Tissue distribution on a novel derivate of all-trans-retinoic acid,ATPR / 中国药理学通报

ABSTRACT

Aim To develop a sensitive,specific and accurate method for quantifying a novel derivate of all-trans-retinoic acid, 4-amino-2-trifluoromethyl-phenyl retinate (ATPR)in rat tissues to investigate the tissue distribution of ATPR in rats.Methods Sprague-Daw-ley (SD)rats were killed by exsanguination at 2,4,7 h after a single intragastric administration with one dose of ATPR (20 mg·kg-1 )or at 5 min,1 h,5 h after a single intravenous administration with one dose of AT-PR (7 mg·kg-1 ).The concentration of ATPR in the tissues was determined by high performance liquid chromatography (HPLC)method.Results After the rats were administrated intragastrically, the highest concentration of ATPR was observed in intestine,fol-lowed by liver,spleen and lung,while the distribution in heart,kidney,fat and brain was very little.Howev-er,the highest concentration of ATPR was in liver after given intravenously,followed by spleen and lung,and very low in heart,kidney,intestines,fat and brain. Conclusion The distribution of ATPR is higher in liv-er after administrated both intragastrically and intrave-nously,suggesting the potential anti-proliferation and differentiation inducing effects of ATPR targeting at liv-er cancer.