来自潮间带沉积物菌株 sp. 的安卡环素糖苷及其对肝癌细胞的细胞毒性活性。
Angucycline Glycosides from an Intertidal Sediments Strain sp. and Their Cytotoxic Activity against Hepatoma Carcinoma Cells.
机构信息
Department of Pharmacy, College of Marine Science, Shandong University, Weihai 264209, China.
State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China.
出版信息
Mar Drugs. 2018 Nov 27;16(12):470. doi: 10.3390/md16120470.
Four angucycline glycosides including three new compounds landomycin N (), galtamycin C () and vineomycin D (), and a known homologue saquayamycin B (), along with two alkaloids 1-acetyl-β-carboline () and indole-3-acetic acid (), were isolated from the fermentation broth of an intertidal sediments-derived sp. Their structures were established by IR, HR-ESI-MS, 1D and 2D NMR techniques. Among the isolated angucyclines, saquayamycin B () displayed potent cytotoxic activity against hepatoma carcinoma cells HepG-2, SMMC-7721 and plc-prf-5, with IC values 0.135, 0.033 and 0.244 μM respectively, superior to doxorubicin. Saquayamycin B () also induced apoptosis in SMMC-7721 cells as detected by its morphological characteristics in 4',6-diamidino-2-phenylindole (DAPI) staining experiment.
从潮间带沉积物来源的 sp. 的发酵液中分离得到四个angucycline 糖苷，包括三个新化合物 landomycin N ()、galtamycin C () 和 vineomycin D ()，以及一个已知的同源物 saquayamycin B ()，以及两个生物碱 1-acetyl-β-carboline () 和吲哚-3-乙酸 (). 通过 IR、HR-ESI-MS、1D 和 2D NMR 技术确定了它们的结构。在所分离的 angucyclines 中，saquayamycin B () 对肝癌细胞 HepG-2、SMMC-7721 和 plc-prf-5 表现出很强的细胞毒性活性，IC 值分别为 0.135、0.033 和 0.244 μM，优于阿霉素。Saquayamycin B () 还通过 4',6-二脒基-2-苯基吲哚 (DAPI) 染色实验检测到其在 SMMC-7721 细胞中的形态特征，诱导了细胞凋亡。
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