Mandala S M, Thornton R A, Frommer B R, Curotto J E, Rozdilsky W, Kurtz M B, Giacobbe R A, Bills G F, Cabello M A, Martín I
Merck Research Laboratories, Rahway, NJ 07065, USA.
J Antibiot (Tokyo). 1995 May;48(5):349-56. doi: 10.7164/antibiotics.48.349.
Potent antifungal activity was detected in fermentation extracts of Sporormiella australis and two related components were isolated from solid fermentations using silica gel and high speed countercurrent chromatography. The most active antifungal component, australifungin, contained a unique combination of alpha-diketone and beta-ketoaldehyde functional groups. Australifungin exhibited broad spectrum antifungal activity against human pathogenic fungi with MICs against Candida spp., Cryptococcus neoformans, and Aspergillus spp. between 0.015 and 1.0 microgram/ml. Mode of action studies revealed that australifungin interfered with fungal lipid metabolism by specifically inhibiting sphingolipid synthesis at the step converting sphinganine to ceramide.
在澳大利亚孢堆黑粉菌的发酵提取物中检测到了强大的抗真菌活性，并且使用硅胶和高速逆流色谱法从固体发酵物中分离出了两种相关成分。活性最强的抗真菌成分澳大利亚菌素含有α-二酮和β-酮醛官能团的独特组合。澳大利亚菌素对人类致病真菌表现出广谱抗真菌活性，对念珠菌属、新型隐球菌和曲霉菌属的最低抑菌浓度在0.015至1.0微克/毫升之间。作用方式研究表明，澳大利亚菌素通过在将鞘氨醇转化为神经酰胺的步骤中特异性抑制鞘脂合成来干扰真菌脂质代谢。
