The search for new antihypertensive drugs has grown in recent years because of high rate of morbidity among hypertensive patients and several side effects that are associated with the first-line medications. The current study sought to investigate the antihypertensive effect of a newly synthesized pyrazole derivative known as 5-(1-(3 fluorophenyl)-1H-pyrazol-4-yl)-2H-tetrazole (LQFM-21). Spontaneously hypertensive rats (SHR) were used to evaluate the effect of LQFM-21 on mean arterial pressure (MAP), heart rate (HR), renal vascular conductance (RVC), arterial vascular conductance (AVC), baroreflex sensitivity (BRS) index, and vascular reactivity. Acute intravenous (iv) administration of LQFM-21 (0.05, 0.1, 0.2, and 0.4 mg kg-1) reduced MAP and HR, and increased RVC and AVC. Chronic oral administration of LQFM-21 (15 mg kg-1) for 15 days reduced MAP without altering BRS. The blockade of muscarinic receptors and nitric oxide synthase by intravenous infusion of atropine and L-NAME, respectively, attenuated cardiovascular effects of LQFM-21. In addition, ex vivo experiments showed that LQFM-21 induced an endothelium-dependent relaxation in isolated aortic rings from SHR. This effect was blocked by guanylyl cyclase inhibitor (ODQ) and L-NAME. These findings suggest the involvement of muscarinic receptor and NO/cGMP pathway in the antihypertensive and vasodilator effects of LQFM-21.

Abstract:The hydrolysis of bradykinin (Bk) by different classes of proteases in plasma and tissues leads to a decrease in its half-life. Here, Bk actions on smooth muscle and in vivo cardiovascular assays in association with a protease inhibitor, Black eyed-pea trypsin and chymotrypsin inhibitor (BTCI) and also under the effect of trypsin and chymotrypsin were evaluated. Two synthetic Bk-related peptides, Bk1 and Bk2, were used to investigate the importance of additional C-terminal amino acid residues on serine protease activity. BTCI forms complexes with Bk and analogues at pH 5.0, 7.4 and 9.0, presenting binding . Formation of BTCI-Bk complexes is probably driven by hydrophobic forces, coupled with slight conformational changes in BTCI. In vitro assays using guinea pig (Cavia porcellus) ileum showed that Bk retains the ability to induce smooth muscle contraction in the presence of BTCI. Moreover, no alteration in the inhibitory activity of BTCI in complex with Bk and analogous was observed. When the BTCI and BTCI-Bk complexes were tested in vivo, a decrease of vascular resistance and consequent hypotension and potentiating renal and aortic vasodilatation induced by Bk and Bk2 infusions was observed. These results indicate that BTCI-Bk complexes may be a reliable strategy to act as a carrier and protective approach for Bk-related peptides against plasma serine proteases cleavage, leading to an increase in their half-life. These findings also indicate that BTCI could remain stable in some tissues to inhibit chymotrypsin or trypsin-like enzymes that cleave and inactivate bradykinin in situ.

Escopo e Objetivos: estudar as causas de internação hospitalar é uma forma de conhecer o perfil de morbi-mortalidade de uma população. O objetivo deste estudo foi avaliar as causas de internação hospitalar entre adultos num hospital municipal da Amazônia Legal, MT. Metodologia: Foram analisados 400 prontuários de pacientes internados de 19 a 59 anos de idade. Resultados: Houve predominância do gênero masculino, jovem, internado para procedimentos cirúrgicos (64,3%), prevalecendo como causa de internação os acidentes e causas externas. Ademais, houve o uso em média de 4,1 medicamentos por prescrição, caracterizando polifarmácia o que não é recomendado pela OMS. Conclusões: neste hospital os principais casos de internação de adultos, do gênero masculino, foram internados para cirurgia e acometidos por causas externas, o que revela falhas na prevenção primária a acidentes de trânsito e outras causas externas.           Palavras-chave: hospitalização; adultos; prescrições de medicamentos

OBJETIVO: Comparar a percepção relacionada à qualidade de vida entre pacientes submetidos à hemodiálise e voluntários saudáveis.MÉTODOS: Trata-se de um estudo caracterizado como transversal. A qualidade de vida foi avaliada pelo questionário Kidney of Disease Quality of Life-Short Form. O estudo foi realizado com pacientes (n=35) de um centro de diálise da cidade de Goiânia-GO (Brasil) e voluntários de uma Unidade de Estratégia de Saúde da Família (n=34) entre janeiro e março de 2013. A análise estatística foi descritiva, associativa, comparativa, consistência interna e regressão linear múltipla.RESULTADOS: Os sintomas da doença, sobrecarga da doença e função sexual tiveram o coeficiente Cronbach α superiores a 0.70. A regressão múltipla mostrou associação da idade com declínio da qualidade de vida dos pacientes.CONCLUSÕES: Os pacientes em hemodiálise tiveram redução dos aspectos relacionados à qualidade de vida quando comparados com sujeitos saudáveis nas dimensões físicas e emocionais. Além disso, a idade foi a única variável que influenciou a qualidade de vidas nestes pacientes.

Objective: To evaluate the effect of curcumin supplementation on the body compositions and biochemical parameters of Brazilian women with high waist circumferences. Materials and methods: This is a blind, randomized, placebo-controlled clinical trial conducted in 2016 with 35 Brazilian women with high waist circumference (WC). In total, 80 participants were randomized [38 in the placebo group (PG) and 42 in the supplemented group (SG)], but at the end of the protocol, 20 individuals in the PG and 15 in the SG were evaluated. The sample consumed one capsule of curcumin (500 mg/day) (Curcumin C3 Complex ® ) or a placebo for 90 days. Body weight, height, body mass index, WC, body fat, fat free mass, fasting glucose (FG), lipid profile [triglycerides (TGs), total cholesterol (TC), HDL-c and LDL-c], physical activity level and food intake (energy, carbohydrate, total fat and protein) data were evaluated before and after the intervention. Results: Curcumin supplementation reduced body mass (p < 0.040) but did not alter other anthropometric parameters or body composition (p ≥ 0.050). In relation to the biochemical profile, the SG saw reductions in FG (p < 0.001), TGs (p < 0.001) and TC (p = 0.001) compared with the PG. At the baseline and during the intervention, the practice of physical activity and food intake did not differ between the SG and PG (p ≥ 0.050). Conclusion: Curcumin supplementation improved the blood glucose and lipid profile of Brazilian women with high WC, without altering body composition. New studies with larger sample sizes and longer durations are important for identifying more robust data regarding the proposal of this work.