Department of Clinical Pharmacology and Medicine, College of Medicine, ALmustansiriyia University, Baghdad, Iraq.
Department of Clinical Laboratories Sciences, College of Applied Medical Sciences, Taif University, PO Box 11099, Taif, 21944, Saudi Arabia.
Mol Biol Rep. 2021 Dec;48(12):8195-8202. doi: 10.1007/s11033-021-06770-7. Epub 2021 Oct 18.
AIM/PURPOSE: Niclosamide (NCL) is an anthelminthic drug, which is widely used to treat various diseases due to its pleiotropic anti-inflammatory and antiviral activities. NCL modulates of uncoupling oxidative phosphorylation and different signaling pathways in human biological processes. The wide-spectrum antiviral effect of NCL makes it a possible candidate for recent pandemic SARS-CoV-2 infection and may reduce Covid-19 severity. Therefore, the aim of the present study was to review and clarify the potential role of NCL in Covid-19.
This study reviewed and highlighted the protective role of NCL therapy in Covid-19. A related literature search in PubMed, Scopus, Web of Science, Google Scholar, and Science Direct was done.
NCL has noteworthy anti-inflammatory and antiviral effects. The primary antiviral mechanism of NCL is through neutralization of endosomal PH and inhibition of viral protein maturation. NCL acts as a proton carrier, inhibits homeostasis of endosomal PH, which limiting of viral proliferation and release. The anti-inflammatory effects of NCL are mediated by suppression of inflammatory signaling pathways and release of pro-inflammatory cytokines. However, the major limitation in using NCL is low aqueous solubility, which reduces oral bioavailability and therapeutic serum concentration that reducing the in vivo effect of NCL against SARS-CoV-2.
NCL has anti-inflammatory and immune regulatory effects by modulating the release of pro-inflammatory cytokines, inhibition of NF-κB /NLRP3 inflammasome and mTOR signaling pathway. NCL has an anti-SARS-CoV-2 effect via interruption of viral life-cycle and/or induction of cytopathic effect. Prospective clinical studies and clinical trials are mandatory to confirm the potential role of NCL in patients with Covid-19 concerning the severity and clinical outcomes.
尼氯苯脒（NCL）是一种驱虫药，由于其具有广泛的抗炎和抗病毒活性，因此被广泛用于治疗各种疾病。NCL 可调节人体生物过程中的解偶联氧化磷酸化和不同信号通路。NCL 的广谱抗病毒作用使其成为最近 SARS-CoV-2 感染的潜在候选药物，并可能降低 COVID-19 的严重程度。因此，本研究旨在综述并阐明 NCL 在 COVID-19 中的潜在作用。
本研究综述并强调了 NCL 治疗在 COVID-19 中的保护作用。在 PubMed、Scopus、Web of Science、Google Scholar 和 Science Direct 上进行了相关文献检索。
NCL 具有显著的抗炎和抗病毒作用。NCL 的主要抗病毒机制是通过中和内体 PH 和抑制病毒蛋白成熟。NCL 作为质子载体，抑制内体 PH 的动态平衡，限制病毒的增殖和释放。NCL 的抗炎作用是通过抑制炎症信号通路和促炎细胞因子的释放来介导的。然而，使用 NCL 的主要限制是其低水溶性，这降低了口服生物利用度和治疗血清浓度，从而降低了 NCL 对 SARS-CoV-2 的体内作用。
NCL 通过调节促炎细胞因子的释放、抑制 NF-κB/NLRP3 炎性小体和 mTOR 信号通路，具有抗炎和免疫调节作用。NCL 通过中断病毒生命周期和/或诱导细胞病变效应发挥抗 SARS-CoV-2 作用。需要进行前瞻性临床研究和临床试验，以确认 NCL 在 COVID-19 患者中的潜在作用，特别是在疾病严重程度和临床结局方面。
