Abstract
The application of an OSMAC (One Strain-Many Compounds) approach on the sponge-derived fungus Aspergillus sp. LS34, using two different media including solid rice medium and potato dextrose broth (PDB) resulted in the isolation and identification of two new compounds, named asperspin A (1) and asperther A (2) along with seven known compounds 3–9. Compounds 1–5 were detected in fungal extracts from rice medium, while compounds 6–9 were isolated from PDB medium. Their structures were unambiguously characterized by HRESIMS and NMR spectroscopic data. The growth inhibitory activity of these compounds against four pathogenic bacteria (Vibrio parahaemolyticus, Vibrio harveyi, Escherichia coli, and Staphylococcus aureus) were evaluated. All the compounds were also tested for their cytotoxicity against seven cancer cell lines, including CCRF-CEM, K562, BGC823, AGS, HCT-116, MDA-MB-453, and COR-L23. Among them, compound 9 showed strong activity against CCRF-CEM and K562 cells with IC50 values of 1.22 ± 0.05 µM and 10.58 ± 0.19 µM, respectively. Notably, compound 7 also showed pronounced activity against S. aureus with an MIC value of 3.54 µM.
Highlights
Marine microorganisms, in particular marine-derived fungi, have proven to be a promising producer of biologically active secondary metabolites for new chemicals in drug discovery [1,2,3,4,5]
Whole genome sequencing of fungi has showed the existence of silent pathways, which are not expressed under standard culture conditions [6]
Changing culture conditions can activate potentially silent gene clusters thereby increasing the variety of secondary metabolites [7]
Summary
In particular marine-derived fungi, have proven to be a promising producer of biologically active secondary metabolites for new chemicals in drug discovery [1,2,3,4,5]. Whole genome sequencing of fungi has showed the existence of silent pathways, which are not expressed under standard culture conditions [6]. Changing culture conditions can activate potentially silent gene clusters thereby increasing the variety of secondary metabolites [7]. The OSMAC (One. Strain−Many Compounds) approach has been shown to be a powerful strategy for triggering silent gene clusters by changing different parameters [8]. One successful application was the isolation of novel pimarane diterpenoids from Arctic soil-derived fungus Eutypella sp.
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