Browsing by Autor "A. Fournet"

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Antileishmanial Activity of a Tetralone Isolated from<i>Ampelocera edentula</i>, a Bolivian Plant Used as a Treatment for Cutaneous Leishmaniasis
(Thieme Medical Publishers (Germany), 1994) A. Fournet; Amy Barrios; Verónica Francisca Loewe Muñoz; Reynald Hocquemiller; F. Roblot; A. Cavé
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.
Antiprotozoal activity of Jatrogrossidione from Jatropha grossidentata and Jatrophone from Jatropha isabellii
(Wiley, 1996) Guillermo Schmeda‐Hirschmann; Iván Razmilic; Michel Sauvain; Christian Moretti; Verónica Francisca Loewe Muñoz; E. Ruiz; Elfride Balanza; A. Fournet
The activity of jatrogrossidione, the main diterpene of Jatropha grossidentata and jatrophone from Jatropha isabellii was determined against Leishmania and Trypanosoma cruzi strains in vitro as well as against Leishmania amazonensis in vivo. Jatrogrossidione showed a strong in vitro leishmanicidal and trypanocidal activity with IC100 of 0.75 and 1.5–5.0 μg/mL, respectively. Under similar conditions, the IC100 of glucantime, ketoconazole and pentamidine towards Leishmania strains were >100, 50–100 and 1 μg/mL, respectively. The IC50 of jatrogrossidione was <0.25 μg/mL against amastigote forms of Leishmania infecting macrophages, with toxicity at concentrations higher than 0.5 μg/mL. BALB/c mice infected with L. amazonensis strain PH 8 were treated 24 h after infection with jatrogrossidione and jatrophone for 13 consecutive days. Jatrophone at 25 mg/kg/day subcutaneously administered was significantly active (p<0.05) against the virulent strain PH 8 of L. amazonesis; it was more active than Glucantime at 112 mg Sbv per kg/day. Subcutaneous administration of jatrophone, however, proved to be too toxic under our assay conditions. Assays of single local treatment on the footpad infection 2 weeks after inoculation of L. amazonensis indicated that jatrogrossidione and jatrophone were inactive at the selected doses.