In vitro leishmanicidal activity of monomeric and dimeric naphthoquinones.
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, Leishmania infanturn, Leishmania enriettii, and Leishmania 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.
Institute of Pharmacy, Pharmazeutische Technologie, Biopharmazie und Biotechnologie, Freie Universität Berlin, Germany. kayser@zedat.fu-berlin.de
O
O
Kayser
A F
AF
Kiderlen
H
H
Laatsch
S L
SL
Croft
D000818:Animals; D006801:Humans; D007891:Leishmania / Q000187:drug effects*; D007893:Leishmania donovani / Q000187:drug effects; D018313:Leishmania enriettii / Q000187:drug effects; D018314:Leishmania infantum / Q000187:drug effects; D018320:Leishmania major / Q000187:drug effects; D007896:Leishmaniasis / Q000188:drug therapy*; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D009285:Naphthoquinones / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000469:parasitology
D009285:Naphthoquinones