Antihypertensive effect of carvacrol is improved after incorporation in ß-cyclodextrin as a drug delivery system.

Carvacrol (CARV), has been shown to possess various pharmacological properties, especially in the treatment of cardiovascular diseases. We evaluated the antihypertensive effect of the CARV free and encapsulation of CARV in ß-cyclodextrin (CARV/ß-CD), and whether CARV/ß-CD is able to improve the antihypertensive effects of CARV free in spontaneously hypertensive rats (SHR). The rats were randomly divided into four groups, each treated daily for 21 days and the mean arterial pressure and heart rate was measured every 5 days: group 1, Wistar-vehicle solution; group 2, SHR-vehicle; group 3, SHR-CARV 50 mg/kg/d; and group 4, CARV/ß-CD 50 mg/kg/d. After 21 days of treatment, the mesenteric artery from treated animals was tested for phenylephrine (Phe) and sodium nitroprusside (SNP) sensitivity. In addition, administration of CARV/ß-CD induced important antihypertensive activity when compared with the uncomplexed form, reducing the progression of arterial hypertension in SHR. Moreover, pharmacological potency to Phe in the SHR-CARV and CARV/ß-CD groups was increased, approaching values expressed in the Wistar-vehicle. Furthermore, CARV/ß-CD reduced the production of the pro-inflammatory mediator, IL-1ß, and increased anti-inflammatory cytokine, IL-10. Together, these results produced evidence that the encapsulation of CARV in ß-CD can improve cardiovascular activity, showing potential anti-inflammatory and antihypertensive effects.

Itaconimides derivatives induce relaxation in mesenteric artery and negative inotropism by inhibition of CA2+ influx.

BACKGROUND: The aim of this study was to evaluate the cardiovascular effects of N-phenyl-itaconimide (Imide-1), N-4-methyl-phenyl-itaconimide (Imide-2), N-4-methoxy-phenyl-itaconimide (Imide-3) and N-4-chloro-phenyl-itaconimide (Imide-4), and investigate the mechanisms of action involved in the observed responses. METHODS: The relaxant effect was investigated in rat superior mesenteric arteries by using isometric tension measurements. Additionally, in isolated atria were evaluated the heart rate and force of cardiac contraction and in vivo experiments was evaluated blood pressure and heart rate. RESULTS: Cumulative administration of itaconimides (3 × 10-8 to 3 × 10-4 M) in pre-contracted mesenteric artery rings with phenylephrine, 1 µM, induced endothelium-independent vasorelaxation. The itaconimides showed similar maximum efficacies. Additionally, Imide-3 induced vasorelaxation in rings exposed to a depolarizing-tyrode solution containing 60 mM KCl or 20 mM KCl similar to the control, suggesting the non-participation of K+ channels. Imide-3 attenuated Ca2+ influx in a concentration-dependent manner. As well, imide-3 reduced CaCl2-induced contraction in nominally calcium-free medium, in the presence of cyclopiazonic acid (20 µM), phenylephrine (1 µM) and nifedipine (1 µM), indicating a reduction of Ca2+ influx by receptor-operated channels (ROC) and store-operated channels (SOC). The presence of SKF 96365 (10-5 M), SOC blocker, did not significantly alter the vasorelaxant effect induced by imide-3. Moreover, imide-3 induced a negative inotropic effect. In vivo studies, in non-anesthetized normotensive rats, imide-3 lowered blood pressure and induced bradycardia. CONCLUSIONS: These results suggest that itaconimides have concentration-dependent vascular effects and the vasorelaxation seems to be endothelium-independent. The vasodilatory effect induced by imide-3 may be due to a possible influence on the CaV and ROC. In addition, imide-3 is able to reduce force of cardiac contraction, blood pressure and promote bradycardia.

Antihypertensive potential of linalool and linalool complexed with ß-cyclodextrin: Effects of subchronic treatment on blood pressure and vascular reactivity.

Linalool (LIN) is a monoterpene alcohol present in some aromatic medicinal plants with biological activities that can impact cardiovascular diseases. This chemical class is highly volatile and ß-cyclodextrin (ß-CD) has been employed to improve the pharmacological properties of monoterpenes. Thus, the aim of this study was to evaluate the cardiovascular effects of LIN free focusing on the antihypertensive properties of this monoterpene and to study whether LIN, complexed in ß-cyclodextrin (LIN-ßCD) is able to improve the pharmacological activity of LIN. Spontaneously hypertensive rats (SHR) were randomly divided into 5 groups, each treated daily for 21 days, in the following manner: group 1 (vehicle solution); group 2 (captopril; 30 mg/kg/day); group 3 (LIN; 100 mg/kg/day); group 4 (LIN; 50 mg/kg/day) and group 5 (LIN/ß-CD; 50 mg/kg/day). Daily body weight measurements were conducted and mean arterial pressure and heart rate were measured every 5 days. The mesenteric artery from treated animals was tested for phenylephrine and sodium nitroprusside (SNP) sensitivity. The SHR treated with vehicle demonstrated progressive increase in mean arterial pressure and captopril, a positive control, induced a significant decrease. After 21 days of treatment, the blood pressure of the SHR treated by (-)-LIN (100 mg/kg) was significantly reduced. In addition, various important cardiovascular parameters improved, including: the treatment with LIN prevented the development of cardiac hypertrophy, increased levels of the anti-inflammatory cytokine (IL-10), increased vasodilator responsiveness and reduced sensitivity to the sympathetic agonist. Furthermore, the inclusion complex containing LIN in ß-CD produced a higher antihypertensive profile when compared with uncomplexed form. Taking together, our results suggested that LIN shown a potential antihypertensive effect and ß-CD may be an important tool to improve the cardiovascular activity of LIN and other water-insoluble compounds.

Scientometric profile of physiotherapists Brazilian scientists / Perfil cientométrico dos fisioterapeutas cientistas brasileiros

Abstract Introduction: Knowledge of Brazilian scientists profile is important to understand the factors that influence the behavior of those interested in developing science. Objective: To outline the profile of Brazilian physiotherapist researchers, permanent, or collaborator professors of PhD programs in physiotherapy. Methods: Study of documentary analysis with scientometric techniques on physiotherapist data in Brazilian doctors associated professors in PhD programs. To identify the professors, the Sucupira and Lattes Platforms were used, and the research areas were categorized according to COFFITO. Data on the research area, the number of orientations, publications and impact factor average (JCR) were analyzed by 1-way ANOVA test (p < 0.05), and a collaboration network was built using Gephi 0.9.1 software. Results: Nine institutions of higher education in Brazil have a PhD in physiotherapy. A total of 119 professors are associated with UFMG (20.2%), UFSCAR (17.6%), UFRN (13.4%), and UNINOVE (10.9%). The median number of doctors graduated by the professors was 1.0 (0.0 - 6.0) and in publications in the period was 4.6 (2.4 - 8.4). The main study designs were observational 71 (59.7%), and the main research area was neurofunctional 25 (21.0%). The collaboration between UFSCAR and UFMG professors is strengthened. Conclusion: There are few specific doctoral programs for physiotherapists in Brazil. The majority of them are concentrated in the southeast region, and the professor staff have very heterogeneous characteristics related to the duration of the programs, the nature of the institution, or the affiliation of the professor.

Resumo Introdução: Conhecer o perfil dos cientistas brasileiros é importante para compreender fatores que influenciam os comportamentos dos interessados em desenvolver ciência. Objetivo: Delinear o perfil dos Fisioterapeutas doutores pesquisadores brasileiros, docentes permanentes ou colaboradores dos programas de doutorado em Fisioterapia. Métodos: Estudo de análise documental com técnicas de Cientometria sobre dados de fisioterapeutas doutores brasileiros docentes de programas de doutorado. Para identificar os profissionais, foram utilizadas as Plataformas Sucupira e Lattes e as áreas de pesquisa foram categorizadas de acordo com o COFFITO. Dados sobre área de pesquisa, número de orientações, publicações e média do fator de impacto (JCR) foram analisados pelo teste ANOVA Oneway (p<0,05) e uma rede de colaboração foi construída com auxílio do software Gephi 0.9.1. Resultados: Nove instituições de ensino superior no Brasil possuem doutorado específico em Fisioterapia. Um total de 119 doutores estão vinculados majoritariamente à UFMG (20,2%), UFSCAR (17,6%), UFRN (13,4%) e UNINOVE (10,9%). A mediana de doutores formados pelos docentes foi de 1,0 (0,0 - 6,0) e de publicações foi de publicações no período foi de 4,6 (2,4;8,4). Os principais desenhos de estudo foram observacionais 71 (59,7%) e a principal área de pesquisa foi a neurofuncional 25 (21,0%). A colaboração entre os docentes da UFSCAR e UFMG é consolidada. Conclusão: Existem poucos programas de doutoramento específico para Fisioterapeutas no Brasil. Sua maioria se concentra na região sudeste e os docentes pesquisadores apresentam características bastante heterogêneas, relacionadas ao tempo de existência dos programas, à natureza da instituição ou filiação do docente.