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Lippia alba (erva-cidreira) is often mentioned in Brazilian ethnopharmacological studies. Although its leaves have been used to treat hypertension, few studies have evaluated its hypotensive effects. This work aimed to evaluate the haemodynamic effects of Lippia alba methanolic extract and to characterise its chemical composition. Normotensive rats received an intravenous injection of L. alba extract. Systolic, diastolic, mean arterial pressures, and electrocardiographic data were analysed.1H-qNMR and LC-MS were used to assess the chemical composition. L. alba extract had significant hypotensive effects on systolic, diastolic, and mean arterial pressure. Acteoside was identified as major compound (292.6 ± 2.7 mg/g). Sixty-one other compounds were tentatively identified, mainly phenylethanoids, flavonoids, and iridoids. L. alba extract reduces systolic, diastolic, mean arterial pressure, and appears to be associated with a reduction in heart rate. Acteoside, a known hypotensive compound, may be responsible for these effects, but other structurally similar minority compounds may also contribute.
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Drimys winteri J.R. Forst. & G. Forst (D.C) G. Gray, var. chilensis (canelo) is an endemic tree from Chile. Since pre-Columbian times, it has produced a fruit known as the canelo pepper, (pimienta de canelo) or Foye pepper, which can be used as a spice. The chemical and biological analysis of canelo fruits is reported for the first time in this study, that is, its phenolic fingerprinting by UHPLC-PDA- Q-orbitrap MS, the antioxidant activity, the enzymatic inhibitory activity, and its relaxation effects on rat aorta. The proximal composition and the mineral content (Ca: 1.45 ± 0.03 mg/100 g; Mg: 7.72 ± 0.03 mg/100 g; Fe: 4.54 ± 0.21 mg/100 g; Zn: 2.99 ± 0.02 mg/100 g; Mn: 1.08 ± 0.03 mg/100 g; Cu: 0.82 ± 0.02 mg/100 g; K: 53.03 ± 0.20 mg/100 g; Na: 0.087 ± 0.00 mg/100 g) are also reported. The canelo fruits showed a total phenolic content of 57.33 ± 0.82 mg GAE/g dry weight. In addition, the total flavonoid content was 38.42 ± 1.32 mg equivalent of QE/g dry weight. The antioxidant activity was evaluated by employing DPPH and ABTS methods (IC50 of 6.65 ± 0.5 and 9.5 ± 0.05 µg/mL, respectively), ORAC (25.33 ± 1.2 µmol Trolox/g dry plant) and FRAP (45.56 ± 1.32 µmol Trolox/g dry plant). The enzymatic inhibition of acetylcholinesterase, butyrylcholinesterase, and tyrosinase (IC50: 1.94 ± 0.07, 2.73 ± 0.05, and 9.92 ± 0.05 µg extract/mL, respectively) is also reported. Canelo extract led to an 89% relaxation of rat aorta. Our results confirm that D. winteri fruits are a rich source of secondary metabolites and can inhibit enzymes associated with neurodegenerative diseases; the results also suggest that canelo may induce a potentially hypotensive effect in rat aorta. The study demonstrates the medicinal properties of canelo fruit and spice.
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Gypothamnium pinifolium Phil. (Asteraceae) is a small shrub that grows in the Paposo Valley of the II Antofagasta Region of Chile. This initial study is of the high-resolution phenolic fingerprinting, antioxidant activity, the relaxation effects in rat aorta, the inhibitory enzyme potential, plus the antiproliferative activity of the ethyl acetate and n-hexane extract from G. pinifolium and its two major isolated secondary metabolites (one coumarin: 2-nor-1,2-secolycoserone, and one diterpene: ent-labda-8,13-E-diene-15-ol). The study involves using ultra-high-performance liquid chromatography todiode array detection coupled with Q-Orbitrap mass spectrometry analysis (UHPLC-PDA-Orbi-trap-MS), in which various compounds were identified, including specific coumarins. The n-hexane extract showed total phenolic and flavonoid contents of 517.4 ± 12.5 mg GAE/100 g extract and 72.3 ± 3.7 mg QE/100 g extract, respectively. In addition, the antioxidant activity of the n-hexane extract was assessed using in-vitro assays such as bleaching of DPPH and ABTS (IC50: 14.3 ± 0.52 and 2.51 ± 0.43 µg extract/mL, respectively), FRAP (347.12 ± 1.15 µmol Trolox equivalent/g extract), and ORAC (287.3 ± 1.54 µmol Trolox equivalents/g extract). Furthermore, the inhibition against cholinesterases (acetylcholinesterase (AChE) 4.58 ± 0.04 µg/mL, butyrylcholinesterase (BChE) IC50: 23.44 ± 0.03 µg/mL) and tyrosinase (IC50: 9.25 ± 0.15 µg/mL) enzymes of the n-hexane extract, and main compounds (IC50: 1.21 ± 0.03 µg/mL, 11.23 ± 0.02 µg/mL, 3.23 ± 0.12 µg/mL, and 103.43 ± 16.86 µg/mL, correspondingly for the most active coumarin 1) were measured. The antiproliferative potential of the extracts and the two principal compounds against several solid human cancer cells was investigated. All of them showed good activity against cancer cells. Label-free live-cell imaging studies on HeLa cells exposed to the isolated coumarin and the diterpene enabled the observation of cell death and several apoptotic hallmarks. Our results indicate that G. pinifolium Phil. is a valuable source of secondary metabolites with potential activity against noncommunicable diseases.
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Abstract Aim: to compare the impact of different resistance exercise orders on postexercise hemodynamic measures in resistance-trained nonhypertensive middle-aged and older women. Methods: Twenty-three women (age 50-78 yrs) were randomized into two resistance training (RT) groups: one group started training sessions performing multi-joint exercises followed by single-joint exercises (MS, n = 12; 58.92 ± 5.53 yrs), while the other group performed their sessions in the opposite order (SM, n = 11; 57.93 ± 11.89 yrs). Both groups performed their RT sessions composed of 7 exercises performed in 3 sets of 10-15 repetitions maximum. Blood pressure was measured by automated equipment during pre-training and at 10, 20, 30, 40, 50, and 60 min after the training session. Results: Repeated-measures analysis of variance (ANOVA) identified an isolated effect of time only for systolic blood pressure (p = 0.003) with statistically significant reductions in pre-session measurement at 60 min post-session in both groups (MS: 117.67 ± 15.89 mmHg vs. 111.25 ± 11.84 mmHg and SM: 118.64 ± 15.13 mmHg vs. 111.50 ± 15.62 mmHg). Regarding diastolic blood pressure and subjective perception of effort, no difference was identified between groups (p > 0.05). Conclusion: We conclude that a RT session can promote post-exercise hypotension for systolic blood pressure after 60 min of recovery in middle-aged and nonhypertensive older women regardless of the exercise order.
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ETHNOPHARMACOLOGICAL RELEVANCE: Cecropia pachystachya Trécul (Urticaceae) is a medicinal plant popularly known as 'embaúba'. In Brazil, the leaves of this species are used for the treatment of various kidney and cardiovascular diseases. However, there are no detailed studies on the renal and cardiovascular activities of this species. No studies on the anatomy or the quality control of this herbal drug is available thus far. AIM: This study was aimed to investigate the ethnopharmacological properties of the leaves of C. pachystachya. MATERIAL AND METHODS: The leaves of C. pachystachya were analyzed by light and scanning electron microscopy for pharmacobotanical and anatomical characterization. The ethanol-soluble fraction of C. pachystachya leaf extract (ESCP) was characterized by high-performance liquid chromatograph equipped with diode array detector and mass spectrometry (HPLC-DAD-MS). The acute oral toxicity of ESCP on female Wistar rats was assessed. The acute and prolonged diuresis and antioxidant effects of ESCP (30, 100, and 300 mg/kg) were evaluated in male Wistar rats. In addition, the hypotensive effects of the ESCP as well as the vasodilatory activity in isolated and perfused mesenteric vascular beds were investigated. RESULTS: The anatomical markers obtained in this study can help in the identification of C. pachystachya, as well as to distinguish it from the other 'embaúbas'. The metabolites found in the ESCP were phenolic compounds, mainly C- and O-glycosylated flavonoids. The ESCP did not exhibit any toxic effects at a dose of 2000 mg/kg. Significant diuretic activities were observed at the doses of 30, 100, and 300 mg/kg. In addition, a significant modulating activity of the tissue redox state was observed after prolonged treatment. On the other hand, no hypotensive or vasodilator activity was observed. CONCLUSION: The key findings of the present study can contribute to the taxonomy, species identification and quality control of C. pachystachya. Chemical studies have shown the presence of glycosylated flavonoids, phenylpropanoid derivative and proanthocyanidins. The pharmacological studies showed significant diuretic and antioxidant effects of C. pachystachya leaf extract, indicating a possible validation of its popular medicinal use.
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Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Cecropia/química , Diuréticos/farmacologia , Diuréticos/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Animais , Pressão Arterial/efeitos dos fármacos , Brasil , Feminino , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Frequência Cardíaca/efeitos dos fármacos , Masculino , Oxirredução/efeitos dos fármacos , Fenilpropionatos/farmacologia , Fenilpropionatos/uso terapêutico , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/citologia , Plantas Medicinais/química , Proantocianidinas/farmacologia , Proantocianidinas/uso terapêutico , Ratos Wistar , Urina/química , Vasodilatadores/farmacologia , Vasodilatadores/uso terapêuticoRESUMO
Resumen Actualmente, se recomienda el ejercicio contra resistencia (ECR) como una de las estrategias no farmacológicas para el control y tratamiento de la presión arterial (PA). Sin embargo, es necesario profundizar esta línea de investigación. El propósito del estudio fue comparar el efecto del tipo de descanso al realizar ECR sobre la PA de participantes normotensos. Participaron nueve hombres; siguiendo un diseño de investigación de medidas repetidas, realizaron tres condiciones experimentales en orden aleatorio: a) Descanso Activo (DA), b) Descanso Pasivo (DP), c) Sesión Control. En las 3 sesiones, se midió la PA y la frecuencia cardíaca (FC) pre-tratamiento, 1 minuto post-sesión y cada 10 minutos post-tratamiento durante 120 minutos. Las sesiones experimentales estuvieron precedidas por: mediciones antropométricas, familiarización y aplicación del test de 1RM. En el análisis estadístico se aplicó ANOVA de 2 vías para medidas repetidas, análisis de efectos simples y post hoc de Tukey. Entre los principales resultados, se encontró que, en comparación con la sesión control, los valores de PA disminuyen de forma significativa (p < .05): 1) al realizar ECR utilizando DP y DA a los 50, 100, 110 minutos post-ejercicio; 2) posterior a ejecutar ECR utilizando DA a los 20, 30, 70, 80,100, 120 minutos; 3) después de finalizada la sesión ECR con DP a los 10, 40 y 120 minutos. Respecto a la medición pre-test, los valores de PA disminuyeron de forma significativa (p < .05) a los 10, 20, 40, 50, 60, 100 y 120 minutos post ECR utilizando DP. En conclusión, al comparar con los valores de PA mostrados en un día de control, la ejecución de ECR aplicando DP y DA es funcional en el control de la PA de hombres jóvenes normotensos. En relación al pre-test, se podría indicar que el DP es el que promueve el efecto hipotensivo del ECR.
Abstract Resistance exercise is currently recommended as a non-pharmacological strategy to control and treat blood pressure, but further research is necessary concerning this topic. The purpose of this paper is to compare the effect of types of rest on the blood pressure of normotensive individuals while performing resistance exercise. Following a random methodological design with repeated measurements, nine men performed three experimental conditions on different days: a) Active Rest, b) Passive Rest, and c) Control Session. During the three sessions, blood pressure and heart rate measurements were taken pre-treatment, one-minute post-session, and every 10 minutes post-treatment for 120 minutes. Experimental sessions were preceded by anthropometric measurements, familiarization, and taking the 1RM test. The statistical analysis was conducted using two-way ANOVA with repeated measurements and Tukey post-hoc analysis. One of the main results indicated that, compared to the control session, blood pressure decreased significantly (p<0.05): 1) When performing resistance exercise with active and passive rest at 50, 100, 110 minutes post-exercise; 2) After executing resistance exercise with active rest at 20, 30, 70, 80,100, and 120 minutes; 3) After performing resistance exercise session with passive rest at 10, 40, and 120 minutes. With respect to pre-test levels, blood pressure decreased significantly (p<0.05) at 10, 20, 40, 50, 60, 100, and 120 minutes after performing resistance exercise with passive rest. In conclusion, compared with a control day, in the case of young normotensive males, the inclusion of both passive and active rest is functional for controlling blood pressure. In relation to the pre-test, passive rest promotes a hypotensive effect in the study population.
Resumo Recomenda-se, atualmente, o exercício contrarresistência (ECR) como uma das estratégias não farmacológicas para o controle e tratamento da pressão arterial (PA). Não obstante, é preciso aprofundamento nesta linha de pesquisa. O propósito do estudo foi comparar o efeito do tipo de descanso ao realizar ECR sobre a PA de participantes normotensos. Participaram nove homens; seguindo um desenho de pesquisa de medidas repetidas, realizaram três condições experimentais em ordem aleatória: a) Descanso Ativo (DA), b) Descanso Passivo (DP) e c) Sessão Controle. Nas 3 sessões, foram solicitadas a PA e a frequência cardíaca (FC) pré-tratamento, 1 minuto pós-sessão e a cada 10 minutos pós-tratamento durante 120 minutos. As sessões experimentais foram precedidas por: medições antropométricas, familiarização e aplicação do teste de 1RM. Na análise estatística aplicou-se a ANOVA de 2 vias com medidas repetidas, a análise de efeitos simples e o teste pós-hoc de Tukey. Entre os principais resultados, observou-se que, em comparação com a sessão controle, os valores de PA diminuíram de maneira significativa (p < 0,05): 1) ao realizar ECR, usando DP e DA nos 50, 100, 110 minutos pós-exercício; 2) posterior à execução do ECR usando DA nos 20, 30, 70, 80,100, 120 minutos; 3) depois de finalizar a sessão ECR com DP nos 10, 40 e 120 minutos. Com relação à medição pré-teste, os valores de PA diminuíram de maneira significativa (p < 0,05) nos 10, 20, 40, 50, 60, 100 e 120 minutos pós-ECR usando DP. Em conclusão, ao fazer a comparação com os valores de PA mostrados em um dia de controle, a execução de ECR aplicando DP e DA é funcional no controle da PA de homens jovens normotensos. Com relação ao pré-teste, poderia indicar-se que o DP é o promotor do efeito hipotensivo do ECR.
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Humanos , Adulto , Pressão Arterial , Treino Aeróbico , DescansoRESUMO
Abstract Purpose: To establish a hypotensive brain death pig model and observe the effects of hypotension on small bowel donors. Methods: The hypotensive brain death model was produced using the modified intracranial water sac inflation method in ten domestic crossbred pigs. Effects of hypotensive brain death on small bowel tissue morphology were evaluated through changes in intestinal tissue pathology, tight junction protein of the intestinal mucosa and plasma intestinal fatty acid-binding protein (i-FABP) levels. The pathophysiological mechanism was examined based on changes in superior mesenteric artery (SMA) blood flow and systemic hemodynamics. Results: After model establishment, SMA blood flow, and the mean arterial pressure (MAP) significantly decreased, while heart rate increased rapidly and fluctuated significantly. Small bowel tissue morphology and levels of tight junction protein of the intestinal mucosa showed that after model establishment, small bowel tissue injury was gradually aggravated over time (P<0.05). Plasma i-FABP levels significantly increased after brain death (P<0.05). Conclusions: A hypotensive brain death pig model was successfully established using an improved intracranial water sac inflation method. This method offers a possibility of describing the injury mechanisms more clearly during and after brain death.
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Animais , Masculino , Feminino , Morte Encefálica/fisiopatologia , Modelos Animais de Doenças , Hipotensão/fisiopatologia , Intestino Delgado/patologia , Intestino Delgado/transplante , Suínos , Fatores de Tempo , Biópsia , Ensaio de Imunoadsorção Enzimática , Western Blotting , Reprodutibilidade dos Testes , Microscopia Eletrônica de Transmissão , Proteínas de Ligação a Ácido Graxo/sangue , Proteína da Zônula de Oclusão-1/análise , Hemodinâmica , Intestino Delgado/irrigação sanguíneaRESUMO
To explore the mechanistic basis behind smooth muscle relaxant prospective of Bismarckia nobilis in gastrointestinal, respiratory and cardiovascular ailments. The methanolic extract of B. nobilis and sub-fractions have been evaluated in vitro rabbit isolated tissues, in vivo castor oil-induced diarrhea in rats and charcoal meal activity in mice. The B. nobilis extract relaxed spontaneous and K+(80 mM)- induced contractions in rabbit isolated jejunum preparations, CCh (1 µM) and K+ (80 mM)-induced contractions in tracheal and bladder preparations, PE (1 µM) and K+ (80 mM)-induced concentrations in aorta preparations, likewise verapamil. Spasmolytic activity of dichloromethane fraction is stronger as compared to aqueous fraction. In vivo castor oil-induced diarrhea in rats and charcoal meal activity in mice further supported spasmolytic activity. B. nobilis extract possess anti-spasmodic, anti-diarrheal, airway relaxant and vasodilator activities possible mediated through calcium channel blocking mechanism, justifying therapeutic utility of B. nobilis in diarrhea, asthma and hypertension.
El objetivo de trabajo fue explorar el mecanismo de acción relacionado con el efecto relajante del músculo liso inducido por Bismarckia nobilis (B. nobilis) en enfermedades gastrointestinales, respiratorias y cardiovasculares. El extracto metanólico de B. nobilis y subfracciones fue evaluado in vitro en tejidos aislados de conejos. Además se evaluó diarrea in vivo inducida con aceite de ricino en ratas y la actividad de harina de carbón vegetal en ratones. El extracto de B. nobilis relajó tanto las contracciones espontáneas como las inducidas por K+(80 mM) en preparaciones de yeyuno aisladas de conejos, las contracciones inducidas por PE (1 µM) y K+(80 mM) inducidas en preparaciones de aorta; de manera similar a verapamilo. La actividad espasmolítica de la fracción de diclorometano es más potente en comparación con la fracción acuosa. La diarrea inducida in vivo por el aceite de ricino en ratas y la actividad de la harina de carbón vegetal en ratones apoyaron aún más la actividad espasmolítica. El extracto de B. nobilis posee actividades antiespasmódicas, antidiarreicas, relajantes de las vías respiratorias y vasodilatadoras, posibles a través del mecanismo de bloqueo de los canales de calcio, lo que justifica la utilidad terapéutica de B. nobilis en la diarrea, el asma y la hipertensión.
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Animais , Coelhos , Ratos , Extratos Vegetais/farmacologia , Antiasmáticos/farmacologia , Arecaceae , Antidiarreicos/farmacologia , Anti-Hipertensivos/farmacologia , Aorta/efeitos dos fármacos , Asma/metabolismo , Traqueia/efeitos dos fármacos , Bloqueadores dos Canais de Cálcio/farmacologia , Diarreia/metabolismo , Metanol , Hipotensão/metabolismo , Jejuno/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacosRESUMO
Purpose: To establish a hypotensive brain death pig model and observe the effects of hypotension on small bowel donors. Methods: The hypotensive brain death model was produced using the modified intracranial water sac inflation method in ten domestic crossbred pigs. Effects of hypotensive brain death on small bowel tissue morphology were evaluated through changes in intestinal tissue pathology, tight junction protein of the intestinal mucosa and plasma intestinal fatty acid-binding protein (i-FABP) levels. The pathophysiological mechanism was examined based on changes in superior mesenteric artery (SMA) blood flow and systemic hemodynamics. Results: After model establishment, SMA blood flow, and the mean arterial pressure (MAP) significantly decreased, while heart rate increased rapidly and fluctuated significantly. Small bowel tissue morphology and levels of tight junction protein of the intestinal mucosa showed that after model establishment, small bowel tissue injury was gradually aggravated over time (P 0.05). Plasma i-FABP levels significantly increased after brain death (P 0.05). Conclusions: A hypotensive brain death pig model was successfully established using an improved intracranial water sac inflation method. This method offers a possibility of describing the injury mechanisms more clearly during and after brain death.(AU)
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Animais , Suínos/cirurgia , Transplantes/classificação , Intestinos/cirurgia , Morte Encefálica/veterináriaRESUMO
Talisia esculenta (A. St.-Hil.) Radlk. is a large tree belonging to family Sapindaceae and popularly known as "pitombeira" or "pitomba." Although species have relevant economic and medicinal uses in Brazil, no study has investigated its effectiveness as a diuretic, hypotensive, and antihypertensive agent. The aim of this study was to present a detailed anatomical and histochemical study for T. esculenta and provide important safety and efficacy parameters. After morpho-anatomical and microchemical study, a purified aqueous extract (ethanol soluble fraction obtained from T. esculenta [ESTE]) was obtained, and detailed phytochemical investigation was performed. Subsequently, acute oral toxicity test was performed in male and female rats. Moreover, diuretic, hypotensive, and antihypertensive effects on normotensive and spontaneously hypertensive rats (SHR) were investigated. Finally, the effects of prolonged treatment with ESTE on serum levels of nitrite, thiobarbituric acid reactive species, and nitrotyrosine were also measured in SHR. Oral treatment with ESTE did not induce acute toxic effects and did not affect urine production, blood pressure, or heart rate of normotensive and SHR. Prolonged treatment with ESTE was able to increase serum nitrite levels and significantly reduce oxidative and nitrosative stress markers in SHR. Data obtained showed that ESTE has a significant antioxidant activity without showing any clinical signs of acute toxicity. The use of this species as a diuretic, hypotensive, or antihypertensive agent should be carried out with caution, since administration in rodents did not produce renal and/or hemodynamic responses that justify this indication.
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Anti-Hipertensivos/uso terapêutico , Hipertensão/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Sapindaceae , Animais , Anti-Hipertensivos/administração & dosagem , Anti-Hipertensivos/química , Biodiversidade , Brasil , Dieta , Modelos Animais de Doenças , Etnofarmacologia , Feminino , Masculino , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Ratos , Ratos WistarRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Luehea divaricata Mart. (Malvaceae) is an important medicinal species that is widely used as a diuretic in the Brazilian Pantanal region. An ethanolic supernatant that was obtained from an infusion of leaves of this species (ESLD) was recently shown to exert hypotensive and diuretic activity. Nevertheless, the secondary metabolites that are responsible for this activity and the molecular mechanisms of pharmacological action remain unknown. AIM: We performed a detailed study to identify possible active metabolites that are present in different ESLD fractions and investigated their effects on renal and peripheral arteriolar tone. We further evaluated their interrelations with sustained diuretic and hypotensive actions. MATERIALS AND METHODS: The ESLD was first obtained from L. divaricata leaves, and liquid-liquid fractionation was performed. The fractions were analyzed by liquid chromatography-mass spectrometry. An ethyl acetate fraction (AceFr), n-butanolic fraction (ButFr), and aqueous fraction (AqueFr) were then orally administered in male Wistar rats in a single dose or daily for 7 days. The doses were previously defined based on the yield that was obtained from each fraction. Hydrochlorothiazide was used as a positive control. Blood pressure, heart rate, urinary volume, pH, density, and urinary sodium, potassium, chloride, and calcium levels were measured. Serum levels of nitrite, thiobarbituric acid reactive species, nitrotyrosine, aldosterone, vasopressin, and plasma angiotensin converting enzyme activity were also measured. Finally, the direct effects of the ButFr on renal and mesenteric arteriolar tone and the role of nitric oxide and prostaglandins in the renal and hemodynamic effects were investigated. RESULTS: Of the fractions that were tested, only the ButFr exerted significant diuretic and saluretic effects. The AceFr and ButFr also had acute hypotensive effects, but only the ButFr maintained its response after 7 days of treatment. Prolonged treatment with the ButFr increased serum nitrite levels and significantly reduced oxidative and nitrosative markers of stress. Additionally, the ButFr caused a vasodilatory response in the renal and mesenteric arteriolar beds through the release of nitric oxide and prostaglandins. Finally, the diuretic and hypotensive effects of the ButFr were completely blocked by pretreatment with Nω-nitro-L-arginine methyl ester and indomethacin, thus demonstrating the direct involvement of nitric oxide and prostaglandins in these effects. CONCLUSION: The ButFr that was obtained from Luehea divaricata exerted sustained diuretic and hypotensive effects. These effects were apparently attributable to the release of nitric oxide and prostaglandins, which reduce renal and peripheral arteriolar tone and lead to an increase in the glomerular filtration rate and a reduction of global peripheral resistance. These findings suggest that the ButFr may be a potential complementary therapy for several conditions in which diuretic and hypotensive effects are required.
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Anti-Hipertensivos/farmacologia , Diuréticos/farmacologia , Malvaceae , Extratos Vegetais/farmacologia , Animais , Anti-Hipertensivos/análise , Arteríolas/efeitos dos fármacos , Arteríolas/fisiologia , Pressão Sanguínea/efeitos dos fármacos , Diuréticos/análise , Rim/irrigação sanguínea , Rim/efeitos dos fármacos , Rim/fisiologia , Masculino , Mesentério/efeitos dos fármacos , Mesentério/fisiologia , Óxido Nítrico/fisiologia , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/análise , Folhas de Planta , Prostaglandinas/fisiologia , Ratos Wistar , Artéria Renal/efeitos dos fármacos , Artéria Renal/fisiologiaRESUMO
The genus Eugenia sp. (Myrtaceae) comprises plants with reported antioxidant and antidiarrheal capability among other therapeutic potentials. The aim of this study was to evaluate the antimicrobial activity of essential oil; diuretic and hypotensive activities of aqueous extracts from leaves of Eugenia uniflora. The antimicrobial activity was evaluated . The diuretic and hypotensive activities were evaluated in normotensive Wistar rats by measuring blood pressure and urine flow after received four different concentrations of aqueous extracts (10%, 15%, 20% and 25%). Essential oil inhibited the growth of Candida parapsilosis and Candida albicans with MIC values lower than 14.41 mg/mL, equal to 57.75 mg/mL for Candida krusei. Among antibacterial effect, essential oil inhibited growth with a MIC equals to 153.93 mg/mL for all strains tested, except for Escherichia coli (MIC equals to 307.96 mg/mL. Aqueous extracts showed powerful reductions of the arterial pressure (34% and 31% lower than the control), after administration of 10% and 25% of aqueous extract, respectively. However, the animals that received the aqueous extract at the 15% and 20% concentrations presented a discrete hypotensive effect (20% and 21% lower than control group, respectively) concomitantly to powerful diuretic effect (280% and 91% higher than control group, respectively). These data confirmed the potential biological effect of this species, and represents an important step toward a depth study on the therapeutic properties of this species
O gênero Eugenia sp. (Myrtaceae) compreende plantas com capacidade antimicrobiana e antioxidante entre outros potenciais terapêuticos. O objetivo deste estudo foi avaliar a atividade antimicrobiana de óleo essencial; atividade diurética e hipotensora de extrato aquoso de folhas de Eugenia uniflora. A atividade antimicrobiana foi avaliada pela determinação da concentração inibitória mínima (MIC) e concentração mínima bactericida (MBC) de cepas bacterianas e concentração fungicida mínima (MFC) para fungos. A atividade diurética e hipotensora foi avaliada em ratos Wistar normotensos pela mensuração da pressão sanguínea e fluxo urinário após administração de quatro diferentes concentrações de extrato aquoso (10%, 15%, 20% e 25%). Óleo essencial inibiu o crescimento de Candida parapsilosis e Candida albicans com valores de MIC menores que 14,41 mg/mL, igual a 57,75 mg/mL para Candida krusei. A respeito do efeito antimicrobiano, o óleo essencial inibiu o crescimento de todas as cepas testadas, com MIC igual a 153,93 mg/mL, exceto para Escherichia coli (MIC igual a 307.96 mg/mL). O extrato aquoso mostrou redução importante da pressão arterial (34% e 31% quando comparado ao controle), após administração de 10% e 25% do extrato aquoso, respectivamente. Contudo, os animais que receberam o extrato aquoso na concentração de 15% e 20% apresentaram discreto efeito hipotensor (20% e 21% menor que o grupo controle, respectivamente) concomitantemente ao importante efeito diurético (280% e 91% maior quando comparado ao grupo controle, respectivamente). Esses achados confirmam o potencial efeito biológico dessa espécie, e representa um importante embasamento para estudos relacionados as propriedades terapêuticas da Eugenia uniflora
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Humanos , Óleos , Diuréticos , Eugenia , Hiperglicemia , Anti-Infecciosos , Antifúngicos , Anti-Hipertensivos , Brasil , DNA Polimerase Dirigida por DNA , AntioxidantesRESUMO
This study compared the effect of a strength training session performed at different exercise orders and rest intervals on blood pressure and heart rate variability (HRV). Fifteen trained men performed different upper body exercise sequences [large to small muscle mass (SEQA) and small to large muscle mass (SEQB)] in randomized order with rest intervals between sets and exercises of 40 or 90 seconds. Fifteen repetition maximum loads were tested to control the training intensity and the total volume load. The results showed, significant reductions for systolic blood pressure (SBP) for all sequences compared to baseline and, post-exercise: SEQA90 at 20, 30, 40, 50 and 60 minutes; SEQA40 and SEQB40 at 20 minutes and SEQB90 at 10, 20, 30, 40, 50 and 60 minutes. For diastolic blood pressure (DBP), significant reductions were found for three sequences compared to baseline and, post-exercise: SEQA90 and SEQA40 at 50 and 60 minutes; SEQB40 at 10, 30 and 60 minutes. For HRV, there were significant differences in frequency domain for all sequences compared to baseline. In conclusion, when performing upper body strength training sessions, it is suggested that 90 second rest intervals between sets and exercises promotes a post-exercise hypotensive response in SBP. The 40 second rest interval between sets and exercises was associated with greater cardiac stress, and might be contraindicated when working with individuals that exhibit symptoms of cardiovascular disease.
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ETHNOPHARMACOLOGICAL RELEVANCE: Although Luehea divaricata Mart. (Malvaceae) is popularly used by the population of the Brazilian Pantanal for the treatment of different types of kidney diseases, no study has been carried out to prove this ethnobotanical indication. AIM: To investigate the possible cardiorenal effects of an herbal preparation obtained from L. divaricata leaves. MATERIALS AND METHODS: First, to provide quality control standards, a detailed morphological and microchemical characterization of L. divaricata leaves was performed. Then, the purified aqueous extract was obtained from the leaves of this species (ESLD) and a thorough phytochemical characterization was performed. Subsequently, acute oral toxicity test was performed after single administration of different doses (5, 50, 300, 2000mg/kg) in male and female Wistar rats. Finally, the diuretic, hypotensive and antioxidant properties of ESLD (30, 100, 300mg/kg) were evaluated after acute and prolonged treatment and the role of angiotensin converting enzyme, aldosterone, vasopressin, and nitric oxide in these effects was investigated. RESULTS: Analyses performed by liquid chromatography-mass spectrometry showed that the main secondary metabolites present in ESLD were flavonol O-glycosides and flavone C-glycosides. Acute and prolonged treatment with ESLD was able to expressively increase urinary volume and electrolyte excretion. Mean blood pressure and systolic blood pressure were also significantly reduced after acute treatment. Moreover, treatment with ESLD was able to reduce thiobarbituric acid reactive species and increase serum nitrate levels. CONCLUSION: The data obtained showed that ESLD has an important diuretic and hypotensive effect, which is probably dependent on the reduction of oxidative stress and increased bioavailability of nitric oxide.
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Anti-Hipertensivos/farmacologia , Antioxidantes/farmacologia , Diuréticos/farmacologia , Malvaceae , Extratos Vegetais/farmacologia , Animais , Anti-Hipertensivos/toxicidade , Antioxidantes/toxicidade , Pressão Sanguínea/efeitos dos fármacos , Brasil , Diuréticos/toxicidade , Etnofarmacologia , Feminino , Nefropatias , Masculino , Óxido Nítrico/sangue , Extratos Vegetais/toxicidade , Folhas de Planta , Ratos Wistar , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Testes de Toxicidade AgudaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Acanthospermum hispidum DC. is an important medicinal herb that belongs to family Asteraceae, popularly used as a diuretic and hypotensive in the region of Pantanal, state of Mato Grosso do Sul, Brazil. Despite the relevance of this species throughout the country, there are no detailed studies about its possible ethnobotanical indication. AIM: To carry out a detailed ethnopharmacological investigation of the cardio-renal properties of A. hispidum. MATERIALS AND METHODS: First, a detailed morpho-anatomical study with the purpose of characterizing and providing quality control parameters for the species was carried out. Then, purified aqueous extract (ESAH) was obtained and a detailed phytochemical investigation about its main secondary metabolites was performed. In addition, a thorough acute toxicological study was conducted to evaluate the actual toxic effects of this preparation. Finally, the possible diuretic and hypotensive effects of ESAH on male Wistar rats (30, 100, 300mg/kg; intraduodenally) were evaluated, and using pharmacological antagonists or inhibitors, the involvement of prostaglandin/cAMP and nitric oxide/cGMP pathway and potassium channels in ESAH-induced hypotension was investigated. RESULTS: The analyses performed by liquid chromatography-mass spectrometry showed that the main secondary metabolites present in ESAH were phenolic compounds, such as caffeoylquinic acids (chlorogenic acid), dicaffeoylquinic acids and glycosylated flavonoids (quercetin glucoside and galactoside). ESAH did not induce any acute toxic effects and did not affect the urinary volume or renal excretion of electrolytes in Wistar rats. On the other hand, intraduodenal administration of ESAH induces a significant acute hypotensive effect. Previous treatment with N(G)-nitro-L-arginine methyl ester, methylene blue, or tetraethylammonium fully avoided the hypotensive effect of ESAH. All other parameters were not affected by treatment with ESAH. CONCLUSION: Data obtained in this study allow us to suggest that ESAH obtained from A. hispidum presents an important acute hypotensive effect, which appears to be dependent on the nitric oxide/cGMP pathway. This study presents new evidences about the therapeutic potential of this species when acute hypotensive response is required.
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Asteraceae/química , Coração/efeitos dos fármacos , Rim/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Pressão Sanguínea/efeitos dos fármacos , Brasil , Cromatografia Líquida , Relação Dose-Resposta a Droga , Frequência Cardíaca/efeitos dos fármacos , Masculino , Ratos , Ratos Wistar , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
BACKGROUND: Previous studies have not been able to correlate manometry findings with bolus perception. The aim of this study was to evaluate correlation of different variables, including traditional manometric variables (at diagnostic and extreme thresholds), esophageal shortening, bolus transit, automated impedance manometry (AIM) metrics and mood with bolus passage perception in a large cohort of asymptomatic individuals. METHODS: High resolution manometry (HRM) was performed in healthy individuals from nine centers. Perception was evaluated using a 5-point Likert scale. Anxiety was evaluated using Hospitalized Anxiety and Depression scale (HAD). Subgroup analysis was also performed classifying studies into normal, hypotensive, vigorous, and obstructive patterns. KEY RESULTS: One hundred fifteen studies were analyzed (69 using HRM and 46 using high resolution impedance manometry (HRIM); 3.5% swallows in 9.6% of volunteers were perceived. There was no correlation of any of the traditional HRM variables, esophageal shortening, AIM metrics nor bolus transit with perception scores. There was no HRM variable showing difference in perception when comparing normal vs extreme values (percentile 1 or 99). Anxiety but not depression was correlated with perception. Among hypotensive pattern, anxiety was a strong predictor of variance in perception (R2 up to .70). CONCLUSION AND INFERENCES: Bolus perception is less common than abnormal motility among healthy individuals. Neither esophageal motor function nor bolus dynamics evaluated with several techniques seems to explain differences in bolus perception. Different mechanisms seem to be relevant in different manometric patterns. Anxiety is a significant predictor of bolus perception in the context of hypotensive motility.
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Ansiedade/psicologia , Transtornos da Motilidade Esofágica/diagnóstico , Manometria/métodos , Percepção , Adolescente , Adulto , Idoso , Esôfago , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Adulto JovemRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Although Alibertia edulis (L.C. Rich.) A.C. Rich decoction is used in Brazilian folk medicine due to its possible antihypertensive effect, this species has never been critically investigated as a hypotensive drug. So, the aim of this study was to evaluate the possible hypotensive and antihypertensive effects of the oral administration of Alibertia edulis aqueous extract (AEAE) in normotensive and hypertensive rats, and evaluate its inter-relation with a possible diuretic activity. MATERIAL AND METHODS: Different doses of AEAE (20, 65 and 200mg/kg) were tested on the mean arterial pressure (MAP) of normotensive Wistar rats and after induction of renovascular hypertension (two-kidney, one-clip Goldblatt model). In addition, the diuretic effects of AEAE were compared with hydrochlorothiazide (HCTZ) in an acute and repeated-dose treatment for 7 days. Volume, sodium, potassium, chloride, calcium contents, pH and density were estimated in urine samples collected after 8 or 24h. Plasma sodium, potassium, total protein, urea, creatinine, AST and ALT concentrations were measured in samples collected at the end of the experimental period (seventh day). Finally, the antioxidant activity of the AEAE was assessed using the DPPH radical scavenging and ferric ions reducing power assay. RESULTS: The intraduodenal administration of the HCTZ and AEAE significantly reduced, in a dose-dependent manner, the MAP in both normotensive and hypertensive rats. Otherwise, the heart rate was not affected by any treatment. Acute and prolonged oral administration of AEAE (200mg/kg) and HCTZ caused a significant increase in volume and urinary concentrations of sodium, potassium and chloride. Moreover, urinary calcium concentration was significantly increased after administration of AEAE (200mg/kg). Finally, AEAE was able to present important in vitro antioxidant properties. CONCLUSION: The results obtained have shown that AEAE presents potent diuretic activity and significant hypotensive and antihypertensive effect. In addition, this study may confirm part of the pharmacological activity popularly attributed to this species and opens perspective for the future use in various renal and cardiovascular diseases.
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Anti-Hipertensivos/uso terapêutico , Diuréticos/uso terapêutico , Hipertensão/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Rubiaceae , Animais , Pressão Sanguínea/efeitos dos fármacos , Brasil , Rim/efeitos dos fármacos , Masculino , Compostos Fitoquímicos/análise , Folhas de Planta , Ratos WistarRESUMO
ABSTRACT Celery (Apium graveolens L., Apiaceae) is one of the popular aromatic vegetables and part of the daily diet around the world. In this study, aqueous-ethanolic and hexane extracts of celery seed were prepared and the amount of n-butylphthalide, as an active component, was determined in each extract. Then the effects of hexanic extract on systolic, diastolic, mean arterial blood pressure and heart rate were evaluated in an invasive rat model. The vasodilatory effect and possible mechanisms of above mentioned extracts on aorta ring were also measured. High performance liquid chromatography analysis revealed that hexanic extract contains significantly higher amounts of n-butylphthalide, compared to aqueous-ethanolic extract. The results indicated that hexanic extract significantly decreased the systolic, diastolic, mean arterial blood pressure and heart rate in normotensive and hypertensive rats. Our data revealed that celery seed extract exerts its hypotensive effects through its bradycardic and vasodilatory properties. Moreover, the active components in celery seed extracts could induce their vasodilatory properties through Ca2+ channel blocking activity in endothelial and non-endothelial pathways and particularly by interference with the extra or intracellular calcium.
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The effects of the dietary addition of 2.5% (w/w) Amaranthus mantegazzianus protein isolate (AI) on blood pressure, lipid profiles and antioxidative status of Wistar rats were evaluated. Six diets were used to feed animals during 28 days: (base (AIN93G), Chol (cholesterol 1%, w/w), CE (α-tocopherol 0.005%, w/w), CholE (cholesterol 1% (w/w) + α-tocopherol 0.005%, w/w), CAI (AI 2.5% w/w), CholAI (cholesterol 1% (w/w) + AI 2.5%, w/w). Lipid profiles of plasma and liver and faecal cholesterol content were analyzed. Antioxidant status was evaluated by the ferric reducing activity of plasma (FRAP), the 2-thiobarbituric acid (TBA) assay and superoxide dismutase (SOD) activity in plasma and liver. Blood pressure was measured in the tail artery of rats. CholA group presented a significant (α < 0.05) reduction (16%) in the plasma total cholesterol. In liver, the intake of cholesterol (Chol group) induced a significant increment in cholesterol and triglycerides (2.5 and 2.3 times, respectively), which could be decreased (18% and 47%, respectively) by the addition of AI (CholA group). This last group also showed an increased faecal cholesterol excretion (20%). Increment (50%) in FRAP values, diminution of TBA value in plasma and liver (70% and 38%, respectively) and diminution of SOD activity (20%) in plasma of CholA group suggest an antioxidant effect because of the intake of AI. In addition, CA and CholA groups presented a diminution (18%) of blood pressure after 28 days.
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Amaranthus/química , Antioxidantes/análise , Pressão Sanguínea/efeitos dos fármacos , Dieta , Lipídeos/análise , Proteínas de Plantas/farmacologia , Animais , Antioxidantes/química , Colesterol/análise , Colesterol/sangue , Colesterol na Dieta/administração & dosagem , Fezes/química , Lipídeos/sangue , Fígado/química , Fígado/enzimologia , Masculino , Oxirredução , Proteínas de Plantas/administração & dosagem , Ratos , Ratos Wistar , Superóxido Dismutase/sangue , Superóxido Dismutase/metabolismo , Triglicerídeos/sangue , alfa-Tocoferol/administração & dosagemRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Although Echinodorus grandiflorus, Cuphea carthagenensis, and Phyllanthus tenellus infusions are used in Brazilian folk medicine due to their possible diuretic effect, none of these species was critically investigated as a diuretic drug. So, the aim of this study was to evaluate the possible acute diuretic activity of ethanol soluble fractions (ES) obtained from these species and assess the relationship between renal cortical blood flow and their antioxidant and hypotensive activity using normotensive Wistar rats. MATERIAL AND METHODS: The preparation obtained from E. grandiflorus (ES-EG), C. carthagenensis (ES-CC), and P. tenellus (ES-PT) infusions was orally administered in a single dose to rats. Urine excretion rate, pH, density, conductivity and Na(+), K(+), Cl(-) and HCO3(-) contents were measured in the urine of saline-loaded animals. Concentration of electrolytes, total protein, urea, creatinine, and angiotensin converting enzyme (ACE) activity were evaluated in collected serum. The involvement of the renal cortical blood flow and antioxidative activity in the hypotensive and diuretic effects was also determined. RESULTS: Water and Na(+), Cl(-) and Na(+) excretion rates were significantly increased by ES-EG, while urinary bicarbonate excretion was reduced. Moreover, ES obtained from E. grandiflorus was able to significantly increase renal blood flow and reduce mean arterial pressure and oxidative stress in "in vitro" and "in vivo" models. All other parameters evaluated were not affected by any treatment. CONCLUSION: The results presented here shown that the ES-EG obtained from E. grandiflorus leaves shown a significant diuretic and hypotensive activity and suggest that these effects could be related with an important renal and systemic vasodilator effect. In addition, it was shown for the first time that the pharmacological effects of ES obtained from P. tenellus and C. carthagenensis do not support its popular use as a diuretic agent.