利用基于酿酒酵母 12 基因Δ0HSR-iERG6 的测定法发现的抗真菌化合物 Pestynol。
Pestynol, an Antifungal Compound Discovered Using a Saccharomyces cerevisiae 12geneΔ0HSR-iERG6-Based Assay.
机构信息
Graduate School of Infection Control Sciences , Kitasato University , 5-9-1 Shirokane , Minato-ku, Tokyo 108-8641 , Japan.
Kitasato Institute for Life Sciences , Kitasato University , 5-9-1 Shirokane , Minato-ku, Tokyo 108-8641 , Japan.
出版信息
J Nat Prod. 2018 Jul 27;81(7):1604-1609. doi: 10.1021/acs.jnatprod.8b00200. Epub 2018 Jul 5.
The multidrug-sensitive budding yeast, Saccharomyces cerevisiae 12geneΔ0HSR-iERG6, is very useful in antifungal screens. A novel compound, named pestynol (1), was discovered from a culture of the fungus Pestalotiopsis humus FKI-7473 using the multidrug-sensitive yeast. The structure of 1 was elucidated by NMR studies and modified Mosher's method as (1 R,2 R,3 R,4 R)-( E)-5-(7,11-dimethyl-3-methylenedodeca-6,10-dien-1-yn-1-yl)cyclohex-5-ene-1,2,3,4-tetraol. Compound 1 showed antimicrobial activity against the Gram-positive bacteria, Klebsiella pneumoniae, and S. cerevisiae 12geneΔ0HSR-iERG6 and Mucor racemosus, but displayed only weak cytotoxicity against various human cancer cell lines. Compound 1 displayed antifungal activities against S. cerevisiae 12geneΔ0HSR-iERG6 and Mucor racemosus at 10 μg/disc.
多药敏感出芽酵母，酿酒酵母 12 基因Δ0HSR-iERG6，在抗真菌筛选中非常有用。一种新型化合物，命名为 pestynol（1），是从真菌 Pestalotiopsis humus FKI-7473 的培养物中使用多药敏感酵母发现的。通过 NMR 研究和改进的 Mosher 方法确定了 1 的结构为（1R,2R,3R,4R）-（E）-5-（7,11-二甲基-3-亚甲基十二烷-6,10-二烯-1-炔-1-基）环己-5-烯-1,2,3,4-四醇。化合物 1 对革兰氏阳性菌肺炎克雷伯菌和酿酒酵母 12 基因Δ0HSR-iERG6 和毛霉表现出抗菌活性，但对各种人类癌细胞系仅显示出微弱的细胞毒性。化合物 1 在 10 μg/disc 时对酿酒酵母 12 基因Δ0HSR-iERG6 和毛霉表现出抗真菌活性。
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