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一种经皮应用的水杨酸铜制剂(Alcusal)的抗炎活性。

Anti-inflammatory activity of a dermally applied copper salicylate preparation (Alcusal).

作者信息

Walker W R, Beveridge S J, Whitehouse M W

出版信息

Agents Actions. 1980 Apr;10(1 Pt 2):38-47. doi: 10.1007/BF02024177.

DOI:10.1007/BF02024177
PMID:7386307
Abstract

In rats, dermal (dorsum) application of an ethanolic copper salicylate complex (ECS) in ethanol with glycerol (Alcusal) effectively suppressed established polyarthritis, carrageenan-induced paw oedema and the inflammatory response to hydroxylapatite microcrystals. These responses appear to be due to some degree of synergism between the copper(II) and salicylate, i.e. not solely due to either species alone. Evidence for transdermal absorption of 64Cu from 64Cu-ECS is provided. Some safety aspects of this novel drug are discussed.

摘要

在大鼠中,将乙醇水杨酸铜络合物(ECS)与甘油在乙醇中配制成的溶液(Alcusal)经皮(背部)给药,可有效抑制已形成的多关节炎、角叉菜胶诱导的爪肿胀以及对羟基磷灰石微晶的炎症反应。这些反应似乎是由于铜(II)和水杨酸之间存在一定程度的协同作用,即并非仅由单一成分所致。文中提供了64Cu-ECS经皮吸收64Cu的证据。还讨论了这种新型药物的一些安全性问题。

相似文献

1
Anti-inflammatory activity of a dermally applied copper salicylate preparation (Alcusal).一种经皮应用的水杨酸铜制剂(Alcusal)的抗炎活性。
Agents Actions. 1980 Apr;10(1 Pt 2):38-47. doi: 10.1007/BF02024177.
2
Lipophilic copper(II) formulations: some correlations between their composition and anti-inflammatory/anti-arthritic activity when applied to the skin of rats.亲脂性铜(II)制剂:应用于大鼠皮肤时其组成与抗炎/抗关节炎活性之间的一些相关性。
Agents Actions. 1982 Apr;12(1-2):225-31. doi: 10.1007/BF01965151.
3
Copper salicylate and copper phenylbutazone as topically applied anti-inflammatory agents in the rat and horse.水杨酸铜和苯基丁氮酮作为大鼠和马的局部抗炎剂
J Vet Pharmacol Ther. 1990 Mar;13(1):67-75. doi: 10.1111/j.1365-2885.1990.tb00749.x.
4
Biodistribution of 64Cu in rats after topical application of two lipophilic anti-inflammatory Cu(II) formulations.
Agents Actions. 1984 Feb;14(2):291-5. doi: 10.1007/BF01966655.
5
Biodistribution of 64Cu in inflamed rats following administration of two anti-inflammatory copper complexes.两种抗炎铜配合物给药后64Cu在炎症大鼠体内的生物分布
Agents Actions. 1985 Oct;17(1):104-11. doi: 10.1007/BF01966692.
6
Anti-inflammatory activity of copper salicylates applied to rats percutaneously in dimethyl sulphoxide with glycerol.在二甲基亚砜与甘油中经皮应用于大鼠的水杨酸铜的抗炎活性。
J Pharm Pharmacol. 1980 Jun;32(6):425-7. doi: 10.1111/j.2042-7158.1980.tb12957.x.
7
Dermal copper drugs: the copper bracelet and cu(II) salicylate complexes.
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The pharmacologic activity of complexes and mixtures with copper and salicylates or aminopyrine following oral dosing in rats.大鼠口服给药后,铜与水杨酸盐或氨基比林的复合物及混合物的药理活性。
Agents Actions. 1989 Mar;26(3-4):355-9. doi: 10.1007/BF01967301.
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Copper salicylate as an anti-inflammatory and analgesic agent in arthritic rats.水杨酸铜作为关节炎大鼠的抗炎和镇痛剂
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Effects of salicylate-copper complex on the metabolic activation in phagocytizing granulocytes.水杨酸盐-铜络合物对吞噬性粒细胞代谢激活的影响。
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引用本文的文献

1
Orally active antioxidative copper(II) aspirinate: synthesis, structure characterization, superoxide scavenging activity, and in vitro and in vivo antioxidative evaluations.口服活性抗氧化阿司匹林铜(II):合成、结构表征、超氧化物清除活性以及体外和体内抗氧化评估。
J Biol Inorg Chem. 2005 Dec;10(8):831-41. doi: 10.1007/s00775-005-0031-3. Epub 2005 Oct 28.
2
Anti-inflammatory properties of copper implants in the rat paw edema: a preliminary study.铜植入物对大鼠爪肿胀的抗炎特性:一项初步研究。
Agents Actions. 1981 Dec;11(6-7):746-9. doi: 10.1007/BF01978800.
3
Lipophilic copper(II) formulations: some correlations between their composition and anti-inflammatory/anti-arthritic activity when applied to the skin of rats.

本文引用的文献

1
Some copper coordination compounds and their antiinflammatory and antiulcer activities.一些铜配合物及其抗炎和抗溃疡活性。
Inflammation. 1976 Jun;1(3):317-31. doi: 10.1007/BF00917871.
2
Sodium gamma-resorcylate in rheumatic fever.γ-间苯二酚钠在风湿热中的应用
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3
Chelation as a mechanism of pharmacological action.螯合作用作为一种药理作用机制。
亲脂性铜(II)制剂:应用于大鼠皮肤时其组成与抗炎/抗关节炎活性之间的一些相关性。
Agents Actions. 1982 Apr;12(1-2):225-31. doi: 10.1007/BF01965151.
4
Biodistribution of 64Cu in rats after topical application of two lipophilic anti-inflammatory Cu(II) formulations.
Agents Actions. 1984 Feb;14(2):291-5. doi: 10.1007/BF01966655.
5
Biodistribution of 64Cu in inflamed rats following administration of two anti-inflammatory copper complexes.两种抗炎铜配合物给药后64Cu在炎症大鼠体内的生物分布
Agents Actions. 1985 Oct;17(1):104-11. doi: 10.1007/BF01966692.
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Microvascular lesions as a target of anti-inflammatory and certain other drugs.微血管病变作为抗炎药及某些其他药物的作用靶点。
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Some biochemical and pharmacological properties of anti-inflammatory drugs.
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Free radicals and inflammation: protection of synovial fluid by superoxide dismutase.自由基与炎症:超氧化物歧化酶对滑液的保护作用
Science. 1974 Aug 9;185(4150):529-31. doi: 10.1126/science.185.4150.529.
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Free radical production by metallic copper.金属铜产生自由基。
Contraception. 1974 Sep;10(3):273-80. doi: 10.1016/0010-7824(74)90005-5.
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Experimental inflammation induced by naturally occurring microcrystalline calcium salts.由天然存在的微晶钙盐诱导的实验性炎症。
J Rheumatol. 1976 Mar;3(1):54-62.
10
Synthesis and biological evaluation of tetrakis(acetylsalicylato)-mu-dicopper(II).四(乙酰水杨酸根)-μ-二铜(II)的合成与生物学评价
J Pharm Sci. 1976 Jan;65(1):126-8. doi: 10.1002/jps.2600650129.