新维生素甲酸衍生物抑制小鼠前胃鳞状上皮癌变的研究
INHIBITORY EFFECT OF SOME NEW RETINOIDS ON CARCINOGENESIS
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摘要: 本文报道9种维生素甲酸衍生物对小鼠前胃上皮癌变的影响,其中有抑制作用的有:RⅠ、RⅡ、RⅢ、RⅥ及RⅧ,尤以RⅠN-(4-乙氧羰基苯基)维甲酰胺N-(4-Ethoxycarbophenyl)Retinamide抑制上皮癌变作用明显,并可重复,文献上未见报道。RⅠ在治疗剂量下(1.1×10-4M/kg)未出现毒性,六倍于治疗剂量,亦未见高维生素甲症,而相应剂量的维甲酸,引起明显的高维生素甲症,RⅠ毒性远较维甲酸小。用氚—胸腺嘧啶核苷放射自显影方法,观察到RⅡ对小鼠前胃上皮细胞DNA合成有明显的抑制作用。Abstract: Effects of nine retinoids on carinogenesis of the forestomach in mice were studied. RⅠ, RⅡ, RⅢ, RⅥ, and RⅧ showed significaut inhibitory effect. RⅠN-(4-ethoxycarbophenyl) Retinanide appeared to be the most effective, reproducible and has not been reported in the literature. No toxic effect was observed with therapeutic dose of RⅠ, and no sign of hypervitaminosis A was noticed with dosage as high as 6 times the therapeutic dose. However hypervitamnosis A was induced with retinoic acid at the some dose. The toxiciity of RⅡ appeared to the much less than that of retinoic acid.Autoradiography using H3-thymidine showed marked inhibitory effect of RⅡ on DNA synthesis in the forestomach epithelium of mice.
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