Abstract
A new depsidone derivative (1), aspergillusidone G, was isolated from a marine fungus Aspergillus unguis, together with eight known depsidones (2‒9) and a cyclic peptide (10): agonodepside A (2), nornidulin (3), nidulin (4), aspergillusidone F (5), unguinol (6), aspergillusidone C (7), 2-chlorounguinol (8), aspergillusidone A (9), and unguisin A (10). Compounds 1‒4 and 7‒9 were obtained from the plasma induced mutant of this fungus, while 5, 6, and 10 were isolated from the original strain under chemical induction. Their structures were identified using spectroscopic analysis, as well as by comparison with literature data. The HPLC fingerprint analysis indicates that chemical induction and plasma mutagenesis effectively influenced the secondary metabolism, which may be due to their regulation in the key steps in depsidone biosynthesis. In bioassays, compound 9 inhibited acetylcholinesterase (AChE) with IC50 in 56.75 μM. Compounds 1, 5, 7, 8, and 9 showed moderate to strong activity towards different microbes. Compounds 3, 4, and 5 exhibited potent larvicidality against brine shrimp. In docking studies, higher negative CDOCKER interaction energy and richer strong interactions between AChE and 9 explained the greater activity of 9 compared to 1. Chemical induction and plasma mutagenesis can be used as tools to expand the chemodiversity of fungi and obtain useful natural products.
Highlights
Metabolites from marine fungi are substantial source for drug discovery
Secondary metabolic genes and increase chemodiversity, which has been demonstrated by the Plasma refers to an ionized gas-like physical state consisting of highly electrified nuclei and free application of epigenetic remodeling methods with DNA methyltransferase and histone deacetylase electrons.inhibitors
In the present work, 10 natural compounds—including a new despidone (1) together with eight known despidones (2–9), and a cyclic peptide (10)—were obtained from a marine fungus
Summary
Metabolites from marine fungi are substantial source for drug discovery. The unique structures produced by marine fungi are highly valued in the development of clinical drugs, such as antitumor, anti-HIV, antifungal, antibacterial, anti-acetylcholinesterase, and antioxidant drugs [1,2,3,4]. PEER REVIEW metabolic genes increase chemodiversity, which has been demonstrated by the application of epigenetic remodeling methods with DNA methyltransferase and histone deacetylase inhibitors [10,11]. Secondary metabolic genes and increase chemodiversity, which has been demonstrated by the Plasma refers to an ionized gas-like physical state consisting of highly electrified nuclei and free application of epigenetic remodeling methods with DNA methyltransferase and histone deacetylase electrons.inhibitors. It is a highly excited, unstable state,gas-like whichphysical contains a variety ofofphysical and chemical [10,11]. Plasma refers to an ionized state consisting highly electrified mutagenic factors [12]
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