生物活性 | |||
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描述 | F-5-Aminosalicylic acid (5-ASA) is a specific agonist for PPARγ, and only PPARγ but not PPARα or PPARδ induces p65 degradation. 5-Aminosalicylic acid induces degradation of p65 protein indicative of PPARγ's E3 ubiquitin ligase activity. 5-Aminosalicylic acid blocks NF-κB in intestinal epithelial cells (IECs) through inhibition of PAK1[3]. Pretreatment with 5-Aminosalicylic acid (5-ASA) or Nimesulide at different concentration (10-1000 μmol/L) for 12-96 h, inhibits the growth of HT-29 colon carcinoma cells in a dose and time-dependent manner. Combined 5-Aminosalicylic acid (final concentration 100 μM) and Nimesulide (final concentration 10-1000 μM) inhibits the proliferation of HT-29 colon carcinoma cells in a dose-dependent manner, being more potent than corresponding dose of Nimesulide. In A/JOlaHsd mice, 5-ASA suppressed colon carcinogenesis by decreasing the number of aberrant crypt foci (75%) and aberrant crypts (22%) induced by AOM (azoxymethane) treatment with an absence of 5-ASA response after GW9662 administration[4]. Pretreatment with 5-ASA or nimesulide at the concentration of 10-1000 micromol/L inhibited proliferation of HT-29 colon carcinoma cells in a dose-dependent manner in vitro. The inhibition rate of HT-29 colon carcinoma cell proliferation was also increased when pretreated with 5-ASA (100 micromol/L) or nimesulide (100 micromol/L) for 12-96 h, which showed an obvious time-effect relationship. 5-ASA and nimesulide may inhibit the proliferation of HT-29 colon carcinoma cells and coadministration of these agents may have additional chemopreventive potential[5]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00746447 | Colitis, Ulcerative ... 展开 >> Recurrence 收起 << | Phase 3 | Completed | - | Germany ... 展开 >> Evangelisches Krankenhaus Kalk, Medical Dept. Cologne, Germany, 51103 收起 << |
NCT01699438 | Irritable Bowel Syndrome | Phase 2 | Completed | - | Sweden ... 展开 >> Sahlgrenska University Hospital Göteborg, Sweden Karolinska University Hospital Huddinge, Sweden Norrland's University Hospital Umeå, Sweden 收起 << |
NCT01257399 | Ulcerative Colitis in Remissio... 展开 >>n 收起 << | Phase 3 | Completed | - | China ... 展开 >> Shanghai Hospital Shanghai, China 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
6.53mL 1.31mL 0.65mL |
32.65mL 6.53mL 3.27mL |
65.30mL 13.06mL 6.53mL |
参考文献 |
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