title: Chemotherapeutic efficacy of ascofuranone in Trypanosoma vivax-infected mice without glycerol.
abstract: Ascofuranone, an antibiotic isolated from Ascochyta visiae, showed trypanocidal activity in Trypanosoma vivax-infected mice. A single dose of 50 mg/kg ascofuranone effectively cured the mice without the help of glycerol. Repeated administrations of this drug further enhanced its chemotherapeutic effect. After two, three, and four consecutive days treatment, the doses needed to cure the infection decreased to 25, 12, and 6 mg/kg, so that the total doses administered were 50, 36 and 24 mg/kg, respectively. Ascofuranone (50 mg/kg) also had a prophylactic effect against T. vivax infection within the first two days after administration. This prophylactic activity diminished to 80% by day 3 and completely disappeared four days after administration. Of particular interest in this study was that ascofuranone had trypanocidal activity in T. vivax-infected mice in the absence of glycerol, whereas co-administration of glycerol or repeated administrations of this drug are needed for Trypanosoma brucei brucei infection. Our present results strongly suggest that ascofuranone is also an effective tool in chemotherapy against African trypanosomiasis in domestic animals.
authors.affiliation: Department of Molecular Parasitology, Nagoya City University, Graduate School of Medical Sciences, Nagoya 467-8601, Japan. yabu@med.nagoya-cu.ac.jp
authors.forename: Yoshisada
authors.initials: Y
authors.lastname: Yabu
authors.forename: Takashi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Coh-ichi
authors.initials: C
authors.lastname: Nihei
authors.forename: Nobuko
authors.initials: N
authors.lastname: Minagawa
authors.forename: Tomoyoshi
authors.initials: T
authors.lastname: Hosokawa
authors.forename: Kazuo
authors.initials: K
authors.lastname: Nagai
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Kita
authors.forename: Nobuo
authors.initials: N
authors.lastname: Ohta
mesh_terms: D000818:Animals; D004195:Disease Models, Animal; D005990:Glycerol / Q000008:administration & dosage; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D012717:Sesquiterpenes / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D016896:Treatment Outcome; D014344:Trypanocidal Agents / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D016689:Trypanosoma vivax / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy* / Q000469:parasitology
chemical_list: D012717:Sesquiterpenes; D014344:Trypanocidal Agents; C006640:ascofuranone; D005990:Glycerol