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Isovitexin Is a Direct Inhibitor of Staphylococcus aureus Coagulase
( Hua Xiang ),( Panpan Yang ),( Li Wang ),( Jiaxin Li ),( Tiedong Wang ),( Junze Xue ),( Dacheng Wang ),( Hongxia Ma ) 한국미생물 · 생명공학회 2021 Journal of microbiology and biotechnology Vol.31 No.10
Staphylococcus aureus (S. aureus) is a major pathogen that causes human pneumonia, leading to significant morbidity and mortality. S. aureus coagulase (Coa) triggers the polymerization of fibrin by activating host prothrombin, which then converts fibrinogen to fibrin and contributes to S. aureus pathogenesis and persistent infection. In our research, we demonstrate that isovitexin, an active traditional Chinese medicine component, can inhibit the coagulase activity of Coa but does not interfere with the growth of S. aureus. Furthermore, we show through thermal shift and fluorescence quenching assays that isovitexin directly binds to Coa. Dynamic simulation and structure-activity relationship analyses suggest that V191 and P268 are key amino acid residues responsible for the binding of isovitexin to Coa. Taken together, these data indicate that isovitexin is a direct Coa inhibitor and a promising candidate for drug development against S. aureus infection.