Gracilin-Derivatives as Lead Compounds for Anti-inflammatory Effects
| العنوان: | Gracilin-Derivatives as Lead Compounds for Anti-inflammatory Effects |
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| المؤلفون: | Sandra Gegunde, Luis M. Botana, Amparo Alfonso, Rebeca Alvariño, Eva Alonso |
| المصدر: | Cellular and Molecular Neurobiology. 40:603-615 |
| بيانات النشر: | Springer Science and Business Media LLC, 2019. |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | Lipopolysaccharides, 0301 basic medicine, Lipopolysaccharide, Cell Survival, NF-E2-Related Factor 2, medicine.drug_class, Anti-Inflammatory Agents, Nitric Oxide Synthase Type II, Inflammation, Nitric Oxide, Anti-inflammatory, Cell Line, Nitric oxide, Mice, 03 medical and health sciences, Cellular and Molecular Neuroscience, chemistry.chemical_compound, 0302 clinical medicine, medicine, Animals, Humans, Cyclophilin, Membrane Potential, Mitochondrial, biology, Microglia, Interleukin-6, Tumor Necrosis Factor-alpha, NF-kappa B, Cell Biology, General Medicine, Nitric oxide synthase, 030104 developmental biology, medicine.anatomical_structure, chemistry, Biochemistry, Cyclosporine, biology.protein, Tumor necrosis factor alpha, Diterpenes, medicine.symptom, Reactive Oxygen Species, 030217 neurology & neurosurgery |
| الوصف: | Gracilins are diterpenes derivative, isolated from the marine sponge Spongionella gracilis. Natural gracilins and synthetic derivatives have shown antioxidant, immunosuppressive, and neuroprotective capacities related to the affinity for cyclophilins. The aim of this work was to study anti-inflammatory and immunosuppressive pathways modulated by gracilin L and two synthetic analogues, compound 1 and 2, on a cellular model of inflammation. In this way, the murine BV2 microglia cell line was used. To carry out the experiments, microglia cells were pre-treated with compounds for 1 h and then stimulated with lipopolysaccharide for 24 h to determine reactive oxygen species production, mitochondrial membrane potential, the release of nitric oxide, interleukin-6 and tumor necrosis factor-α and the expression of Nuclear factor-erythroid 2-related factor 2, Nuclear Factor-κB, the inducible nitric oxide synthase, and the cyclophilin A. Finally, a co-culture of neuron SH-SY5Y and microglia BV2 cells was used to check the neuroprotective effect of these compounds. Cyclosporine A was used as a control of effect. The compounds were able to decrease inflammatory mediators, the expression of inflammatory target proteins as well as they activated anti-oxidative mechanism upon inflammatory conditions. For this reason, natural and synthetic gracilins could be interesting for developing anti-inflammatory drugs. |
| تدمد: | 1573-6830 0272-4340 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24dc28c8c10218eaac99420b149d9e8cTest https://doi.org/10.1007/s10571-019-00758-5Test |
| حقوق: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....24dc28c8c10218eaac99420b149d9e8c |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15736830 02724340 |
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