Comparative physicochemical, anti-inflammatory, and analgesic activity assay of synthesized chromium and nickel complexes of indomethacin

Abhijit Sukul, Sanjana Haque, S. Poddar, M. Hossain, K. Niloy, S. Saha
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引用次数: 4

Abstract

Abstract Objectives: Complexation of non-steroidal anti-inflammatory drugs (NSAIDs) with transition metals—chromium and nickel is a unique approach of masking the inherent side effect of gastrointestinal hemorrhage and ulceration of NSAID along with imparting beneficial pharmacological effects. Methods: Chromium and nickel complexes of indomethacin were synthesized followed by characterization of these complexes by FT-IR spectroscopy, UV–Visible spectroscopy, atomic absorption spectroscopy, calorimetric DSC analysis, and melting point analysis. For screening of biological activities to uncover potentially interesting pharmacological properties, the metal complexes were assayed for peripheral analgesic, central analgesic, and anti-inflammatory activity. Results: Nickel-indomethacin complex at dose of 20 mg/kg showed peripheral analgesia of 67.03% by inhibiting writhing and at its dose of 20 mg/kg showed potent central analgesic action at 60 min (92% elongation of tail flicking time). In anti-inflammatory study, nickel-indomethacin and chromium indomethacin complex at its 15 mg/kg dose in the 2 h showed inhibition of paw edema of 78.35 and 73.23%, respectively, which is comparable to the standard indomethacin. Conclusion: Based upon the results, it can be predicted that chromium and nickel complex of indomethacin may show promising pharmacological effects which can be revealed by extensive analysis using pharmacokinetic and pharmacodynamic test model.
吲哚美辛铬镍复合物的理化、抗炎和镇痛活性比较测定
摘要目的:非甾体抗炎药(NSAIDs)与过渡金属铬和镍的络合是一种独特的方法,可以掩盖NSAID胃肠道出血和溃疡的固有副作用,并赋予其有益的药理作用。方法:合成吲哚美辛的铬和镍配合物,并通过红外光谱、紫外-可见光谱、原子吸收光谱、量热DSC分析和熔点分析对其进行表征。为了筛选生物活性以揭示潜在的有趣药理学特性,对金属配合物的外周镇痛、中枢镇痛和抗炎活性进行了测定。结果:镍-吲哚美辛复合物20mg/kg对扭体反应的抑制作用为67.03%,20mg/kg对60min(甩尾时间延长92%)有较强的中枢镇痛作用。在抗炎研究中,15 mg/kg剂量的镍-吲哚美辛和铬-消炎痛复合物在2小时内对爪水肿的抑制率分别为78.35%和73.23%,与标准消炎痛相当。结论:根据这些结果,可以预测吲哚美辛的铬镍复合物可能显示出良好的药理作用,这可以通过药代动力学和药效学测试模型的广泛分析来揭示。
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Cogent Chemistry
Cogent Chemistry CHEMISTRY, MULTIDISCIPLINARY-
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