title: Sensitivities of Leishmania species to hexadecylphosphocholine (miltefosine), ET-18-OCH(3) (edelfosine) and amphotericin B.
abstract: The sensitivities of both promastigote and amastigote stages of six species of Leishmania, L. donovani, L. major, L. tropica, L. aethiopica, L. mexicana and L. panamensis, were determined in vitro to the phospholipid drugs hexadecylphosphocholine (HPC, miltefosine) and ET-18-OCH(3) (edelfosine). In all assays L. donovani was the most sensitive species, with ED(50) values in the range of 0.12-1.32 microM against promastigotes and 1.2-4.6 microM against amastigotes. L. major was the least sensitive species in the majority of assays with ED(50) values for HPC in the range of 4.8-13.1 microM against promastigotes and for HPC and ET-18-OCH(3) in the range of 7.5-37.1 microM against amastigotes. Amphotericin B deoxycholate was used as the standard drug and gave submicromolar ED(50) values in all assays; L. mexicana was the least sensitive species to this drug.
authors.affiliation: Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK.
authors.forename: Patricia
authors.initials: P
authors.lastname: Escobar
authors.forename: Sangeeta
authors.initials: S
authors.lastname: Matu
authors.forename: Cláudia
authors.initials: C
authors.lastname: Marques
authors.forename: Simon L
authors.initials: SL
authors.lastname: Croft
mesh_terms: D000666:Amphotericin B / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007891:Leishmania / Q000187:drug effects*; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000469:parasitology; D051379:Mice; D010742:Phospholipid Ethers / Q000494:pharmacology*; D010767:Phosphorylcholine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D013045:Species Specificity
chemical_list: D000981:Antiprotozoal Agents; D010742:Phospholipid Ethers; D010767:Phosphorylcholine; C026659:edelfosine; C039128:miltefosine; D000666:Amphotericin B