The biological significance of glycyrrhizin- and glycyrrhetinic acid derivative-induced selective phosphorylation of histones H2A and H2B by A-kinase in vitro.
Histones H2A and H2B were found to be glycyrrhizin (GL)-binding proteins, because (i) the two histones H2A-H2B pairs were isolated selectively from the crude histone preparations of calf thymus by means of GL-affinity column chromatography (HPLC); (ii) phosphorylation of these two histones by A-kinase was remarkably stimulated by native GL or oGA (a derivative of glycyrrhetinic acid) at 20 microM; and (iii) in the crude histone preparations of calf thymus, these two histones were selectively phosphorylated by A-kinase in the presence of both dsDNA and 20 microM oGA or 20 microM GL. The provided data suggest that the GL-induced selective phosphorylation of histones H2A and H2B by A-kinase may be implicated in the transcriptional activation involved in the biological activities of the drug.
Shamsa
F
F
Department of Bioscience, Kitasato University School of Hygienic Sciences, Sagamihara, Japan.
Iwasa
T
T
Saito
H
H
Nagata
N
N
Ohtsuki
K
K
D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology; D002286:Carcinoma, Ehrlich Tumor / Q000201:enzymology; D002417:Cattle; D002846:Chromatography, Affinity; D004247:DNA / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004591:Electrophoresis, Polyacrylamide Gel; D006034:Glycyrrhetinic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D006657:Histones / Q000302:isolation & purification / Q000378:metabolism*; D010766:Phosphorylation / Q000187:drug effects; D011485:Protein Binding; D011494:Protein Kinases / Q000494:pharmacology*; D013950:Thymus Gland / Q000737:chemistry; D014407:Tumor Cells, Cultured
D000890:Anti-Infective Agents; D006657:Histones; D004247:DNA; D011494:Protein Kinases; D006034:Glycyrrhetinic Acid