School of Chinese Materia Medica, Nanjing University of Chinese Medicine, 138 Xianlin Avenue, Nanjing 210023, PR China; Glycochemistry and Glycobiology Lab, Key Laboratory of Receptor Research, PR China.
State Key Laboratory of Virology, Wuhan Institute of Virology, Center for Biosafety Mega-Science, Chinese Academy of Sciences, Wuhan 430071, PR China.
Carbohydr Polym. 2022 Jan 1;275:118779. doi: 10.1016/j.carbpol.2021.118779. Epub 2021 Oct 16.
Previous researches suggested that polysaccharides from brown algae had anti-virus activity. We hypothesized that nature polysaccharide from marine plants might have the effect on anti-SARS-CoV-2 activity. By high throughput screening to target 3CLpro enzyme using polysaccharides library, we discover a crude polysaccharide 375 from seaweed Ecklonia kurome blocked 3CLpro enzymatic activity and shows good anti-SARS-CoV-2 infection activity in cell. Further, we show that homogeneous polysaccharide 37502 from the 375 may bind to 3CLpro well and disturb spike protein binding to ACE2 receptor. The structure characterization uncovers that 37502 is alginate. These results imply that the bioactivities of 375 on SARS-CoV-2 may target multiple key molecules implicated in the virus infection and replication. The above results suggest that 375 may be a potential drug candidate against SARS-CoV-2.
先前的研究表明,褐藻多糖具有抗病毒活性。我们假设海洋植物中的天然多糖可能对抗 SARS-CoV-2 活性有影响。通过使用多糖文库对 3CLpro 酶进行高通量筛选,我们发现海藻裙带菜中的一种粗多糖 375 可阻断 3CLpro 酶的活性,并在细胞中表现出良好的抗 SARS-CoV-2 感染活性。此外,我们表明 375 中的均一多糖 37502 可以与 3CLpro 结合良好,并干扰刺突蛋白与 ACE2 受体的结合。结构特征揭示 37502 是藻酸盐。这些结果表明,375 对 SARS-CoV-2 的生物活性可能针对病毒感染和复制过程中涉及的多个关键分子。上述结果表明,375 可能是一种针对 SARS-CoV-2 的潜在药物候选物。