Lee Jong-Kook, Park Soyoung, Kim Young-Min, Guk Taeuk, Lee Min-Young, Park Seong-Cheol, Lee Jung Ro, Jang Mi-Kyeong
Department of Chemical Engineering, Sunchon National University, Suncheon 57922, Korea.
Department of Clinical Laboratory Science, Daejeon Health Institute of Technology, Daejeon 34504, Korea.
Pharmaceutics. 2022 Jul 31;14(8):1602. doi: 10.3390/pharmaceutics14081602.
The recent emergence of antibiotic-resistant fungi has accelerated research on novel antifungal agents. In particular, infections are related to biofilm formation on medical devices, such as catheters, stents, and contact lenses, resulting in high morbidity and mortality. In this study, we aimed to elucidate the antifungal and antibiofilm effects of a peptide against drug-resistant . α-Helical peptides in which the sequence of KWYK was repeated twice and four times, designated peptide series 1 (PS1)-1 and PS1-3, respectively, were generated, and the candidacidal activities of PS1-1, PS1-3, and fluconazole against drug-resistant cells were assessed. The PS1-3 peptide showed higher killing activity than PS1-1 or fluconazole and acted via a membranolytic mechanism. In addition, the PS1-3 peptide exhibited more potent activity than PS1-1 and fluconazole in terms of fungal biofilm inhibition and reduction at the minimum fungicidal concentration on the contact lens surface. Overall, these findings established PS1-3 as a potential candidacidal agent for applications on contact lenses.
近期出现的抗生素耐药真菌加速了新型抗真菌药物的研究。特别是，感染与医疗设备（如导管、支架和隐形眼镜）上生物膜的形成有关，导致高发病率和死亡率。在本研究中，我们旨在阐明一种肽对耐药菌的抗真菌和抗生物膜作用。分别生成了KWYK序列重复两次和四次的α-螺旋肽，分别命名为肽系列1（PS1）-1和PS1-3，并评估了PS1-1、PS1-3和氟康唑对耐药菌细胞的杀念珠菌活性。PS1-3肽显示出比PS1-1或氟康唑更高的杀伤活性，并且通过溶膜机制起作用。此外，在隐形眼镜表面的最低杀菌浓度下，PS1-3肽在抑制和减少真菌生物膜方面表现出比PS1-1和氟康唑更强的活性。总体而言，这些发现确立了PS1-3作为一种潜在的可应用于隐形眼镜的杀念珠菌剂。
