Proangiogenic Azaphilones from the Marine-Derived Fungus <i>Neopestalotiopsis</i> sp. HN-1-6

Abstract

Developing novel, safe, and efficient proangiogenic drugs is an important approach for the prevention and treatment of cardiovascular diseases. In this study, 4 new compounds, including 3 azaphilones (1–3) and 1 dihydroisocoumarin (4), as well as 13 known compounds (5–17), were isolated from the sea-mud-derived fungus Neopestalotiopsis sp. HN-1-6 from the Beibu Gulf of China. The structures of the new compounds were determined by NMR, MS, ECD, and NMR calculations. Compounds 3, 5, and 7 exhibited noteworthy proangiogenic activities in a zebrafish model at a concentration of 40 μM, without displaying cytotoxicity toward five human cell lines. In addition, some compounds demonstrated antibacterial effects against Staphylococcus aureus, Escherichia coli, and Candida albicans, with MIC values ranging from 64 μg/mL to 256 μg/mL.

Keywords

• fungus
• <i>Neopestalotiopsis</i>
• secondary metabolites
• antibacterial activity
• proangiogenic activity