaccines or specific treatments against this highly contagious virus; therefore, there is an urgent need to advocate novel prophylactic or therapeutic interventions for COVID-19. This brief opinion critically discusses the potential of Silymarin, a flavonolignan with diverse pharmacological activity having antiinflammatory, antioxidant, antiplatelet, and antiviral properties, with versatile immune-cytokine regulatory functions, that able to bind with transmembrane protease serine 2 (TMPRSS2) and induce endogenous antiviral cytokine interferon-stimulated gene 15, for the management of COVID-19. Silymarin inhibits the expression of host cell surface receptor TMPRSS2 with a docking binding energy corresponding to -1,350.61 kcal/mol and a full fitness score of -8.11. The binding affinity of silymarin with an impressive virtual score exhibits significant potential to interfere with SARS-CoV-2 replication. We propose in-depth pre-clinical and clinical review studies of silymarin for the development of anti-COVID-19 lead, based on its clinical manifestations of COVID-19 and multifaceted bioactivities.

摘要

由新型病毒病原体引起的 2019 年冠状病毒病(COVID-19),被命名为严重急性呼吸系统综合症冠状病毒 2(SARS-CoV-2),现已成为全球卫生紧急事件。这种使人虚弱的病毒性大流行不仅使全球社区的正常日常生活瘫痪,而且还通过全球旅行迅速传播。迄今为止,针对这种高传染性病毒尚无有效的疫苗或特定疗法;因此,迫切需要提倡针对 COVID-19 的新型预防或治疗干预措施。本文简要讨论了水飞蓟素的潜力,水飞蓟素是一种具有多种药理活性的类黄酮木脂素,具有抗炎、抗氧化、抗血小板和抗病毒特性,具有多功能的免疫细胞因子调节功能,能够与跨膜丝氨酸蛋白酶 2(TMPRSS2)结合并诱导内源性抗病毒细胞因子干扰素刺激基因 15,从而治疗 COVID-19。水飞蓟素通过 -1,350.61 kcal/mol 的对接结合能和-8.11 的完全拟合评分抑制宿主细胞表面受体 TMPRSS2 的表达。水飞蓟素与令人印象深刻的虚拟评分的结合亲和力表明,其具有显著的潜力可干扰 SARS-CoV-2 的复制。我们建议根据 COVID-19 的临床表现和多方面的生物活性,对水飞蓟素进行深入的临床前和临床研究,以开发抗 COVID-19 的先导化合物。

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