Department of Chemical Biology, Susan Lehman Cullman Laboratory for Cancer Research, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854-8020, USA.
Carcinogenesis. 2011 Feb;32(2):233-9. doi: 10.1093/carcin/bgq235. Epub 2010 Nov 15.
2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), the most abundant heterocyclic amine produced during the cooking of meats and fish, is suspected to be a human carcinogen. Metabolic activation of PhIP is primarily mediated by the enzyme cytochrome P450 (CYP) 1A2. Metabolism of PhIP by CYP1A2 differs considerably between humans and rodents, with more N(2)-hydroxylation (activation) and less 4'-hydroxylation (detoxication) in humans. Transgenic CYP1A-humanized mice (hCYP1A-mice), which have the human CYP1A1 and CYP1A2 genes but lack the murine orthologs Cyp1a1 and Cyp1a2, provide an excellent opportunity to develop a relevant model to study dietary-induced colon carcinogenesis. The treatment with 200 mg/kg PhIP by oral gavage, followed by 1.5% dextran sodium sulfate (DSS) in the drinking water for 7 days, was found to be an effective combination to induce colon carcinogenesis in hCYP1A-mice. Tumor multiplicity at week 6 was calculated to be 3.75 ± 0.70 and for week 10 was 3.90 ± 0.61 with 80-95% of the tumors being adenocarcinomas. No tumors were found in the similarly treated wild-type mice. Western blots revealed overexpression of β-catenin, c-Myc, cyclin D1, inducible nitric oxide synthase and cyclooxygenase-2 in colon tumor samples. Strong nuclear localization of β-catenin was observed in tumors. These results illustrate that PhIP and DSS combination produces rapid colon carcinogenesis in hCYP1A-mice and this is an effective model to mimic human colon carcinogenesis.
2-氨基-1-甲基-6-苯基咪唑并[4,5-b]吡啶(PhIP)是在烹饪肉类和鱼类过程中产生的最丰富的杂环胺,被怀疑是人类的致癌物质。PhIP 的代谢激活主要由细胞色素 P450(CYP)1A2 酶介导。PhIP 被 CYP1A2 代谢在人类和啮齿动物之间有很大的不同,人类的 N(2)-羟化(激活)较多,而 4'-羟化(解毒)较少。具有人类 CYP1A1 和 CYP1A2 基因但缺乏鼠同源物 Cyp1a1 和 Cyp1a2 的转基因 CYP1A-人源化小鼠(hCYP1A-小鼠)为研究饮食诱导的结肠癌发生提供了一个很好的机会。通过口服灌胃给予 200mg/kg PhIP,随后在饮用水中添加 1.5%葡聚糖硫酸钠(DSS)持续 7 天,被发现是诱导 hCYP1A-小鼠结肠癌发生的有效组合。第 6 周的肿瘤多发性计算为 3.75±0.70,第 10 周为 3.90±0.61,其中 80-95%的肿瘤为腺癌。在接受类似处理的野生型小鼠中未发现肿瘤。Western blot 显示β-连环蛋白、c-Myc、细胞周期蛋白 D1、诱导型一氧化氮合酶和环氧化酶-2在结肠肿瘤样本中过表达。β-连环蛋白在肿瘤中观察到强烈的核定位。这些结果表明,PhIP 和 DSS 联合在 hCYP1A-小鼠中快速产生结肠癌,这是模拟人类结肠癌发生的有效模型。