Anti-Inflammatory Azaphilones from the Edible Alga-Derived Fungus Penicillium sclerotiorum
Autor: | Jui-Sheng Chang, Ya-Chen Ko, Tzu-Yi Ke, Jue-Jun Lin, Yuan-Bin Cheng, Hui-Chun Wang |
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Jazyk: | angličtina |
Rok vydání: | 2021 |
Předmět: |
Aquatic Organisms
medicine.drug_class QH301-705.5 azaphilone Anti-Inflammatory Agents Pharmaceutical Science Antineoplastic Agents Fungus Article Anti-inflammatory Penicillium sclerotiorum Neuroblastoma Structure-Activity Relationship chemistry.chemical_compound Algae Functional Food Cell Line Tumor Drug Discovery Microalgae medicine Animals Benzopyrans Biology (General) Fibroblast Pharmacology Toxicology and Pharmaceutics (miscellaneous) anti-inflammatory Natural product biology Penicillium Pigments Biological Fibroblasts biology.organism_classification medicine.anatomical_structure chemistry Biochemistry Cell culture Toxicity Phosphorylation |
Zdroj: | Marine Drugs Volume 19 Issue 10 Marine Drugs, Vol 19, Iss 529, p 529 (2021) |
ISSN: | 1660-3397 |
DOI: | 10.3390/md19100529 |
Popis: | To discover the new medical entity from edible marine algae, our continuously natural product investigation focused on endophytes from marine macroalgae Grateloupia sp. Two new azaphilones, 8a-epi-hypocrellone A (1), 8a-epi-eupenicilazaphilone C (2), together with five known azaphilones, hypocrellone A (3), eupenicilazaphilone C (4), ((1E,3E)-3,5-dimethylhepta-1,3-dien-1-yl)-2,4-dihydroxy-3-methylbenzaldehyde (5), sclerotiorin (6), and isochromophilone IV (7) were isolated from the alga-derived fungus Penicillium sclerotiorum. The structures of isolated azaphilones (1–7) were elucidated by spectrometric identification, especially HRESIMS, CD, and NMR data analyses. Concerning bioactivity, cytotoxic, anti-inflammatory, and anti-fibrosis activities of those isolates were evaluated. As a result, compound 1 showed selective toxicity toward neuroblastoma cell line SH-SY5Y among seven cancer and one fibroblast cell lines. 20 μM of compounds 1, 3, and 7 inhibited the TNF-α-induced NFκB phosphorylation but did not change the NFκB activity. Compounds 2 and 6 respectively promoted and inhibited SMAD-mediated transcriptional activities stimulated by TGF-β. |
Databáze: | OpenAIRE |
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