EGCG氧化对抗SARS-CoV-2主要蛋白酶的抑制活性的影响
Yufeng He1, Meng Hao1, Mingchuan Yang1
1State Key Laboratory of Tea Plant Biology and Utilization, School of Tea & Food Science, Joint Research Center for Food Nutrition and Health of IHM, Anhui Agricultural University, Hefei 230036, China.
International journal of biological macromolecules
|June 29, 2024
概括
绿茶绿茶是一种绿茶.
科学领域:
- 生物化学 生物化学
- 药理学 药理学是指药理学的学科.
- 分子生物学分子生物学
背景情况:
- SARS-CoV-2 主蛋白酶 (Mpro) 是COVID-19抗病毒疗法的关键标.
- 绿茶中的 (-) - - epigallocatechin-3-gallate (EGCG) 显示Mpro抑制活性,但氧化作用尚不清楚.
- 由于EGCG具有氧化倾向,因此需要了解其对Mpro抑制的影响.
研究的目的:
- 研究EGCG氧化如何影响其Mpro抑制活性.
- 阐明EGCG的Mpro抑制背后的机制.
- 评估EGCG在治疗环境中作为选择性Mpro抑制剂的潜力.
主要方法:
- 在Mpro.的存在和缺席下研究了EGCG氧化.
- 确定EGCG-Mpro抑制的IC50值.
- 研究了氧化EGCG与Mpro活性部位的结合机制.
- 评估EGCG在细胞溶解物和活细胞中对Mpro的影响.
- 研究了酸在促进EGCG氧化和抑制方面的作用.
主要成果:
- 使用Mpro的长时间EGCG氧化显著增强了抑制活性 (IC50 = 0.26μM).
- 氧化EGCG (EGCG-) 优先结合Mpro的活性部位Cys145-SH,形成一种蛋白.
- 在细胞溶解物中,EGCG选择性地消耗Mpro thiols,并在活细胞中形成蛋白.
- 酸有助于EGCG氧化,但不会进一步促进协同抑制.
- 在Mpro化前EGCG的前氧化显著降低了抑制活性.
结论:
- EGCG,特别是当在Mpro的存在下被氧化时,是SARS-CoV-2 Mpro的强效和选择性饮食抑制剂.
- 形成EGCG-氨酸-Mpro附加物是主要的抑制机制.
- 优化EGCG氧化条件对于最大限度地发挥其对抗COVID-19的治疗潜力至关重要.
- EGCG的选择性作用表明,它有望在感染细胞中以最小的细胞毒性向Mpro.
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