Heterocornols from the Sponge-Derived Fungus Pestalotiopsis heterocornis with Anti-Inflammatory Activity
| Autor: | Bin Yang, Dan Zhang, Xiaoxu Bi, Hui Lei, Xiuping Lin, Jianglian She, Hong Niu, Xiaowei Luo |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Ceramide
medicine.drug_class Stereochemistry QH301-705.5 sponge-derived fungus Pharmaceutical Science heterocornols Antimicrobial Polyene Anti-inflammatory Blot Polyketide chemistry.chemical_compound chemistry Drug Discovery medicine Fermentation Pestalotiopsis heterocornis Nonane Biology (General) anti-inflammatory activity Pharmacology Toxicology and Pharmaceutics (miscellaneous) |
| Zdroj: | Marine Drugs Volume 19 Issue 11 Marine Drugs, Vol 19, Iss 585, p 585 (2021) |
| ISSN: | 1660-3397 |
| DOI: | 10.3390/md19110585 |
| Popis: | 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 μg/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. |
| Databáze: | OpenAIRE |
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