化学
抗真菌
肽
对偶(语法数字)
生物化学
微生物学
艺术
文学类
生物
作者
Hongwei Zhao,Simei Sun,Xiang Ding,Yiling Zhang,Boyan Li,Shuyu Wang,Guo Guo,Jin Zhang
标识
DOI:10.1021/acs.jmedchem.4c02917
摘要
Cryptococcus neoformans infections pose a significant global health threat. This study introduces mesoricin, a novel dual-domain antimicrobial peptide (AMP) scaffold derived from Mesorhizobium sp. identified using an in silico quantitative antifungal activity index (AFI). The peptide structure comprises an α-helix domain, which disrupts microbial membranes but exhibits highly hemolytic activity, and a β-sheet domain, which targets intracellular energy metabolism and resilient pathways. Rational design through α-helix domain removal and AFI-guided mutations yielded a mesoricin variant with enhanced antifungal activity and reduced cytotoxicity. The optimized mesoricin exhibited broad-spectrum antifungal activity against various Cryptococcus and Candida species (MIC 8-16 μg/mL) while maintaining high biosafety (IC50 > 128 μg/mL against human cell lines). Particularly, the variant demonstrated enhanced fungicidal effects at sub-MIC levels and superior biofilm control capabilities compared to the prototype peptide. These findings highlight mesoricins as a promising scaffold for AMP development targeting Cryptococcus infections.
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