Peptide Prodrugs for the Treatment of CNS Disorders: A Perspective for New Drugs

The treatment of central nervous system (CNS) diseases is a major challenge. The presence of the barrier intended to protect the brain from unwanted molecules also impairs the efficacy of CNS-targeted drugs. The discovery of drug targets for CNS diseases opens a door for the selective treatment of these diseases. However, the physicochemical properties of drugs, including their hydrophilic properties and their peripheral metabolism, as well as the blood-brain barrier, can adversely affect the therapeutic potential of CNS-targeted drugs. Although peptides are often metabolized by enzymes, they are of particular interest for the treatment of CNS diseases or as carriers to deliver drugs to the brain. In this review, we discuss the use of peptides as potential prodrugs for the treatment of CNS diseases.

Determinação das alterações biomecânicas de idosos caidores e não caidores submetidos a protocolo incremental de fadiga

Pós-graduação em Fisioterapia - FCT

Efeitos da estimulação elétrica neuromuscular nas circuitarias medulares inibitórias de sujeitos crônicos após acidente vascular cerebral

Pós-graduação em Fisioterapia - FCT

New drugs with antiprotozoal activity from marine algae: a review

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Risk factors that may signify a propensity to the use of drugs in students at a public university

Introduction: We sought to evaluate the risk factors that may increase the propensity to use licit and illicit drugs among students at a public university. Methods: The project involved students (n = 268) enrolled in the first and fourth years of courses in the areas of the social and biological sciences at a public university. Data collection was conducted by means of self-administered, semistructured questionnaires, based on such standardized assessment instruments as Audit, Assist, Cage and Duse. Collected data were analyzed quantitatively by calculating the percentages and evaluating the data in terms of categories of risk, classifying them by age, gender, religion, schooling, use (before or after entering university) and contexts of use. By means of this survey the researchers were able to correlate the use of drugs to the risk factors that might increase the students’ propensity to use these substances. Results: The results revealed a high proportion of current drug-using students, but showed no significant differences between the first and fourth year students as regards contexts of use. However, 67% of students regarded the university environment as encouraging the use of drugs. Students pointed to such major risk factors as friends’ and fellow-students’ influence, university parties, excessive curiosity and desire to experiment. Conclusion: Due to the high rate of drug use among university students, by the determination of the risk factors related to the university environment and also knowing that the process of addiction is one of growing chemical dependence, the importance of the development and implementation of public health policies at all levels, especially in terms of approaches and specific interventions addressing this population, should be noted.

Discriminant analysis of neuromuscular variables in chronic low back pain

Background: Investigation and discrimination of neuromuscular variables related to the complex aetiology of low back pain could contribute to clarifying the factors associated with symptoms. Objective: Analysing the discriminative power of neuromuscular variables in low back pain. Methods: This study compared muscle endurance, proprioception and isometric trunk assessments between women with low back pain (LBP, n=14) and a control group (CG, n=14). Multivariate analysis of variance and discriminant analysis of the data were performed. Results: The muscle endurance time (s) was shorter in the LBP group than in the CG (p=0.004) with values of 85.81 (37.79) and 134.25 (43.88), respectively. The peak torque (Nm/kg) for trunk extension was 2.48 (0.69) in the LBP group and 3.56 (0.88) in the GG (p=0.001); for trunk flexion, the mean torque was 1.49 (0.40) in the LBP group and 1.85 (0.39) in the CG (p=0.023). The repositioning error (degrees) before the endurance test was 2.66 (1.36) in the LBP group and 2.41 (1.46) in the CG (p=0.664), and after the endurance test, it was 2.95 (1.94) in the LBP group and 2.00 (1.16) in the CG (p=0.06). Furthermore, the variables showed discrimination between the groups (p=0.007), with 78.6% of the individuals with low back pain correctly classified in the LBP group. In turn, variables related to muscle activation showed no difference in discrimination between the groups (p=0.369). Conclusion: Based on these findings, the clinical management of low back pain should consist of both resistance and strength training, particularly in the extensor muscles.

Mucoadhesive beads of gellan gum/pectin intended to controlled delivery of drugs

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

5CN05 partitioning in an aqueous two-phase system: A new approach to the solubilization of hydrophobic drugs

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Antiplatelet drugs reduce the immunoinflammatory response in a rat model of periodontal disease

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Nanotechnological Strategies for Vaginal Administration of Drugs-A Review

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Mutagenic potential of Cordia ecalyculata alone and in association with Spirulina maxima for their evaluation as candidate anti-obesity drugs

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Eletroestimulação neuromuscular na reabilitação da disfagia orofaríngea

The rehabilitation of oropharyngeal dysphagia has a new therapeutic tool, the neuromuscular electrical stimulation (NMES), and the most renowned researchers have been studying the applicability and the results of this approach. The aim of this study was to present a literature review regarding the applicability of NMES in the rehabilitation of oropharyngeal dysphagia. An extensive literature review was carried out, considering the last two decades of research in the area. The review showed that there is still no consensus on the use of NMES in the rehabilitation of dysphagia. It was found that most studies described the use of NMES in isolation, did not describe the techniques associated with speech-language therapy associated to electrotherapy, and used heterogeneous samples that clustered mechanical and neurogenic oropharyngeal dysphagia. Only recently specific programs have been designed and tested in more homogeneous populations.

Métodos de estudo da transmissão neuromuscular

Este trabalho tem como objetivo documentar as atividades realizadas no Estágio Curricular Obrigatório do curso de Graduação em Física Médica, realizado no Laboratório de Farmacologia da Junção Neuromuscular do Departamento de Farmacologia do Instituto de Biociências da UNESP de Botucatu. O estágio englobou atividades relacionadas à Instrumentação e à Iniciação Científica, ambas visando ao estudo da Farmacologia da Transmissão Neuromuscular. Desta forma, neste relatório serão apresentados, inicialmente, uma breve revisão dos aspectos fundamentais da morfologia e da fisiologia da junção neuromuscular. Posteriormente, serão descritos os métodos de estudo da transmissão neuromuscular aprendidos no decorrer do estágio, especificamente, as técnicas miográfica, que permite o registro da contração muscular, e eletrofisiológica, que possibilita o registro de atividade elétrica celular, ambas in vitro. Finalizando, serão apresentados os resultados do Projeto de Iniciação Científica desenvolvido, cujo objetivo foi estudar a ação do extrato etanólico da planta Tabernaemontana catharinensis sobre o bloqueio neuromuscular induzido por toxinas ofídicas na preparação do nervo frênico-músculo diafragma isolado de camundongos

Efeito da interação entre Bothropstoxina-I e Crotapotina na junção neuromuscular de camundongos “in vitro”: estágio em iniciação científica

A bothropstoxina-I (BthTX-I) é uma fosfolipase A2 (PLA2) Lys49 miotóxica isolada do veneno da Bothrops jararacussu. Embora seja desprovida de atividade neurotóxica in vivo, esta toxina bloqueia a transmissão neuromuscular in vitro. A relação entre as atividades miotóxica e paralisante da BthTX-I ainda não está esclarecida. A crotapotina corresponde à subunidade não-enzimática da crotoxina, principal fração tóxica do veneno da Crotalus durissus terrificus. Isoladamente a crotapotina é atóxica, porém atua como carreadora da PLA2 Asp49 da crotoxina, potencializando sua ação neurotóxica. Esta proteína também é capaz de se complexar com outras PLA2s (Asp49 ou Lys49) de venenos ofídicos, alterando suas toxicidades. Neste trabalho avaliamos a influência da crotapotina sobre o bloqueio neuromuscular e a atividade miotóxica da BthTX-I in vitro. Preparações do nervo frênico-músculo diafragma de camundongos machos foram montadas em cubas para o registro das contrações musculares evocadas direta e indiretamente. Cortes transversais do músculo foram submetidos à coloração por hematoxilina e eosina para a avaliação do padrão morfológico. A BthTX-I (1 μM) isoladamente, ou pré-incubada com crotapotina (2 M) à 35 ºC por 30 minutos, foram adicionadas às preparações. A análise dos dados foi realizada por testes não paramétricos (p<0.05). A BthTX-I induziu bloqueio irreversível e tempo-dependente das contrações musculares diretas e indiretas. O tempo para o bloqueio de 50% das contrações indiretas (18,98 ± 1,94 min, n=4) foi significativamente menor que o das diretas (45,97 ± 5,61 min, n=5). A pré-incubação com a crotapotina não alterou de forma significativa o bloqueio das contrações diretas ou indiretas induzidos pela BthTX-I. Isoladamente, a crotapotina não afetou as contrações... (Resumo completo, clicar acesso eletrônico abaixo)