Chopra D P, Wilkoff L J
J Natl Cancer Inst. 1977 Apr;58(4):923-30. doi: 10.1093/jnci/58.4.923.
The antihyperplastic activity of beta-retinoic acid (RA) and nine synthetic analogues (retinoids) was examined in organ cultures of mouse prostate made hyperplastic by treatment with N-methyl-N'-nitro-N-nitrosoguanidine (MNNG). After 8 or 10 days, when most explants developed hyperplasia, the carcinogen was withdrawn and explants were incubated in control medium and medium containing different concentrations of a retinoid. The antimitotic activity of retinoids was compared with that of RA. Different retinoids produced variable degrees of mitotic inhibition in the hyperplastic prostate epithelium. The methylketo cyclopentenyl and 1-methoxyethyl cyclopentenyl analogues of RA were at least 50-fold more active than RA in reversing MNNG-induced hyperplasia. The trimethylmethoxyphenyl analogue of RA and retinyl methyl ether were significantly more active than RA. Three analogues, N-acetyiretinylamine, retinal acetyl hydrazone, and retinal oxime, were as active as RA. The chlorotrimethylphenyl analogue showed less activity than RA, and alpha-retinyl acetate was completely devoid of mitotic inhibitory activity.
在经N-甲基-N'-硝基-N-亚硝基胍（MNNG）处理而发生增生的小鼠前列腺器官培养物中，检测了β-视黄酸（RA）及九种合成类似物（类视黄醇）的抗增生活性。8或10天后，当大多数外植体出现增生时，撤去致癌物，将外植体在对照培养基及含有不同浓度类视黄醇的培养基中培养。将类视黄醇的抗有丝分裂活性与RA的抗有丝分裂活性进行比较。不同的类视黄醇在增生的前列腺上皮中产生了不同程度的有丝分裂抑制。RA的甲基酮环戊烯基和1-甲氧基乙基环戊烯基类似物在逆转MNNG诱导的增生方面比RA至少活跃50倍。RA的三甲基甲氧基苯基类似物和视黄基甲基醚比RA的活性显著更高。三种类似物，N-乙酰视黄基胺、视黄醛乙酰腙和视黄醛肟，与RA的活性相当。氯代三甲基苯基类似物的活性低于RA，而α-视黄醇乙酸酯完全没有有丝分裂抑制活性。
