Browsing by Autor "Alain Fournet"

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Antiprotozoal activity of aporphine alkaloids isolated from Unonopsis buchtienii (Annonaceae)
(Wiley, 1999) Anne‐Isabelle Waechter; André Cavé; Reynald Hocquemiller; Christian Bories; Victoria Muñoz; Alain Fournet
On a preliminary screening, substantial leishmanicidal activity was observed for the petroleum ether and alkaloidal extracts of the stem bark of Unonopsis buchtienii, the alkaloids and sterols isolated from these were studied. Of the alkaloids, liriodenine exhibited the highest activity against Leishmania major and L. donovani (IC100 = 3.12 µg/mL). On the other hand, O-methylmoschatoline and the petroleum ether extract without alkaloids showed an interesting in vitro activity against Trypanosoma brucei with an IC100 of 6.25 µg/mL. The highest cytotoxic activities were found with the petroleum ether extracts without alkaloids and with all alkaloids isolated (IC50 < 9 µg/mL for Vero cell line). Copyright © 1999 John Wiley & Sons, Ltd.
Antiprotozoal activity of aporphine alkaloids isolated fromUnonopsis buchtienii (Annonaceae)
(Wiley, 1999) Anne-Isabelle Waechter; André Cavé; Reynald Hocquemiller; Christian Bories; Victoria Muñoz; Alain Fournet
On a preliminary screening, substantial leishmanicidal activity was observed for the petroleum ether and alkaloidal extracts of the stem bark of Unonopsis buchtienii, the alkaloids and sterols isolated from these were studied. Of the alkaloids, liriodenine exhibited the highest activity against Leishmania major and L donovani (IC100 = 3.12 micrograms/mL). On the other hand, O-methylmoschatoline and the petroleum ether extract without alkaloids showed an interesting in vitro activity against Trypanosoma brucei with an IC100 of 6.25 micrograms/mL. The highest cytotoxic activities were found with the petroleum ether extracts without alkaloids and with all alkaloids isolated (IC50 < 9 micrograms/mL for Vero cell line).
Antiprotozoal activity of dehydrozaluzanin C, a sesquiterpene lactone isolated from Munnozia maronii (asteraceae)
(Wiley, 1993) Alain Fournet; Victoria Muñoz; François Roblot; Reynald Hocquemiller; André Cavé; Jean-Charles Gantier
Abstract The petroleum ether extract of the leaves of Munnozia maronii was found to inhibit in vitro the growth of promastigote forms of Leishmania and epimastigote forms of Trypanosoma cruzi with an IC 90 of 25 μg/mL. Activity‐guided fractionation of the extract by chromatography identified the sesquiterpene lactone 1 of the guaiane series. The complete structure of 1 was elucidated using 1 H and 13 C NMR experiments at high field. The isolated compound was shown to be a new natural guaianolid, dehydrozaluzanin C, previously known as synthetic oxidative derivative of zaluzanin C (Romo de Vivar et al. , 1967). This compound inhibited, in vitro , the growth of 12 strains of Leishmania and 15 strains of T. cruzi at concentrations between 50 and 2.5 μg/mL. The leishmanicidal activity of dehydrozaluzanin C was tested on BALB/ c mice infected with amastigote forms of Leishmania amazonensis . Dehydrozaluzanin C reduced the severity of L. amazonesis lesions in BALB/ c mice but was less active than the reference compound Glucantime.
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; Alain 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.
Antiprotozoal activity of quinoline alkaloids isolated from Galipea longiflora, 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.
Biological and chemical studies of Pera benensis, a Bolivian plant used in folk medicine as a treatment of cutaneous leishmaniasis
(Elsevier BV, 1992) Alain Fournet; A. Angelo; Victoria Muñoz; François Roblot; Reynald Hocquemiller; André Cavé
Bis-benzylisoquinoline alkaloids from Abuta pahni
(Elsevier BV, 1987) Alain Fournet; Adrien Cavé; Pascale Dute ́; Jean-Frédéric F. Weber; J. Bruneton
Chemical Composition and Insecticidal Activity ofHedeoma mandonianaEssential Oils
(Taylor & Francis, 2004) Antonio Vilaseca; Isabelle Guy; Brigitte Charles; Hélène Guinaudeau; Antonieta Rojas de Árias; Alain Fournet
Abstract The analysis by GC/MS of samples of essential oils obtained from aerial parts of Hedeoma mandoniana allowed the identification of 58 components. The main components were pulegone (37–46%), 1,8-cineole (10–14%), linalool (7–12%) and 1-octen-3-yl acetate (7–12%). We investigated the efficacy of these oils against the Chagas' insect disease vectors (Triatoma infestans Klug or Rhodnius neglectus Lent) bugs by topical application. Two samples showed a moderate activity (33.3% of mortality) on Rhodnius neglectus exemplars.
Effect of some bisbenzylisoquinoline alkaloids on American Leishmania sp. in BALB/c mice
(Wiley, 1993) Alain Fournet; Angel Barrios; Victoria Muñoz; Reynald Hocquemiller; André Cavé
Abstract Four bisbenzylisoquinoline alkaloids, antioquine, berbamine, gyrocarpine and isotetrandrine were tested in BALB/c mice infected with Leishmania amazonensis (IFLA/BR/67/PH8 or MHOM/GF/84/CAY‐H‐142) or L. venezuelensis (VE/74/PM‐H3). The treatments were initiated 1 day after the parasitic infection, with alkaloid at 100 mg/kg/day for 14 days and the reference compound, meglumine antimonate (Glucantime R ) at 200 mg/kg/day. Antioquine, berbamine and gyrocarpine were less potent than Glucantime against L. amazonensis (PH8). Only isotetrandrine exhibited activity approximately equal to or greater than Glucantime in BALB/c mice infected with L. amazonensis (PH8 or H‐142) and showed significant activity against L. venezuelensis . Experiments with a single local treatment on the footpad, 2 weeks after parasitic infection with L. amazonensis (PH8), showed that isotetrandrine at 200 mg/kg was less active than Glucantime at 400 mg/kg.
Isoquinoline Alkaloids fromCardiopetalum calophyllum
(Thieme Medical Publishers (Germany), 1991) Corinne Séguineau; Pascal Richomme; Alain Fournet; H. Guinaudeau; J. Bruneton
Leishmanicidal and Trypanocidal activities of Acetogenins isolated fromAnnona glauca
(Wiley, 1998) Anne-Isabelle Waechter; Gloria Yaluff; Alba Inchausti; Antonieta Rojas de Árias; Reynald Hocquemiller; André Cavé; Alain Fournet
The dichloromethane extract of seeds of Annona glauca (Annonaceae) was active against three strains of Leishmania species. Nine known acetogenins were isolated and identified and then evaluated in vitro against Leishmania species and the bloodstream forms of Trypanosoma cruzi. Annonacin A and goniothalamicin showed activity against Leishmania, and glaucanisin, squamocin, annonacin A and annonacin against Trypanosoma cruzi reducing the parasites by 78%, 67%, 71% and 85%, respectively. Copyright © 1998 John Wiley & Sons, Ltd.
Leishmanicidal and trypanocidal activities of Bolivian medicinal plants
(Elsevier BV, 1994) Alain Fournet; Angel Barrios; Victoria Muñoz