Browsing by Autor "Fournet, Alain"

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2-Substituted quinoline alkaloids as potential antileishmanial drugs
(Facultad de Medicina, Enfermería, Nutrición y Tecnología Médica, 1993) Fournet, Alain
Abstract. Ten 2-substituted quinoline alkaloids isolated from a plant used for treatment of New World cutaneous leishmaniasis have antileishmanial in vitro activities against the extracellular forms of Leishmania spp. BALB/c mice infected with Leishmania amazonensis PH8 or H-142 or Leishmania venezuelensis were treated 1 day after the parasitic infection with a quinoline alkaloid (100 mg/kg of body weight per day) or with reference drug N-methylglucamine antimonate (Glucantime) (56 mg of pentavalent antimony [Sbv] per kg per day) for 14 days. Lesion development was the criterium used to assess disease severity. Two three-carbon chain quinolines [2-n-propylquinoline and 2-(1',2'-trans-epoxypropyl)quinoline (chimanine D)] were more potent than N-methylglucamine antimonate against L. amazonensis PH8, and five quinoline alkaloids [2-(3,4-methylenedioxyphenylethyl)quinoline, cusparine, 2-(3,4-dimethoxyphenylethyl)quinoline, 2-(E)-prop-1'-enylquinoline (chimanine B), and skimmianine] were as effective as the reference drug. Single treatment near the site of infection, 14 days after infection with L. amazonensis, with 2-n-propylquinoline or chimanine B reduced the severity of lesions but less notably than N-methylglucamine antimonate. 2-n-Propylquinoline exhibited significant activity against the virulent strain L. venezuelensis. The active products did not show any apparent toxicities during the experiment. This study is, to our knowledge, the first to show the activity of 2-substituted quinoline alkaloids for experimental treatment of New World cutaneous leishmaniasis. Further investigations of these compounds might yet prove helpful for the development of new antileishmanial drugs.
Antiprotozoal activity of dehydrozaluzanin C, a sesquiterpene lactone isolated from munnozia maronii (Asteraceae)
(Facultad de Medicina, Enfermería, Nutrición y Tecnología Médica, 1993) Fournet, Alain
The petrolelum 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 and IC 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 H and C NMR experimets 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., 1976). 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 dehidrozaluzanin C was tested on BALB/c mice infected with amatigote 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.
Aryl-2 et alkyl-2 quinoléines nouvelles isolées d'une rutacée bolivienne: Galipea longiflora
(Facultad de Medicina, Enfermería, Nutrición y Tecnología Médica, 1989) Fournet, Alain
Cinq aryl-2 et alkyl-2 quinoléines nouvelles ont été isolées des écorces de tiges de Galipea longiflora Krause (Rutacées) : la phényl-2 quinoléine 1, la (méthylènedioxy-3', 4') phénéthyl-2 quinoléine 2, la (diméthoxy-3',4') phénéthyl-2 quinoléine 3. la (méthylénedioxy-3',4') styryle-2 méthoxy-4 quinoléine 4 et la (pentèn- 1 ',2' yl)-2méthoxy-4-quinoléine 6. Ces alcaloïdes sont accompagnés de trois quinoléines substituées en 2, la n-amyl-2 méthoxy-4 quinoléine 5, la (méthylénedioxy-3',4') phénéthyl-2 méthoxy-4 quinoléine (cusparine) 7 et la phényl-2 méthoxy-4 quinoléine 8, et de deux furo[2,3b] quinoléines déjà connues, l'évolitrine et la skimmianine.
Biological and chemical studies of Pera benensis, a Bolivian plant used in folk medicine as a treatment of cutaneous leishmaniasis
(Facultad de Medicina, Enfermería, Nutrición y Tecnología Médica, 1992) Fournet, Alain
The stem barks of Pera benensis are employed by the Chimane Indians in the Bolivian Amazonia as treatment of cutaneous leishmaniasis caused by the protozoan Leishmania braziliensis. The chloroform extracts containing quinones were found active against the promastigote forms of Leishmania and the epimastigote forms of Trypanosoma cruzi at 10 ug ml-1. The activity guided fractionation of the extract by chromatography afforded active compounds. Their structures were elucidated, by spectral and chemical studies, as known naphthoquinones, plumbagin, 3,3’ - biplumbagin, 8-8’ –biplumbagin, and triterpene, lupeol. The activity in vitro of each compound was evaluated against 5 strains of Leishmania (promastigote), 6 strains of Trypasonoma cruzi (epimastigote) and the intracellular form (amastigote) of Leishmania amazonensis. The baseline drugs used were Glucantime and pentamidine (Leishmania spp.), nifurtimox and benznidazole (T. cruzi). Plumbagin was the most active compound in vitro. This study has demonstrated that Pera benensis, a medicinal plant used in folk medicine, is an efficient treatmen of cutaneous leismaniasis.
Effect of some bisbenzylisoquinoline alkaloids on American Leishmania sp. in BALB/c mice
(Facultad de Medicina, Enfermería, Nutrición y Tecnología Médica, 1993) Fournet, Alain
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 (GlucantimeR) 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.
Leishmanicidal and trypanocidal activities of Bolivian medicinal plants
(Facultad de Medicina, Enfermería, Nutrición y Tecnología Médica, 1994) Fournet, Alain
Abstract. Cutaneous and mucocutaneous leishmaniasis are endemic diseases in South America, especially in the subandean areas of the humid lowlands of Bolivia. Fourteen plants used topically in folk medicine to treat cutaneous leishmaniasis were collected in the tropical regions of colonization and in the rain forest occupied by Chimane Indians. Three of four plants used by the Chimane Indians exhibited an in vitro activity against three species of Leishmania. Two of ten plants used by the colonists showed an in vitro activity. We have also included results obtained with extracts from 53 Bolivian medicinal plants used for other diseases and from 43 plants collected with basis of chemotaxonomic criteria from all parts of Bolivia. All extracts were also screened in vitro against three strains of Trypanosoma cruzi (Trypanosomatidae), the causative agent of Chagas' disease.