龙胆紫的代谢和作用方式。
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Docampo R,莫雷诺SN
龙胆紫的代谢和作用方式。
药物金属底座启1990;22 (3):161 - 78。
- PubMed ID
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2272286 (在PubMed]
- 文摘
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龙胆紫一直用于医学近100年:作为防腐剂外用,作为antihelminthic剂口服,而最近,作为血添加剂防止南美洲锥虫病的传播。到目前为止,没有严重的副作用报道使用时外部。然而,口服可引起胃肠道刺激,静脉注射可引起抑郁的白细胞计数。令人惊讶的是,没有急性毒性副作用报告后政府大量的龙胆violet-treated血。没有研究已经完成长期影响(慢性毒性、致癌性)龙胆violet-treated血液在人体或动物实验室。结晶紫是诱变剂,有丝分裂毒药,clastogen。龙胆紫的致癌效应在啮齿动物中最近报道。此外,许多triphenylmethane-classed染料、龙胆紫的成员,被认为是动物和人类致癌物。光动力作用的龙胆紫,显然是由一个自由基的机制,被描述在t . cruzi细菌和。然而,在黑暗中龙胆紫毒性的主要目标是线粒体。 Gentian violet is actively demethylated by liver microsomes from different animals and is reduced to leucogentian violet by intestinal microflora. Although the first process may represent a detoxication reaction, the second pathway may have toxicological significance because the completely demethylated derivative leucopararosaniline has been demonstrated to be carcinogenic in rats. A free-radical derivative of gentian violet is also formed by the action of rat liver microsomes, but whether this radical is involved in the cytotoxic effects of gentian violet in mammalian cells remains to be elucidated. Other pathways of gentian violet metabolism have recently been investigated that involve its oxidative N-demethylation by peroxidases. The N-demethylation of gentian violet by prostaglandin synthetase deserves further study. In this regard, the PGS system is being studied as an alternative activating pathway in xenobiotic metabolism because some carcinogenic intermediates can be formed during this cooxidation reaction.