Hexadecylphosphocholine: oral treatment of visceral leishmaniasis in mice.
Hexadecylphosphocholine (He-PC), a novel phospholipid derivative, was tested against Leishmania donovani and Leishmania infantum, the causative agents of visceral leishmaniasis. In vitro, promastigotes were highly susceptible to He-PC; the 50% inhibitory concentrations were between 0.89 and 2.25 micrograms/ml for the different leishmanial strains. In vivo, a marked antileishmanial activity in infected BALB/c mice could be demonstrated after oral administration of He-PC. Whereas parasite suppression and killing in the liver were comparable after 5 days of treatment with He-PC (10 or 20 mg/kg of body weight per day administered orally) and sodium stibogluconate (120 mg of pentavalent antimonal agent per kg/day administered subcutaneously), a superior reduction in the parasite load in the spleen and bone marrow was observed after oral treatment with He-PC. After a 4-week treatment period, parasite suppression in the spleen was better than that observed with standard sodium stibogluconate therapy by a factor of more than 600.
Kuhlencord
A
A
Institut für Allgemeine Hygiene and Tropenhygiene, Windausweg, Göttingen, Germany.
Maniera
T
T
Eibl
H
H
Unger
C
C
D000284:Administration, Oral; D000818:Animals; D000967:Antimony Sodium Gluconate / Q000494:pharmacology; D001853:Bone Marrow / Q000469:parasitology; D005260:Female; D007891:Leishmania / Q000187:drug effects; D007893:Leishmania donovani / Q000187:drug effects; D007898:Leishmaniasis, Visceral / Q000188:drug therapy* / Q000469:parasitology; D008099:Liver / Q000469:parasitology; D051379:Mice; D008807:Mice, Inbred BALB C; D010767:Phosphorylcholine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D013154:Spleen / Q000469:parasitology
D010767:Phosphorylcholine; C039128:miltefosine; D000967:Antimony Sodium Gluconate