No abstract

Bioassay-guided fractionation of the bark extract of Annona foetida afforded a new antileishmanial pyrimidine-beta-carboline alkaloid, N-hydroxyannomontine (1), together with the previously reported annomontine (2), O-methylmoschatoline (3), and liriodenine (4). The structure of compound 1 was established on the basis of extensive 1D and 2D NMR and MS analyses. This is the third reported pyrimidine-beta-carboline-type alkaloid and is particularly important for Annona genus chemotaxonomy. In addition, all compounds exhibit in vitro antileishmanial activity against promastigote forms of Leishmania braziliensis. Compounds 2 and 4 showed better activity than compounds 1 and 3 against L. braziliensis. Compound 2 was not active against L. guyanensis.

No abstract

No abstract

Recebido em 2/1/08; aceito em 6/8/08; publicado na web em 15/12/08The essential oil from leaves of Annona foetida obtained by hydrodistillation was analyzed by GC/FID and GC/MS. The results showed that the major constituents were bicyclogermacrene (35.12%), (E)-caryophyllene (14.19%) and α-copaene (8.19%). The antimicrobial and antileishmanial activities were investigated. The oil showed potent antimicrobial activity against Candida albicans and Rhodococcus equi. The oil also showed significant antileishmanial activity, giving the best results against Leishmania guyanensis. A preliminary cytotoxicity assay for this oil was carried out on hamster and mice (Balb/c) peritoneal macrophages. The results obtained were similar to pentamidine and considered not to be cytotoxic to macrophages.

Essential oil of Cymbopogon citratus collected from Brazil and Cuba was tested to a chemical characterization and then was tested on the post-embryonic development of Musca domestica. The chemical composition analysis by GC-MS of the oils from Brazil/Cuba allowed the identification of 13 and 12 major constituents respectively; nine of them common to both. In the both oils, the main components were the isomers geranial and neral, which together form the compound citral. This corresponds to a total of 97.92%/Brazil and 97.69%/Cuba of the compounds identified. The monoterpene myrcene, observed only in the sample of Cuba, presented a large relative abundance (6.52%). The essential oil of C. citratus (Brazil/Cuba) was dissolved in DMSO and tested at concentrations of 5, 10, 25, 50, 75 and 100% and citral was prepared by mixing 16.8 mg with 960 µL DMSO. Both essential oils and monoterpene citral were applied topically to newly-hatched larvae (1µL/larva). The results showed a lethal concentration (LC50) of 4.25 and 3.24% for the Brazilian and Cuban essential oils, respectively. Mortalities of larval and newly-hatched larvae to adult periods were dose-dependent for the two both oils as for monoterpene citral, reaching 90%. Both essential oils and citral caused morphological changes in adult specimens.Keywords: Vector control, essential oil, house-fly, lemongrass, Cymbopogon citratus. ResumoO óleo essencial de Cymbopogon citratus, coletado no Brasil e em Cuba, foi caracterizado quimicamente e testado no desenvolvimento pós-embrionário de Musca domestica. A análise da composição química dos óleos essenciais (Brasil/Cuba), por Cromatografia Gasosa acoplada ao espectrômetro de massa (GC-EM), permitiu a identificação de 13 e 12 componentes principais, respectivamente; nove deles comuns aos dois. Em ambos os óleos, os principais componentes foram os isômeros geranial e neral, que, juntos, formam o composto citral. Esse corresponde a um total de 97,92%/Brasil e 97,69%/Cuba dos compostos identificados. O monoterpeno mirceno, observado na amostra cubana, apresentou grande abundância relativa (6,52%). O óleo de C. citratus (Brasil/Cuba) foi dissolvido em DMSO, obtendo-se as concentrações de 5, 10, 25, 75 e 100%; e o citral (16,8 mg) foi misturando com 960mL de DMSO. Tanto o óleo essencial como o monoterpeno citral foram aplicados topicamente nas neolarvas (1µL/larva). Os resultados mostraram uma concentração letal (CL50)

Este trabalho compara pela primeira vez a composição química do óleo essencial das folhas de Licaria canella coletadas em duas estações climáticas. Os resultados foram comparados com os obtidos para o óleo essencial das folhas de outra espécie da família Lauraceae, Aniba canelilla, coletada no mesmo período. Ambos os óleos essenciais foram analisados por CG-DIC e CG-EM, e os resultados indicaram uma grande quantidade de benzenóides, sendo o principal constituinte em L. canella o benzoato de benzila e para A. canelilla, o 1-nitro-2-feniletano. A comparação das atividades biológicas mostrou que o óleo de L. canella (IC 50 19 µg mL-1) foi mais ativo contra as cepas de Leishmania amazonensis e menos citotóxico em cultura de macrófagos do que o de A. canelilla (IC 50 40 µg mL-1). Por outro lado, o óleo de L. canella exibiu uma maior citotoxicidade contra Artemia salina com uma concentração letal (CL 50) igual a 5,25 µg mL-1. This work compares the chemical composition of the essential oils from the leaves of Licaria canella collected in two different seasons. The results of this investigation were compared with the leaf essential oils of other species of the Lauraceae family, Aniba canelilla, collected at the same time. Both essential oils were analyzed by GC-FID and GC-MS. The results demonstrated a larger predominance of benzenoids, being the main constituent benzyl benzoate for L. canella and 1-nitro-2-phenylethane for A. canelilla. The comparison of the biological activities showed that L. canella (IC 50 19 µg mL-1) was more active against Leishmania amazonensis strains and less cytotoxic in macrophage cultures than A. canelilla (IC 50 40 µg mL-1). On the other hand, the L. canella oil displayed a higher cytotoxicity against Artemia salina with a lethal concentration (LC 50), equal to 5.25 µg mL-1 .

Leishmaniasis is a vector-borne disease that affects several populations worldwide, against which there are no vaccines available and the chemotherapy is highly toxic. Depending on the species causing the infection, the disease is characterized by commitment of tissues, including the skin, mucous membranes, and internal organs. Despite the relevance of host inflammatory mediators on parasite burden control, Leishmania and host immune cells interaction may generate an exacerbated proinflammatory response that plays an important role in the development of leishmaniasis clinical manifestations. Plant-derived natural products have been recognized as bioactive agents with several properties, including anti-protozoal and anti-inflammatory activities. The present review focuses on the antileishmanial activity of plant-derived natural products that are able to modulate the inflammatory response in vitro and in vivo. The capability of crude extracts and some isolated substances in promoting an anti-inflammatory response during Leishmania infection may be used as part of an effective strategy to fight the disease.