Gurtoo H L, Koser P L, Bansal S K, Fox H W, Sharma S D, Mulhern A I, Pavelic Z P
Carcinogenesis. 1985 May;6(5):675-8. doi: 10.1093/carcin/6.5.675.
Effects of beta-naphthoflavone (beta NF) on the activity of hepatic microsomal aflatoxin B1 (AFB1)-4-hydroxylase - the cytochrome P-450-dependent enzyme system which catalyzes the metabolism of AFB1 to AFM1 - and on AFB1-induced in vivo hepatocarcinogenesis were investigated in weanling male Fischer rats. A single i.p. injection of beta NF in doses of 20 mg/kg and 150 mg/kg induced AFB1-4-hydroxylase 3- and 4-fold, respectively, 48 h post injection. Feeding of diet containing 0.01% beta NF for a period of 9-weeks induced AFB1-4-hydroxylase approximately 2-fold. AFB1, given by intubation in a dose of 25 micrograms five times/week for 8 weeks, produced 42 weeks later a 100% incidence of liver lesions (neoplastic foci, nodules or tumors), but feeding beta-NF in diet at a concentration of 0.015% for one week prior to and during the 8 weeks of AFB1 treatment inhibited AFB1 hepatocarcinogenesis by approximately 75%. These results are in accord with the suggestion that AFB1-4-hydroxylase induction may be associated with the inhibition of AFB1 carcinogenesis, possibly occurring as a consequence of accelerated detoxification of AFB1 via its conversion to AFM1.
在断乳雄性Fischer大鼠中研究了β-萘黄酮（β-NF）对肝微粒体黄曲霉毒素B1（AFB1）-4-羟化酶（一种催化AFB1代谢为AFM1的细胞色素P-450依赖性酶系统）活性以及对AFB1诱导的体内肝癌发生的影响。单次腹腔注射剂量为20mg/kg和150mg/kg的β-NF，在注射后48小时分别诱导AFB1-4-羟化酶活性增加3倍和4倍。喂食含0.01%β-NF的饲料9周，诱导AFB1-4-羟化酶活性增加约2倍。以每周5次、每次25微克的剂量经插管给予AFB1，持续8周，42周后肝脏病变（肿瘤灶、结节或肿瘤）的发生率为100%，但在AFB1治疗的8周期间及之前1周，喂食浓度为0.015%的β-NF饮食可使AFB1诱导的肝癌发生抑制约75%。这些结果与以下观点一致，即诱导AFB1-4-羟化酶可能与抑制AFB1致癌作用有关，这可能是由于AFB1通过转化为AFM1而加速解毒的结果。
