Cytotoxic and Antibacterial Cyclodepsipeptides from an Endophytic Fungus <i>Fusarium avenaceum</i> W8

Abstract

Seven cyclic depsipeptides, including two new cyclic pentadepsipeptides avenamides A (1) and B (2), were isolated from a plant-derived fungus Fusarium avenaceum W8 by using the bioassay-guided fractionation method. The planar structures were elucidated by using comprehensive spectroscopic analyses, including 1D and 2D NMR, as well as MS/MS spectrometry. The absolute configuration of the amino acid and hydroxy acid residues was confirmed by using the advanced Marfey’s method and chiral HPLC analysis, respectively. Compounds 1–7 were evaluated for their cytotoxic activities against A549 and NCI-H1944 human lung adenocarcinoma cell lines and their antimicrobial activities against Staphylococcus aureus and Saccharomyces cerevisiae. As a result, compounds 1–4 showed moderate cytotoxicity, with IC50 values of 6.52~45.20 µM. Compounds 1 and 3 exhibited significant antimicrobial activities against S. aureus and S. cerevisiae, with an MIC80 of 11.1~30.0 µg/mL.

Keywords

• endophytic fungus
• <i>Fusarium avenaceum</i> W8
• cyclic depsipeptides
• antimicrobial activity
• cytotoxic activity