抗炎和超氧化物歧化酶活性Cu(II)-水杨酸酯的反应性

Ulrich Weser, Christoph Richter, Albrecht Wendel, Maged Younes
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引用次数: 71

摘要

研究了四种阿斯匹林类药物螯合铜(II)在各种超氧化物歧化酶测定中的活性。在这些研究之前,用x射线光电子能谱法测量了所涉及的铜的氧化态,并发现整个氧化态为+II。所有铜配合物都能以特定的方式抑制黄嘌呤-黄嘌呤氧化酶介导的细胞色素c和硝基蓝四氮唑的还原以及KO2形成甲酸。Cu(II)螯合物可以成功地抑制大鼠肝微粒体对苯并[α]-芘的羟基化和7-乙氧基香豆素的去甲基化。铜(II)-乙酰水杨酸酯是最活跃的铜配合物。我们的研究结果支持Cu(II)螯合物是阿司匹林样抗炎剂的活性形式的建议。
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Reactivity of antiinflammatory and superoxide dismutase active Cu(II)-salicylates

The activity of chelated Cu(II) with four different aspirin-like drugs in various superoxide dismutase assays was examined. Prior to these studies the oxidation state of the involved copper was measured by x-ray photoelectron spectrometry and was found to be +II throughout. All copper complexes were able to suppress the xanthine-xanthine oxidase mediated reduction of both cytochrome c and nitroblue tetrazolium as well as the formazan formation by KO2 in a specific manner. The hydroxylation of benzo-[α]-pyrene as well as the demethylation of 7-ethoxycoumarin using induced hepatic rat microsomes could be successfully inhibited by the employed Cu(II) chelates. Cu(II)-acetylsalicylate was the most active copper complex. Our findings support the proposal that Cu(II) chelates are the active forms of aspirin-like antiinflammatory agents.

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Chapter III. Complexes containing carbon monoxide: synthesis, reactivity, structure, bonding and therapeutic aspects of carbon monoxide–releasing molecules (CORMs) in human beings and plants Frontmatter Chapter IV Advantageous role of gaseous signalling molecule, H2S: hydrogen sulphide and their respective donors, in ophthalmic diseases and physiological implications in plants Chapter I. Coordination chemistry of chlorophylls/ bacteriochlorophylls and its functional aspects in photosynthesis Index
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