Anti-Inflammatory Polyketide Derivatives from the Sponge-Derived Fungus Pestalotiopsis sp. SWMU-WZ04-2

Five undescribed polyketide derivatives, pestaloketides A–E (1–5), along with eleven known analogues (6–16), were isolated from the sponge-derived fungus Pestalotiopsis sp. Their structures, including absolute configurations, were elucidated by analyses of NMR spectroscopic HRESIMS data and electron...

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Published in:Marine drugs 2022-11, Vol.20 (11), p.711
Main Authors: Jiang, Peng, Luo, Jinfeng, Jiang, Yao, Zhang, Liping, Jiang, Liyuan, Teng, Baorui, Niu, Hong, Zhang, Dan, Lei, Hui
Format: Article
Language:English
Subjects:
anti-inflammatory activity
Anti-inflammatory agents
Biocompatibility
Biological activity
Cancer
Carbon
Cell lines
Circular dichroism
Cytotoxicity
Dichroism
Fungi
Inflammation
Lipopolysaccharides
Metabolites
Molecular docking
NMR
Nuclear magnetic resonance
Pestalotiopsis
Pestalotiopsis sp
polyketide
sponge-derived fungus
Toxicity
Tumor cell lines
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Summary:Five undescribed polyketide derivatives, pestaloketides A–E (1–5), along with eleven known analogues (6–16), were isolated from the sponge-derived fungus Pestalotiopsis sp. Their structures, including absolute configurations, were elucidated by analyses of NMR spectroscopic HRESIMS data and electronic circular dichroism (ECD) calculations. Compounds 5, 6, 9, and 14 exhibited weak cytotoxicities against four human cancer cell lines, with IC50 values ranging from 22.1 to 100 μM. Pestaloketide A (1) is an unusual polyketide, featuring a rare 5/10/5-fused ring system. Pestaloketides A (1) and B (2) exhibited moderately inhibited LPS-induced NO production activity, with IC50 values of 23.6 and 14.5 μM, respectively, without cytotoxicity observed. Preliminary bioactivity evaluations and molecular docking analysis indicated that pestaloketides A (1) and B (2) had the potential to be developed into anti-inflammatory activity drug leads.
ISSN:1660-3397
1660-3397
DOI:10.3390/md20110711