新型吖啶酮类、菲莫松 A-C，具有生物活性，来源于内生真菌 Phomopsis sp. CGMCC No.5416。
New azaphilones, phomopsones A-C with biological activities from an endophytic fungus Phomopsis sp. CGMCC No.5416.
机构信息
School of Pharmacy, Shanghai University of Medine&Health Sciences, Pudong, Shanghai 201318, China; Microbial Pharmacology Laboratory, Shanghai University of Medine&Health Sciences, Pudong, Shanghai 201318, China.
School of Pharmacy, Shanghai University of Medine&Health Sciences, Pudong, Shanghai 201318, China.
出版信息
Fitoterapia. 2020 Sep;145:104573. doi: 10.1016/j.fitote.2020.104573. Epub 2020 Mar 25.
Three undescribed azaphilones, phomopsones A-C (1-3) and two known azaphilones (4-5) were isolated from the culture of endophytic fungus Phomopsis sp. CGMCC No.5416 from the stems of Achyranthes bidentata. Their structures were determined by spectroscopic analysis (HRESIMS, 1D and 2D NMR), and the absolute configurations were determined by CD spectroscopy. Compounds 2 and 3 showed significant inhibitory activities against HIV-1 with against HIV-1 with IC values of 7.6 and 0.5 μmol/L, respectively. Compounds 2 and 3 also displayed moderate cytotoxicity with CC values of 3.2-303 μmol/L against A549, MDA-MB-231 and PANC-1 cell lines. Moreover, compound 3 can induce the early apoptosis of PANC-1 cancer cells with the apoptosis rate of 28.54%.
从牛膝（Achyranthes bidentata）茎内分离得到的内生真菌 Phomopsis sp. CGMCC No.5416 的培养物中，分离得到三种未描述的氮杂菲酮类化合物（1-3）、两种已知氮杂菲酮类化合物（4-5）。通过光谱分析（HRESIMS、1D 和 2D NMR）确定了它们的结构，并通过 CD 光谱确定了它们的绝对构型。化合物 2 和 3 对 HIV-1 具有显著的抑制活性，其对 HIV-1 的 IC 值分别为 7.6 和 0.5 μmol/L。化合物 2 和 3 对 A549、MDA-MB-231 和 PANC-1 细胞系的细胞毒性也具有中等活性，CC 值分别为 3.2-303 μmol/L。此外，化合物 3 可以诱导 PANC-1 癌细胞的早期凋亡，凋亡率为 28.54%。
Zotero 插件