Candida glabrata, the most common non-albicans Candida species and one of the primary causes of candidemia, exhibits decreased susceptibility to azoles and more recently to echinocandins. Polyalthic acid 1, a furan diterpene, has been shown promising biological potential and in this study ent-polyalthic acid derivatives with antifungal activity against Candida glabrata were produced by microbial transformation. Incubation of 1 with Aspergillus brasiliensis afforded two known (compounds 5 and 10) and eight new derivatives (compounds 2-4, 6-9 and 11). The most common reaction was hydroxylation, but isomerization of the double bond and acetylation were also detected. None of the tested compounds showed cytotoxicity against HeLa, MCF-7 and MCF-10A cell lines showing IC50 values ranging from 62.6 µM to > 500 µM. Compounds 1, 5, 6, 8 and 11 showed fungistatic effects (ranging from 34.1 µM to 39.5 µM) on C. glabrata at lower concentrations than fluconazole (163.2 µM). Compounds 1, 6 and 8 were more potent fungicides (ranging from 79.0 to 143.6 µM) than fluconazole, which showed fungicidal effect at concentrations higher than 163.2 µM. These results suggest that ent-polyalthic acid and some of its derivatives could be used as lead compounds to develop new antifungal agents.

中文翻译：

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通过对映聚丙氨酸的微生物转化制得的抗光滑念珠菌的新型抗真菌新戊二烷二萜。

光滑念珠菌（Candida glabrata）是最常见的非白色念珠菌，是念珠菌血症的主要原因之一，其对唑类药物和对棘球more素的敏感性降低。呋喃二萜聚丙氨酸1已被证明具有广阔的生物学潜力，在这项研究中，通过微生物转化生产了对光滑念珠菌具有抗真菌活性的对苯二甲酸聚丙氨酸衍生物。将1与巴西曲霉一起孵育可得到两种已知化合物（化合物5和10）和八种新衍生物（化合物2-4、6-9和11）。最常见的反应是羟基化，但也检测到双键的异构化和乙酰化。所测试的化合物均未显示出对HeLa，MCF-7和MCF-10A细胞系的细胞毒性，IC50值范围为62.6 µM至> 500 µM。化合物1、5、6 图8和图11显示了对毛毛梭菌的抑菌作用（范围从34.1 µM到39.5 µM），其浓度低于氟康唑（163.2 µM）。与氟康唑相比，化合物1、6和8是更有效的杀真菌剂（范围为79.0至143.6 µM），在浓度高于163.2 µM时显示出杀菌作用。这些结果表明，对苯二甲酸和其一些衍生物可以用作先导化合物来开发新的抗真菌剂。