Antiproliferative trichothecene derivatives from an endophytic fungus fusarium equiseti Z8

Abstract

Feature-based molecular networking analysis combined with bioassay-guided method was applied to afford two previously undescribed trichothecenes derivatives (1–2), together with eleven trichothecenes derivatives (3−13) and three β-resorcylic macrolides (14–16) from an endophytic fungus Fusarium equiseti Z8. The new structures were elucidated by using comprehensive spectroscopic analyses of NMR, HR-ESI-MS, and ECD calculations. MSⁿ fragmentation of trichothecenes was also elucidated. All isolated compounds were evaluated the antiproliferative effects against A549, NCI-H1944, and NCI-H1650 human lung adenocarcinoma cell lines, as well as the antibacterial activity against Staphylococcus aureus. Most of the trichothecenes possessed significant antiproliferative activities, especially compounds 6 and 11 exhibited the most potent antiproliferative activities against the three tumor cells, with the IC₅₀ values of 1.6–3.8 nM. Compounds 1–2 are relatively nontoxic to BEAS-2B human lung normal epithelial cells. Additionally, compound 14 displayed significant inhibition against S. aureus (MIC₈₀: 4.17 μg/mL).