College of Pharmacy, University of Mosul, Mosul, Iraq,
Department of Pharmaceutical Chemistry, University of Mosul, Mosul, Iraq,
Pharmacology. 2020;105(11-12):645-651. doi: 10.1159/000506232. Epub 2020 Apr 14.
Peptic lesions usually develop when there is an imbalance between aggressive drivers and gastro-protective mediators that guard the lining of the gastrointestinal tract. The most crucial of these mediators are antioxidants, whose loss may predispose to oxidative stress, which is believed to be the main aggravator of several diseases including peptic ulcer. Proton pump inhibitors (PPIs) are drugs that are highly effective and widely used for therapeutic management of peptic disorders through inhibition of gastric acid secretion. In spite of this, oxidative damage may continue to be a major issue that can predispose to future lesions.
The present study is designed to explore the possible antioxidant capability of different PPIs, including omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole, in an aim to suggest an agent that, in addition to its acid-suppression properties, can provide antioxidant profit.
The antioxidant activity of different PPIs was evaluated calorimetrically to test the ability of each drug to quench oxygen free radical, using the well-known stable free radical α,α-diphenyl-β-picrylhydrazyl (DPPH), and compared to ascorbic acid (AA; vitamin C). The measurements were performed using a spectrophotometer at 517 nm.
All the studied drugs reduced DPPH, but to different extents. However, omeprazole and esomeprazole showed the highest ability to scavenge free radicals (50% inhibitory concentrations [IC50s] of the percentage for free radical scavenging activity are 18.7 ± 5.7 and 18.7 ± 5.7, respectively, and the AA equivalents are 83,772 ± 11,887 and 81,732 ± 8,523 mg AA/100 g, respectively). Conversely, lansoprazole, pantoprazole, and rabeprazole might be having no role in this story (IC50s of the percentage for free radical scavenging activity are 49.3 ± 3.1, 49 ± 9.4, and 40.7 ± 7.2, respectively, and the AA equivalents are 30,458 ± 3,884, 32,222 ± 10,377, and 37,876 ± 8,816 mg AA/100 g, respectively).
Thus, omeprazole and esomeprazole may confer a significant dual action in gastrointestinal protection by providing potent antioxidant properties in addition to their major role as acid-suppression agents. However, further studies are essential to elucidate the mechanism behind the difference between the drugs of the same class.
当侵袭因素和胃黏膜保护因素之间失去平衡时，通常会发生消化性溃疡。这些保护因素中最重要的是抗氧化剂，其损失可能导致氧化应激，而氧化应激被认为是包括消化性溃疡在内的多种疾病的主要加重因素。质子泵抑制剂（PPIs）是通过抑制胃酸分泌而对消化性疾病进行治疗管理的高度有效且广泛使用的药物。尽管如此，氧化损伤仍可能是导致未来病变的主要问题。
本研究旨在探索不同的质子泵抑制剂（包括奥美拉唑、埃索美拉唑、兰索拉唑、泮托拉唑和雷贝拉唑）的可能抗氧化能力，以寻找一种既能抑制胃酸分泌又能提供抗氧化益处的药物。
通过使用稳定的自由基α，α-二苯基-β-苦基肼（DPPH）来检测每种药物清除氧自由基的能力，对不同的质子泵抑制剂的抗氧化活性进行了比色法评估，并与抗坏血酸（AA；维生素 C）进行了比较。测量是在分光光度计上于 517nm 处进行的。
所有研究的药物均能降低 DPPH，但降低程度不同。然而，奥美拉唑和埃索美拉唑表现出最强的清除自由基能力（清除自由基活性的 50%抑制浓度[IC50]分别为 18.7 ± 5.7%和 18.7 ± 5.7%，AA 当量分别为 83772 ± 11887 和 81732 ± 8523mg AA/100g）。相反，兰索拉唑、泮托拉唑和雷贝拉唑可能在这方面没有作用（清除自由基活性的 50%抑制浓度[IC50]分别为 49.3 ± 3.1%、49 ± 9.4%和 40.7 ± 7.2%，AA 当量分别为 30458 ± 3884、32222 ± 10377 和 37876 ± 8816mg AA/100g）。
因此，奥美拉唑和埃索美拉唑除了作为主要的抑酸剂外，还可能通过提供强大的抗氧化特性，从而在胃肠道保护方面发挥重要的双重作用。然而，需要进一步的研究来阐明同一类药物之间差异的背后机制。
