993 resultados para antifungal glycoalkaloids


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Fanconi anemia (FA) is a rare autosomal recessive disorder, characterized by pancytopenia and progressive hypoplasia of the bone marrow. A 23-year-old woman with FA showed severe pancytopenia and developed an abscess on the infraorbicular region on the right side of the face that progressed to phlegmon and caused tissue necrosis of the nostrils, nasal septum, nasal fossa, and posterior orbital region. Laboratory examination showed Streptococcus parasanguis as the etiologic agent of the phlegmon. Supportive treatment was recommended due to donor incompatibility for bone marrow transplant. The intraoral examination showed spontaneous gingival bleeding, edema of the interdental papillae, hematomas on the superior and inferior lips, bacterial and fungal infections, and adequate oral hygiene. The patient was treated with the administration of an antibiotic (imipenem), an antifungal (amphotericin B), and mouth washing with antiseptic solutions. Periodontal prophylaxis and orientation to and control of oral hygiene and diet were also used during the remission period. For functional and esthetic rehabilitation of the alar regions and nasal dorsum, an acrylic resin nasal prosthesis was made, supported by a spectacle frame.

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The microorganism Sclerotinia was isolated from roots of Stevia rebaudiana (Bert.) Bertoni in plantations in the northwest of Parana and submitted to the cultivation in the presence of extracts and vegetable balsams of Tarragon (Artemisia draconculus), Thyme (Thymus vulgaris), Manjerona (Origanum majorona), Mint citrata (Mintpiperita var. citrata), Purple Basil (Ocimum basilicum L.), Andiroba (Carapa guanensis) and Copaíba (Copaifera reticulata Ducke). The first five oils were extracted by steam drags, after the drying of the vegetable in greenhouse with circulation of air at 45°C. The last two were used in natura. A suspension (100ìl) of fungus previously cultivated, was added to each plate. The results show that after 7 days of incubation the thyme oils 10ìl, purple basil 25ìl, manjerona 25ìl, mint citrata 50ìl, tarragon 50ìl were capable to inhibit the growth of Sclerotinia, while the andiroba oil only reached this result with 200ìl. The copaiba balsam, even in the concentration of 500ìl, was unable to inhibit the growth of the microorganism.

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Communiols E-H (1-4), four new polyketide-derived natural products containing furanocyclopentane, furanocyclopentene, cyclopentene, or γ-lactone moieties, have been isolated from two geographically distinct isolates of the coprophilous fungus Podospora communis. The structures of these compounds were determined by analysis of NMR and MS data. © 2005 American Chemical Society and American Society of Pharmacognosy.

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The aim of this study was to evaluate in vitro the antimicrobial activity of glass ionomer (GIC) and zinc oxide-eugenol (ZOE) cements against Candida albicans. Standardized GIC and ZOE specimens were maintained in contact with C. albicans suspension (1 x 10(6) cells/ml) at 37 degrees C for 24 h, 48 h or 7 days. A control group without any testing cement was included. After the incubation period, aliquots of 0.1 ml were plated on Sabouraud's agar, and then the number of colonies was counted. The results were expressed as values of logarithms of colony-forming units per milliliter (log CFU/mL) and were analyzed statistically by Kruskal-Wallis ANOVA. After 48 h of incubation, the ZOE group presented no growth of C. albicans. GIC and control groups presented similar mean values at all tested periods. According to the results obtained, it could be concluded that, under the experimental conditions, ZOE cement was more effective in vitro against C. albicans than GIC.

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A 14-year-old, male patient was referred for the treatment of mucositis, idiopathic facial asymmetry, and candidiasis. The patient had been undergoing chemotherapy for 5 years for acute lymphoblastic leukemia. He presented with a swollen face, fever, and generalized symptomatology in the mouth with burning. On physical examination, general signs of poor health, paleness, malnutrition, and jaundice were observed. The extraoral clinical examination showed edema on the right side of the face and cutaneous erythema. On intraoral clinical examination, generalized ulcers with extensive necrosis on the hard palate mucosa were observed, extending to the posterior region. Both free and attached gingivae were ulcerated and edematous with exudation and spontaneous bleeding, mainly in the superior and inferior anterior teeth region. The tongue had no papillae and was coated, due to poor oral hygiene. The patient also presented with carious white lesions and enamel hypoplasia, mouth opening limitation, and foul odor. After exfoliative cytology of the affected areas, the diagnosis was mixed infection by Candida albicans and bacteria. Recommended treatment was antibiotics and antifungal administration, periodontal prophylaxis, topical application of fluor 1.23%, and orientation on and control of proper oral hygiene and diet during the remission phase of the disease.

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Crude extracts from roots, stems, branches, fruits and leaves of Cedrela fissilis were tested to verify their toxicity to Atta sexdens rubropilosa workers and to their symbiotic fungus Leucoagaricus gongylophorus. The workers that were fed daily on an artificial diet to which crude extracts from this plant were added had a higher mortality rate than the controls, especially for the hexane, dichloromethane and methanol crude extracts from roots (RH, RD and RM) and from leaves (LH, LD and LM). Fungal growth was inhibited by the hexane (RH) and dichloromethane crude extract from roots (RD). The RH, RD and FD crude extracts were fractioned and their fractions were tested. All the fractions tested presented toxicity to the ants and some fractions (RH-H, RH-D, RD-4 and RD-5) completely inhibited fungus development. The possibility of controlling these insects in the future using Cedrela fissilis compounds that can simultaneously target both organisms is discussed.

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The present communication reports the isolation and identification of four triterpenoid saponins from the chloroform extract of the leaves of Tocoyena brasiliensis: 3-O-β-D-quinovopyranosyl quinovic acid, 3-O-β-D- quinovopyranosyl cincholic acid, 3-O-β-D-glucopyranosyl quinovic acid and the 28-O-β-D-glucopyranosyl ester derivative of quinovic acid as binary mixtures, respectively. From the ethanol extract a flavonoid identified as ramnazin-3-O-rutinoside was obtained. The structures of these compounds were assigned by data analysis of ID and 2D NMR spectrometry and comparison with data recorded in the literature for these compounds.

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An isolate of Curvularia sp. was obtained from the leaves of Ocotea corymbosa, a native plant of the Brazilian Cerrado. The ethyl acetate extract from culture of this fungus afforded two benzopyran derivatives: (2′S)-2-(propan-2′-ol)-5-hydroxy-benzopyran-4-one (2) and 2,3-dihydro-2-methyl-benzopyran-4,5-diol (4); and two known benzopyrans: 2-methyl-5-methoxy-benzopyran-4-one (1) and (2R)-2,3-dihydro-2-methyl-5-methoxy- benzopyran-4-one (3). The structures of 2 and 4 were established on the basis of comprehensive spectroscopic analysis, mainly using 1D and 2D NMR experiments. The benzopyrans 1 and 2 showed weak in vitro antifungal activity against Cladosporium sphaerospermum and C. cladosporioides. Analyses of the biological activities were also carried out on HeLa (human cervix tumor) and CHO (Chinese hamster ovary) cells, aiming to evaluate their potential effects on mammalian cell line proliferation. Results from both cell lines indicated that compound 2 was able to induce cell proliferation: 70% on HeLa cells and 25% on CHO cells. © 2005 Elsevier Ltd. All rights reserved.

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Two new metabolites, ethyl 2,4-dihydroxy-5,6-dimethylbenzoate (1) and phomopsilactone (2) were isolated from Phomopsis cassiae, an endophytic fungus in Cassia spectabilis. Their structures were elucidated by 1D and 2D NMR, MS and IR spectral data. Compounds 1 and 2 displayed strong antifungal activity against the phytopatogenic fungi Cladosporium cladosporioides and C. sphaerospermum, as well as cytotoxicity against human cervical tumor cell line (HeLa), in in vitro assays. ©2005 Sociedade Brasileira de Química.

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In this study we investigated the effect of β-glucan derived from Saccharomyces cerevisiae on fungicidal activity, cytokine production and natural killer activity. Spleen and peritoneal cells from female C57BL/6 mice, previously injected (24 or 48 h) with 20 or 100 μg of glucan by i.p. route, were assayed. In vivo β-glucan administration primed spleen cells for a higher production of IL-12 and TNF-α when S. aureus was used as a stimulus. In addition, β-glucan increased NK spleen cells activity against YAC target cells. Some immunomodulatory activities not yet described for β-glucan were observed in this work. © 2005 Institute of Physiology, Academy of Sciences of the Czech Republic.

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With the significant increase in the incidence of invasive fungal infections during the last decade, mainly in patients with cancer, AIDS and other hospitalized patients who stay for long periods in intensive care units, there is an urgent need to screen for new antifungal agents possessing some advantages over known ones. This article reports a search in the field for a microorganism producing antibacterial and antifungal substances. Strains from soil samples collected in the region of Araraquara, Brazil, were isolated and analyzed for their antimicrobial potential against standard microorganisms (fungi Candida albicans and Aspergillus oryzae and bacteria Staphylococcus aureus and Escherichia coli). Out of the 64 strains isolated, 34 produced detectable antimicrobial activity. The streptomycete strain Ar4014 was chosen for further study, owing to its good antimicrobial activity against Candida albicans. Two of the fermentation media tested, 608-K and 602-B, were found to be best for the production and extraction of the antibiotic from Ar4014. After chromatographic separation of the crude extract on a silica column, the active fractions obtained showed UV-VIS absorption peaks characteristic of normal pentaenic antibiotics. The antibiotic was provisionally designated Ara 4014-75.

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Purpose: This study evaluated the ultimate tensile strength of a tissue conditioner without nystatin incorporation (GI - control group) and the same tissue conditioner modified by the addition of nystatin in two concentrations: GII - 500,000 International Units (U) and GIII - 1,000,000 U, in which each milligram of the medicament corresponded to 6079 U. Materials and Methods: Dumbbell-shaped specimens (N = 7) with a central cross-sectional area of 33 × 6 × 3 mm were produced for the three experimental groups. After polymerization following manufacturer's instructions, specimens were immersed in distilled water at 37°C for either 24 hours or 7 days and then tested in tension in the MTS 810 at 40 mm/minute. Data were analyzed by two-way ANOVA followed by Tukey's test, at 95% level of confidence. Results: The means (force-grams (gf) ± standard deviation) of the ultimate tensile strength were: GI - 634.29 ± 122.80; GII - 561.92 ± 133.56; and GIII - 547.30 ± 73.47 for 24-hour storage, and GI - 536.68 ± 54.71; GII - 467.50 ± 143.51; and GIII - 500.62 ± 159.76 for 7-day storage. There were no statistically significant differences among the three experimental groups (p > 0.05). The ultimate tensile strength means of all experimental groups after 7 days were significantly lower than those observed after 24 hours (p = 0.04). Conclusions: The results of this study suggest that the addition of nystatin into the tissue conditioner investigated in concentrations below 1,000,000 U did not affect its ultimate tensile strength. Copyright © 2006 by The American College of Prosthodontists.

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The increase in incidence of infectious diseases worldwide, particularly in developing countries, is worrying. Each year, 14 million people are killed by infectious diseases, mainly HIV/AIDS, respiratory infections, malaria and tuberculosis. Despite the great burden in the poor countries, drug discovery to treat tropical diseases has come to a standstill. There is no interest by the pharmaceutical industry in drug development against the major diseases of the poor countries, since the financial return cannot be guaranteed. This has created an urgent need for new therapeutics to neglected diseases. A possible approach has been the exploitation of the inhibition of unique targets, vital to the pathogen such as the shikimate pathway enzymes, which are present in bacteria, fungi and apicomplexan parasites but are absent in mammals. The chorismate synthase (CS) catalyses the seventh step in this pathway, the conversion of 5-enolpyruvylshikimate-3-phosphate to chorismate. The strict requirement for a reduced flavin mononucleotide and the anti 1,4 elimination are both unusual aspects which make CS reaction unique among flavin-dependent enzymes, representing an important target for the chemotherapeutic agents development. In this review we present the main biochemical features of CS from bacterial and fungal sources and their difference from the apicomplexan CS. The CS mechanisms proposed are discussed and compared with structural data. The CS structures of some organisms are compared and their distinct features analyzed. Some known CS inhibitors are presented and the main characteristics are discussed. The structural and kinetics data reviewed here can be useful for the design of inhibitors. © 2007 Bentham Science Publishers Ltd.

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EPSP synthase (EPSPS) is an essential enzyme in the shikimate pathway, transferring the enolpyruvyl group of phosphoenolpyruvate to shikimate-3-phosphate to form 5-enolpyruvyl-3-shikimate phosphate and inorganic phosphate. This enzyme is composed of two domains, which are formed by three copies of βαβαββ-folding units; in between there are two crossover chain segments hinging the nearly topologically symmetrical domains together and allowing conformational changes necessary for substrate conversion. The reaction is ordered with shikimate-3-phosphate binding first, followed by phosphoenolpyruvate, and then by the subsequent release of phosphate and EPSP. N-[phosphomethyl]glycine (glyphosate) is the commercial inhibitor of this enzyme. Apparently, the binding of shikimate-3-phosphate is necessary for glyphosate binding, since it induces the closure of the two domains to form the active site in the interdomain cleft. However, it is somehow controversial whether binding of shikimate-3-phosphate alone is enough to induce the complete conversion to the closed state. The phosphoenolpyruvate binding site seems to be located mainly on the C-terminal domain, while the binding site of shikimate-3-phosphate is located primarily in the N-terminal domain residues. However, recent results demonstrate that the active site of the enzyme undergoes structural changes upon inhibitor binding on a scale that cannot be predicted by conventional computational methods. Studies of molecular docking based on the interaction of known EPSPS structures with (R)- phosphonate TI analogue reveal that more experimental data on the structure and dynamics of various EPSPS-ligand complexes are needed to more effectively apply structure-based drug design of this enzyme in the future. © 2007 Bentham Science Publishers Ltd.

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