Journal
MARINE DRUGS
Volume 19, Issue 11, Pages -Publisher
MDPI
DOI: 10.3390/md19110585
Keywords
Pestalotiopsis heterocornis; heterocornols; anti-inflammatory activity; sponge-derived fungus
Categories
Funding
- Open Project of Sichuan Industrial Institute of Antibiotics, Chengdu University [ARRLKF20-04]
- Applied Basic Research Fund of Luzhou municipal government-Southwest Medical University [2018LZXNYD-ZK13]
- Project of Southwest Medical University [2017-ZRQN-093]
- Special Funds for Promoting Economic Development (Marine Economic Development) of Guangdong Province [[2020]039]
- Guangdong Local Innovation Team Program [2019BT02Y262]
- Guangdong Basic and Applied Basic Research Foundation [2019B151502042]
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Manipulation of one strain-many compounds (OSMAC) in the sponge-derived fungus Pestalotiopsis heterocornis XWS03F09 led to the production of new secondary metabolites with potential antimicrobial and anti-inflammatory activities.
One strain-many compounds (OSMAC) manipulation of the sponge-derived fungus Pestalotiopsis heterocornis XWS03F09 resulted in the production of new secondary metabolites. The chemical study of the fermentation, cultivated on 3% artificial sea salt in the rice media, led to the isolation of twelve compounds, including eight new polyketide derivatives, heterocornols Q-X (1-8), one new ceramide (9), and three known analogues (10-12). The structures and absolute configurations of the new compounds were elucidated by spectroscopic data and calculated ECD analysis. Heterocornols Q (1) and R (2) are novel 6/5/7/5 tetracyclic polyketide derivatives featuring dihydroisobenzofuran and benzo-fused dioxabicyclo [4.2.1] nonane system, which might be derived from the acetyl-CoA by epoxidation, polyene cyclization, and rearrangement to form the core skeleton. Compound 12 showed moderate or weak antimicrobial activities against with MIC values ranging from 25 to 100 mu g/mL. Heterocornols T and X (7 and 8) could inhibit the production of LPS-induced NO significantly, comparable to dexamethasone. Further Western blotting analysis showed 7 and 8 markedly suppressed the iNOS protein expression in LPS-induced RAW 264.7 cells in a dose-dependent manner. The result showed that 7 and 8 might serve as potential leads for development of anti-inflammatory activity.
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