2,3-DITHIOERYTHRITOL, A POSSIBLE NEW ARSENIC ANTIDOTE
2,3-DITHIOERYTHRITOL, A POSSIBLE NEW ARSENIC ANTIDOTE
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DOI：
10.1021/tx00011a006
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发表时间：
1989-09-01
影响因子：
4.1
通讯作者：
MCGOWN, EL
中科院分区：
文献类型：
--
作者：
BOYD, VL;HARBELL, JW;MCGOWN, EL
英国抗路易氏剂（2，3-二巯基丙醇; BAL）长期以来一直被用作砷解毒剂，但其治疗效果受到其固有毒性的限制。我们合成了两种毒性较小的BAL衍生物，并研究了它们作为有机砷解毒剂的潜力。新化合物2，3-二硫杂环戊烷（DTE）和2，2-二甲基-4-羟甲基-1，3-二硫杂环戊烷（BAL的异亚丙基衍生物）与苯二氯胂（PDA）反应，生成相应的环状1，3-二硫杂环胂。BAL衍生物进行了比较，BAL在其细胞毒性和他们的能力，以挽救PDA中毒的小鼠淋巴瘤细胞培养。二硫戊环在培养细胞系统中不是一个很好的解毒剂。相比之下，DTE的毒性低于BAL或DMSA，并且在提高PDA暴露细胞的细胞存活率方面具有上级优势。
British antilewisite (2,3-dimercaptopropanol; BAL) has long been used as an arsenic antidote, but its therapeutic efficacy is limited by its inherent toxicity. We synthesized two less toxic derivatives of BAL and investigated their potential as antidotes to organic arsenic. The new compounds, 2,3-dithioerythritol (DTE) and 2,2-dimethyl-4-(hydroxymethyl)-1,3-dithiolane (isopropylidene derivative of BAL), react readily with phenyldichloroarsine (PDA) to yield the expected corresponding cyclic 1,3-dithioarsolanes. The BAL derivatives were compared to BAL in terms of their cytotoxicity and their ability to rescue PDA-poisoned mouse lymphoma cells in culture. The dithiolane was not a good antidote in the cultured cell system. In contrast, DTE was less toxic than BAL or DMSA and was superior at improving cell survival in PDA-exposed cells.