Inhibition of immune complex-mediated neutrophil oxidative metabolism: A pharmacophore model for 3-phenylcoumarin derivatives using GRIND-based 3D-QSAR and 2D-QSAR procedures

In this study, twenty hydroxylated and acetoxylated 3-phenylcoumarin derivatives were evaluated as inhibitors of immune complex-stimulated neutrophil oxidative metabolism and possible modulators of the inflammatory tissue damage found in type III hypersensitivity reactions. By using lucigenin- and luminol-enhanced chemiluminescence assays (CL-luc and CL-lum, respectively), we found that the 6,7-dihydroxylated and 6,7-diacetoxylated 3-phenylcoumarin derivatives were the most effective inhibitors. Different structural features of the other compounds determined CL-luc and/or CL-lum inhibition. The 2D-QSAR analysis suggested the importance of hydrophobic contributions to explain these effects. In addition, a statistically significant 3D-QSAR model built applying GRIND descriptors allowed us to propose a virtual receptor site considering pharmacophoric regions and mutual distances. Furthermore, the 3-phenylcoumarins studied were not toxic to neutrophils under the assessed conditions. (C) 2007 Elsevier Masson SAS. All rights reserved

Inhibiting effect of Dorstenia asaroides extracts on cariogenic properties of Streptococcus mutans

The aim of this study was to examine the effects of Dorstenia asaroides extracts on cariogenic properties of the most cariogenic bacteria, Streptococcus mutans. Hexane (HFr), ethyl-acetate (EFr) and chloroform (CFr) extracts obtained from D. asaroides rhizomes were submitted to chemical analyses, Minimal Inhibitory Concentrations (MIC), glycolysis assay and S. mutans 12-h-old initial biofilms. Chemical characterization showed that all the extracts present furanocoumarins. The MIC values were 80 (HFr and CFr) and 50 mu g/mL (EFr). Acid production by S. mutans cells was significantly disrupted by HFr (12.5 mg/mL), EFr (at 2.5; 6.25 and 12.5 mg/mL) and CFr (at 2.5, 6.25 and 12.5 mg/mL) (p < 0.01). Topical applications of HFr, EFr and CFr significantly reduced the colony forming units of S. mutans biofilms compared with those treated with control group in order to 20,30 and 25% respectively (p < 0.01). The results of the present study suggest that rhizomes of D. asaroides had inhibitory effects on cariogenic properties of S. mutans. (C) 2012 Elsevier Ltd. All rights reserved

In vitro study of antioxidant and scavenger properties of phenolic compounds from Lychnophora species

This paper describes the antioxidant effects of thirteen phenolic compounds isolated from plants of the genus Lychnophora. Two assays were performed to evaluate these effects: a cellular test that measured the luminol-enhanced chemiluminescence produced by neutrophils stimulated with opsonized zymosan and a cell-free test involving horseradish peroxidase-H2O2-luminol. In both assays, the antioxidant activity of the phenolic compounds was dependent on their concentration and chemical structure. Our results suggest that the ability of phenolic compounds from Lychnophora species to scavenge and inhibit the generation of ROS may be a mechanism underlying the anti-inflammatory activity of extracts from Lychnophora spp

Inhibiting effect of Dorstenia asaroides extracts on cariogenic properties of Streptococcus mutans

The aim of this study was to examine the effects of Dorstenia asaroides extracts on cariogenic properties of the most cariogenic bacteria, Streptococcus mutans. Hexane (HFr), ethyl-acetate (EFr) and chloroform (CFr) extracts obtained from D. asaroides rhizomes were submitted to chemical analyses, Minimal Inhibitory Concentrations (MIC), glycolysis assay and S. mutans 12-h-old initial biofilms. Chemical characterization showed that all the extracts present furanocoumarins. The MIC values were 80 (HFr and CFr) and 50 mu g/mL (EFr). Acid production by S. mutans cells was significantly disrupted by HFr (12.5 mg/mL), EFr (at 2.5; 6.25 and 12.5 mg/mL) and CFr (at 2.5, 6.25 and 12.5 mg/mL) (p < 0.01). Topical applications of HFr, EFr and CFr significantly reduced the colony forming units of S. mutans biofilms compared with those treated with control group in order to 20,30 and 25% respectively (p < 0.01). The results of the present study suggest that rhizomes of D. asaroides had inhibitory effects on cariogenic properties of S. mutans. (C) 2012 Elsevier Ltd. All rights reserved

Método para avaliação clínica da capacidade tamponante salivar A method for the clinical evaluation of salivary buffer capacity

O presente estudo teve por objetivo o desenvolvimento e a padronização de um método colorimétrico para avaliar a capacidade tamponante salivar média de nossa população. As amostras de saliva estimulada foram tituladas sem eliminação do CO2. Estudos foram realizados para verificar a influência da perda de CO2 das amostras durante o período necessário para a realização das titulações e para a padronização do tempo de leitura do pH. A partir das titulações realizadas nas amostras de saliva de 206 indivíduos de ambos os sexos na faixa etária de 5 a 50 anos, na proporção de 0,77:1:0,44, respectivamente para crianças, jovens e adultos, foram feitas as distribuições de freqüências dos casos, a determinação média do pH inicial, do pKa, microequivalentes relativos ao final da titulação, pH final da titulação e uma estimativa da porcentagem da saliva titulada em pH 5. Com base nestas variáveis foi estabelecida uma classificação dos indivíduos quanto à capacidade tamponante. Análise dos resultados utilizando-se 11, 12 ou 13 microequivalentes de H+/ml indicam que o valor de 11 microequivalentes/ml de saliva é o mais apropriado para a avaliação da capacidade tamponante salivar em nossa população.<br>The present study aimed to develop and standardize a colorimetric method for assessing salivary buffer capacity adapted to the features of the Brazilian population. Samples of stimulated saliva were titrated without CO2 elimination. The assessment was carried out to study the influence of the loss of CO2 from the samples during the few minutes necessary for titration, and to standardize the instants for measuring pH. Saliva samples were titrated from 206 individuals from both genders, between 5 and 50 years of age, and in a proportion of 0.77 : 1 : 0.44, respectively of children, youngsters, and adults. Case frequency distribution; determination of average values of initial pH, pKa, µ equivalents related to titration end point and final pH; and estimate of the percentage of saliva titrated at a pH of 5.0 were calculated based on the data collected. The results were used to classify individuals according to their salivary buffer capacity by colorimetric pH determinations using 11,12, and 13 µ equivalents of H+/ml saliva, and were compared to case frequency distribution obtained from saliva titration data. The results indicate that 11 µ equivalents H+/ml of saliva is the most appropriate for clinically evaluating the salivary buffer capacity of our population

Propriedades mecânicas do gastrocnêmio eletroestimulado pós-imobilização Mechanical properties of gastrocnemius eletrostimulated after immobilization

INTRODUÇÃO: As propriedades mecânicas (PM) consistem num instrumento de aplicabilidade clínica para profissionais de saúde que atuam no sistema músculo-esquelético. OBJETIVOS: Avaliar dois protocolos de estimulação elétrica neuromuscular (NMES) na potencialização do restabelecimento das PM no complexo músculo-tendíneo após imobilização segmentar de ratas. MATERIAIS E MÉTODOS: Foram utilizados 50 animais distribuídos em: Controle (GC, n=10); Imobilizado (GI, n=10); Imobilizado e remobilizado livre (GIL, n=10), Imobilizado e NMES uma vez ao dia (GIE1, n=10) e Imobilizado e NMES duas vezes ao dia (GIE2, n=10). A imobilização foi realizada por 14 dias. O GIL foi liberado posteriormente por 10 dias. A NMES foi aplicada pós-imobilização por 10 dias, GIE1 aplicado pela manhã (10 minutos) e, GIE2 aplicado pela manhã e à tarde (totalizando 20 minutos). Posteriormente, o músculo gastrocnêmio foi submetido ao ensaio mecânico de tração sendo as PM de rigidez, resiliência, carga e o alongamento no limite máximo avaliadas. RESULTADOS: A imobilização reduziu os valores das propriedades de carga e rigidez (p<0,05). A NMES utilizada duas vezes ao dia determinou resultados menos satisfatórios das PM avaliadas que àqueles obtidos uma vez ao dia e no grupo remobilizado (p>0,05). CONCLUSÃO: O músculo gastrocnênio tornou-se estruturalmente mais organizado frente à aplicação unitária da NMES e na remobilização.<br>INTRODUCTION: Mechanical properties (MP) are clinically applicable tools for healthcare professionals working on the musculoskeletal system. OBJECTIVES: The aim of this study was to evaluate two protocols of neuromuscular electric stimulation (NMES) to improve MP regeneration of the myotendinous complex after segment immobilization in female rats. MATERIALS AND METHODS: Fifty animals were equally distributed into five groups: Control (CG, n=10); Immobilized (IG, n=10); Immobilized and freely remobilized (IFG, n=10); Immobilized and NMES once /day (IEG1, n=10); Immobilized and MNES twice/day (IEG2, n=10). Immobilization was kept for 14 days, and remobilization was subsequently released for 10 days. NMES was applied for 10 days, post-immobilization, every morning for 10 minutes to IEG1 animals and every morning and afternoon (total 20 minutes) to the IEG2 group. After these procedures, the gastrocnemius muscle was submitted to the mechanical traction assay to evaluate stiffness, resilience, load and stretching at maximum limit MPs. RESULTS: Immobilization reduced the MP values concerning load and stiffness (p<0.05). Results for NMES applied twice a day were less satisfactory than the ones obtained with one application or in the remobilized group (p> 0.05). CONCLUSION: It is concluded that the gastrocnemius muscle became structurally better organized through a single NMES application and by remobilization

Propriedades mecânicas do músculo gastrocnêmio de ratas, imobilizado e posteriormente submetido a diferentes protocolos de alongamento Mechanical properties of gastrocnemius muscle of female rats immobilized and posteriorly submitted to different stretching protocols

O alongamento é amplamente utilizado na prática clínica da fisioterapia e no desporto, porém, as alterações mecânicas que essa técnica gera no músculo esquelético são pouco exploradas cientificamente. Este estudo avaliou as alterações mecânicas que acometem o músculo gastrocnêmio de ratas Wistar, adultas jovens, após 14 dias de imobilização e, secundariamente, submetido a alongamento manual passivo por 10 dias consecutivos, aplicado uma ou duas vezes ao dia. Foram utilizados 50 animais, sendo 10 para cada grupo: Controle (GC); Imobilizado (GI); Imobilizado e Liberado (GIL); Imobilizado e alongado uma vez ao dia (GIA1); e Imobilizado e alongado duas vezes ao dia (GIA2). O músculo gastrocnêmio foi submetido ao ensaio mecânico de tração, onde foram avaliadas as propriedades de carga e alongamento nos limites máximo e proporcional, além de rigidez e resiliência. A imobilização reduziu os valores das propriedades mecânicas de carga no limite máximo (CLM), carga no limite proporcional (CLP), alongamento no limite máximo (ALM), rigidez e resiliência, em 44,4%, 34,4%, 27,6%, 64,4% e 54%, respectivamente, quando comparados com os valores do GC. A remobilização livre e o alongamento restauraram as propriedades de CLM, CLP, ALM, rigidez e resiliência do músculo, exceto para o GIA2, que foi incapaz de restabelecer a propriedade de ALM (31,3% menor que GC). Concluí-se, portanto que, após 14 dias de imobilização segmentar, cargas individuais de alongamento e a livre movimentação permitem restituir as propriedades mecânicas do tecido muscular.<br>Stretching is widely employed in physiotherapeutic clinical practice and in sportive activities; however, the mechanical alterations of the skeletal muscle generated by this technique are poorly scientifically investigated. This study evaluated the mechanical alterations suffered by the gastrocnemius muscle of young adult female Wistar rats, submitted to14 days of immobilization followed by passive manual stretching during 10 consecutive days once or twice a day. Fifty animals were equally distributed in five groups, Control (CG); Immobilized (IG); Immobilized and liberated (ILG); Immobilized and submitted to stretching once a day (IEG1); Immobilized and submitted to stretching twice a day (IEG2). The gastrocnemius muscle was analyzed by mechanical traction assay and the properties related to load and maximal and proportional stretching evaluated in addition to stiffness and resilience. Immobilization decreased load at maximal thresholds (MTL), load at proportional thresholds (LPT), stretch at maximal thresholds (SMT), stiffness and resilience were reduced in 44.4%, 34.4%, 27.6%, 64.4% and 54% respectively, compared to CG values. With subsequent free remobilization and stretching, all parameters were restored except for IEG2 in which SMT remained reduced in 31.3%, when compared to CG. It is concluded that after 14 days of segmental immobilization, individual stretching loads and free movements contribute to regain muscle mechanical properties