Levinson W, Mikelens P, Oppermann H, Jackson J
Biochim Biophys Acta. 1978 Jun 22;519(1):65-75. doi: 10.1016/0005-2787(78)90062-x.
Antabuse (disulfiram) is widely used in the treatment of chronic alcoholism. We have examined the effect of this drug on malignant transformation by Rous sarcoma virus, on eukaryotic cell synthesis, and on nucleic acid binding. It was found that: (1) Disulfiram inhibits the activity of the RNA dependent DNA polymerase of Rous sarcoma virus and inactivates the ability of the virus to malignantly transform chick embryo cells. The monomer of disulfiram, diethyldithiocarbamate does not affect the virus. (2) Disulfiram induced the synthesis of four proteins in normal chick embryo and human foreskin cells. The monomer diethyldithiocarbamate, induced these proteins also. Cellular DNA synthesis is more sensitive to disulfiram than are RNA and protein synthesis. (3) Disulfiram binds to neither DNA or RNA in the presence or absence of copper. However, diethyldithiocarbamate in the presence of, but not in the absence of, copper binds to HeLa cell DNA and to Rous sarcoma virus 70 S genome RNA. These results indicate that this compound, which causes no symptoms in people who do not consume alcohol, may have significant effects on a cellular level.
安塔布司(双硫仑)广泛用于治疗慢性酒精中毒。我们研究了这种药物对劳斯肉瘤病毒致恶性转化、对真核细胞合成以及对核酸结合的影响。结果发现:(1)双硫仑抑制劳斯肉瘤病毒的依赖RNA的DNA聚合酶活性,并使该病毒恶性转化鸡胚细胞的能力失活。双硫仑的单体二乙二硫代氨基甲酸盐对病毒无影响。(2)双硫仑在正常鸡胚细胞和人包皮细胞中诱导合成四种蛋白质。单体二乙二硫代氨基甲酸盐也诱导这些蛋白质的合成。细胞DNA合成比RNA和蛋白质合成对双硫仑更敏感。(3)无论有无铜存在,双硫仑都不与DNA或RNA结合。然而,二乙二硫代氨基甲酸盐在有铜存在时(但无铜时不)与HeLa细胞DNA和劳斯肉瘤病毒70S基因组RNA结合。这些结果表明,这种在不饮酒者中不产生症状的化合物,可能在细胞水平上有显著影响。