Slaga T J, Bracken W M, Viaje A, Berry D L, Fischer S M, Miller D R
J Natl Cancer Inst. 1978 Aug;61(2):451-5.
The skin tumor-initiating activities of benzo[a]pyrene (BP), 6-hydroxymethylbenzo[a]pyrene (6-OH-CH2-BP), and 6-methylbenzo[a]pyrene (6-CH3-BP), as well as the effects of 7,8-benzoflavone (7,8-BF), quercetin, and 1-benzylimidazole on their activity, were determined in outbred female CD-1 mice by use of a two stage system of tumorigenesis. The skin tumor-initiating activity of 6-OH-CH2-BP and 6-CH3-BP was 12.5 and 20%, respectively, of the activity of BP, 7,8-BF had little effect on the skin tumor-initiating activity of 6-OH-CH2-BP and 6-CH3-BP. However, a dose-dependent inhibition of BP tumorigenesis by 7,8-BF was noted. Quercetin and 1-benzylimidazole also inhibited BP skin tumor-initiating activity. These findings indicated that direct hydroxymethylation of BP is not an important pathway in the activation of BP in mouse skin tumor initiation.
通过肿瘤发生的两阶段系统，在远交系雌性CD-1小鼠中测定了苯并[a]芘（BP）、6-羟甲基苯并[a]芘（6-OH-CH2-BP）和6-甲基苯并[a]芘（6-CH3-BP）的皮肤肿瘤起始活性，以及7,8-苯并黄酮（7,8-BF）、槲皮素和1-苄基咪唑对它们活性的影响。6-OH-CH2-BP和6-CH3-BP的皮肤肿瘤起始活性分别为BP活性的12.5%和20%，7,8-BF对6-OH-CH2-BP和6-CH3-BP的皮肤肿瘤起始活性影响很小。然而，注意到7,8-BF对BP肿瘤发生有剂量依赖性抑制作用。槲皮素和1-苄基咪唑也抑制BP的皮肤肿瘤起始活性。这些发现表明，BP的直接羟甲基化在小鼠皮肤肿瘤起始中BP的活化不是一个重要途径。
