title: Possible mechanism of steroid action of the plant herb extracts glycyrrhizin, glycyrrhetinic acid, and paeoniflorin: inhibition by plant herb extracts of steroid protein binding in the rabbit.
abstract: To assess the action of some components of herbal medicine, glycyrrhizin, glycyrrhetinic acid, and paeoniflorin, on steroids, their binding to several classes of intracellular and serum steroid-binding proteins were studied in the rabbit. The affinity (inhibitor constant) for binding of dihydrotestosterone-sex hormone binding globulin in the serum (dissociation constant of 2.0 nmol/L for dihydrotestosterone) was approximately 520 nmol/L, and that for the binding of cortisol-corticosteroid-binding globulin in the serum (dissociation constant of 2.0 nmol/L for cortisol) was approximately 10 mumol/L. In the uterine cytosol, the inhibitor constant value for estradiol receptor binding (dissociation constant of 1.0 nmol/L) was 0.9 mumol/L, and these compounds did not influence progestin receptor binding (dissociation constant of 1.4 nmol/L). The inhibitor constant values for glucocorticoid receptor binding (dissociation constant of 1.0 nmol/L) in the liver cytosol were 3.0 nmol/L for paeoniflorin, 2.0 nmol/L for glycyrrhizin, and 1.7 nmol/L for glycyrrhetinic acid, and those for mineralocorticoid receptor binding (dissociation constant = 1.1 nmol/L) in the kidney cytosol were 3.5 nmol/L for paeoniflorin and glycyrrhetinic acid and 3.0 nmol/L for glycyrrhizin. These results suggest that herbal extracts such as the above compounds influence steroid effects by glucocorticoid and mineralocorticoid receptors and to a lesser extent by estrogen receptors or serum sex hormone-binding globulin and corticosteroid-binding globulin.
mesh_terms: D000818:Animals; D001565:Benzoates; D001667:Binding, Competitive; D001952:Bridged-Ring Compounds; D005260:Female; D005960:Glucosides / Q000378:metabolism*; D006027:Glycosides / Q000378:metabolism*; D006034:Glycyrrhetinic Acid / Q000031:analogs & derivatives* / Q000378:metabolism*; D019695:Glycyrrhizic Acid; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D039821:Monoterpenes; D011817:Rabbits; D011987:Receptors, Steroid / Q000378:metabolism*; D014599:Uterus / Q000378:metabolism
chemical_list: D001565:Benzoates; D001952:Bridged-Ring Compounds; D005960:Glucosides; D006027:Glycosides; D039821:Monoterpenes; D011987:Receptors, Steroid; C015423:peoniflorin; D019695:Glycyrrhizic Acid; D006034:Glycyrrhetinic Acid