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Acta Trop. 2000 Dec 1;77(3):307-14.

In vitro leishmanicidal activity of monomeric and dimeric naphthoquinones.

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Institute of Pharmacy, Pharmaceutical Technology, Biopharmacy and Biotechnology, Freie Universit├Ąt Berlin, Kelchstrasse 31, D-12169, Berlin, Germany.


A series of monomeric and dimeric naphthoquinones with potential for treatment of Leishmania infections was identified in vitro using both a direct cytotoxicity assay against extracellular promastigotes of Leishmania donovani, L. infantum, L. enriettii, and L. major and a test against intracellular amastigote L. donovani residing within murine macrophages. Several naphthoquinones proved to be active at concentrations in the microgram range (EC(50) 0.9-17.0 microg/ml). When tested against a panel of human cancer cell lines (KB, SKMel, A549, MDA) and murine bone marrow culture-derived macrophages (BMMPhi) as mammalian host cell controls, compounds with anti-Leishmania-activity showed moderate (EC(50)>25 microg/ml) to pronounced (EC(50)<10 microg/ml) toxic effects.

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