来自Humulus lupulus的化合物抑制了SARS-CoV-2类似帕帕因的蛋白酶和病毒复制
Anna-Maria Herzog1, Katharina Göbel1, Luigi Marongiu2
1Department of Cellular Microbiology, University of Hohenheim, 70599 Stuttgart, Germany.
概括
蜂化合物如桑托胡醇 (XN) 抑制了SARS-CoV-2的帕帕因类蛋白酶 (PLpro),这是一个关键的病毒标. 这些天然化合物还阻碍了病毒复制,显示了新的抗病毒药物开发的潜力.
科学领域:
- 病毒学 病毒学
- 自然产品化学 自然产品化学
- 药物发现 药物发现 药物发现
背景情况:
- 自然化合物具有抗病毒性质.
- 蜂 (Humulus lupulus) 含有具有抗病毒活性的代谢物.
- 来自蜂的桑托摩尔 (XN) 抑制了SARS-CoV-2的主要蛋白酶 (Mpro).
研究的目的:
- 研究XN及其衍生物 (异松醇,6-prenylnaringenin,8-prenylnaringenin) 对SARS-CoV-2类似帕帕因蛋白酶 (PLpro) 的作用.
- 评估这些蜂化合物对宿主细胞中SARS-CoV-2复制的抗病毒活性.
主要方法:
- 在式对接分析以预测与PLpro活性部位的结合亲和力.
- 试验室研究包括重组PLpro的表征,去ISGylation试验和动力学分析.
- 使用光标记的SARS-CoV-2在Caco-2宿主细胞中的抗病毒活性评估.
主要成果:
- 蜂化合物与SARS-CoV-2 PLpro活性部位结合,抑制其功能.
- 由蜂衍生化合物抑制PLpro,观察到IC50值在59-162μM之间.
- 桑托胡醇 (XN) 和6-prenylnaringenin (6-PN) 显著阻碍病毒复制,IC50值分别为3.3微米和7.3微米.
结论:
- 包括XN在内的hops衍生化合物抑制了SARS-CoV-2 Mpro和PLpro.
- SARS-CoV-2 PLpro 是抗病毒药物开发的一个有前途的治疗点.
- 这些发现支持开发针对人类冠状病毒的麻衍生新型抗病毒药物.
关键词:
在 COVID-19 疫情中,蜂化合物 蜂化合物 蜂化合物帕帕因类蛋白酶是一种类似帕帕因的蛋白酶.这就是SARS-CoV-2病毒.病毒蛋白酶是一种病毒蛋白酶.桑托摩尔 (Xanthohumol) 是一种类型的更多相关视频
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