Heterocornols from the Sponge-Derived Fungus <i>Pestalotiopsis heterocornis</i> with Anti-Inflammatory Activity
One strain-many compounds (OSMAC) manipulation of the sponge-derived fungus <i>Pestalotiopsis heterocornis</i> 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 isol...
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| Autores principales: | , , , , , , , |
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| Formato: | article |
| Lenguaje: | EN |
| Publicado: |
MDPI AG
2021
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| Materias: | |
| Acceso en línea: | https://doaj.org/article/3ddc666bd49f47f493e0351e629a0a39 |
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| Sumario: | One strain-many compounds (OSMAC) manipulation of the sponge-derived fungus <i>Pestalotiopsis heterocornis</i> 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 (<b>1</b>–<b>8</b>), one new ceramide (<b>9</b>), and three known analogues (<b>10</b>–<b>12</b>). The structures and absolute configurations of the new compounds were elucidated by spectroscopic data and calculated ECD analysis. Heterocornols Q (<b>1</b>) and R (<b>2</b>) 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 <b>12</b> showed moderate or weak antimicrobial activities against with MIC values ranging from 25 to 100 μg/mL. Heterocornols T and X (<b>7</b> and <b>8</b>) could inhibit the production of LPS-induced NO significantly, comparable to dexamethasone. Further Western blotting analysis showed <b>7</b> and <b>8</b> markedly suppressed the iNOS protein expression in LPS-induced RAW 264.7 cells in a dose-dependent manner. The result showed that <b>7</b> and <b>8</b> might serve as potential leads for development of anti-inflammatory activity. |
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