Furihata C, Yamakoshi A, Matsushima T, Kato T, Kikugawa K
Department of Molecular Oncology, University of Tokyo, Japan.
Mutagenesis. 1988 Jul;3(4):299-301. doi: 10.1093/mutage/3.4.299.
3-Diazo-N-nitrosobamethan (DNB), a mutagen produced by nitrite treatment of bamethan, a cardiovascular drug, induced unscheduled DNA synthesis in the pyloric mucosa of the stomach of male F344 rats 2 h after its administration by gastric tube at doses of 75 to 225 mg/kg body wt. DNB at a dose of 225 mg/kg body wt induced up to a 13-fold increase in replicative DNA synthesis with a maximum at 16 h after its administration. Moreover at doses of 75 to 225 mg/kg body wt, it induced up to a 12-fold increase in ornithine decarboxylase activity with a maximum after 16 h. The present results suggest that DNB has possible tumour-initiating and -promoting activities in the pyloric mucosa of the rat stomach. However, the possible risks to patients posed by clinical use of bamethan cannot be evaluated until further work is completed.
3-重氮-N-亚硝基巴美生(DNB)是一种由心血管药物巴美生经亚硝酸盐处理产生的诱变剂。以75至225毫克/千克体重的剂量通过胃管给雄性F344大鼠给药2小时后,DNB可诱导大鼠胃幽门黏膜中出现非预定DNA合成。以225毫克/千克体重的剂量给药时,DNB可使复制性DNA合成增加多达13倍,在给药后16小时达到最大值。此外,在75至225毫克/千克体重的剂量下,它可使鸟氨酸脱羧酶活性增加多达12倍,在16小时后达到最大值。目前的结果表明,DNB在大鼠胃幽门黏膜中可能具有肿瘤启动和促进活性。然而,在完成进一步研究之前,无法评估临床使用巴美生对患者可能造成的风险。