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(甲酚氧基乙酸)铜配合物的抗炎活性

[Anti-inflammatory activity of (cresoxyacetate)copper complexes].

作者信息

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

机构信息

Katedra chemickej teórie lieciv Farmaceutickej fakulty Univerzity Komenského, Bratislava.

出版信息

Ceska Slov Farm. 1998 Jul;47(4):166-9.

PMID:9748757
Abstract

In groups of mononuclear aqua(cresoxyacetato)copper(II) complexes of the composition [Cu(ROCH2COO)2(H2O)n] (R= 2- and 3-methylphenyl, n = 2; 4-methylphenyl, n = 3) and binu- clear phenazone(o-, m-, p-cresoxyacetato)copper(II) complexes of the composition [Cu2(ROCH2COO)4(phz)2] the anti-inflammatory activity was assayed in rat paw carrageenan-induced edema. The effects of the complexes were compared with each other and with those of the free acids. Salicylic acid and its cupric salt (tetrahydrate) were used as standards of comparison. All copounds were applied i.p. in a single dose of 50 mumol/kg body weight (calculated for the RCOO-fragment). In general, all Cu(II) complexes tested were clearly more effective (71-88%) than the corresponding free isomeric cresoxyacetic acids (47, 37, 45%), with the exception of diaquabis (o-cresoxyacetato)copper(II) complex (43%). Copper(II) salicylate tetrahydrate (57%) and salicylic acid (41%) were less active, too. The observed activities of complexes are discussed in relation to their structures.

摘要

在组成式为[Cu(ROCH₂COO)₂(H₂O)ₙ](R = 2-甲基苯基和3-甲基苯基,n = 2;4-甲基苯基,n = 3)的单核水合(甲酚氧基乙酸根)铜(II)配合物以及组成式为[Cu₂(ROCH₂COO)₄(phz)₂]的双核非那宗(邻、间、对甲酚氧基乙酸根)铜(II)配合物中,测定了它们在大鼠足趾角叉菜胶诱导水肿模型中的抗炎活性。将这些配合物的效果相互比较,并与游离酸的效果进行比较。使用水杨酸及其铜盐(四水合物)作为比较标准。所有化合物均以50 μmol/kg体重的单剂量腹腔注射(按RCOO-片段计算)。总体而言,除了二水双(邻甲酚氧基乙酸根)铜(II)配合物(43%)外,所有测试的Cu(II)配合物的效果明显优于相应的游离异构甲酚氧基乙酸(分别为47%、37%、45%)。水杨酸铜(II)四水合物(57%)和水杨酸(41%)的活性也较低。根据配合物的结构对观察到的活性进行了讨论。

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