Differentiation-inducing activity of retinoic acid isomers and their oxidized analogs on human promyelocytic leukemia HL-60 cells.
Retinoidal activity of retinoic acid isomers [all-trans-retinoic acid (ATRA), 9-cis-retinoic acid (9CRA) and 13-cis-retinoic acid (13CRA)] and their oxidized derivatives [19-hydroxy and 19-oxo derivatives of ATRA (19-hydroxy-ATRA and 19-oxo-ATRA), 19-oxo derivative of 9CRA (19-oxo-9CRA), and 19-hydroxy derivative of 13CRA (19-hydroxy-13CRA)] was evaluated by means of a human promyelocytic leukemia HL-60 cell differentiation induction assay. All the compounds examined showed this activity with ED50 values of 2-30 nM, which are in accordance with their binding activity to nuclear retinoic acid receptors (RARs).
Matsushima
Y
Y
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Kawachi
E
E
Tanaka
H
H
Kagechika
H
H
Hashimoto
Y
Y
Shudo
K
K
D001667:Binding, Competitive; D002352:Carrier Proteins / Q000378:metabolism; D002454:Cell Differentiation / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007536:Isomerism; D015473:Leukemia, Promyelocytic, Acute; D015394:Molecular Structure; D010084:Oxidation-Reduction; D018168:Receptors, Retinoic Acid; D013329:Structure-Activity Relationship; D014212:Tretinoin / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D002352:Carrier Proteins; D018168:Receptors, Retinoic Acid; D014212:Tretinoin