Biological Evaluation of 2-(4-Amino-Phenyl)-3-(3,5-Dihydroxylphenyl) Propenoic Acid
| العنوان: | Biological Evaluation of 2-(4-Amino-Phenyl)-3-(3,5-Dihydroxylphenyl) Propenoic Acid |
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| المؤلفون: | Liang Xi, Ting Xue, Fei Liu, Min Ju, Guizhen Ao, Yue Zhao, Guang-Lin Xu |
| المصدر: | Basic & Clinical Pharmacology & Toxicology. 105:350-356 |
| بيانات النشر: | Wiley, 2009. |
| سنة النشر: | 2009 |
| مصطلحات موضوعية: | Male, Anti-Inflammatory Agents, Inflammation, Pharmacology, Resveratrol, Carrageenan, Toxicology, Inhibitory postsynaptic potential, Rats, Sprague-Dawley, Mice, chemistry.chemical_compound, Caffeic Acids, In vivo, medicine, Animals, Edema, Cyclooxygenase Inhibitors, Lipoxygenase Inhibitors, Stomach Ulcer, chemistry.chemical_classification, Mice, Inbred ICR, Aniline Compounds, biology, Stomach, General Medicine, In vitro, Rats, medicine.anatomical_structure, Enzyme, chemistry, biology.protein, Cyclooxygenase, medicine.symptom |
| الوصف: | 2-(4-Aminophenyl)-3-(3,5-dihydroxylphenyl) propenoic acid (CSN-07001) is a new compound based on the combination of resveratrol and propenoic acid derivatives. In vitro cyclooxygenase (COX)/5-lipoxygenase (5-LOX) inhibition assays showed that the test compound exhibited a dual inhibitory activity against the COX (COX-1 IC(50) = 2.20 microM, COX-2 IC(50) = 1.76 microM) and 5-LOX (IC(50) = 0.28 microM) enzymes. Further, the enhanced COX-1/COX-2/5-LOX expression in lipopolysaccaride-induced lung inflammation in mice was also suppressed by CSN-07001 in a concentration-dependent manner. In vivo studies showed that CSN-07001 exhibited potent anti-inflammatory and antinociceptive effects in different experimental models. We further examined the risk of gastric damage induced by CSN-07001. The test compound was gastric-sparing in that it elicited markedly fewer stomach lesions than indomethacin in rats. Taken together, our data indicate that CSN-07001 exhibits a novel class of dual inhibitors of COX and 5-LOX having therapeutic potential as non-steroidal anti-inflammatory agents with an enhanced gastric safety profile. |
| تدمد: | 1742-7843 1742-7835 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af79b3bc7814c84c12f8188644ca93f2Test https://doi.org/10.1111/j.1742-7843.2009.00463.xTest |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....af79b3bc7814c84c12f8188644ca93f2 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 17427843 17427835 |
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