HPLC-DAD analysis, antinociceptive and anti-inflammatory properties of the ethanolic extract of Hyptis umbrosa in mice

Hyptis umbrosa (syn. Mesosphaerum sidifolium) (Lamiaceae Family) has been used to treat several conditions such as gastrointestinal disorders, skin infections, nasal congestion, fever and cramps. The objective of this study was to evaluate the chemical composition, analgesic and anti-inflammatory profiles of ethanol extract from leaves of Hyptis umbrosa (EEB). HPLC-DAD was used to determine the fingerprint chromatogram of the extract. Male Swiss mice were orally pretreated with EEB (100, 200 or 400 mg/kg; 60 min before initiating algesic stimulation) and antinociceptive activity was assessed using the acetic acid-induced writhing model, formalin test and hyperalgesia induced by glutamate or capsaicin. Also, peritonitis was induced by the intrathoracic injection of carrageenan to quantify the total number of leukocytes. The presence of phenolic compounds in the extract was confirmed using HPLC-DAD. The treatment with EEB, at all doses, produced a significant analgesic effect against acetic acid-induced antinociceptive activity. In the formalin test, only the 400-mg/kg-dose of EEB had a significant effect in the first phase. However, all doses tested were able to reverse nociception in the second phase. The effect of all doses of EEB also showed a significant antinociceptive effect in the glutamate and capsaicin tests and inhibited the carrageenan-induced leukocyte migration to the peritoneal cavity. The present study suggests that the EEB possesses peripheral analgesic action and showed potential in reducing the spreading of the inflammatory processes. Also, it seems to be related with vanilloid and glutamate receptors

Brazilian Morus nigra

Morus nigra has been used popularly for several proposes, including diabetic. In an attempt to support medicinal value, the acute hypoglycemic, hypolipidemic, and antioxidant effects of the ethanolic extract of Morus nigra (EEMn 200 or 400 mg/kg b.w.) were evaluated in normal and alloxan-induced diabetic treated for 14 days. Serum biochemical and antioxidant analysis were performed at the end of experiment. Oral glucose tolerance test was performed at 10th and 15th days. Chromatographic analysis by HPLC-DAD of EEMn was performed. Insulin was used as positive control to glycemic metabolism as well as fenofibrate to lipid metabolism. EEMn (400 mg/kg/day) reduced fasting and postprandial glycaemia, improved oral glucose tolerance, and reduced lipolysis and proteolysis in diabetic rats. EEMn decreased the blood levels of total cholesterol and increased HDL level when compared to the diabetic control rats. At higher levels, EEMn reduced triglycerides and VLDL levels in diabetic rats. Also, EEMn reduced malondialdehyde and increased the reduced glutathione levels in liver of diabetic rats. Chromatographic analysis identified the presence of the flavonoids rutin, isoquercetin, and kaempferitrin. Acute EEMn treatment reduced hyperglycemia, improved oral glucose tolerance, and minimized dyslipidemia and oxidative stress leading to a reduction in atherogenic index in alloxan-induced diabetic rats

Assessment of global motor performance and gross and fine motor skills of infants attending day care centers

OBJETIVO: Analisar o desempenho motor global em habilidades motoras axiais e apendiculares de lactentes que frequentavam, em tempo integral, duas Escolas Municipais de Educação Infantil. MÉTODOS: Estudo longitudinal do qual participaram 30 lactentes avaliados aos 12 e 17 meses de vida com a escala motora das Bayley Scales of Infant and Toddler Development-III, que possibilita a análise do desempenho motor global, apendicular e axial e a discrepância entre eles. Utilizaram-se o teste de Wilcoxon e o Coeficiente de Correlação de Spearman. RESULTADOS: A maioria dos participantes apresentou desempenho motor global dentro dos limites de normalidade, porém abaixo da média de referência aos 12 e 17 meses, com 30% classificados como suspeitos de atraso em pelo menos uma das avaliações. O desempenho motor axial foi inferior ao apendicular aos 12 e aos 17 meses, com grande discrepância entre eles especialmente na 2ª avaliação. Observou-se marcada variabilidade individual nas habilidades motoras apendiculares, com fraca correlação linear no desempenho entre a 1ª e a 2ª avaliações nesse domínio. Nas habilidades axiais e no desempenho motor global, encontrou-se menor variabilidade individual, com correlações moderadas e positivas entre a 1ª e a 2ª avaliações. Identificaram-se quatro lactentes com suspeita de atraso no desenvolvimento motor em ambas as avaliações. CONCLUSÕES: O estudo aponta necessidade de maior atenção ao desenvolvimento motor durante os primeiros 17 meses de crianças que frequentam creches, com especial vigilância à motricidade axial (considerando que ela é parte integrante do desenvolvimento global da criança) e às crianças com desempenho suspeito de atraso em duas avaliações consecutivas.<br>OBJECTIVE: To analyze the global motor performance and the gross and fine motor skills of infants attending two public child care centers full-time. METHODS: This was a longitudinal study that included 30 infants assessed at 12 and 17 months of age with the Motor Scale of the Bayley Scales of Infant and Toddler Development, Third Edition (Bayley-III). This scale allows the analysis of global motor performance, fine and gross motor performance, and the discrepancy between them. The Wilcoxon test and Spearman's correlation coefficient were used. RESULTS: Most of the participants showed global motor performance within the normal range, but below the reference mean at 12 and 17 months, with 30% classified as having "suspected delays" in at least one of the assessments. Gross motor development was poorer than fine motor development at 12 and at 17 months of age, with great discrepancy between these two subtests in the second assessment. A clear individual variability was observed in fine motor skills, with weak linear correlation between the first and the second assessment of this subtest. A lower individual variability was found in the gross motor skills and global motor performance with positive moderate correlation between assessments. Considering both performance measurements obtained at 12 and 17 months of age, four infants were identified as having a "possible delay in motor development". CONCLUSIONS: The study showed the need for closer attention to the motor development of children who attend day care centers during the first 17 months of life, with special attention to gross motor skills (which are considered an integral part of the child's overall development) and to children with suspected delays in two consecutive assessments

The Importance of MDP Priming, Silica Blasting or Glazing on the Retention Force of Y-TZP Copings to Varying Geometry Tooth Abutments

To evaluate the influence of the convergence angle of tooth preparations and abutments height and several surface treatments for zirconia copings through the tensile retention test. 120 crown preparations were made in Nema G10 with the maxillary first molar anatomy. In total, 60 abutments of 5 mm height were divided into two groups of 6° and 20° convergence angles of tooth preparations, and 60 abutments with a convergence angle of tooth preparations of 12° were divided into groups of 4 and 6 mm heights. Three surface treatments used were MDP-primer (10-Methacryloyloxydecyl dihydrogen phosphate), glazing or silica blasting. The abutments were scanned to make zirconia copings (3Y-TZP–Yttria-Stabilized Tetragonal Zirconia Polycrystals, Vita In-Ceram YZ). After cementation, the mechanical cycling (2 × 106 cycles, 3 Hz, 100 N) was performed to aging. After cycling, the copings were tested in tensile (1 kN load cell; 0.5 mm/s speed). Both abutments support base and copings were embedded in acrylic resin with the aid of a device that maintained the long axis perpendicular to the horizontal plane. Data were analyzed with the two-way ANOVA and Tukey test (95%). ANOVA revealed that the convergence angle influenced the tensile retention (p = 0.0232), but the abutments height showed no statistically significant difference (p = 0.086). The MDP-primer and silica blasting showed higher retention forces in the specimens with height variations. For bonded zirconia crowns, the retention force provided by high convergence angle preparation is critical and cannot be improved by surface treatments. For short and long crown preparations, MDP-based Primers or Silica blasting are advisable to aid restoration longevity

SÍNTESE, CARACTERIZAÇÃO E AVALIAÇÃO DA ATIVIDADE CITOTÓXICA DE COMPOSTOS CICLOPALADADOS CONTENDO COMO LIGANTES BENZALDEIDOXIMA ORTOMETALADA E ETILENOTIOURÉIA

The halide-bridge cleavage reaction of the [Pd(C2 ,N-bzox)(µ-Cl)]2 compound (bzox = benzaldehydeoxime) with ethylenethiourea (L) in the 1:2 molar ratio at room temperature yielded the cyclopalladated compound [Pd(C2 ,N-bzox)(Cl)(L)] (1) whose replacement of the halide group by the addition of suitable salts afforded compounds of general formulae [Pd(C2 ,N-bzox)(X)(L)] {X = Br- (2), I- (3)}. All compounds were characterized by melting point, elemental analyses, infrared and 1H- and 13C{1H}-NMR spectroscopies revealing the complexes formation with the oxime coordinated to Pd(II) as C,N-chelating and the ethylenethiourea as a monodentate ligand via the sulfur atom. The cytotoxicity of cyclopalladated compounds has been evaluated in vitro against murine mammary tumor cell (LM3) showing cytotoxic activity similar to cisplatin

Computational Studies of Benzoxazinone Derivatives as Antiviral Agents against Herpes Virus Type 1 Protease

Herpes simplex virus infections have been described in the medical literature for centuries, yet the the drugs available nowadays for therapy are largely ineffective and low oral bioavailability plays an important role on the inefficacy of the treatments. Additionally, the details of the inhibition of Herpes Virus type 1 are still not fully understood. Studies have shown that several viruses encode one or more proteases required for the production new infectious virions. This study presents an analysis of the interactions between HSV-1 protease and benzoxazinone derivatives through a combination of structure-activity relationships, comparative modeling and molecular docking studies. The structure activity relationship results showed an important contribution of hydrophobic and polarizable groups and limitations for bulky groups in specific positions. Two Herpes Virus type 1 protease models were constructed and compared to achieve the best model which was obtained by MODELLER. Molecular docking results pointed to an important interaction between the most potent benzoxazinone derivative and Ser129, consistent with previous mechanistic data. Moreover, we also observed hydrophobic interactions that may play an important role in the stabilization of inhibitors in the active site. Finally, we performed druglikeness and drugscore studies of the most potent derivatives and the drugs currently used against Herpes virus