2 resultados para ANTIFUNGAL COMPOUNDS

em Universidade Federal do Rio Grande do Norte(UFRN)


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Malaria, also popularly known as maleita , intermittent fever, paludism, impaludism, third fever or fourth fever, is an acute infectious febrile disease, which, in human beings, is caused by four species: Plasmodium falciparum, P. vivax, P. malariae and P. ovale. Malaria, one of the main infectious diseases in the world, is the most important parasitoses, with 250 million annual cases and more than 1 million deaths per year, mainly in children younger than live years of age. The prophylactic and therapeutic arsenal against malaria is quite restricted, since all the antimalarials currently in use have some limitation. Many plant species belonging to several families have been tested in vivo, using the murine experimental model Plasmodium berghei or in vitro against P. falciparum, and this search has been directed toward plants with antithermal, antimalarial or antiinflammatory properties used in popular Brazilian bolk medicine. Studies assessing the biological activity of medicinal plant essential oils have revealed activities of interest, such as insecticidal, spasmolytic and antiplasmodic action. It has also been scientifically established that around 60% of essential oils have antifungal properties and that 35% exhibit antibacterial properties. In our investigation, essential oils were obtained from the species Vanillosmopsis arborea, Lippia sidoides and Croton zethneri which are found in the bioregion of Araripe-Ceará. The chemical composition of these essential oils was partially characterized and the presence of monoterpenes and sesquiterpenes. The acute toxicity of these oils was assessed in healthy mice at different doses applied on a single day and on four consecutive days, and in vitro cytotoxicity in HeLa and Raw cell lines was determined at different concentrations. The in vivo tests obtained lethal dose values of 7,1 mg/Kg (doses administered on a single day) and 1,8 mg/Kg (doses administered over four days) for 50% of the animals. In the in vitro tests, the inhibitory concentration for 50% of cell growth in Hela cell lines was 588 μg/mL (essential oil from C. zethneri after 48 h), from 340-555 μg/mL (essential oil from L. sidoides, after 24 and 48 h). The essential oil from V. arborea showed no cytotoxicity and none of the essential oils were cytotoxic in Raw cell lines. These data suggest a moderate toxicity in the essential XVIII oils under study, a finding that does not impede their testing in in vivo antimalarial assays. Was shown the antimalarial activity of the essential oils in mice infected with P. berghei was assessed. The three species showed antimalarial activity from 36%-57% for the essential oil from the stem of V. arborea; from 32%-82% for the essential oil from the leaves of L. sidoides and from 40%-70% of reduction for the essential oil from the leaves of C. zethneri. This is the first study showing evidence of antimalarial activity with these species from northeast Brazil. Further studies to isolate the active ingredients of these oils are needed to determine if a single active ingredient accounts for the antimalarial activity or if a complex integration of all the compounds present occurs, a situation reflected in their biological activity

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The increase in the incidence of fungal infections due to the drug-resistance or to the number of patients with immune alterations such as AIDS, chemotherapy or organ transplantation, has done the research necesseray for new antifungal drugs. The species from Northeastern Brazil may become an important source of innovative natural molecules. To evaluate the antifungal activity of 10 medicinal plants from Northeastern Brazil, traditionally used as antimicrobial agents, 30 crude extracts (CE) were tested in vitro against four standard species of Candida spp. The CE most promising of these plants were evaluated against yeasts of the oral cavity of kidney transplant patients and through a bioassay-guided fractionation. The extracts form leaves of E. uniflora, the stem bark of L. ferrea and leaves of P. guajava showed significant activity against all yeasts evaluated, with MIC values between 15.62 and 62.5 μg/mL. E. uniflora also showed fungicidal properties against all yeasts, especially against Candida dubliniensis. In patients with immune systems compromised, such as transplanted, oral candidiasis manifests mainly due to immunosuppressive therapy, and resistance to conventional antifungals. The CE of E. uniflora presented range of MIC values between 1.95 to 1000 μg/mL, and lower MIC50 and MIC90 values were observed against C. non-albicans. Due the better results, the CE of E. uniflora was elected to performe the bioassay-guided fractionation. Thus it was possible to obtain enriched fractions, which showed good inhibitory ability against ATCC strains of Candida spp. It was also possible to perform experiments to verify the production of biofilm in two strains of C. dubliniensis and action of extracts and fractions on the same. With this, we observed a behavior between the yeast ATCC and clinical isolate. In addition, CE, fractions and subfractions of E. uniflora inhibit planktonic cells to preventing the growth of biofilm. The preliminary chemical characterization of the fractions obtained revealed the presence of polyphenols (especially flavonoids and tannins). Finally, the results suggests that among the plant species studied, E. uniflora showed a pattern very promising as regards the antifungal, requiring further study of purification and structural elucidation of compounds in order to verify that the antifungal effect found can be attributed to a specific compound or some mechanism depends on synergistic the mixture of polyphenols