Demsie Desalegn Getnet, Gebre Abadi Kahsu, Yimer Ebrahim M, Alema Niguse Meles, Araya Ephrem Mebrahtu, Bantie Abere Tilahun, Allene Mengesha Dessie, Gebremedhin Hagazi, Yehualaw Adane, Tafere Chernet, Tadese Haileslassie Tesfay, Amare Bekalu, Weldekidan Etsay, Gebrie Desye
Adigrat University, College of Medicine and Health Sciences, Department of Pharmacy, Adigrat, Ethiopia.
Mekelle University, College of Health Sciences, Department of Pharmacology and Toxicology, Mekelle, Ethiopia.
Biologics. 2020 Oct 13;14:107-114. doi: 10.2147/BTT.S262705. eCollection 2020.
Coronavirus disease 2019 (COVID-19), an infectious disease that primarily attacks the human pulmonary system, is caused by a viral strain called severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The outbreak emerged from Wuhan, China, and later spread throughout the world. Until the first week of May 2020, over 3.7 million cases had been reported worldwide and more than 258,000 had died due to the disease. So far, off label use of various drugs has been tried in many clinical settings, however, at present, there is no vaccine or antiviral treatment for human and animal coronaviruses. Therefore, repurposing of the available drugs may be promising to control emerging infections of SARS-COV2; however, new interventions are likely to require months to years to develop. Glycopeptides, which are active against gram-positive bacteria, have demonstrated significant activity against viral infections including SARS-COV and MERS-COV and have a high resemblance of sequence homology with SARS-COV2. Recent in vitro studies have also shown promising activities of aglycon derivative of glycopeptides and teicoplanin against SARS-COV2. Hydrophobic aglycon derivatives and teicoplanin, with minimal toxicity to human cell lines, inhibit entry and replication of SARS-COV2. These drugs block proteolysis of polyprotein a/b with replicase and transcription domains. Teicoplanin use was associated with complete viral clearance in a cohort of patients with severe COVID-19 symptoms. This review attempts to describe the activity, elucidate the possible mechanisms and potential clinical applications of existing glycopeptides against corona viruses, specifically SARS-COV2.
2019冠状病毒病(COVID-19)是一种主要侵袭人类肺部系统的传染病,由一种名为严重急性呼吸综合征冠状病毒2(SARS-CoV-2)的病毒株引起。该疫情起源于中国武汉,随后蔓延至全球。截至2020年5月的第一周,全球报告的病例已超过370万例,超过25.8万人死于该疾病。到目前为止,在许多临床环境中都尝试过各种药物的非标签使用,然而,目前尚无针对人类和动物冠状病毒的疫苗或抗病毒治疗方法。因此,重新利用现有药物可能有望控制SARS-CoV-2的新出现感染;然而,新的干预措施可能需要数月至数年才能研发出来。糖肽类药物对革兰氏阳性菌有活性,已证明对包括SARS-CoV和MERS-CoV在内的病毒感染具有显著活性,并且与SARS-CoV-2具有高度的序列同源性。最近的体外研究也显示了糖肽类药物的苷元衍生物和替考拉宁对SARS-CoV-2具有有前景的活性。疏水性苷元衍生物和替考拉宁对人类细胞系毒性最小,可抑制SARS-CoV-2的进入和复制。这些药物阻断具有复制酶和转录结构域的多聚蛋白a/b的蛋白水解。在一组患有严重COVID-19症状的患者中,使用替考拉宁与病毒完全清除有关。本综述试图描述现有糖肽类药物对冠状病毒,特别是SARS-CoV-2的活性,阐明其可能的机制和潜在的临床应用。