Abstract
Ten polyketide derivatives (1–10), including a new natural product named (E)-2,4-dihydroxy-3-methyl-6-(2-oxopent-3-en-1-yl) benzaldehyde (1), and five known diketopiperazines (11–15), were isolated from the mangrove-sediment-derived fungus Aspergillus sp. SCSIO41407. The structures of 1–15 were determined via NMR and MS spectroscopic analysis. In a variety of bioactivity screening, 3 showed weak cytotoxicity against the A549 cell line, and 2 exhibited weak antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). Compounds 3, 5, and 6 showed inhibition against acetylcholinesterase (AChE) with IC50 values of 23.9, 39.9, and 18.6 μM. Compounds 11, 12, and 14 exhibited obvious inhibitory activities of lipopolysaccharide (LPS)-induced nuclear factor-κB (NF-κB) with IC50 values of 19.2, 20.9, and 8.7 μM, and they also suppressed RANKL-induced osteoclast differentiation in bone marrow macrophages cells (BMMCs), with the concentration of 5 μM. In silico molecular docking with AChE and NF-κB p65 protein were also performed to understand the inhibitory activities, and 1, 11–14 showed obvious protein/ligand-binding effects to the NF-κB p65 protein.
Highlights
Mangrove is a unique ecosystem with high salinity, low pH value, and periodic tidal immersion, which is mainly distributed between the tropical and subtropical intertidal regions around the world and located at the junction of terrestrial and marine ecosystems.The variety and complexity of the mangrove soil environment leads to the diversity of soil microorganisms [1,2]
The fungus Aspergillus is the main part of the mangrove-sediment-derived fungi, which can produce bioactive compounds such as alkaloids [4], terpenoids [5], sterides [6], and polyketides [7]
Compound 1 was isolated as tan crystalline solid, and its molecular formula was Compound 1 was isolated as tan crystalline solid, and its molecular formula was esestablished as C13 H14 O4 according to the HRESIMS ion peak at m/z 235.0966 [M ++ H]+
Summary
Mangrove is a unique ecosystem with high salinity, low pH value, and periodic tidal immersion, which is mainly distributed between the tropical and subtropical intertidal regions around the world and located at the junction of terrestrial and marine ecosystems. The fungus Aspergillus is the main part of the mangrove-sediment-derived fungi, which can produce bioactive compounds such as alkaloids [4], terpenoids [5], sterides [6], and polyketides [7]. These compounds have a variety of activities, including antibacterial [7], enzyme inhibitory [8], Molecules 2021, 26, 4851 of 10 the main part of the mangrove-sediment-derived fungi, which can produce bioactive2compounds such as alkaloids [4], terpenoids [5], sterides [6], and polyketides [7] These compounds have a variety of activities, including antibacterial [7], enzyme inhibitory [8], antiinflammatory [9], antioxidant [10], antivirus [11], and activities [12].
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