Isobavachalcone Exhibits Potent Antifungal Efficacy by Inhibiting Enolase Activity and Glycolysis in Candida albicans,ACS Infectious Diseases

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Isobavachalcone Exhibits Potent Antifungal Efficacy by Inhibiting Enolase Activity and Glycolysis in Candida albicans
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2024-07-12 , DOI: 10.1021/acsinfecdis.4c00399
Hao Wu ₁ , Zhe Ji ₁ , Xin Huang ₂ , Liping Li ₁ , Sijin Hang ₁ , Jinhua Yu ₁ , Hui Lu ₁ , Yuanying Jiang ₁

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Invasive fungal diseases (IFDs) are becoming increasingly acknowledged as a significant concern linked to heightened rates of morbidity and mortality. Regrettably, the available antifungal therapies for managing IFDs are constrained. Emerging evidence indicates that enolase holds promise as a potential target protein for combating IFDs; however, there is currently a deficiency in antifungal medications specifically targeting enolase. This study establishes that isobavachalcone (IBC) exhibits noteworthy antifungal efficacy both in vitro and in vivo. Moreover, our study has demonstrated that IBC effectively targets Eno1 in Candida albicans (CaEno1), resulting in the suppression of the glycolytic pathway. Additionally, our research has indicated that IBC exhibits a higher affinity for CaEno1 compared to human Eno1 (hEno1), with the presence of isoprenoid in the side chain of IBC playing a crucial role in its ability to inhibit enolase activity. These findings contribute to the comprehension of antifungal approaches that target Eno1, identifying IBC as a potential inhibitor of Eno1 in human pathogenic fungi.

中文翻译：

异罂粟查尔酮通过抑制白色念珠菌的烯醇酶活性和糖酵解而表现出强大的抗真菌功效

越来越多的人认识到侵袭性真菌病（IFD）是与发病率和死亡率升高相关的重大问题。遗憾的是，用于治疗 IFD 的可用抗真菌疗法受到限制。新的证据表明烯醇化酶有望成为对抗 IFD 的潜在靶蛋白；然而，目前缺乏专门针对烯醇化酶的抗真菌药物。这项研究证实异巴伐查尔酮 (IBC) 在体外和体内均表现出显着的抗真菌功效。此外，我们的研究表明，IBC 有效靶向白色念珠菌(CaEno1) 中的 Eno1，从而抑制糖酵解途径。此外，我们的研究表明，与人 Eno1 (hEno1) 相比，IBC 对 CaEno1 表现出更高的亲和力，IBC 侧链中类异戊二烯的存在在其抑制烯醇酶活性的能力中发挥着至关重要的作用。这些发现有助于理解针对 Eno1 的抗真菌方法，将 IBC 确定为人类病原真菌中 Eno1 的潜在抑制剂。

更新日期：2024-07-12

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