Darwish Rula M, Salama Ali H
Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, the University of Jordan, Amman 11942, Jordan.
Department of Pharmacy, Faculty of Pharmacy, Middle East University, Amman 11831, Jordan.
Vet World. 2023 Jun;16(6):1284-1288. doi: 10.14202/vetworld.2023.1284-1288. Epub 2023 Jun 9.
Human infections caused by are common and range in severity from relatively treatable skin and mucosal conditions to systemic, fatal invasive candidiasis. The treatment of fungal infections is challenged by major obstacles, including the scarcity of effective therapeutic options, the toxicity of available medications, and the escalating antifungal resistance. Hence, there exists an urgent need to develop new classes of antimicrobial agents. This study was conducted to investigate the effect of KW-23 peptide against standard and resistant strains of alone and in combination with fluconazole.
A conjugated ultrashort antimicrobial peptide (KW-23) was designed and synthesized. KW-23 was challenged against standard and multidrug-resistant alone and in combination with fluconazole using standard antimicrobial and checkerboard assays. The toxicity of the peptide was examined using hemolytic assays.
KW-23 positively affected the standard and resistant Candidal strains (at 5 and 15 μg/mL respectively), exhibiting potent synergistic antimicrobial activity against the standard strain when combined with fluconazole. The effect of the combination was additive against the resistant strain (0.6 μg/mL). Furthermore, the peptide exhibited negligible toxicity on human erythrocytes.
KW-23 and its combination with fluconazole could be a promising candidate for developing anticandidal agents.
由[具体真菌名称未给出]引起的人类感染很常见，严重程度从相对易于治疗的皮肤和黏膜疾病到全身性、致命的侵袭性念珠菌病不等。真菌感染的治疗面临重大障碍，包括有效治疗选择稀缺、现有药物的毒性以及不断上升的抗真菌耐药性。因此，迫切需要开发新型抗菌药物。本研究旨在单独及与氟康唑联合考察KW - 23肽对[具体真菌名称未给出]标准菌株和耐药菌株的作用。
设计并合成了一种共轭超短抗菌肽（KW - 23）。使用标准抗菌和棋盘格试验，单独及与氟康唑联合对KW - 23进行针对标准菌株和多重耐药[具体真菌名称未给出]菌株的试验。使用溶血试验检测该肽的毒性。
KW - 23对标准和耐药念珠菌菌株有积极影响（分别在5和15μg/mL时），与氟康唑联合时对标准菌株表现出强效协同抗菌活性。该联合用药对耐药菌株（0.6μg/mL）的作用是相加的。此外，该肽对人红细胞的毒性可忽略不计。
KW - 23及其与氟康唑的联合用药可能是开发抗念珠菌药物的有前景的候选药物。
