Key Laboratory of Marine Drugs, The Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China , Qingdao 266003, People's Republic of China.
J Nat Prod. 2012 May 25;75(5):935-41. doi: 10.1021/np300103w. Epub 2012 Apr 30.
Chemical investigation of a marine-derived fungus Nigrospora sp., isolated from an unidentified sea anemone, yielded two new hydroanthraquinone analogues, 4a-epi-9α-methoxydihydrodeoxybostrycin (1) and 10-deoxybostrycin (2), together with seven known anthraquinone derivatives (3-9). The structures of the two new compounds were established through extensive NMR spectroscopy as well as a single-crystal X-ray diffraction analysis using Cu Kα radiation. The antibacterial activities of compounds 1-9 and 10 acetyl derivatives (6a, 7a, 8a-8g, 9a) were evaluated in vitro. Compound 6a, the acetylated derivative of 6, exhibited promising activity against Bacillus cereus with an MIC value of 48.8 nM, which was stronger than that of the positive control ciprofloxacin (MIC = 1250 nM). Analysis of the antibacterial screening data for the metabolites and their acetyl derivatives revealed the key structural features required for this activity.
从一种未鉴定的海葵中分离得到的海洋来源真菌 Nigrospora sp. 的化学成分研究得到了两个新的氢蒽醌类似物，4a-表-9α-甲氧基二氢去氧博斯他汀（1）和 10-去氧博斯他汀（2），以及 7 个已知的蒽醌衍生物（3-9）。通过广泛的 NMR 光谱以及使用 Cu Kα 辐射的单晶 X 射线衍射分析，确定了这两个新化合物的结构。对化合物 1-9 和 10 的乙酰化衍生物（6a、7a、8a-8g、9a）进行了体外抗菌活性评估。化合物 6a 是 6 的乙酰化衍生物，对蜡状芽孢杆菌具有良好的活性，MIC 值为 48.8 nM，比阳性对照环丙沙星（MIC = 1250 nM）更强。对代谢产物及其乙酰化衍生物的抗菌筛选数据的分析揭示了这种活性所必需的关键结构特征。
