Faculty of Health Sciences, Department of Clinical Microbiology and Infectious Diseases, School of Pathology, University of the Witwatersrand, Johannesburg, South Africa.
Faculty of Health Sciences, Department of Oral Biological Sciences, School of Oral Health Sciences, University of the Witwatersrand, Johannesburg, South Africa.
PLoS One. 2023 Jun 21;18(6):e0285473. doi: 10.1371/journal.pone.0285473. eCollection 2023.
Candida auris, the youngest Candida species, is known to cause candidiasis and candidemia in humans and has been related to several hospital outbreaks. Moreover, Candida auris infections are largely resistant to the antifungal drugs currently in clinical use, necessitating the development of novel medications and approaches to treat such infections. Following up on our previous studies that demonstrated eugenol tosylate congeners (ETCs) to have antifungal activity, several ETCs (C1-C6) were synthesized to find a lead molecule with the requisite antifungal activity against C. auris. Preliminary tests, including broth microdilution and the MUSE cell viability assay, identified C5 as the most active derivative, with a MIC value of 0.98 g/mL against all strains tested. Cell count and viability assays further validated the fungicidal activity of C5. Apoptotic indicators, such as phosphatidylserine externalization, DNA fragmentation, mitochondrial depolarization, decreased cytochrome c and oxidase activity and cell death confirmed that C5 caused apoptosis in C. auris isolates. The low cytotoxicity of C5 further confirmed the safety of using this derivative in future studies. To support the conclusions drawn in this investigation, additional in vivo experiments demonstrating the antifungal activity of this lead compound in animal models will be needed.
耳念珠菌是最年轻的念珠菌种,已知可引起人类念珠菌病和念珠菌血症,并与几起医院感染暴发有关。此外,耳念珠菌感染对目前临床使用的抗真菌药物有很大的耐药性,因此需要开发新的药物和方法来治疗此类感染。继我们之前的研究表明丁香酚甲苯磺酸盐(ETCs)具有抗真菌活性之后,我们合成了几种 ETC(C1-C6),以寻找具有抗耳念珠菌所需抗真菌活性的先导分子。初步测试,包括肉汤微量稀释法和 MUSE 细胞活力测定法,确定 C5 是最活跃的衍生物,对所有测试菌株的 MIC 值为 0.98 g/mL。细胞计数和活力测定进一步验证了 C5 的杀菌活性。凋亡指标,如磷脂酰丝氨酸外翻、DNA 片段化、线粒体去极化、细胞色素 c 和氧化酶活性降低以及细胞死亡,证实 C5 导致耳念珠菌分离株凋亡。C5 的低细胞毒性进一步证实了在未来研究中使用该衍生物的安全性。为了支持本研究得出的结论,还需要进行额外的体内实验,以证明该先导化合物在动物模型中的抗真菌活性。