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Repurposing the mucolytic cough suppressant and TMPRSS2 protease inhibitor bromhexine for the prevention and management of SARS-CoV-2 infection.将黏液溶解型止咳药及跨膜丝氨酸蛋白酶2（TMPRSS2）蛋白酶抑制剂溴己新重新用于预防和治疗新型冠状病毒肺炎（SARS-CoV-2）感染。
Pharmacol Res. 2020 Jul;157:104837. doi: 10.1016/j.phrs.2020.104837. Epub 2020 Apr 22.
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Pharmacol Res. 2020 Jul;157:104853. doi: 10.1016/j.phrs.2020.104853. Epub 2020 Apr 30.
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Nafamostat Mesylate Blocks Activation of SARS-CoV-2: New Treatment Option for COVID-19.甲磺酸那法莫司他可阻断新型冠状病毒激活：新冠肺炎的新治疗选择。
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ACE-2 blockade and TMPRSS2 inhibition mitigate SARS-CoV-2 severity following cigarette smoke exposure in airway epithelial cells .在气道上皮细胞中，抑制血管紧张素转换酶2（ACE-2）和跨膜丝氨酸蛋白酶2（TMPRSS2）可减轻香烟烟雾暴露后新型冠状病毒肺炎（SARS-CoV-2）的严重程度。
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Early treatment with fluvoxamine, bromhexine, cyproheptadine, and niclosamide to prevent clinical deterioration in patients with symptomatic COVID-19: a randomized clinical trial.使用氟伏沙明、溴己新、赛庚啶和氯硝柳胺进行早期治疗以预防有症状的COVID-19患者临床病情恶化：一项随机临床试验。
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Drugs for COVID-19 Treatment: A New Challenge.新冠病毒治疗药物：新的挑战。
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Highlights on molecular targets in the management of COVID-19: Possible role of pharmacogenomics.新型冠状病毒肺炎治疗的分子靶点概述：药物基因组学的可能作用。
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Efficacy of Bromhexine versus Standard of Care in Reducing Viral Load in Patients with Mild-to-Moderate COVID-19 Disease Attended in Primary Care: A Randomized Open-Label Trial.氨溴索与标准治疗在降低基层医疗中轻症至中症新冠肺炎患者病毒载量方面的疗效：一项随机开放标签试验
J Clin Med. 2022 Dec 24;12(1):142. doi: 10.3390/jcm12010142.
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Drugs for the prevention and treatment of COVID-19 and its complications: An update on what we learned in the past 2 years.用于预防和治疗新型冠状病毒肺炎及其并发症的药物：过去两年我们所了解情况的最新进展
Front Pharmacol. 2022 Oct 10;13:987816. doi: 10.3389/fphar.2022.987816. eCollection 2022.
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COVID-19: Artificial sputum, respiratory obstruction method and screening of pyolitic and antihypoxic drugs.新型冠状病毒肺炎：人工痰液、呼吸道阻塞方法以及溶石和抗缺氧药物的筛选
Bioimpacts. 2022;12(4):393-394. doi: 10.34172/bi.2022.23877. Epub 2022 Jun 30.
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Discovery of diminazene as a dual inhibitor of SARS-CoV-2 human host proteases TMPRSS2 and furin using cell-based assays.利用基于细胞的检测方法发现地美硝唑是严重急性呼吸综合征冠状病毒2（SARS-CoV-2）人类宿主蛋白酶跨膜丝氨酸蛋白酶2（TMPRSS2）和弗林蛋白酶的双重抑制剂。
Curr Res Chem Biol. 2022;2:100023. doi: 10.1016/j.crchbi.2022.100023. Epub 2022 Mar 14.
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An insight into SARS-CoV-2 structure, pathogenesis, target hunting for drug development and vaccine initiatives.对严重急性呼吸综合征冠状病毒2（SARS-CoV-2）的结构、发病机制、药物研发靶点探寻及疫苗研发进展的深入了解
RSC Med Chem. 2022 Jan 25;13(6):647-675. doi: 10.1039/d2md00009a. eCollection 2022 Jun 22.
10
Peptidomimetic inhibitors of TMPRSS2 block SARS-CoV-2 infection in cell culture.肽模拟物抑制剂可阻断细胞培养中的 SARS-CoV-2 感染。
Commun Biol. 2022 Jul 8;5(1):681. doi: 10.1038/s42003-022-03613-4.

本文引用的文献

1
SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor.严重急性呼吸综合征冠状病毒 2 型（SARS-CoV-2）进入细胞依赖于 ACE2 和 TMPRSS2，可被一种临床验证的蛋白酶抑制剂所阻断。
Cell. 2020 Apr 16;181(2):271-280.e8. doi: 10.1016/j.cell.2020.02.052. Epub 2020 Mar 5.
2
TMPRSS2 Contributes to Virus Spread and Immunopathology in the Airways of Murine Models after Coronavirus Infection.TMPRSS2 促进冠状病毒感染后小鼠模型呼吸道中的病毒传播和免疫病理。
J Virol. 2019 Mar 5;93(6). doi: 10.1128/JVI.01815-18. Print 2019 Mar 15.
3
TMPRSS2: A potential target for treatment of influenza virus and coronavirus infections.TMPRSS2：抗流感病毒和冠状病毒感染治疗的潜在靶标。
Biochimie. 2017 Nov;142:1-10. doi: 10.1016/j.biochi.2017.07.016. Epub 2017 Aug 1.
4
The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis.雄激素调节的蛋白酶TMPRSS2激活了一个涉及肿瘤微环境成分的蛋白水解级联反应，并促进前列腺癌转移。
Cancer Discov. 2014 Nov;4(11):1310-25. doi: 10.1158/2159-8290.CD-13-1010. Epub 2014 Aug 13.
5
Simultaneous treatment of human bronchial epithelial cells with serine and cysteine protease inhibitors prevents severe acute respiratory syndrome coronavirus entry.丝氨酸和半胱氨酸蛋白酶抑制剂同时处理人支气管上皮细胞可预防严重急性呼吸综合征冠状病毒进入。
J Virol. 2012 Jun;86(12):6537-45. doi: 10.1128/JVI.00094-12. Epub 2012 Apr 11.
6
Proteolytic activation of influenza viruses by serine proteases TMPRSS2 and HAT from human airway epithelium.人呼吸道上皮细胞中的丝氨酸蛋白酶TMPRSS2和HAT对流感病毒的蛋白水解激活作用。
J Virol. 2006 Oct;80(19):9896-8. doi: 10.1128/JVI.01118-06.

Repurposing the mucolytic cough suppressant and TMPRSS2 protease inhibitor bromhexine for the prevention and management of SARS-CoV-2 infection.

作者信息

Maggio Roberto, Corsini Giovanni U

机构信息

Department of Biotechnological and Applied Clinical Sciences, University of L'Aquila, Italy.

Former Professor of Pharmacology, School of Medicine, University of Pisa, Italy.

出版信息

Pharmacol Res. 2020 Jul;157:104837. doi: 10.1016/j.phrs.2020.104837. Epub 2020 Apr 22.

DOI:10.1016/j.phrs.2020.104837
PMID:32334052
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7175911/
Abstract
摘要