Department of Biochemistry, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9038, USA.
J Nat Prod. 2012 Oct 26;75(10):1759-64. doi: 10.1021/np3004326. Epub 2012 Oct 11.
Four new anthraquinone analogues including galvaquinones A-C (1-3) and an isolation artifact, 5,8-dihydroxy-2,2,4-trimethyl-6-(3-methylbutyl)anthra[9,1-de][1,3]oxazin-7(2H)-one (4), were isolated from a marine-derived Streptomyces spinoverrucosus based on activity in an image-based assay to identify epigenetic modifying compounds. The structures of 1-4 were elucidated by comprehensive NMR and MS spectroscopic analysis. Galvaquinone B (2) was found to show epigenetic modulatory activity at 1.0 μM and exhibited moderate cytotoxicity against non-small-cell lung cancer (NSCLC) cell lines Calu-3 and H2887.
从海洋来源的链霉菌属中分离到四种新的蒽醌类似物,包括 galvaquinones A-C(1-3)和分离副产物 5,8-二羟基-2,2,4-三甲基-6-(3-甲基丁基)蒽[9,1-de][1,3]恶嗪-7(2H)-酮(4),这是基于用于鉴定表观遗传修饰化合物的基于图像的测定法的活性。通过全面的 NMR 和 MS 光谱分析阐明了 1-4 的结构。Galvaquinone B(2)在 1.0 μM 时表现出表观遗传调节活性,并对非小细胞肺癌(NSCLC)细胞系 Calu-3 和 H2887 表现出中等的细胞毒性。