Gao Lu, Wu Hao, Feng Jia, Liu Yu, Wang Ruina, Yan Lan, Lv Quanzhen, Jiang Yuanying
Department of Pharmacology, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai, China.
School of Pharmacy, Naval Medical University, Shanghai, China.
Antimicrob Agents Chemother. 2025 Mar 5;69(3):e0177524. doi: 10.1128/aac.01775-24. Epub 2025 Jan 24.
Invasive fungal infections have become an increasingly serious threat to global human health, underscoring the urgent need for the development of new antifungal drugs. In this study, we found a natural polyphenolic compound 1,2,3,4,6-O-pentagalloyl-glucose (PGG), which is present in various plants and herbs. PGG showed broad-spectrum antifungal activities, enhancing the efficacy of fluconazole. Furthermore, PGG could protect mice against gastrointestinal and systemic infection with . Our mechanistic studies revealed that PGG exerts its antifungal effects partially by binding to the CaEno1 protein to inhibit its activity. As a crucial therapeutic target, Eno1 has been reported to be closely associated with cancer, hypertension, and infectious diseases. Our findings indicated that PGG, a new Eno1 inhibitor, is a potential candidate for further antifungal development.
侵袭性真菌感染已对全球人类健康构成日益严重的威胁，凸显了开发新型抗真菌药物的迫切需求。在本研究中，我们发现了一种天然多酚化合物1,2,3,4,6 - O - 五没食子酰葡萄糖（PGG），它存在于各种植物和草药中。PGG表现出广谱抗真菌活性，增强了氟康唑的疗效。此外，PGG可保护小鼠免受胃肠道和全身性感染。我们的机制研究表明，PGG部分通过与CaEno1蛋白结合以抑制其活性来发挥抗真菌作用。作为一个关键的治疗靶点，烯醇化酶1（Eno1）已被报道与癌症、高血压和传染病密切相关。我们的研究结果表明，新型Eno1抑制剂PGG是进一步抗真菌开发的潜在候选药物。
