Differentiation-inducing activity of retinoic acid isomers and their oxidized analogs on human promyelocytic leukemia HL-60 cells

Y Matsushima; E Kawachi; H Tanaka; H Kagechika; Y Hashimoto; K Shudo

doi:10.1016/0006-291x(92)92322-o

Differentiation-inducing activity of retinoic acid isomers and their oxidized analogs on human promyelocytic leukemia HL-60 cells

Biochem Biophys Res Commun. 1992 Dec 15;189(2):1136-42. doi: 10.1016/0006-291x(92)92322-o.

Authors

Y Matsushima¹, E Kawachi, H Tanaka, H Kagechika, Y Hashimoto, K Shudo

Affiliation

¹ Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

PMID: 1335240
DOI: 10.1016/0006-291x(92)92322-o

Abstract

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).

MeSH terms

Binding, Competitive
Carrier Proteins / metabolism
Cell Differentiation / drug effects*
Dose-Response Relationship, Drug
Humans
Isomerism
Leukemia, Promyelocytic, Acute
Molecular Structure
Oxidation-Reduction
Receptors, Retinoic Acid
Structure-Activity Relationship
Tretinoin / analogs & derivatives*
Tretinoin / metabolism
Tretinoin / pharmacology*
Tumor Cells, Cultured

Substances

Carrier Proteins
Receptors, Retinoic Acid
Tretinoin