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, 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.

• Authors: O Kayser, A F Kiderlen, H Laatsch, S L Croft
• Journal: Acta tropica (Acta Trop) Vol. 77 Issue 3 Pg. 307-14 (Dec 01 2000) ISSN: 0001-706X [Print] Netherlands
• PMID: 11114393 (Publication Type: Journal Article)

Chemical References

• Antiprotozoal Agents
• Naphthoquinones

Topics

• Animals
• Antiprotozoal Agents (pharmacology)
• Humans
• Leishmania (drug effects)
• Naphthoquinones (pharmacology)
• Structure-Activity Relationship