In vitro leishmanicidal activity of monomeric and dimeric naphthoquinones (vol 76, pg 131, 2000)

A series of monomeric and dimeric naphthoquinones with potential for treatm ent of Leishmania infections was identified in vitro using both a direct cy totoxicity 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 naphthoq uinones proved to be active at concentrations in the microgram range (EC50 0.9-17.0 mug/ml). When tested against a panel of human cancer cell lines (K B, SKMel, A549, MDA) and murine bone marrow culture-derived macrophages (BM M Phi) as mammalian host cell controls, compounds with anti-Leishmania-acti vity showed moderate (EC50 > 25 mug/ml) to pronounced (EC50 < 10 <mu>g/ml) toxic effects. (C) 2000 Elsevier Science B.V. All rights reserved.