Interaction of steroids with the transport system of glucose in human erythrocytes.
Steroids inhibit the exchange transport of glucose in human erythrocytes. The extent of inhibition is roughly correlated to the affinity of the steroids to the membrane lipids. All C-21-steroids tested show a competitive inhibition while the C-19-steriods show different types of inhibition. 5Beta-androstane-3,17-dione acts as a competitive inhibitor. The inhibition by testosterone is of mixed type, while with androst-4-ene-3,17-dione and 5alpha-androstane-3,17-dione a non-competitive inhibition is observed. In this case two inhibitor molecules can be bound per transport molecule. The "non-competitive" inhibitors compete also to some extent with the glucose binding. This effect, however, is at high inhibitor concentrations masked by the more powerful non-competitive inhibition. Competitive and non-competitive inhibitors compete with each other. The structural requirements for the different types of inhibition are discussed.
D015068:17-Ketosteroids / Q000494:pharmacology*; D000450:Aldosterone / Q000494:pharmacology; D000731:Androstanes / Q000494:pharmacology*; D000735:Androstenedione / Q000494:pharmacology; D001665:Binding Sites; D001667:Binding, Competitive; D001693:Biological Transport, Active / Q000187:drug effects; D003345:Corticosterone / Q000494:pharmacology; D003348:Cortisone / Q000494:pharmacology; D003350:Cortodoxone / Q000494:pharmacology; D004912:Erythrocytes / Q000378:metabolism*; D005947:Glucose / Q000378:metabolism*; D006801:Humans; D006854:Hydrocortisone / Q000494:pharmacology; D007700:Kinetics; D011283:Pregnenes / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013739:Testosterone / Q000494:pharmacology
D015068:17-Ketosteroids; D000731:Androstanes; D011283:Pregnenes; D013739:Testosterone; D000735:Androstenedione; D000450:Aldosterone; D005947:Glucose; D003348:Cortisone; D003345:Corticosterone; D003350:Cortodoxone; D006854:Hydrocortisone