1. New azaphilones, phomopsones A-C with biological activities from an endophytic fungus Phomopsis sp. CGMCC No.5416
- Author
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Yi-Fan Zhang, Meng Xiangguo, Wu Kai, Mei Ge, Lei Shao, Yi-Xin Xu, Zhi-Jun Yang, and Zhi-Teng Jiang
- Subjects
China ,Anti-HIV Agents ,Phomopsis ,Antineoplastic Agents ,Apoptosis ,01 natural sciences ,Plant use of endophytic fungi in defense ,Microbiology ,Cell Line, Tumor ,Drug Discovery ,Endophytes ,Humans ,Benzopyrans ,Cytotoxicity ,Achyranthes bidentata ,Achyranthes ,Pharmacology ,Biological Products ,biology ,Molecular Structure ,Plant Stems ,010405 organic chemistry ,Chemistry ,General Medicine ,Pigments, Biological ,biology.organism_classification ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Cell culture ,Phomopsis sp ,Cancer cell ,HIV-1 ,Two-dimensional nuclear magnetic resonance spectroscopy - Abstract
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 IC50 values of 7.6 and 0.5 μmol/L, respectively. Compounds 2 and 3 also displayed moderate cytotoxicity with CC50 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%.
- Published
- 2020