Takahashi S, Nakae D, Yokose Y, Emi Y, Denda A, Mikami S, Ohnishi T, Konishi Y
Carcinogenesis. 1984 Jul;5(7):901-6. doi: 10.1093/carcin/5.7.901.
The effect of inhibitors of NAD+ ADP ribosyl transferase (ADPRT) on the early stage of liver carcinogenesis of diethylnitrosamine (DEN) was studied by estimating the number and size of gamma-glutamyltranspeptidase (gamma-GTP) positive foci assayed as markers of cell populations initiated by DEN in the rat liver. ADPRT inhibitors investigated were 3-aminobenzamide (ABA), 5-methylnicotinamide (MNAM), and thymidine. A single i.p. injection of ABA at greater than 150 mg/kg body weight (B.W.) enhanced dose-dependently the induction of gamma-GTP positive foci in rat liver initiated by 20 mg/kg B.W. of DEN. The magnitude of the effect was similar to that observed when partial hepatectomy (PH) was performed instead of ABA administration. Single i.p. injections of MNAM or thymidine at a dose of 600 mg/kg B.W. also enhanced the induction of foci in rat liver initiated by the 20 mg/kg dose of DEN. Based on the above results, ABA was used as a representative ADPRT inhibitor for clarifying the mechanisms underlying the effects. Administration of ABA at a dose of 600 mg/kg B.W. was effective in enhancing the induction of foci if given 1 day before DEN, simultaneously to DEN, and 1 day after DEN initiation but it was ineffective if it was given 3 days after DEN or thereafter. Liver cell necrosis was not detectable either by analysis of serum enzymes or histologically 1, 3, 5, 7 and 14 days after 20 mg/kg B.W. of DEN with or without administration of 600 mg/kg B.W. of ABA. No initiating activity was observed for ABA administered at doses of 600 and 1200 mg/kg B.W. as assayed by development of gamma-GTP positive foci. Long term ABA administration in the diet at concentrations of 0.05, 0.1 and 0.2% did not show any promoting activity for liver carcinogenesis initiated by DEN. Furthermore, chronic administration of 0.2% ABA in the diet did not result in detectable toxicity and/or carcinogenic effects. These results suggest that ADPRT and associated DNA repair plays an important role in the early initiating stage of liver carcinogenesis and provide the basis for a new experimental approach to the analysis of the mechanisms of chemical carcinogenesis and in establishing a more sensitive assay system for liver carcinogenesis in rats.
通过评估γ-谷氨酰转肽酶(γ-GTP)阳性灶的数量和大小,研究了NAD⁺ ADP核糖基转移酶(ADPRT)抑制剂对二乙基亚硝胺(DEN)诱导大鼠肝癌早期阶段的影响,γ-GTP阳性灶作为DEN启动的细胞群体标志物。所研究的ADPRT抑制剂为3-氨基苯甲酰胺(ABA)、5-甲基烟酰胺(MNAM)和胸腺嘧啶核苷。以大于150mg/kg体重(B.W.)单次腹腔注射ABA,剂量依赖性地增强了由20mg/kg B.W. DEN启动的大鼠肝脏中γ-GTP阳性灶的诱导。该效应的程度与进行部分肝切除术(PH)而非给予ABA时观察到的相似。以600mg/kg B.W.的剂量单次腹腔注射MNAM或胸腺嘧啶核苷也增强了由20mg/kg剂量DEN启动的大鼠肝脏中灶的诱导。基于上述结果,ABA被用作代表性的ADPRT抑制剂以阐明其作用的潜在机制。如果在DEN之前1天、与DEN同时或DEN启动后1天给予600mg/kg B.W.的ABA,对增强灶的诱导有效,但在DEN后3天或更晚给予则无效。在给予20mg/kg B.W. DEN(无论是否给予600mg/kg B.W.的ABA)后1、3、5、7和14天,通过血清酶分析或组织学检查均未检测到肝细胞坏死。以γ-GTP阳性灶的形成检测,在600和1200mg/kg B.W.剂量下给予的ABA未观察到启动活性。在饮食中以0.05%、0.1%和0.2%的浓度长期给予ABA对DEN启动的肝癌没有显示出任何促进活性。此外,在饮食中慢性给予0.2%的ABA未导致可检测到的毒性和/或致癌作用。这些结果表明ADPRT及相关的DNA修复在肝癌发生的早期启动阶段起重要作用,并为分析化学致癌机制以及建立更敏感的大鼠肝癌检测系统提供了新的实验方法基础。