Department of Clinical Analysis, School of Pharmaceutical Sciences, São Paulo State University-UNESP, Araraquara, SP, Brazil.
Future Microbiol. 2023 Sep;18:939-947. doi: 10.2217/fmb-2022-0210. Epub 2023 Sep 13.
An IsCT analogue peptide (PepM3) was designed based on structural studies of wasp mastoparans and tested against . Its effects on fungal cell membranes and toxicity were evaluated. Antifungal activity was analyzed using a microdilution susceptibility test. Toxicity was assessed using human skin keratinocytes (HaCaT) and zebrafish embryos. PepM3 demonstrated activity against and a synergistic effect with amphotericin B. The peptide presented fungicidal action with damage to the fungal cell membrane, low toxicity in HaCat cells and was nonteratogenic in zebrafish embryos. Evaluating structural modifications is essential for the development of new agents with potential activity against fungal pathogens and for the reduction of toxic and teratogenic effects.
基于蜂毒神经肽的结构研究，设计了一种 IsCT 类似肽（PepM3），并对其进行了测试。评估了它对真菌细胞膜的作用及其毒性。采用微量稀释法敏感性试验分析抗真菌活性。用人皮肤角质形成细胞（HaCaT）和斑马鱼胚胎评估毒性。PepM3对 和两性霉素 B 具有协同作用。该肽对真菌细胞膜具有杀菌作用，对 HaCat 细胞的毒性低，对斑马鱼胚胎无致畸作用。评估结构修饰对于开发针对真菌病原体的具有潜在活性的新型药物以及减少毒性和致畸作用至关重要。
