Biomedical Engineering Institute, Jinan University, Guangzhou, 510632, PR China.
Department of Pharmacology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, 3568 CG, Utrecht, the Netherlands.
Carbohydr Polym. 2021 Jan 15;252:117138. doi: 10.1016/j.carbpol.2020.117138. Epub 2020 Sep 28.
Bacterial adhesion infection caused by medical materials in clinical application has become a serious threat, and it urgently needs new strategies to deal with these clinical challenges. In this work, LED209, a highly selective histidine sensor kinase inhibitor of Gram-negative bacteria, was covalently attached on cellulose membrane (CM) via click reaction. The data of contact angle measurements, ATR-FTIR and X-ray photoelectron spectroscopy confirmed the successful synthesis of LED-CM. In addition, the results of antibacterial activity of the membranes shown that LED-CM exhibited excellent anti-adhesion ability to Enterohemorrhagic Escherichia coli (EHEC), and significantly reduced the formation of bacterial biofilm. Importantly, LED-CM was able to repress the expression of virulence genes in EHEC. Furthermore, LED209-functionalized cellulose membrane indicated no cytotoxicity to mammalian cells. Hence, our present work demonstrated that CM modified with LED209 possessed markedly anti-adhesion activity against EHEC, which offered a potent antimicrobial material for combating bacterial infections.
临床应用中医用材料引起的细菌黏附感染已成为严重威胁，迫切需要新的策略来应对这些临床挑战。在这项工作中，通过点击反应将 LED209（一种高度选择性的革兰氏阴性菌组氨酸传感器激酶抑制剂）共价连接到纤维素膜（CM）上。接触角测量、ATR-FTIR 和 X 射线光电子能谱的数据证实了 LED-CM 的成功合成。此外，膜的抗菌活性结果表明，LED-CM 对肠出血性大肠杆菌（EHEC）表现出优异的抗黏附能力，并显著减少了细菌生物膜的形成。重要的是，LED-CM 能够抑制 EHEC 中毒力基因的表达。此外，LED209 功能化的纤维素膜对哺乳动物细胞没有细胞毒性。因此，我们的工作表明，用 LED209 修饰的 CM 对 EHEC 具有明显的抗黏附活性，为对抗细菌感染提供了一种有效的抗菌材料。
