Beijing Institute of Radiation Medicine, Beijing, China.
College of Life Sciences, Henan Normal University, Xinxiang, China.
J Med Virol. 2021 Oct;93(10):5825-5832. doi: 10.1002/jmv.27117. Epub 2021 Jun 9.
The coronavirus disease 2019 (COVID-19) pandemic has focused attention on the need to develop effective therapeutics against the causative pathogen, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and also against other pathogenic coronaviruses. In this study, we report on a kind of bisbenzylisoquinoline alkaloid, neferine, as a pan-coronavirus entry inhibitor. Neferine effectively protected HEK293/hACE2 and HuH7 cell lines from infection by different coronaviruses pseudovirus particles (SARS-CoV-2, SARS-CoV-2 [D614G, N501Y/D614G, 501Y.V1, 501Y.V2, 501Y.V3 variants], SARS-CoV, MERS-CoV) in vitro, with median effect concentration (EC ) of 0.13-0.41 μM. Neferine blocked host calcium channels, thus inhibiting Ca -dependent membrane fusion and suppressing virus entry. This study provides experimental data to support the fact that neferine may be a promising lead for pan-coronaviruses therapeutic drug development.
新型冠状病毒病（COVID-19）大流行引起了人们对开发针对致病病原体，即严重急性呼吸系统综合征冠状病毒 2（SARS-CoV-2），以及其他致病冠状病毒的有效疗法的关注。在这项研究中，我们报告了一种双苄基异喹啉生物碱，小檗碱，作为一种泛冠状病毒进入抑制剂。小檗碱可有效保护 HEK293/hACE2 和 HuH7 细胞系免受不同冠状病毒假病毒颗粒（SARS-CoV-2、SARS-CoV-2[D614G、N501Y/D614G、501Y.V1、501Y.V2、501Y.V3 变体]、SARS-CoV、MERS-CoV）的体外感染，其半数效应浓度（EC ）为 0.13-0.41 μM。小檗碱可阻断宿主钙通道，从而抑制 Ca 依赖性膜融合并抑制病毒进入。这项研究提供了实验数据，支持小檗碱可能是开发泛冠状病毒治疗药物的有前途的先导化合物的事实。
