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, 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.
Kayser
O
O
Institute of Pharmacy, Pharmaceutical Technology, Biopharmacy and Biotechnology, Freie Universität Berlin, Kelchstrasse 31, D-12169, Berlin, Germany. kayser@zedat.fu-berlin.de
Kiderlen
A F
AF
Laatsch
H
H
Croft
S L
SL
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D006801:Humans; D007891:Leishmania / Q000187:drug effects*; D009285:Naphthoquinones / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D009285:Naphthoquinones