Synthesis and Biological Evaluation of Novel Resveratrol-NSAID Derivatives as Anti-inflammatory Agents
| Autor: | Yan-Yan Ma, Deng-Gao Zhao, Kun Zhang, Wei Peng, Yu Zhang, Ai-Yu Zhou, Zhiyun Du, Wang Huaqian |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Lipopolysaccharides Lipopolysaccharide medicine.drug_class Cell Survival Interleukin-1beta Anti-Inflammatory Agents Enzyme-Linked Immunosorbent Assay Ibuprofen Pharmacology Resveratrol Nitric Oxide Anti-inflammatory Dietary Polyphenol Nitric oxide 03 medical and health sciences chemistry.chemical_compound Mice Drug Discovery Stilbenes medicine Gastric mucosa Animals Tumor Necrosis Factor-alpha organic chemicals Macrophages Anti-Inflammatory Agents Non-Steroidal General Chemistry General Medicine 030104 developmental biology medicine.anatomical_structure RAW 264.7 Cells chemistry Gastric Mucosa Tumor necrosis factor alpha medicine.drug |
| Zdroj: | Chemicalpharmaceutical bulletin. 64(6) |
| ISSN: | 1347-5223 |
| Popis: | Long-term use of nonsteroidal antiinflammatory drugs (NSAIDs) may cause serious side effects such as gastric mucosal damage. Resveratrol, a naturally dietary polyphenol, exhibited anti-inflammatory activity and a protective effect against gastric mucosa damage induced by NSAIDs. In this regard, we synthesized a series of resveratrol-based NSAIDs derivatives and evaluated their anti-inflammatory activity against nitric oxide (NO) overproduction in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. We identified mono-substituted resveratrol-ibuprofen combination 21 as the most potent anti-inflammatory agent, which is more active than a physical mixture of ibuprofen and resveratrol, individual ibuprofen, or individual resveratrol. In addition, compound 21 exerted potent inhibitory effects on the LPS-induced expression of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β). Furthermore, compound 21 significantly increased the survival rate in an LPS-induced acute inflammatory model and produced markedly less gastric damage than ibuprofen. It was found that compound 21 may be a potent anti-inflammatory agent for the treatment of inflammation-related diseases. |
| Databáze: | OpenAIRE |
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