Epipolythiodiketopiperazines from the Marine Derived Fungus Dichotomomyces cejpii with NF-κB Inhibitory Potential
| العنوان: | Epipolythiodiketopiperazines from the Marine Derived Fungus Dichotomomyces cejpii with NF-κB Inhibitory Potential |
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| المؤلفون: | Gabriele M. König, Seungwon Ji, Henrik Harms, Damun Nesaei-Mosaferan, Barbora Orlikova, Marc Diederich |
| المصدر: | Marine Drugs Marine Drugs, Vol 13, Iss 8, Pp 4949-4966 (2015) Volume 13 Issue 8 Pages 4949-4966 |
| بيانات النشر: | MDPI AG, 2015. |
| سنة النشر: | 2015 |
| مصطلحات موضوعية: | Aquatic Organisms, gliotoxin, Pharmaceutical Science, Jurkat cells, Article, NF-κB, Piperazines, Microbiology, Jurkat Cells, Polyketide, chemistry.chemical_compound, Ascomycota, Cell Line, Tumor, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Drug Discovery, Dichotomomyces, Animals, Humans, Ascomycete, lcsh:QH301-705.5, Pharmacology, Toxicology and Pharmaceutics (miscellaneous), Biological Products, biology, Gliotoxin, leukemia, Fungi, NF-kappa B, Myeloid leukemia, DNA, biology.organism_classification, Callyspongia, Porifera, lcsh:Biology (General), chemistry, Biochemistry, Polyketides, K562 Cells, K562 cells |
| الوصف: | The Ascomycota Dichotomomyces cejpii was isolated from the marine sponge Callyspongia cf. C. flammea. A new gliotoxin derivative, 6-acetylmonodethiogliotoxin (1) was obtained from fungal extracts. Compounds 2 and 3, methylthio-gliotoxin derivatives were formerly only known as semi-synthetic compounds and are here described as natural products. Additionally the polyketide heveadride (4) was isolated. Compounds 1, 2 and 4 dose-dependently down-regulated TNFα-induced NF-κB activity in human chronic myeloid leukemia cells with IC50s of 38.5 ± 1.2 µM, 65.7 ± 2.0 µM and 82.7 ± 11.3 µM, respectively. The molecular mechanism was studied with the most potent compound 1 and results indicate downstream inhibitory effects targeting binding of NF-κB to DNA. Compound 1 thus demonstrates potential of epimonothiodiketopiperazine-derived compounds for the development of NF-κB inhibitors. |
| وصف الملف: | application/pdf |
| تدمد: | 1660-3397 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::160697cf7a5c1ed46b42b945e4350ed8 https://doi.org/10.3390/md13084949 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....160697cf7a5c1ed46b42b945e4350ed8 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 16603397 |
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