LaVoie E J, Amin S, Hecht S S, Furuya K, Hoffmann D
Carcinogenesis. 1982;3(1):49-52. doi: 10.1093/carcin/3.1.49.
The tumor initiating activities on mouse skin of benzo[b]fluoranthene, (B[b]F), benzo[j]fluoranthene (B[j]F), benzo[k]fluoranthene (B[k]F] and three of their dihydrodiols, 9,10-dihydro-9,10-dihydroxybenzo[b]fluoranthene (B[b]F-9,10-diol), 9,10-dihydro-9,10-dihydroxybenzo[j]fluoranthene (B[j]F-9,10-diol), and 8,9-dihydro-8,9-dihydroxybenzo[k]fluoranthene (B[k]F-8,9-diol) were evaluated. Among the parent hydrocarbons, B[b]F was the most potent tumor initiator, with activity greater than that of B[j]F but less than that of benzo[a]pyrene. B[k]F also showed tumor initiating activity, in contrast to its lack of complete carcinogenic activity on mouse skin. B[b]F-9,10-diol, which can form a bay region dihydrodiol epoxide, was as active as B[b]F. B[j]F-9,10-diol, which would form its dihydrodiol epoxide in a four sided pseudo-bay region, was less active than B[j]F. B[k]F-8,9-diol was inactive. These results, together with parallel metabolic studies, suggest that the formation of bay region dihydrodiol epoxides may not be the major activation mechanism in benzofluoranthene tumorigenesis.
评估了苯并[b]荧蒽(B[b]F)、苯并[j]荧蒽(B[j]F)、苯并[k]荧蒽(B[k]F)及其三种二氢二醇,即9,10-二氢-9,10-二羟基苯并[b]荧蒽(B[b]F-9,10-二醇)、9,10-二氢-9,10-二羟基苯并[j]荧蒽(B[j]F-9,10-二醇)和8,9-二氢-8,9-二羟基苯并[k]荧蒽(B[k]F-8,9-二醇)对小鼠皮肤的肿瘤起始活性。在母体碳氢化合物中,B[b]F是最有效的肿瘤起始剂,其活性大于B[j]F但小于苯并[a]芘。与它在小鼠皮肤上缺乏完全致癌活性相反,B[k]F也表现出肿瘤起始活性。能形成湾区二氢二醇环氧化物的B[b]F-9,10-二醇与B[b]F活性相当。会在四面假湾区形成其二氢二醇环氧化物的B[j]F-9,10-二醇的活性低于B[j]F。B[k]F-8,9-二醇无活性。这些结果连同平行的代谢研究表明,湾区二氢二醇环氧化物的形成可能不是苯并荧蒽肿瘤发生中的主要活化机制。