Licochalcone A, a novel antiparasitic agent with potent activity against human pathogenic protozoan species of Leishmania

  • M Chen
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.
  • S B Christensen
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.
  • J Blom
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.
  • E Lemmich
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.
  • L Nadelmann
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.
  • K Fich
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.
  • T G Theander
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.
  • A Kharazmi
    Department of Clinical Microbiology, University Hospital, Copenhagen, Denmark.

書誌事項

公開日
1993-12
権利情報
  • https://journals.asm.org/non-commercial-tdm-license
DOI
  • 10.1128/aac.37.12.2550
公開者
American Society for Microbiology

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説明

<jats:p>Licochalcone A, an oxygenated chalcone isolated from the roots of Chinese licorice plant, inhibited the growth of both Leishmania major and Leishmania donovani promastigotes and amastigotes. The structure of the licochalcone A was established by mass and nuclear magnetic resonance spectroscopies and by synthesis, and its purity was verified by high-pressure liquid chromatography. The 50% inhibition of growth of logarithmic- and stationary-phase promastigotes of L. major, as measured by [3H]thymidine uptake, were 4 and 2.5 micrograms/ml, respectively. The growth of L. major promastigotes was totally inhibited after a 20-h incubation period with licochalcone A at 5 micrograms/ml. At a concentration of 0.5 microgram/ml, licochalcone A markedly reduced the infection rate of human peripheral blood monocyte-derived macrophages and U937 cells with L. major promastigotes and exhibited a strong intracellular killing of the parasite. These data show that intracellular Leishmania amastigotes are more susceptible than promastigotes to licochalcone A. Results of studies on the site of action of licochalcone A indicate that the target organelle appears to be the parasite mitochondria. These findings demonstrate that licochalcone A in concentrations that are nontoxic to host cells exhibits a strong antileishmanial activity and that appropriate substituted chalcones might be a new class of antileishmanial drugs.</jats:p>

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