a tropical weapon against Chagas disease.

The present study pretends to evaluate the efficacy of the crude chloroform bark extract of , then the activity will be compared with the reference drug, benznidazole, in acute infected mice when administered by oral route. The chloroformic extract of was administered by oral route at 5, 10 and 50 mg/kg daily for two weeks. This study has shown a moderate efficacy of the bark extract in reducing parasitaemia in 42 to 54% after a monitoring of 60 days post-infection and when compared with control groups.

Phytoelectrochemical analysis of Zanthoxylum chiloperone.

Introduction: An innovative application of the voltammetry of microparticles methodology to characterize the phytochemical composition of extracts of different parts of Zanthoxylum chiloperone var. angustifolium Engl. is described.

Harvesting canthinones: identification of the optimal seasonal point of harvest of Zanthoxylum chiloperone leaves as a source of 5-methoxycanthin-6-one.

This article is focused on the seasonal variation in the contents of 5-methoxycanthin-6-one from the leaves of Zanthoxylum chiloperone (Rutaceae). Based on the pharmacological interest presented by 5-methoxycanthin-6-one, its seasonal variation in Z. chiloperone leaves was analysed in order to determine the best time for harvesting, optimising the 5-methoxycanthin-6-one content.

Antifungal Activity of the Essential Oils of Callitris neocaledonica and C. sulcata Heartwood (Cupressaceae).

Mortality due to fungal infections has increased substantially, becoming a worldwide problem in public health. As a contribution to the discovery of new antifungal agents, the properties of the heartwood essential oils of two trees growing in New Caledonia, Callitris neocaledonica and C. sulcata (Cupressaceae) were investigated.

Antiproliferative activity of trans-avicennol from Zanthoxylum chiloperone var. angustifolium against human cancer stem cells.

Zanthoxylum chiloperone var. angustifolium root bark was studied with the aim of finding novel molecules able to overcome cancer stem cell chemoresistance. Purification of a methanol-soluble extract resulted in the isolation of a known pyranocoumarin, trans-avicennol (1).

Zanthoxylum chiloperone leaves extract: first sustainable Chagas disease treatment.

Ethnopharmacological Relevance: Zanthoxylum chiloperone var. angustifolium Engl. (Rutaceae) stem bark is used traditionally in Paraguay for its antiparasitic properties.

Chemical composition and antimicrobial activity of the essential oils from New Caledonian Citrus macroptera and Citrus hystrix.

The essential oils from the leaves of Citrus macroptera and C. hystrix, collected in New Caledonia, have been analyzed by gas chromatography/mass spectrometry (GC/MS) and evaluated for their antimicrobial activity. A total of 35 and 38 constituents were identified, representing 99.

Antileishmanial activity of furoquinolines and coumarins from Helietta apiculata.

Unlabelled: The bark infusion of H. apiculata are used to treat wound healing related to cutaneous leishmaniasis and as anti-inflammatory.

Aim Of The Study: To isolate, purify active constituents of H.

Oxidation of antiparasitic 2-substituted quinolines using metalloporphyrin catalysts: scale-up of a biomimetic reaction for metabolite production of drug candidates.

A study comparing the chemical oxidation of drug candidates with cell-based metabolism (liver microsomes, hepatocytes) shows that biomimetic oxidation can replace the biological approach, thus allowing access to large quantities of metabolites, which can also be used for the preparation of new products.

Selection of the most promising 2-substituted quinoline as antileishmanial candidate for clinical trials.

The antileishmanial evaluation of more than one hundred 2-substituted quinolines led us to identify three compounds for further studies: compound 1 (2-n-propylquinoline), compound 2 (2-(2methoxyethenyl)quinoline) and compound 3 (2-(2-hydroxyprop-2-enyl)quinoline). The final selection of a potential drug candidate was mainly based on chemical stability and acute oral toxicity as discriminating criteria. The most stable compound in various conditions was 2-n-propylquinoline (compound 1).

Quinoline compounds decrease in vitro spontaneous proliferation of peripheral blood mononuclear cells (PBMC) from human T-cell lymphotropic virus (HTLV) type-1-infected patients.

In vitro spontaneous proliferation is the immunological hallmark of peripheral blood mononuclear cells (PBMC) from HTLV-1-infected individuals. Quinoline compounds down regulate in vitro cell proliferation of HTLV-1 transformed cell lines. In the present study we assessed the capacity of quinolines to inhibit spontaneous cell proliferation of PBMC from HTLV-1-infected individuals.

Development of a SPE/HPLC/DAD method for the determination of antileishmanial 2-substituted quinolines and metabolites in rat plasma.

A SPE/HPLC/DAD method was developed for the in vivo monitoring of three new antileishmanial 2-substituted quinolines under study in our laboratory for the development of an oral treatment. Three phase I metabolites were included in this work for the optimization of the method. Trifunctional tC(18) cartridges (resulting from the reaction of trifunctional silanes with silica surface) were selected among four sorbents tested.

Phytochemical and antiprotozoal activity of Ocotea lancifolia.

Thirteen known isoquinoline alkaloids were isolated from Ocotea lancifolia, popularly known as << canela pilosa >> in Brasil and << laurel né >> by the Guarani people which means smell laurel. Their activities against the promastigote forms of three Leishmania strains and the bloodstream form of Trypanosoma cruzi were evaluated, as well as their hepatocytotoxicity. Among them, the noraporphine alkaloid (-) caaverine has shown the most interesting antiprotozoal activity against Leishmania and T.

Antileishmanial 2-substituted quinolines: in vitro behaviour towards biological components.

Quinolines substituted on their carbon 2 have in vivo antileishmanial activity but some of them could not be detected in plasma when assayed for pharmacokinetic studies, suggesting a sequestration of the drugs by components of the blood compartment. The present study, performed on three quinolines (1, 2 and 3), showed strong affinity for two of them (2 and 3) with red blood cells (RBCs), whereas quinoline 1 did not react with them. This process was saturable, temperature dependant and positively correlated with the in vitro antileishmanial activity of the quinolines.

Metabolism of 2-substituted quinolines with antileishmanial activity studied in vitro with liver microsomes, hepatocytes and recombinantly expressed enzymes analyzed by LC/MS.

Liver microsome and hepatocyte-mediated biotransformation of three oral antileishmanial 2-substituted quinolines were investigated. One quinoline contains an n-propyl group (1) and the other a propenyl chain functionalized at the gamma position either by a nitrile (2) or an alcohol (3). The different isoforms of rat cytochrome P450 responsible for biotransformation of 1 were also investigated.

Antiparasitic activity of some New Caledonian medicinal plants.

Twenty-nine extracts of 18 medicinal plants used in New Caledonia by traditional healers to treat inflammation, fever and in cicatrizing remedies were evaluated in vitro against several parasites (Leishmania donovani, Trypanosoma brucei brucei, Trichomonas vaginalis and Caenorhabditis elegans). Among the selected plants, Scaevola balansae and Premna serratifolia L. were the most active against Leishmania donovani with IC(50) values between 5 and 10microg/ml.

Bioassay-guided isolation of antifungal alkaloids from Melochia odorata.

An alkaloidal extract of the leaves of Melochia odorata exhibited antifungal activity against Candida albicans, Cryptococcus neoformans and Saccharomyces cerevisiae using a TLC bioautographic method. Bioassay-guided fractionation of this extract using separation by normal and reverse high-performance liquid chromatography (HPLC) resulted in the isolation of two active compounds identified as frangulanine, a cyclic peptide alkaloid, and waltherione-A, a quinolinone alkaloid.

Configuration and leishmanicidal activity of (-)-argentilactone epoxides.

Epoxidation of argentilactone (1) with m-chloroperbenzoic acid gave a diasteromeric mixture of 2 and 3 in a ratio 1.8 : 1, with total yield 60%. The configuration of 7,8-oxirane ring for both diasteromers was determined by NMR analysis.

Effects of canthin-6-one alkaloids from Zanthoxylum chiloperone on Trypanosoma cruzi-infected mice.

Canthin-6-one (1), isolated from Zanthoxylum chiloperone (Rutaceae), possesses a broad sprectum of antifungal and leishmanicidal activities. In this study, we have examined the antiparasitic effects of canthin-6-one (1), 5-methoxycanthin-6-one (2), canthin-6-one N-oxide (3), as well as that of the total alkaloids of Zanthoxylum chiloperone stem bark, in Balb/c mice infected either acutely or chronically with Trypanosoma cruzi. The compounds were administered orally or subcutaneously at 5mg/kg/day for 2 weeks, whereas the alkaloidal extract was given at 50mg/kg/day for 2 weeks.

Antileishmanial and trypanocidal activity of Brazilian Cerrado plants.

The side effects and the emerging resistance to the available drugs against leishmaniasis and trypanosomiasis led to the urgent need for new therapeutic agents against these diseases. Thirty one extracts of thirteen medicinal plants from the Brazilian Cerrado were therefore evaluated in vitro for their antiprotozoal activity against promastigotes of Leishmania donovani, and amastigotes of Trypanosoma cruzi. Among the selected plants, Casearia sylvestris var.

Extraction, hemisynthesis, and synthesis of canthin-6-one analogues. Evaluation of their antifungal activities.

Zanthoxylum chiloperone var. angustifolium was investigated. Alkaloids 1-3 from the canthin-6-one series were characterized.

Efficacy of orally administered 2-substituted quinolines in experimental murine cutaneous and visceral leishmaniases.

We report in this study the in vivo efficacy of nine 2-substituted quinolines on the Leishmania amazonensis cutaneous infection murine model and on the Leishmania infantum and Leishmania donovani visceral infection murine models. In the case of the L. amazonensis model, quinolines were administered orally at 25 mg/kg twice daily for 15 days.

Studies on quinones. Part 39: Synthesis and leishmanicidal activity of acylchloroquinones and hydroquinones.

Acylhydroquinone-based compounds are attractive targets for the design of new leishmanicidal drugs. We have previously described sesquiterpene quinones and hydroquinones series, which exhibit different degree of potency against Leishmania amazonensis. The present study details the preparation of acylchloroquinones and hydroquinones possessing lipophilic substituents and examines their in vitro activity against intracellular L.

Nematocidal and trichomonacidal activities of 2-substituted quinolines.

Several quinolines were synthesized and evaluated in vitro and in vivo against the nematodes Caenorhabditis elegans, Heligmosomoides polygyrus and the protozoa Trichomonas vaginalis. If some of them have shown in vitro nematocide activity (at 10 microM), however, their trichomonacidal activity reached 50% reduction at only 100 microM. The in vivo activity on Trichinella spiralis model was evaluated for some of the most in vitro active quinolines.

Biological evaluation of substituted quinolines.

Several quinolines were synthesized and evaluated in vitro against several parasites (Trypanosoma brucei, T. cruzi, Leishmania infantum, L. amazonensis, Plasmodium falciparum).