Slaga T J, Viaje A, Bracken W M, Berry D L, Fischer S M, Miller D R, Leclerc S M
Cancer Lett. 1977 Jul;3(1-2):23-30. doi: 10.1016/s0304-3835(77)93845-9.
The skin-tumor-initiating abilities of various metabolites of benzo(a)pyrene (BP) were determined in mice by using a two-stage system of tumorigenesis. We previously reported that BP-7,8-dihydrodiol (+/- trans) was approximately as potent as BP, suggesting that it may be a proximate carcinogen, but the alleged ultimate carcinogen of BP [BP-7,8-dihydrodiol-9,10-epoxide (anti)] was a weak tumor initiator (Cancer Lett.2: 115, 1976). Because of its high reactivity, the tumor-initiating ability of the BP-7,8-dihydrodiol-9,10-epoxide (anti) was determined by using acetone, benzene, and tetrahydrofuran (THF) as the solvent vehicles. The 'diol-epoxide' of BP was found to be an effective tumor initiator when applied topically in THF. The effectiveness of the various vehicles for the 'diol-epoxide' was as follows: THF greater than benzene greater than acetone; however, acetone was the best solvent for BP tumor initiation. The BP-9,10-dihydrodiol and BP-3-hydroxy were found to be weak tumor initiators. BP-3-hydroxy was also tested for tumor-promoting ability and was found to be inactive in this capacity.
通过使用两阶段肿瘤发生系统，在小鼠中测定了苯并(a)芘（BP）各种代谢产物的皮肤肿瘤起始能力。我们之前报道过，BP - 7,8 - 二氢二醇（±反式）的效力与BP大致相当，这表明它可能是一种直接致癌物，但所谓的BP终极致癌物[BP - 7,8 - 二氢二醇 - 9,10 - 环氧化物（反式）]却是一种弱肿瘤起始剂（《癌症快报》2: 115, 1976）。由于其高反应活性，BP - 7,8 - 二氢二醇 - 9,10 - 环氧化物（反式）的肿瘤起始能力是通过使用丙酮、苯和四氢呋喃（THF）作为溶剂载体来测定的。当以THF局部给药时，发现BP的“二醇环氧化物”是一种有效的肿瘤起始剂。“二醇环氧化物”的各种载体的有效性如下：THF＞苯＞丙酮；然而，丙酮是BP肿瘤起始的最佳溶剂。发现BP - 9,10 - 二氢二醇和BP - 3 - 羟基是弱肿瘤起始剂。还测试了BP - 3 - 羟基的促肿瘤能力，发现其在此方面无活性。
