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Ebselen-binding equilibria between plasma and target proteins

V Ullrich1, P Weber, F Meisch

  • 1Department of Biology, University of Konstanz, Germany.

Biochemical Pharmacology
|July 12, 1996
PubMed
Summary

Ebselen (2-phenyl-1,2-benzisoselenazo-3(2H)-one) covalently binds albumin but rapidly exchanges with intracellular thiols in polymorphonuclear leukocytes (PMN) and platelets, enabling pharmacological effects.

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Medicinal Chemistry

Background:

  • Ebselen is an anti-inflammatory drug known to covalently bind to thiols.
  • Albumin is a primary target due to its reactive thiol group and high plasma concentration.
  • This binding raises questions about ebselen's availability for intracellular targets.

Purpose of the Study:

  • To investigate the interaction of ebselen with albumin and its subsequent availability for intracellular targets.
  • To determine if ebselen, despite binding to albumin, can reach and interact with proteins in human polymorphonuclear leukocytes (PMN) and platelets.

Main Methods:

  • Difference spectroscopy was used to study ebselen interactions.
  • Experiments involved ebselen, albumin, glutathione, N-ethylmaleimide, intact human PMN, and human platelets.

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  • 14C-ebselen was used to track its dynamic equilibrium with thiol groups.

    • Main Results:

    • Ebselen binds stoichiometrically to albumin via ring opening, a reaction reversible by glutathione.
    • Ebselen also reacts stoichiometrically with proteins in intact human PMN, a reaction inhibited by N-ethylmaleimide but not glutathione depletion.
    • Human platelets show distinct spectral changes upon ebselen addition.
    • 14C-ebselen demonstrates dynamic equilibrium with accessible thiols, indicating rapid exchange.

    Conclusions:

    • Despite covalent binding to albumin, ebselen rapidly exchanges with thiol groups.
    • Ebselen is available to interact with intracellular target proteins in PMN and platelets.
    • This dynamic equilibrium explains ebselen's pharmacological effects at intracellular sites.