School of Pharmaceutical Sciences (Shenzhen), Sun Yat-sen University, Guangzhou 510275, China.
College of Agriculture, South China Agricultural University, Guangzhou 510642, China.
Mar Drugs. 2019 Jul 26;17(8):442. doi: 10.3390/md17080442.
is a type of commensal fungi which causes serious infections in immunocompromised patients and contributes to high mortality. In the present study, we identified that the extract from SCSIO T05 inhibited hypha and biofilm formation of . Seven compounds were isolated and evaluated for their effects on the biological functions and virulence of . Two leading compounds, compound (sorbicillin) and compound (3-methyl--(2'-phenethyl)-butyrylamide) were identified as exhibiting strong activity against morphological transition, adhesion activity, cytotoxicity, and adhesion to human cells, in a dose-dependent manner. Notably, compound 2 inhibited infection in mouse oral mucosal models. Transcriptomic analysis and real-time PCR results revealed that compound most likely inhibited the biological functions of cells by regulating the expression levels of , , , and , which are associated with filament formation and cell adhesion. Our results suggest that the candidate compounds present excellent efficacy against s pathogenicity and that they can be developed as potential options for the clinical treatment of candidiasis.
是一种共生真菌，可导致免疫功能低下患者发生严重感染，并导致高死亡率。在本研究中，我们发现 SCSIO T05 的提取物可抑制 的菌丝和生物膜形成。分离并评估了七种化合物对 的生物学功能和毒力的影响。两种主要化合物，化合物 （sorbicillin）和化合物 （3-甲基--（2'-苯乙基）-丁酰酰胺）被鉴定为具有很强的活性，可在剂量依赖性方式下抑制 形态转变、黏附活性、细胞毒性和与人细胞的黏附。值得注意的是，化合物 2 抑制了小鼠口腔黏膜模型中的 感染。转录组分析和实时 PCR 结果表明，化合物 2 通过调节与丝状形成和细胞黏附相关的 、 、 、 和 的表达水平，很可能抑制了 细胞的生物学功能。我们的研究结果表明，候选化合物对 具有优异的疗效，可作为治疗念珠菌病的潜在选择。
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