Inhibition of the specific binding of 12-O-tetradecanoylphorbol-13-acetate to mouse epidermal membrane fractions by glycyrrhetic acid.
Glycyrrhetic acid inhibited the specific binding of 12-O-tetradecanoylphorbol-13-acetate (TPA) to mouse epidermal membrane fractions in a dose- and time-dependent manner. Glycyrrhizic acid, a glycoside of glycyrrhetic acid, has no inhibitory effect on TPA binding. The results of kinetic analysis suggested that glycyrrhetic acid directly binds to the TPA receptor, resulting in the competitive inhibition of the binding of TPA to its receptor without affecting the number of binding sites (Ki = 2.2 X 10(-4) M). The inhibitory effect of glycyrrhetic acid on TPA binding to the membrane receptor may play a role in its antitumor-promoting activity in vivo.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D029742:Caenorhabditis elegans Proteins; D002352:Carrier Proteins; D004305:Dose-Response Relationship, Drug; D004817:Epidermis / Q000378:metabolism*; D005260:Female; D006034:Glycyrrhetinic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D019695:Glycyrrhizic Acid; D008566:Membranes / Q000378:metabolism; D051379:Mice; D008813:Mice, Inbred ICR; D010704:Phorbols / Q000037:antagonists & inhibitors*; D011493:Protein Kinase C; D011955:Receptors, Drug; D011971:Receptors, Immunologic / Q000187:drug effects; D013755:Tetradecanoylphorbol Acetate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013997:Time Factors
D029742:Caenorhabditis elegans Proteins; D002352:Carrier Proteins; D010704:Phorbols; D011955:Receptors, Drug; D011971:Receptors, Immunologic; C083141:phorbol ester binding protein; C027776:phorbol ester receptor; D019695:Glycyrrhizic Acid; D011493:Protein Kinase C; D013755:Tetradecanoylphorbol Acetate; D006034:Glycyrrhetinic Acid