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具有抗炎和超氧化物歧化酶活性的铜(II)-水杨酸盐的反应活性。

Reactivity of antiinflammatory and superoxide dismutase active Cu(II)-salicylates.

作者信息

Weser U, Richter C, Wendel A, Younes M

出版信息

Bioinorg Chem. 1978;8(3):201-13. doi: 10.1016/s0006-3061(00)80196-9.

Abstract

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-[alpha]-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.

摘要

研究了螯合铜(II)与四种不同阿司匹林类药物在各种超氧化物歧化酶测定中的活性。在这些研究之前,通过X射线光电子能谱法测量了所涉及铜的氧化态,发现始终为+II。所有铜配合物都能够以特定方式抑制黄嘌呤-黄嘌呤氧化酶介导的细胞色素c和硝基蓝四唑的还原以及超氧化钾介导的甲臜形成。使用诱导的大鼠肝微粒体,苯并[α]芘的羟基化以及7-乙氧基香豆素的去甲基化可以被所使用的铜(II)螯合物成功抑制。乙酰水杨酸铜(II)是活性最高的铜配合物。我们的研究结果支持了铜(II)螯合物是阿司匹林类抗炎剂活性形式的提议。

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