Abstract
Previously unreported anthraquinone, acetylpenipurdin A (4), biphenyl ether, neospinosic acid (6), dibenzodioxepinone, and spinolactone (7) were isolated, together with (R)-6-hydroxymellein (1), penipurdin A (2), acetylquestinol (3), tenellic acid C (5), and vermixocin A (8) from the culture of a marine sponge-associated fungus Neosartorya spinosa KUFA1047. The structures of the previously unreported compounds were established based on an extensive analysis of 1D and 2D NMR spectra as well as HRMS data. The absolute configurations of the stereogenic centers of 5 and 7 were established unambiguously by comparing their calculated and experimental electronic circular dichroism (ECD) spectra. Compounds 2 and 5–8 were tested for their in vitro acetylcholinesterase and tyrosinase inhibitory activities as well as their antibacterial activity against Gram-positive and Gram-negative reference, and multidrug-resistant strains isolated from the environment. The tested compounds were also evaluated for their capacity to inhibit biofilm formation in the reference strains.
Highlights
Fungi are among organisms that have a remarkable capacity to produce different classes of structurally diverse secondary metabolites with relevant biological and pharmacological activities
The 1 H and 13 C signals as well as correlations observed in the COSY, HSQC, and HMBC spectra of a minor component (Table S3, Figures S13–S17) revealed its identity as acetylquestinol, previously reported from the culture of Eurotium chevalieri KUFA0006 [12]
>64 inhibit biofilm formation in three of the four reference strains used in this study (Table 5):
Summary
Fungi are among organisms that have a remarkable capacity to produce different classes of structurally diverse secondary metabolites with relevant biological and pharmacological activities. Marine-derived fungi have become one of the most important sources of bioactive compounds because they are among the world’s most important resources for unprecedented chemodiversity and because they can produce quantity of compounds with potential for drug development, clinical trials, and even marketing [4]. Marine-derived fungi have become one of the most important sources of bioactive com ofun pounds because they are among the world’s most important resources for precedented chemodiversity and because they can produce quantity of compounds with potential for drug development, clinical trials, and even marketing [4]. The tested compounds were evaluated for their potential synergy with clinically relevant antibiotics on the multidrugresistant isolates, by a disk diffusion method and by the checkerboard assay, as well as their capacity to prevent biofilm formation in all four reference strains, by measuring a total biomass using the crystal violet assay
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