新型维甲酸衍生物ATPR大鼠体内组织分布的研究

发布时间：2018-04-03 16:41

本文选题：-氨基--三氟甲基苯基维甲酸酯　切入点：新型维甲酸衍生物　出处：《中国药理学通报》2014年07期

【摘要】：目的建立大鼠组织中新型维甲酸衍生物4-氨基-2-三氟甲基苯基维甲酸酯(ATPR)浓度的测定方法,并研究其在大鼠体内的组织分布。方法 SD大鼠灌胃给药ATPR(20mg·kg-1)和静脉注射给药ATPR(7 mg·kg-1)后,分别于给药后2、4、7 h和5 min、1、5 h取各脏器组织,经预处理,HPLC法测定各组织中ATPR浓度。结果大鼠灌胃ATPR后,肠组织中药物浓度最高,其次在肝、脾、肺组织浓度较高,在心、肾、脂肪和脑组织中浓度较低。静注给ATPR后,肝组织中药物浓度最高,其次在脾、肺组织浓度较高,在心、肾、肠、脂肪和脑组织中浓度较低。结论两种给药途径给药ATPR后,肝组织的药物浓度均较高,提示ATPR在诱导肝癌细胞分化和抗癌细胞增殖方面可能会有较好的靶向作用。
[Abstract]:Aim to establish a method for the determination of ATPRA, a new type of retinoic acid derivative, in rat tissues, and to study its tissue distribution in rats.Methods Sprague-Dawley rats were given ATPR(20mg kg-1 (iv) and ATPR(7 (mg kg-1) intravenously. The tissue samples were taken at 2h and 5min respectively. The concentration of ATPR in each tissue was determined by pretreatment.Results after intragastric administration of ATPR, the concentration of drug in intestinal tissue was the highest, followed by higher concentration in liver, spleen and lung, and lower concentration in heart, kidney, fat and brain.After intravenous injection of ATPR, the concentration of drug was highest in liver tissue, followed by higher concentration in spleen and lung, and lower concentration in heart, kidney, intestine, fat and brain.Conclusion the concentration of ATPR in liver tissue was higher after administration of ATPR, suggesting that ATPR might have a good targeting effect on inducing the differentiation of hepatoma cells and proliferation of anticancer cells.
【作者单位】：安徽医科大学药学院;
【基金】：国家科技部“重大新药创制”科技重大专项(No2011ZX09401)
【分类号】：R-332;R969.1

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