Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education, Key Laboratory of Analytical Chemistry for Life Science of Shaanxi Province, School of Chemistry and Chemical Engineering , Shaanxi Normal University , Xi'an 710062 , P. R. China.
ACS Appl Mater Interfaces. 2019 May 8;11(18):16320-16327. doi: 10.1021/acsami.9b02643. Epub 2019 Apr 24.
Bacterial infection is one of main causes that threaten global human health. Especially, antibiotic-resistant bacteria like methicillin-resistant Staphylococcus aureus (MRSA) lead to high mortality rate and more expensive treatment cost. Here, a novel amino-acid-modified conjugated oligomer OTE-d-Phe was synthesized by modifying the side chain of conjugated oligo(thiophene ethynylene) with d-phenylalanine. By mixing 9-fluorenylmethyloxycarbonyl-l-phenylalanin (Fmoc-l-Phe) with OTE-d-Phe, a new and biocompatible low-molecular weight hydrogel (HG-2) was prepared through self-assembly. In solution, HG-2 can effectively capture bacteria spontaneously, such as Escherichia coli and MRSA. Most importantly, the hydrogel has specific and strong antibacterial activity against MRSA over methicillin-susceptible S. aureus, Staphylococcus epidermidis, and E. coli. Interestingly, when the hydrogel was put on a model surface, a piece of cloth, it also is able to selectively kill MRSA with low cell cytotoxicity. The antibacterial mechanism was investigated, and it demonstrated that the HG-2 interacts with and physically breaks the cell wall and membrane, which leads to MRSA death. Therefore, this new conjugated oligomer-based hydrogel provides promising applications in disinfection and therapy of MRSA in hospital and in community.
细菌感染是威胁全球人类健康的主要原因之一。特别是像耐甲氧西林金黄色葡萄球菌(MRSA)这样的抗生素耐药菌,导致高死亡率和更高的治疗成本。在这里,通过修饰共轭寡聚噻吩乙炔的侧链,合成了一种新型的氨基酸修饰的共轭寡聚物 OTE-d-Phe。通过将 9-芴甲氧羰基-l-苯丙氨酸(Fmoc-l-Phe)与 OTE-d-Phe 混合,通过自组装制备了一种新的、生物相容性的低分子量水凝胶(HG-2)。在溶液中,HG-2 可以自发有效地捕获细菌,如大肠杆菌和 MRSA。最重要的是,水凝胶对 MRSA 具有特异性和强抗菌活性,而对甲氧西林敏感的金黄色葡萄球菌、表皮葡萄球菌和大肠杆菌则没有活性。有趣的是,当水凝胶放在模型表面,如一块布上时,它也能够选择性地杀死 MRSA,同时细胞毒性很低。研究了其抗菌机制,表明 HG-2 与细胞壁和细胞膜相互作用并物理破坏它们,导致 MRSA 死亡。因此,这种基于新型共轭寡聚物的水凝胶为医院和社区中 MRSA 的消毒和治疗提供了有前途的应用。