title: Antileishmanial activity of a tetralone isolated from Ampelocera edentula, a Bolivian plant used as a treatment for cutaneous leishmaniasis.
abstract: The stem bark of Ampelocera edentula Kuhlm. (Ulmaceae) is used by the Chimanes Indians from Bolivia for the treatment of cutaneous leishmaniasis caused by the protozoan Leishmania braziliensis. A chloroform extract of the stem barks was found to be active against extracellular forms of Leishmania ssp. and Trypanosoma cruzi at 50 micrograms/ml. Bioassay-guided fractionation of this extract allowed us to isolate one active compound. Its structure was elucidated by spectral and chemical studies as 4-hydroxy-1-tetralone. BALB/c mice infected with L. amazonensis (PH8) or L. venezuelensis were treated one day after the parasitic infection with 4-hydroxy-1-tetralone (25 mg/kg/day) or with reference drug, Glucantime (56 mg Sbv/kg/day) for 14 days. Lesion development was the criteria used to evaluate the disease severity. 4-Hydroxy-1-tetralone was slightly less effective than the reference drug against L. amazonensis or L. venezuelensis. Single treatment near the site of infection, 14 days after infection with L. amazonensis, with 4-hydroxy-1-tetralone (50 mg/kg) was more effective than Glucantime (112 mg/kg). This study is, to our knowledge, the first to show the activity of a tetralone for the experimental treatment of New World cutaneous leishmaniasis.
authors.affiliation: Institut Français de Recherche Scientifique pour le Développement en Coopération (ORSTOM), Département Santé, Paris, France.
authors.forename: A
authors.initials: A
authors.lastname: Fournet
authors.forename: A A
authors.initials: AA
authors.lastname: Barrios
authors.forename: V
authors.initials: V
authors.lastname: Muñoz
authors.forename: R
authors.initials: R
authors.lastname: Hocquemiller
authors.forename: F
authors.initials: F
authors.lastname: Roblot
authors.forename: A
authors.initials: A
authors.lastname: Cavé
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D005260:Female; D007891:Leishmania / Q000187:drug effects; D007892:Leishmania braziliensis / Q000187:drug effects*; D016773:Leishmaniasis, Cutaneous / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry*; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*; D044024:Tetralones; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D013764:Tetrahydronaphthalenes; D044024:Tetralones; C086294:4-hydroxy-1-tetralone