Hardej Diane, Billack Blase
Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St John's University, Queens, NY 11439, USA.
Toxicol Ind Health. 2007 May;23(4):209-21. doi: 10.1177/0748233707083541.
Nitrogen mustards are vesicants capable of burning the skin, eyes and respiratory tract of exposed individuals. While generally less toxic than sulfur mustards, these compounds have the potential for use as chemical warfare agents. Presently, no antidote exists for treatment against nitrogen mustard toxicity. The purpose of this study was to investigate the in vitro toxicity of the nitrogen mustard mechlorethamine (HN2) in four cell models: CEM-SS human T cells, A431 human skin epithelial cells, rat hippocampal astrocytes and rat pleural mesothelial cells. Furthermore, the efficacy of the synthetic seleno-organic compound ebselen (Eb) (2-phenyl-1,2- benzisoselenazol-3(2H)-one) as a cytoprotective agent against such toxicity was evaluated. Significant increases in cell viability, as assessed using an MTT assay for viability, was demonstrated when 30 microM Eb was used as a cotreatment with HN2 in all cell models tested at the following doses of HN2: A431 skin cells,10-40 microM; rat astrocytes, 20 and 40 microM; rat mesothelia, 10-40 microM; and human T cells 4-16 microM. Decreases in cell viability and toxicity to HN2 were confirmed using light and scanning electron microscopy. Membrane damage, observed with HN2 exposure, such as blebbing and loss of cell projections, was ameliorated with Eb cotreatment. Our results demonstrate a generalized protective effect observed with Eb cotreatment that suggests that this agent may have potential as an antidote for HN2 exposure and toxicity.
氮芥是一种能够灼伤暴露个体皮肤、眼睛和呼吸道的发泡剂。虽然这些化合物的毒性通常比硫芥低,但它们有被用作化学战剂的可能性。目前,尚无针对氮芥中毒的解毒剂。本研究的目的是在四种细胞模型中研究氮芥氮芥(HN2)的体外毒性:CEM-SS人T细胞、A431人皮肤上皮细胞、大鼠海马星形胶质细胞和大鼠胸膜间皮细胞。此外,还评估了合成的有机硒化合物依布硒啉(Eb)(2-苯基-1,2-苯并异硒唑-3(2H)-酮)作为针对此类毒性的细胞保护剂的功效。当在以下剂量的HN2下测试的所有细胞模型中,将30 microM的Eb与HN2联合使用时,使用MTT活力测定法评估的细胞活力显著增加:A431皮肤细胞,10-40 microM;大鼠星形胶质细胞,20和40 microM;大鼠间皮细胞,10-40 microM;人T细胞4-16 microM。使用光学显微镜和扫描电子显微镜证实了细胞活力的降低和对HN2的毒性。用HN2暴露观察到的膜损伤,如起泡和细胞突起的丧失,通过Eb联合处理得到改善。我们的结果表明,Eb联合处理具有普遍的保护作用,这表明该药物可能具有作为HN2暴露和毒性解毒剂的潜力。