<p>Two new hydrogenated azaphilones (<b>1</b> and <b>2</b>), together with the known azaphilone (<b>3</b>) were isolated from the red soil-derived acid-tolerant fungus <i>Penicillium purpureum</i> OUCMDZ-019 by OSMAC (one strain many compounds) strategy. Their structures were determined by nuclear magnetic resonance (NMR) spectroscopy analysis and electronic circular dichroism (ECD) calculations. Compound <b>1</b> was the first reported azaphilone that salified with pyridine and chlorination occurred at C-1, and it exhibited potential inhibitory activity on melanin production as tyrosinase inhibitor in vivo. Furthermore, (+)-mitorubrinol acetate (<b>3</b>) showed significantly inhibitory activity against H1N1 with IC<sub>50</sub> values of 58.6 μM (ribavirin, IC<sub>50</sub> 85.0 μM) as the first report.</p>

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Bioactive hydrogenated azaphilones from acid-tolerant fungus Penicillium purpureum OUCMDZ-019

  • Chengfeng Hou,
  • Yuqing Wang,
  • Xiangling Meng,
  • Ling Lu,
  • Peng Fu,
  • Weiming Zhu,
  • Yi Wang

摘要

Two new hydrogenated azaphilones (1 and 2), together with the known azaphilone (3) were isolated from the red soil-derived acid-tolerant fungus Penicillium purpureum OUCMDZ-019 by OSMAC (one strain many compounds) strategy. Their structures were determined by nuclear magnetic resonance (NMR) spectroscopy analysis and electronic circular dichroism (ECD) calculations. Compound 1 was the first reported azaphilone that salified with pyridine and chlorination occurred at C-1, and it exhibited potential inhibitory activity on melanin production as tyrosinase inhibitor in vivo. Furthermore, (+)-mitorubrinol acetate (3) showed significantly inhibitory activity against H1N1 with IC50 values of 58.6 μM (ribavirin, IC50 85.0 μM) as the first report.