Flavonols inhibit sortases and sortase-mediated Staphylococcus aureus clumping to fibrinogen
Flavonols inhibit sortases and sortase-mediated Staphylococcus aureus clumping to fibrinogen
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DOI：
10.1248/bpb.29.1751
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发表时间：
2006-08-01
影响因子：
2
通讯作者：
Oh, Ki-Bong
中科院分区：
文献类型：
--
作者：
Kang, Sam Sik;Kim, Jae-Gyu;Oh, Ki-Bong
分选酶是负责将表面蛋白毒力因子锚定到肽聚糖细胞壁层的革兰氏阳性转肽酶家族。在金黄色葡萄球菌中，分选酶同种型的缺失导致毒力和感染潜力显著降低，使其成为重要的抗毒力靶标。我们研究了天然存在的黄酮醇对从S. aureus ATCC 6538 p，发现这些化合物抑制分选酶的活性，而不显示抗菌活性。在所测试的黄酮醇中，桑色素、杨梅苷和槲皮素表现出强的分选酶抑制活性（SrtA IC 50：37.39-52.70 μ M，SrtB IC 50：8.54-36.89 μ M）。纤维蛋白原细胞凝集活性数据突出了黄酮醇治疗S。金黄色葡萄球菌感染通过抑制分选酶。
Sortases are a family of Gram-positive transpeptidases responsible for anchoring surface protein virulence factors to the peptidoglycan cell wall layer. In Staphylococcus aureus, deletion of the sortase isoforms results in marked reduction in virulence and infection potential, making it an important antivirulence target. We examined the effects of naturally occurring flavonols on recombinant sortase A (SrtA) and B (SrtB) prepared from S. aureus ATCC6538p and found that these compounds inhibited the activity of sortases, without exhibiting antibacterial activities. Among the flavonols tested, morin, myricetin, and quercetin exhibited strong sortase inhibitory activities (SrtA IC50: 37.39-52.70 mu M, SrtB IC50: 8.54-36.89 mu M). The fibrinogen cell-clumping activity data highlight the potential of flavonols for the treatment of S. aureus infections via inhibition of sortase.