Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807378, Taiwan.
Department of Marine Biotechnology and Resources, National Sun Yat-sen University, Kaohsiung 804351, Taiwan.
Mar Drugs. 2021 Sep 22;19(10):529. doi: 10.3390/md19100529.
To discover the new medical entity from edible marine algae, our continuously natural product investigation focused on endophytes from marine macroalgae sp. Two new azaphilones, 8a--hypocrellone A (), 8a--eupenicilazaphilone C (), together with five known azaphilones, hypocrellone A (), eupenicilazaphilone C (), ((1,3)-3,5-dimethylhepta-1,3-dien-1-yl)-2,4-dihydroxy-3-methylbenzaldehyde (), sclerotiorin (), and isochromophilone IV () were isolated from the alga-derived fungus . The structures of isolated azaphilones (-) were elucidated by spectrometric identification, especially HRESIMS, CD, and NMR data analyses. Concerning bioactivity, cytotoxic, anti-inflammatory, and anti-fibrosis activities of those isolates were evaluated. As a result, compound showed selective toxicity toward neuroblastoma cell line SH-SY5Y among seven cancer and one fibroblast cell lines. 20 μM of compounds , , and inhibited the TNF-α-induced NFκB phosphorylation but did not change the NFκB activity. Compounds and respectively promoted and inhibited SMAD-mediated transcriptional activities stimulated by TGF-β.
为了从食用海洋藻类中发现新的药用实体，我们持续对海洋大型藻类内生真菌进行天然产物研究。从该海藻来源的真菌中分离得到两个新的氮杂菲酮类化合物 8a--hypocrellone A () 和 8a--eupenicilazaphilone C ()，以及五个已知的氮杂菲酮类化合物 hypocrellone A ()、eupenicilazaphilone C ()、((1,3)-3,5-dimethylhepta-1,3-dien-1-yl)-2,4-dihydroxy-3-methylbenzaldehyde ()、sclerotiorin () 和 isochromophilone IV ()。通过光谱鉴定，特别是高分辨质谱（HRESIMS）、圆二色谱（CD）和 NMR 数据分析，阐明了分离得到的氮杂菲酮类化合物的结构。关于生物活性，评估了这些化合物的细胞毒性、抗炎和抗纤维化活性。结果表明，化合物 对 7 种癌细胞系和 1 种成纤维细胞系中的神经母细胞瘤细胞系 SH-SY5Y 具有选择性毒性。20 μM 的化合物 、 、 抑制 TNF-α 诱导的 NFκB 磷酸化，但不改变 NFκB 活性。化合物 和 分别促进和抑制 TGF-β 刺激的 SMAD 介导的转录活性。
