Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand.
Curr Pharm Biotechnol. 2021 Oct 6;22(14):1919-1931. doi: 10.2174/1389201022666210127115427.
Curcumin is claimed as a potent protectant against Gastric Ulcer (GU) induced by strong necrotizing agents, including NSAIDs through its antioxidant, anti-inflammatory and gastroprotective activities. However, it was found to exert opposite effects to either delay ulcer healing or exacerbate ulcer inflammation through some curative mechanisms differently modified by curcumin dosage. Its ability to inhibit the expression of COX-2 may also delay the healing of NSAIDs-induced GU. Recently, a topical chitosan-curcumin solution has been found to be a safe and potential alternative agent in treating oral ulcer. Therefore, an oral chitosan-curcumin mixture was developed and determined for its efficacy in treating NSAIDs-induced GU in the rat.
A chitosan (150 mg)-curcumin (20 mg) mixture with optimal gastric pH was developed. Indomethacin (30 mg/kg) was given orally to the rat and test preparations were administered orally at 5 h later and then every 24 h for two consecutive days. The sum of all gastric ulcerated areas (mm2) for each stomach was used as ulcer index. Gastric pro-inflammatory mediators and cytoprotective factors were determined.
An oral administration of a chitosan-curcumin mixture exerted a superior efficacy than curcumin, chitosan or lansoprazole (a standard antiulcer agent) in healing indomethacin-induced GU. It was revealed that the mixture exhibited the highest anti-oxidant, anti-inflammatory and gastric mucus producing activities including the high potency in down-regulating pro-inflammatory COX-2 and iNOS expression but up-regulating cytoprotective COX-1, nNOS and eNOS expression.
The present findings indicated the benefit of a chitosan-curcumin mixture as a potential alternative agent in treating NSAIDs-induced gastric ulcers.
姜黄素被认为是一种有效的保护剂，可以预防由强坏死剂引起的胃溃疡 (GU)，包括通过其抗氧化、抗炎和胃保护作用的 NSAIDs。然而，通过姜黄素剂量不同的治疗机制，它被发现会产生相反的效果，要么延迟溃疡愈合，要么加重溃疡炎症。它抑制 COX-2 表达的能力也可能会延迟 NSAIDs 引起的 GU 的愈合。最近，发现一种局部壳聚糖-姜黄素溶液是治疗口腔溃疡的一种安全有效的替代药物。因此，开发了一种口服壳聚糖-姜黄素混合物，并确定其在治疗大鼠 NSAIDs 诱导的 GU 中的疗效。
开发了一种在最佳胃 pH 值下具有壳聚糖（150mg）-姜黄素（20mg）混合物。将吲哚美辛（30mg/kg）口服给予大鼠，在 5 小时后给予测试制剂，并在接下来的两天内每 24 小时口服一次。每个胃的所有胃溃疡面积（mm2）总和用作溃疡指数。测定胃促炎介质和细胞保护因子。
口服壳聚糖-姜黄素混合物在治疗吲哚美辛诱导的 GU 方面比姜黄素、壳聚糖或兰索拉唑（一种标准抗溃疡剂）更有效。结果表明，该混合物表现出最高的抗氧化、抗炎和胃粘液产生活性，包括下调促炎 COX-2 和 iNOS 表达以及上调细胞保护 COX-1、nNOS 和 eNOS 表达的高能力。
本研究结果表明，壳聚糖-姜黄素混合物作为治疗 NSAIDs 诱导的胃溃疡的潜在替代药物具有益处。
