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首页> 外文期刊>Journal of drug targeting >Dextran-5-(4-ethoxycarbonylphenylazo)salicylic acid ester, a polymeric colon-specific prodrug releasing 5-aminosalicylic acid and benzocaine, ameliorates TNBS-induced rat colitis
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Dextran-5-(4-ethoxycarbonylphenylazo)salicylic acid ester, a polymeric colon-specific prodrug releasing 5-aminosalicylic acid and benzocaine, ameliorates TNBS-induced rat colitis

机译：葡聚糖-5-（4-乙氧基羰基苯苯基）水杨酸酯，一种聚合物结肠特异性前药释放5-氨基水杨酸和苯并，改善TNBS诱导的大鼠结肠炎

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摘要

Local anesthetics have beneficial effects on colitis. Dextran-5-(4-ethoxycarbonylphenylazo)salicylic acid ester (Dex-5-ESA), designed as a polymeric colon-specific prodrug liberating 5-ASA and benzocaine in the large intestine, was prepared and its therapeutic activity against colitis was evaluated using a TNBS-induced rat colitis model. Dex-5-ESA liberated 5-ASA and benzocaine in the cecal contents while (bio)chemically stable in the small intestinal contents and mucosa. Oral administration of Dex-5-ESA (equivalent to 10 mg 5-ASA/kg, twice a day) alleviated colonic injury and reduced MPO activity in the inflamed colon. In parallel, pro-inflammatory mediators, COX-2, iNOS and CINC-3, elevated by TNBS-induced colitis, were substantially diminished in the inflamed colon. Dex-5-ESA was much more effective for the treatment of colitis than 5-(4-ethoxycarbonylphenylazo)salicylic acid (5-ESA) that may not deliver benzocaine to the large intestine. Our data suggest that Dex-5-ESA is a polymeric colon-specific prodrug, liberating 5-ASA and benzocaine in the target site (large intestine), probably exerting anti-colitic effects by combined action of 5-ASA and benzocaine.
机译：局部麻醉剂对结肠炎有益的影响。制备设计为大肠中的聚合物结肠特异性前药（大肠杆菌和苯并催化的葡聚糖-5-（4-乙氧基羰基苯基）（DEX-5-ESA），并使用其对结肠炎的治疗活性进行评估TNBS诱导的大鼠结肠炎模型。 DEX-5-ESA释放了5-ASA和苯并肽，而在小肠内容物和粘膜中化学稳定的同时（BIO）。口服施用DEX-5-ESA（相当于10mg 5-ASA / kg，每天两次）缓解结肠损伤并降低发炎的结肠中的MPO活性。在发炎的结肠中并行地，通过TNBS诱导的结肠炎升高的促炎介质，COX-2，INOS和CINC-3升高。 DEX-5-ESA对沉肠炎的治疗比5-（4-乙氧基羰基苯基苯基）水杨酸（5-ESA）的治疗更有效，这些水杨酸可能不会向大肠输送苯并催化。我们的数据表明，DEX-5-ESA是聚合物结肠特异性前药，在靶位点（大肠）中释放5-ASA和苯陶器，可能通过5-ASA和苯会聚的组合作用施加抗菌效应。

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