Browsing by Autor "F. Roblot"

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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.
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    Antiprotozoal activity of quinoline alkaloids isolated from <i>Galipea longiflora</i>, a Bolivian plant used as a treatment for cutaneous leishmaniasis
    (Wiley, 1994) Alain Fournet; Angel Barrios; Verónica Francisca Loewe Muñoz; Reynald Hocquemiller; F. Roblot; A. Cavé; Pascal Richomme; J. Bruneton
    Abstract The stem bark of Galipea longiflora is used by the Chimane Indians in Bolivia for the treatment of cutaneous leishmaniasis produced by Leishmania braziliensis . Petroleum ether and chloroform extracts of stem, root bark and leaves were found active in vitro against Leishmania ssp and Trypanosoma cruzi at 100 μg/mL. The activity guided fractionation of the extracts by chromatography afforded 12 active compounds identified as 2‐substituted quinoline alkaloids. BALB/c mice were infected with Leishmania amazonensis (strain PH8 or H‐142) and treated 24 h after infection with the major alkaloids from the crude alkaloidal extract; 2‐phenylquinoline and 2‐n‐pentylquinoline. 2‐phenylquinoline was as potent as Glucantime (Rhǒne‐Poulenc) against the strain H‐142, but less active than the reference drug against the virulent strain PH8 of L. amazonensis. 2‐n ‐pentylquinoline did not exhibit any activity. Assays of single local treatments on the rear footpad infection, 2 weeks after the parasitic inoculation, indicated an effect for 2‐phenylquinoline by reducing the severity of lesion. However, this activity was found to be slightly lower than that obtained using Glucantime.