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Antimalarial properties of ebselen

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Abstract

The seleno-organic compound ebselen showed anti-malarial activity in vitro against the murinePlasmodium berghei and the humanP. falciparum. InP. berghei, the uptake and incorporation of [3H]-methionine and [3H]-adenosine was inhibited and the infectivity of plasmodia was reduced. Ebselen affects the development of asexual stages of chloroquine-resistant and-sensitiveP. falciparum strains. Its IC50 forP. falciparum was about 14 μmol/l and that forP. berghei, about 10 μmol/l. The growth ofP falciparum was blocked by ebselen at all stages, including the invasion of erythrocytes by merozoites. In a human hepatoma cell line and in mouse peritoneal macrophages, no cytostatic or cytotoxic effects were found, indicating selective inhibition of plasmodia by ebselen. Its in vitro inhibitory effect is discussed in relation to its possible reactivity with thiol groups and its lack of an anti-malarial effect in infected mice.

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Abbreviations

BSA:

bovine serum albumin

FCS:

fetal calf serum

GSH:

reduced glutathione

GSSG:

oxidised glutathione

HBSS:

Hanks' blanced salt solution

PBS:

phosphate-buffered saline

PE:

parasitised erythrocytes

Se:

selenium

TCA:

trichloroacetic acid

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Authors and Affiliations

  1. Rhône-Poulenc/Nattermann, Forschungszentrum Köln, Nattermannallee 1, D-5000, Köln 30, Federal Republic of Germany

    A. M. Hüther, A. Sauer & M. J. Parnham

  2. Physiologisch-chemisches Institut, der Universität, Hoppe-Seyler-Strasse 1, D-7400, Tübingen, Federal Republic of Germany

    Y. Zhang

Authors
  1. A. M. Hüther
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  2. Y. Zhang
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  3. A. Sauer
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  4. M. J. Parnham
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Hüther, A.M., Zhang, Y., Sauer, A. et al. Antimalarial properties of ebselen. Parasitol Res 75, 353–360 (1989). https://doi.org/10.1007/BF00931130

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