Membrane action of phlorizinyl 5'-benzylazide induces volume and shape change of human erythrocytes and sickle cells

Prog Clin Biol Res. 1988:258:235-47.

Abstract

In the absence of light, phlorizinyl benzylazide is a potent competitive inhibitor of sugar transport (app. Ki about 1.5 uM) and a reversible inhibitor of chloride exchange (app. Ki about 2 uM) in the normal red cell. It causes additional membrane alterations at about 10-fold higher concentrations which lead to a time-, pH-, temperature-, and cell storage time-dependent increase in cell volume in isosmotic phosphate-buffered saline. This drug effect may be related to its interaction with Bands 3 and 4.5 (both become covalently labeled when the azide is light activated) such that cation conductance is increased. Apparently, a channel is created or widened through which salt and water (but not sucrose) can enter causing cell swelling and eventually lysis. The membrane probe is capable of inhibiting deoxygenation-induced sickling of SS and SC cells; under conditions that cause normal cell bursting, sickle cells swell but do not lyse.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenosine Triphosphate / blood
  • Anemia, Sickle Cell / blood*
  • Azides / pharmacology
  • Buffers
  • Cold Temperature
  • Energy Metabolism
  • Erythrocyte Membrane / drug effects*
  • Erythrocytes / drug effects*
  • Erythrocytes / pathology
  • Hemolysis
  • Humans
  • Hydrogen-Ion Concentration
  • Ouabain / pharmacology
  • Phlorhizin / analogs & derivatives
  • Phlorhizin / pharmacology
  • Sodium-Potassium-Exchanging ATPase / blood
  • Spectrophotometry
  • Time Factors

Substances

  • Azides
  • Buffers
  • phlorizinyl 5'-benzylazide
  • Ouabain
  • Adenosine Triphosphate
  • Phlorhizin
  • Sodium-Potassium-Exchanging ATPase