Petersen Lene M, Holm Dorte K, Knudsen Peter B, Nielsen Kristian F, Gotfredsen Charlotte H, Mortensen Uffe H, Larsen Thomas O
Chemodiversity Group, Department of Systems Biology, Technical University of Denmark, Kongens Lyngby, Denmark.
Eukaryotic Molecular Cell Biology Group, Department of Systems Biology, Technical University of Denmark, Kongens Lyngby, Denmark.
J Antibiot (Tokyo). 2015 Mar;68(3):201-5. doi: 10.1038/ja.2014.130. Epub 2014 Oct 8.
Four new yanuthone analogs (1-4) were isolated from the filamentous fungus Aspergillus niger. The structures of the new compounds were elucidated on the basis of UHPLC-DAD-HRMS data and one-dimensional and two-dimensional NMR spectroscopy. Labeling studies with (13)C8-6-methylsalicylic acid identified three class I yanuthones originating from the polyketide 6-methylsalicylic acid (yanuthone K, L and M (1-3)) and a class II yanuthone, which was named yanuthone X2 (4). The four new compounds were tested toward the pathogenic yeast Candida albicans and all displayed antifungal activity. Yanuthone X2 represents the first example of a bioactive class II yanuthone, demonstrating the pharmaceutical potential of this class.
从丝状真菌黑曲霉中分离出四种新的亚努酮类似物(1-4)。基于超高效液相色谱-二极管阵列-高分辨质谱数据以及一维和二维核磁共振光谱对新化合物的结构进行了阐明。用(13)C8-6-甲基水杨酸进行的标记研究确定了三种源自聚酮化合物6-甲基水杨酸的I类亚努酮(亚努酮K、L和M(1-3))以及一种II类亚努酮,其被命名为亚努酮X2(4)。对这四种新化合物针对致病性酵母白色念珠菌进行了测试,它们均表现出抗真菌活性。亚努酮X2是具有生物活性的II类亚努酮的首个实例,证明了此类化合物的药用潜力。