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一种具有抗氧化活性和体外自由基清除能力的有机硒药物。

An organoselenium drug with antioxidant activity and free radical scavenging capacity in vitro.

机构信息

Programa de Pós-Graduação em Ciências Biológicas-Bioquímica Toxicológica, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria, Santa Maria, CEP 97105-900 Rio Grande do Sul, Brazil.

出版信息

Biol Trace Elem Res. 2012 Dec;149(3):399-404. doi: 10.1007/s12011-012-9440-7. Epub 2012 May 6.

DOI:10.1007/s12011-012-9440-7
PMID:22562597
Abstract

Organoselenum compounds have been reported to have a wide range of pharmacological properties. Amine-based diselenide, (Z)-N-(4-methylbenzylidene)-1-(2-((2-(1-((E)-4-methyl benzylideneamino)ethyl)phenyl)diselanyl)phenyl)ethanamine ethyl)phenyl) diselanyl) phenyl) ethylimino) methyl)phenol (compound A), and diphenyl diselenide (PhSe)2 were screened for in vitro antioxidant activity. Compound A and (PhSe)2 were tested against sodium nitroprusside (SNP)- and Fe(II)-induced thiobarbituric acid-reactive species (TBARS) in rat brain homogenates. The radical scavenging activity was measured by 1,1-diphenyl-2-picrylhydrazyl assay. Both compounds A and (PhSe)2 decreased Fe(II)- and SNP-stimulated TBARS production in rat brain homogenates. Compound A exhibited the strongest antioxidant activity in the radical scavenging assay, although (PhSe)2, the simplest of the diaryl diselenide, presented no activity. In conclusion, the results of the present investigation indicated that compound A and (PhSe)2 had preventive effects against SNP- and Fe(II)-induced oxidative stress in rat brain homogenates. The amine group in the organic moiety dramatically changed the potency of amine-based diselenide.

摘要

有机硒化合物具有广泛的药理特性。含胺二硒化物,(Z)-N-(4-甲基苄叉基)-1-(2-((2-(1-((E)-4-甲基苄叉基氨基)乙基)苯基)二硒基)苯基)乙胺乙基)苯基)二硒基)苯基)乙基亚氨基)甲基)苯酚(化合物 A)和二苯基二硒化物(PhSe)2 被筛选用于体外抗氧化活性。化合物 A 和 (PhSe)2 测试了对大鼠脑匀浆中硝普钠 (SNP) 和 Fe(II)诱导的硫代巴比妥酸反应性物质 (TBARS) 的影响。自由基清除活性通过 1,1-二苯基-2-苦基肼测定。两种化合物 A 和 (PhSe)2 都降低了大鼠脑匀浆中 Fe(II)和 SNP 刺激的 TBARS 生成。化合物 A 在自由基清除试验中表现出最强的抗氧化活性,尽管最简单的二芳基二硒化物 (PhSe)2 没有活性。总之,本研究结果表明,化合物 A 和 (PhSe)2 对 SNP 和 Fe(II)诱导的大鼠脑匀浆氧化应激具有预防作用。有机部分中的胺基极大地改变了含胺二硒化物的效力。

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