Planta Med 1999; 65(4): 316-319
DOI: 10.1055/s-1999-13993
Original Paper

Georg Thieme Verlag Stuttgart · New York

In Vitro Leishmanicidal Activity of Aurones

O. Kayser1 , A. F. Kiderlen2 , U. Folkens2 , H. Kolodziej1
  • 1Institut für Pharmazeutische Biologie, Freie Universität Berlin, Berlin, Germany
  • 2Abteilung für Infektionskrankheiten, Robert Koch-Institut, Berlin, Germany
Further Information

Publication History

August 7, 1998

December 13, 1998

Publication Date:
31 December 1999 (online)


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 μg/ml in the extra-, and an EC 50 of 1.40 μg/ml in the intracellular assay. Other aurones were active between 0.06 - 12.50 μg/ml and 0.04 - 7.81 μg/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 μg/ml). This is the first report on aurones as a new class of natural products with leishmanicidal activity.