In vitro leishmanicidal activity of monomeric and dimeric naphthoquinones.

Abstract

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.

• Authors: O Kayser, A F Kiderlen, H Laatsch, S L Croft
• Journal: Acta tropica (Acta Trop) Vol. 76 Issue 2 Pg. 131-8 (Sep 18 2000) ISSN: 0001-706X [Print] Netherlands
• PMID: 10936572 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Naphthoquinones

Topics

• Animals
• Humans
• Leishmania (drug effects)
• Leishmania donovani (drug effects)
• Leishmania enriettii (drug effects)
• Leishmania infantum (drug effects)
• Leishmania major (drug effects)
• Leishmaniasis (drug therapy)
• Macrophages (drug effects, parasitology)
• Naphthoquinones (pharmacology)
• Tumor Cells, Cultured (drug effects, parasitology)