Chemically induced isomerization and differential uptake modulate retinoic acid disposition in HL-60 cells
作者： C. Lanvers , G. Hempel , G. Blaschke , J. Boos
DOI: 10.1096/FASEBJ.12.15.1627
关键词: Isomerization 、 Incubation 、 Cell culture 、 Retinoic acid 、 Retinoid X receptor 、 Chemistry 、 Biochemistry 、 In vitro 、 Receptor 、 Retinoic acid receptor
摘要: The successful introduction of 13-cis-retinoic acid (13-cis-RA) and all-trans-retinoic (all-trans-RA) in the chemoprevention treatment cancer along with discovery different retinoic receptors transactivated by isomers resulted a number vitro studies antitumor effects single isomers. Since formation receptor affinities might modulate response vitro, we determined disposition HL-60 cells cell culture medium during incubation 13-cis-, 9-cis-, all-trans-RA. In medium, acids underwent thiol-radical mediated isomerization resulting mixture 9,13-di-cis-, Except for 9,13-di-cis-RA, all generated were also detected cells. Whereas 9-cis-RA 13-cis-RA showed similar cellular pharmacokinetics, all-trans-RA reached about fourfold higher concentrations ce...
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