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水合双(2,Y-二乙酰氧基苯甲酸酯)-铜配合物(Y = 4、5或6)的抗炎活性

[Anti-inflammatory activity of aqua-bis(2,Y-diacetoxybenzoate)-copper complexes (Y=4, 5 or 6)].

作者信息

Sokolík J, Tumová I, Blahová M, Tadlaoui M M, Svec P

机构信息

Katedra chemickej teórie lieciv, Farmaceutickej fakulty, Univerzity Komenského, Bratíslava.

出版信息

Ceska Slov Farm. 1997 Apr;46(2):88-90.

PMID:9244569
Abstract

In a group of binuclear copper (II) complexes of the composition [Cu2(RCOO)4(H2O)2] (R = 2,4-diacetoxyphenyl (I), 2,5-diacetoxyphenyl (II) and 2,6-diacetoxyphenyl (III)), the anti-inflammatory activity was assayed in rat paw carrageenan-induced edema. Copper (II) salicylate tetrahydrate (IV) and salicylic acid were used as standards for comparison. All compounds were applied i.p. in a single dose of 50 mumol/kg body weight, calculated for the R-COO-fragment. The Cu(II) complexes tested were clearly more effective than the corresponding free diacetoxybenzoic acids, with an exception for the 2,5-diacetoxy derivative. The average anti-inflammatory activities of copper (II) complexes were decreasing in the following order: III (71.0%) = (70.6%) > IV (57.4%) > II (18.0%). Of the acids, only 2,6-diacetoxybenzoic acid (45.2%) was effective at the level of salicylic acid (44.9%). The relationship between the coordination-chemical properties and the biological effects of the complexes tested is discussed.

摘要

在一组组成为[Cu2(RCOO)4(H2O)2](R = 2,4 - 二乙酰氧基苯基(I)、2,5 - 二乙酰氧基苯基(II)和2,6 - 二乙酰氧基苯基(III))的双核铜(II)配合物中,在大鼠足趾角叉菜胶诱导的水肿模型中测定了其抗炎活性。以四水合铜(II)水杨酸盐(IV)和水杨酸作为对照标准。所有化合物均以50 μmol/kg体重的单剂量腹腔注射给药,剂量按R - COO片段计算。所测试的铜(II)配合物明显比相应的游离二乙酰氧基苯甲酸更有效,但2,5 - 二乙酰氧基衍生物除外。铜(II)配合物的平均抗炎活性按以下顺序降低:III(71.0%) = I(70.6%) > IV(57.4%) > II(18.0%)。在这些酸中,只有2,6 - 二乙酰氧基苯甲酸(45.2%)在水杨酸(44.9%)的水平上具有抗炎效果。讨论了所测试配合物的配位化学性质与生物学效应之间的关系。

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