978 resultados para TRYPSIN INHIBITORY-ACTIVITY
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Natural products have been studied aiming to understand their biological properties. Thus, this study aimed to investigate the antimicrobial activity of twenty-seven essential oils (EOs) used in aromatherapy procedures, a natural therapy with great emphasis currently used against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa strains. The agar dilution method was carried out and minimal inhibitory concentration against 50% and 90% of strains (MIC50% and MIC90% values) were reported. The S.aureus strains were highly susceptible with MIC90% from 0.21mg/mL to black pepper (Piper nigrum) and tea tree (Melaleuca alternifolia) to 26.52mg/mL with copaiba (Copaifera officinalis) EO. Cinnamon (Cinnamomum cassia) and clove (Syzygium aromaticum) EOs were effective against E.coli (2.0mg/mL) while the S.aromaticum EO was against P.aeruginosa (8.29mg/mL). Thus, the higher susceptibility of Gram-positive bacteria when compared with Gram-negative strains was found, and a large variability in the potential antibacterial has also been observed.
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Despite the resistance developed by the Mycobacterium tuberculosis (MTb) strains, isoniazid (INK) has been recognized as one of the best drug for treatment of Tuberculosis (Tb). The coordination of INH to ruthenium metal centers was investigated as a strategy to enhance the activity of this drug against the sensitive and resistant strains of MTb. The complexes trans-[Ru(NH3)(4)(L)(INH)](2+) (L = SO2 or NH3) were isolated and their chemical and antituberculosis properties studied. The minimal inhibitory concentration (MIC) data show that [Ru(NH3)(5)(INH)](2+) was active in both resistant and sensitive strains, whereas free INK (non-coordinated) showed to be active only against the sensitive strain. The coordination of INH to the metal center in both [Ru(NH3)(5)(INH)](2+) and trans-[Ru(NH3)(4)(SO2)(INH)](2+) complexes led to a shift in the INH oxidation potential to less positive values compared to free INH. Despite, the ease of oxidation of INH did not lead to an increase in the in vitro INH activity against MTb, it might have provided sensitivity toward resistant strains. Furthermore, ruthenium complexes with chemical structures analogous to those described above were synthesized using the oxidation products of INK as ligands (namely, isonicotinic acid and isonicotinamide). These last compounds were not active against any strains of MTb. Moreover, according to DFT calculations the formation of the acyl radical, a proposed intermediate in the INH oxidation, is favored in the [Ru(NH3)(5)(INH)](2+) complex by 50.7 kcal mol(-1) with respect to the free INH. This result suggests that the stabilization of the acyl radical promoted by the metal center would be a more important feature than the oxidation potential of the INH for the antituberculosis activity against resistant strains. (C) 2015 Elsevier B.V. All rights reserved.
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Mouthwashes are used as an adjunct to tooth brushing for improving breath and preventing oral diseases. The aim of this study was to compare the in vitro Maximum Inhibitory Dilution (MID) of 3 mouthwashes with different active ingredients against mutans streptococci (MS). The products analyzed were PeriogardR, CepacolR and PlaxR Fresh Mint. Their antibacterial activity was assessed in duplicate in 96-well microtiter plates against 36 clinical isolates of MS. Each mouthwash was submitted to a serial two-fold dilution (1/2.5 to 1/5120) using double concentration of Tryptose Soy Broth with 1.0% yeast extract. The final volume in each well was 100 mL plus 5 mL of a bacterial suspension, equivalent to 107 CFU/mL. They were incubated microaerobically at 37oC for 48 hours and the MIDs determined. MID was 1/320 for PeriogardR and CepacolR, and 1/20 for PlaxR. Statistical analysis revealed that the MID of PeriogardR MID did not differ from that of CepacolR (p>0.05), and was higher than that of PlaxR (p<0.05). In conclusion, the antiseptic mouthwashes containing chlorhexidine (PeriogardR) and cetylpyridinium chloride (CepacolR) had higher in vitroantibacterial activity (MID) against MS than the antiseptic mouthwash containing triclosan (PlaxR), according to microbiological method employed.
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The genus Astronium (Anacardiaceae) includes species, such as Astronium fraxinifolium, Astronium graveolens, and Astronium urundeuva, which possess anti-inflammatory, anti-ulcerogenic, healing, and antimicrobial properties. Nanostructured lipid systems are able to potentiate the action of plant extracts, reducing the required dose and side effects and improving antimicrobial activity. This work aims to evaluate a nanostructured lipid system that was developed as a strategy to improve the anti-Candida albicans activity of hydroethanolic extracts of stems and leaves from Astronium sp. The antifungal activity against C. albicans (ATCC 18804) was evaluated in vitro by a microdilution technique. In addition to the in vitro assays, the Astronium sp. that showed the best antifungal activity and selectivity index was submitted to an in vivo assay using a model of vulvovaginal candidiasis infection. In these assays, the extracts were either used alone or were incorporated into the nanostructured lipid system (comprising 10% oil phase, 10% surfactant, and 80% aqueous phase). The results indicated a minimal inhibitory concentration of 125.00 µg/mL before incorporation into the nanostructured system; this activity was even more enhanced when this extract presented a minimal inhibitory concentration of 15.62 µg/mL after its incorporation. In vivo assay dates showed that the nanostructure-incorporated extract of A. urundeuva leaves was more effective than both the unincorporated extract and the antifungal positive control (amphotericin B). These results suggest that this nanostructured lipid system can be used in a strategy to improve the in vitro and in vivo anti-C. albicans activity of hydroethanolic extracts of Astronium sp.
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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
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Alterations in the hypothalamic-pituitary-gonadal axis in females determine the transition from regular to irregular reproductive cycles, with loss of fertility. Stimulation of noradrenergic neurons of the anteroventral periventricular neurons (AVPV) is essential for regular reproductive cycles. Therefore, we examined the activity of neurons of the AVPV and measure the noradrenaline (NE) of acyclic rats, in constant estrus, and compared it with that of cyclic rats in estrus. Female cyclic (4-5months) and acyclic (17-18months) rats were euthanized at 10, 14, and 18h in estrus. Brains were processed for immunoreactivity to antigens related to Fos (FRA) in AVPV, and the NE was determined by HPLC-ED. Plasma concentrations of LH, FSH, E2 and P4 were determined. In the acyclic animals, plasma LH was higher but the FSH was lower. There was decreasing P4 at different times, while the E2 was constant and lower in acyclic rats. FRA-ir expression in AVPV neurons of acyclic rats as well as turnover of NE was higher when compared with cyclic group. The preliminary findings showed increased activity in AVPV neurons in aging contribute to changes in the temporal pattern of neuroendocrine signaling, compromising the accuracy of inhibitory and stimulatory effects, causing irregularity in the estrous cycle and determining reproductive senescence.