Inhibitory effects of 5-(2-pyrazinyl)-4-methyl-1,2-dithiol-3-thione (Oltipraz) on carcinogenesis induced by benzo[a]pyrene, diethylnitrosamine and uracil mustard.
Inhibitory effects of 5-(2-pyrazinyl)-4-methyl-1,2-dithiol-3-thione (Oltipraz) on carcinogenesis induced by benzo[a]pyrene, diethylnitrosamine and uracil mustard.
复制标题
5-(2-吡嗪基)-4-甲基-1,2-二硫醇-3-硫酮 (Oltipraz) 对苯并[a]芘、二乙基亚硝胺和尿嘧啶芥子诱导的致癌作用具有抑制作用。
作者：
L. Wattenberg;Ernest Bueding
在雌性ICR/Ha小鼠中研究了5-（2-吡嗪基）-4-甲基-1，2-二巯基-3-丙硫基（奥替普拉）抑制致癌物诱导的肿瘤形成的能力。在苯并[a]芘（BP）给药前48小时经口插管给药（也经口插管给药），奥替普拉可抑制肺腺瘤和前胃肿瘤的发生。在接受奥替普拉的小鼠中发生的肿瘤数量与相应对照组的肿瘤数量之比为：肺0.36，前胃0.38。当口服给予奥替普拉时也发生抑制。BP前24小时在其他实验中，在p.o.给予二乙基亚硝胺或尿嘧啶氮芥抑制肺腺瘤形成，但程度低于BP作为致癌物。先前发现的低毒性的奥替普拉，加上对化学上不同的致癌物的保护作用的证据，表明这种化合物应进一步研究其可能用作肿瘤的化学预防剂。
5-(2-Pyrazinyl)-4-methyl-1,2-dithiol-3-thione (Oltipraz) was studied for its capacity to inhibit carcinogen-induced neoplasia in female ICR/Ha mice. When administered by oral intubation 48 h prior to benzo[a]pyrene (BP), also given by oral intubation, Oltipraz inhibited the occurrence of pulmonary adenomas and tumors of the forestomach. The ratio of the number of tumors occurring in the mice receiving Oltipraz to that of the corresponding controls was: lung, 0.36 and forestomach 0.38. Inhibition also occurred when Oltipraz was given p.o. 24 h prior to BP. In other experiments, oral administration of Oltipraz 48 h prior to p.o. administration of diethylnitrosamine or uracil mustard inhibited pulmonary adenoma formation but to a lesser extent than with BP as the carcinogen. The low toxicity of Oltipraz found previously, coupled with evidence of protective effects against chemically diverse carcinogens, suggests that this compound should be studied further for its possible use as an agent for the chemoprevention of neoplasia.