Dawson M I, Chao W R
Life Sciences Division, SRI International, Menlo Park, CA 94025.
Cancer Lett. 1988 May;40(1):7-12. doi: 10.1016/0304-3835(88)90256-x.
Linear regression analysis of the dose levels of retinoids required to inhibit the formation of papillomas by 50% in mouse dorsal epidermis topically treated with 7,12-dimethylbenz[a]anthracene (DMBA) (200 nmol) and then promoted 2 weeks later with twice-weekly applications of 12-O-tetradecanoylphorbol-13-acetate (TPA) (8.5 nmol) indicated that there was a good correlation (r = 0.9095, P less than 0.02) between retinoid inhibitory activities in the CD-1 mouse at 20 weeks after the start of promotion and in the Sencar mouse after 12 weeks of promotion. The ID50 values (nmol) determined were as follows: all-trans-retinoic acid (RA) (3.5, CD-1; 17, Sencar); 4-[2-(5,6,7,8-tetrahydro-5,5,8,8- tetramethyl-2-naphthalenyl)-1E-propen-1-yl]benzoic acid (0.14, CD-1; 0.71, Sencar); 4-[1-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl- 2-naphthalenyl)- 1E-propen-2-yl]benzoic acid (0.54, CD-1; 1.9, Sencar); 6-[1-(4-carboxyphenyl)-1E-propen-2-yl]- 3,4- dihydro-4,4-dimethyl-2H-1-benzothiopyran (3.0 CD-1; 11, Sencar); 7-[1-(4-carboxyphenyl)-1E-propen-2-yl)- 3,4-dihydro- 4,4-dimethyl-2H-1-benzothiopyran (1.5, CD-1; 0.4, Sencar); 2-[1-(4-carboxyphenyl)-1E-propen-2-yl]- 4,5,6,7-tetrahydro-4,4- dimethyl-benzo[b]thiophene (0.30, CD-1; 2.3, Sencar).
对用7,12-二甲基苯并[a]蒽（DMBA，200纳摩尔）局部处理小鼠背部表皮，然后在2周后用12-O-十四烷酰佛波醇-13-乙酸酯（TPA，8.5纳摩尔）每周两次促进处理后，抑制乳头状瘤形成50%所需维甲酸剂量水平进行线性回归分析表明，在促进开始后20周的CD-1小鼠和促进12周后的Sencar小鼠中，维甲酸抑制活性之间存在良好相关性（r = 0.9095，P小于0.02）。所确定的半数抑制剂量（ID50）值（纳摩尔）如下：全反式维甲酸（RA）（CD-1小鼠为3.5；Sencar小鼠为17）；4-[2-(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)-1E-丙烯-1-基]苯甲酸（CD-1小鼠为0.14；Sencar小鼠为0.71）；4-[1-(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)-1E-丙烯-2-基]苯甲酸（CD-1小鼠为0.54；Sencar小鼠为1.9）；6-[1-(4-羧基苯基)-1E-丙烯-2-基]-3,4-二氢-4,4-二甲基-2H-1-苯并噻喃（CD-1小鼠为3.0；Sencar小鼠为11）；7-[1-(4-羧基苯基)-1E-丙烯-2-基]-3,4-二氢-4,4-二甲基-2H-1-苯并噻喃（CD-1小鼠为1.5；Sencar小鼠为0.4）；2-[1-(4-羧基苯基)-1E-丙烯-2-基]-4,5,6,7-四氢-4,4-二甲基-苯并[b]噻吩（CD-1小鼠为0.30；Sencar小鼠为2.3）。
