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

机译:吲哚美辛合成的铬和镍配合物的比较理化,消炎和镇痛活性测定

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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.
机译:目标:非甾体类抗炎药(NSAID)与过渡金属-铬和镍的复合是掩盖胃肠道出血和NSAID溃疡固有的副作用并具有有益的药理作用的独特方法。方法:合成吲哚美辛的铬和镍配合物,然后通过FT-IR光谱,UV-可见光谱,原子吸收光谱,量热DSC分析和熔点分析对这些配合物进行表征。为了筛选生物学活性以发现潜在的令人感兴趣的药理特性,测定了金属配合物的外周镇痛,中枢镇痛和抗炎活性。结果:镍-吲哚美辛复合物剂量为20?mg / kg时,通过抑制扭动表现出67.03%的外周镇痛;剂量为20?mg / kg时,在60?min时显示出有效的中枢镇痛作用(92%的伸长率甩尾时间)。在抗炎研究中,镍吲哚美辛和吲哚美辛铬复合物在2?h剂量为15?mg / kg时,爪水肿的抑制作用分别为78.35%和73.23%,与标准消炎痛相当。结论:基于该结果,可以预测吲哚美辛的铬和镍配合物可能显示出有希望的药理作用,这可以通过使用药代动力学和药效学测试模型进行的广泛分析来揭示。

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