In vitro leishmanicidal activity of aurones.
A series of aurones with drug-potential for 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 forms of L. donovani residing within murine macrophages. The most active aurone (6-hydroxy-2-[phenylmethylene]-3(2H)-benzofuranone) had an EC50 of 0.45 microgram/ml in the extra-, and an EC50 of 1.40 micrograms/ml in the intracellular assay. Other aurones were active between 0.06-12.50 micrograms/ml and 0.04-7.81 micrograms/ml, respectively. When tested against murine bone marrow-derived macrophages as a mammalian host cell control, the compounds showed only moderate cytotoxicity (EC50 2.32 to > 25.0 micrograms/ml). This is the first report on aurones as a new class of natural products with leishmanicidal activity.
Kayser
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O
Institut für Pharmazeutische Biologie, Freie Universität Berlin, Germany. kayser@zedat.fu-berlin.de
Kiderlen
A F
AF
Folkens
U
U
Kolodziej
H
H
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D001572:Benzofurans / Q000494:pharmacology*; D001597:Benzylidene Compounds / Q000494:pharmacology*; D001854:Bone Marrow Cells / Q000187:drug effects / Q000469:parasitology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D007891:Leishmania / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D051379:Mice; D008810:Mice, Inbred C57BL
C119816:6-hydroxy-2-(phenylmethylene)-3(2H)-benzofuranone; D000981:Antiprotozoal Agents; D001572:Benzofurans; D001597:Benzylidene Compounds