RESUMEN
OBJECTIVES: The COVID-19 pandemic has differentially impacted cardiovascular disease (CVD) mortality worldwide. Causes of death misclassification may be one of the reasons. We evaluated the impact of the pandemic on CVD mortality in Brazil, comparing underlying causes (UCs) and multiple causes (MCs) of death. STUDY DESIGN: Ecological time-series study. METHODS: An ecological, time-series study was conducted analysing age-standardised death rates for CVD, from epidemiological week (EW) 10/2020 to 39/2021, using data from the Mortality Information System, Brazil. CVD was defined using the International Classification of Diseases (ICD-10) coding, if reported as UC or MC of death. Observed and expected data (mean for the same EW, 2017-2019) were compared. Risk ratios (RiRs) were analysed, and 95% confidence intervals (CIs) were calculated. RESULTS: Age-standardised mortality rate for CVD as UC of death was 165.8 (95%CI: 165.4-166.3) per 100,000 inhabitants, similar to what was expected (165.6/100,000, 95%CI: 165.2-166.1, RiR = 1.00). There was increased out-of-hospital mortality (RiR = 1.18; 95%CI: 1.17-1.19) and deaths of ill-defined causes (RiR = 1.43; 95%CI: 1.42-1.44). The increase in out-of-hospital deaths was more pronounced in the North (RiR = 1.33; 95%CI 1.30-1.36) region, with a less resilient health system. Conversely, as MCs of death, there was a 10% increase in CVD mortality (observed: 243.2 [95%CI: 242.7-243.7], expected: 221.6 [95%CI: 221.1-222.1] per 100,000). An increase also occurred in the North and Central West regions (RiR = 1.16; 95%CI: 1.15-1.18), among men (RiR = 1.11; 95%CI: 1.11-1.12) and individuals aged ≥60 years (RiR = 1.11; 95%CI: 1.10-1.11). CONCLUSIONS: During the pandemic, mortality rates for CVD as MCs of death increased in Brazil, whereas as UC mortality rates did not change. Higher out-of-hospital mortality, misclassification, and competing causes of death may explain this pattern.
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Tiliroside is a glycosidic flavonoid present in many plants species including Helicteres velutina K. Schum (Malvaceae sensu lato), commonly known in Brazil as "pitó". This molecule has been shown to have many biological activities, however no study has been carried out to investigate the toxicity of this substance. The present work aimed to evaluate the possible cellular toxicity in silico, in vitro and ex-vivo of the kaempferol-3-O-β-D-(6-E-p-coumaroyl) glucopyranoside (tiliroside), through chemical structure analysis, toxicity assessment and predictive bioactive properties, using human samples for in vitro and ex-vivo tests. The in silico analysis suggests that tiliroside exhibited great absorption index when penetrating biological membranes. In addition, it also displayed considerable potential for cellular protection against free radicals, and anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and antithrombotic activities. The assessment of the hemolytic and genotoxic effects of tiliroside showed low hemolysis rates in red blood cells and absence of cellular toxicity in the oral mucosa cells. The data obtained indicate that this molecule could be a promising therapeutic approach as a possible new drug with biotechnological potential.(AU)
O tilirosídeo é um flavonóide glicosídico presente em muitas espécies de plantas, incluindo Helicteres velutina K. Schum (Malvaceae sensu lato), conhecida no Brasil como pitó. Esta molécula mostrou ter muitas atividades biológicas, porém nenhum estudo foi realizado para investigar a toxicidade dessa substância. O presente trabalho teve como objetivo avaliar a possível toxicidade celular in silico, in vitro e ex-vivo do kaempferol-3-O-β-D- (6 -Ep-coumaroil) glucopiranosídeo (tilirosídeo), por meio de análises de estrutura química, toxicidade avaliação e propriedades bioativas preditivas, utilizando amostras humanas para testes in vitro e ex-vivo. A análise in silico sugere que o tilirosídeo exibe bom índice de absorção para penetrar nas membranas biológicas. Além disso, apresentou considerável potencial de proteção celular contra os radicais livres e com atividades anticarcinogênica, antioxidante, antineoplásica, antiinflamatória, anti-hemorrágica e antitrombótica. A avaliação dos efeitos hemolíticos e genotóxicos do tilirosídeo mostrou baixas taxas de hemólise nas hemácias e ausência de toxicidade em células da mucosa oral. Os dados obtidos indicam que esta molécula pode possuir uma abordagem terapêutica promissora como uma possível nova droga com potencial biotecnológico.(AU)
Asunto(s)
Flavonoides/farmacocinética , Flavonoides/toxicidad , Malvaceae , Técnicas In VitroRESUMEN
Abstract Tiliroside is a glycosidic flavonoid present in many plants species including Helicteres velutina K. Schum (Malvaceae sensu lato), commonly known in Brazil as "pitó". This molecule has been shown to have many biological activities, however no study has been carried out to investigate the toxicity of this substance. The present work aimed to evaluate the possible cellular toxicity in silico, in vitro and ex-vivo of the kaempferol-3-O-β-D-(6"-E-p-coumaroyl) glucopyranoside (tiliroside), through chemical structure analysis, toxicity assessment and predictive bioactive properties, using human samples for in vitro and ex-vivo tests. The in silico analysis suggests that tiliroside exhibited great absorption index when penetrating biological membranes. In addition, it also displayed considerable potential for cellular protection against free radicals, and anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and antithrombotic activities. The assessment of the hemolytic and genotoxic effects of tiliroside showed low hemolysis rates in red blood cells and absence of cellular toxicity in the oral mucosa cells. The data obtained indicate that this molecule could be a promising therapeutic approach as a possible new drug with biotechnological potential.
Resumo O tilirosídeo é um flavonóide glicosídico presente em muitas espécies de plantas, incluindo Helicteres velutina K. Schum (Malvaceae sensu lato), conhecida no Brasil como "pitó". Esta molécula mostrou ter muitas atividades biológicas, porém nenhum estudo foi realizado para investigar a toxicidade dessa substância. O presente trabalho teve como objetivo avaliar a possível toxicidade celular in silico, in vitro e ex-vivo do kaempferol-3-O-β-D- (6 "-Ep-coumaroil) glucopiranosídeo (tilirosídeo), por meio de análises de estrutura química, toxicidade avaliação e propriedades bioativas preditivas, utilizando amostras humanas para testes in vitro e ex-vivo. A análise in silico sugere que o tilirosídeo exibe bom índice de absorção para penetrar nas membranas biológicas. Além disso, apresentou considerável potencial de proteção celular contra os radicais livres e com atividades anticarcinogênica, antioxidante, antineoplásica, antiinflamatória, anti-hemorrágica e antitrombótica. A avaliação dos efeitos hemolíticos e genotóxicos do tilirosídeo mostrou baixas taxas de hemólise nas hemácias e ausência de toxicidade em células da mucosa oral. Os dados obtidos indicam que esta molécula pode possuir uma abordagem terapêutica promissora como uma possível nova droga com potencial biotecnológico.
Asunto(s)
Humanos , Extractos Vegetales , Quempferoles/toxicidad , Flavonoides , Simulación por Computador , BrasilRESUMEN
Tiliroside is a glycosidic flavonoid present in many plants species including Helicteres velutina K. Schum (Malvaceae sensu lato), commonly known in Brazil as "pitó". This molecule has been shown to have many biological activities, however no study has been carried out to investigate the toxicity of this substance. The present work aimed to evaluate the possible cellular toxicity in silico, in vitro and ex-vivo of the kaempferol-3-O-β-D-(6-E-p-coumaroyl) glucopyranoside (tiliroside), through chemical structure analysis, toxicity assessment and predictive bioactive properties, using human samples for in vitro and ex-vivo tests. The in silico analysis suggests that tiliroside exhibited great absorption index when penetrating biological membranes. In addition, it also displayed considerable potential for cellular protection against free radicals, and anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and antithrombotic activities. The assessment of the hemolytic and genotoxic effects of tiliroside showed low hemolysis rates in red blood cells and absence of cellular toxicity in the oral mucosa cells. The data obtained indicate that this molecule could be a promising therapeutic approach as a possible new drug with biotechnological potential.
O tilirosídeo é um flavonóide glicosídico presente em muitas espécies de plantas, incluindo Helicteres velutina K. Schum (Malvaceae sensu lato), conhecida no Brasil como pitó. Esta molécula mostrou ter muitas atividades biológicas, porém nenhum estudo foi realizado para investigar a toxicidade dessa substância. O presente trabalho teve como objetivo avaliar a possível toxicidade celular in silico, in vitro e ex-vivo do kaempferol-3-O-β-D- (6 -Ep-coumaroil) glucopiranosídeo (tilirosídeo), por meio de análises de estrutura química, toxicidade avaliação e propriedades bioativas preditivas, utilizando amostras humanas para testes in vitro e ex-vivo. A análise in silico sugere que o tilirosídeo exibe bom índice de absorção para penetrar nas membranas biológicas. Além disso, apresentou considerável potencial de proteção celular contra os radicais livres e com atividades anticarcinogênica, antioxidante, antineoplásica, antiinflamatória, anti-hemorrágica e antitrombótica. A avaliação dos efeitos hemolíticos e genotóxicos do tilirosídeo mostrou baixas taxas de hemólise nas hemácias e ausência de toxicidade em células da mucosa oral. Os dados obtidos indicam que esta molécula pode possuir uma abordagem terapêutica promissora como uma possível nova droga com potencial biotecnológico.
Asunto(s)
Flavonoides/farmacocinética , Flavonoides/toxicidad , Malvaceae , Técnicas In VitroRESUMEN
Abstract Tiliroside is a glycosidic flavonoid present in many plants species including Helicteres velutina K. Schum (Malvaceae sensu lato), commonly known in Brazil as pitó. This molecule has been shown to have many biological activities, however no study has been carried out to investigate the toxicity of this substance. The present work aimed to evaluate the possible cellular toxicity in silico, in vitro and ex-vivo of the kaempferol-3-O--D-(6-E-p-coumaroyl) glucopyranoside (tiliroside), through chemical structure analysis, toxicity assessment and predictive bioactive properties, using human samples for in vitro and ex-vivo tests. The in silico analysis suggests that tiliroside exhibited great absorption index when penetrating biological membranes. In addition, it also displayed considerable potential for cellular protection against free radicals, and anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and antithrombotic activities. The assessment of the hemolytic and genotoxic effects of tiliroside showed low hemolysis rates in red blood cells and absence of cellular toxicity in the oral mucosa cells. The data obtained indicate that this molecule could be a promising therapeutic approach as a possible new drug with biotechnological potential.
Resumo O tilirosídeo é um flavonóide glicosídico presente em muitas espécies de plantas, incluindo Helicteres velutina K. Schum (Malvaceae sensu lato), conhecida no Brasil como pitó. Esta molécula mostrou ter muitas atividades biológicas, porém nenhum estudo foi realizado para investigar a toxicidade dessa substância. O presente trabalho teve como objetivo avaliar a possível toxicidade celular in silico, in vitro e ex-vivo do kaempferol-3-O--D- (6 -Ep-coumaroil) glucopiranosídeo (tilirosídeo), por meio de análises de estrutura química, toxicidade avaliação e propriedades bioativas preditivas, utilizando amostras humanas para testes in vitro e ex-vivo. A análise in silico sugere que o tilirosídeo exibe bom índice de absorção para penetrar nas membranas biológicas. Além disso, apresentou considerável potencial de proteção celular contra os radicais livres e com atividades anticarcinogênica, antioxidante, antineoplásica, antiinflamatória, anti-hemorrágica e antitrombótica. A avaliação dos efeitos hemolíticos e genotóxicos do tilirosídeo mostrou baixas taxas de hemólise nas hemácias e ausência de toxicidade em células da mucosa oral. Os dados obtidos indicam que esta molécula pode possuir uma abordagem terapêutica promissora como uma possível nova droga com potencial biotecnológico.
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Purpose: To investigate the anti-inflammatory and antioxidant activities of N-salicyloyltryptamine (NST) in experimental models of carrageenan (Cg)-induced peritonitis in mice, and evaluation of the effects of NST on Cg-induced joint disability in rats. Methods: Female Swiss mice were submitted to Cg-induced peritonitis in mice or Cg-induced joint disability in rats after intraperitoneal injection of NST (100 or 200 mg/kg). Total leukocyte count, total protein concentration, myeloperoxidase (MPO) and catalase (CAT) activities, and nitrite (NO2 -) and thiobarbituric acid reactive species (TBARS) levels were determined. Results: NST significantly decrease the migration of leukocytes to peritoneal exudate. Cg induces inflammatory responses mediated by expression of reactive oxygen species (ROS). The results further showed that NST significantly decreased MPO and CAT activities, as well as reduced NO2 - and TBARS levels, compared with the vehicle group. Animals treated with NST significantly reduced paw elevation time (PET) on the first hour after induction of joint injury, and this effect was sustained throughout the analysis. Conclusion: NST presented anti-inflammatory and antioxidant effects in experimental models of carrageenan-induced peritonitis and joint disability in mice and rats, respectively, which may be related to the modulation of neutrophils migration as well as the involvement of antioxidant mechanisms.
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Phytochemical studies of the species Pavonia glazioviana were performed. Quercetin, kaempferol, acacetin, and trimethoxylated flavonoid compounds (which present biological activity) were isolated. We aimed to evaluate the in silico, in vitro, and ex vivo toxicity of flavonoid 5,7-dihydroxy-3,8,4'-trimethoxy (Pg-1) obtained from P. glazioviana through chemical structure analyses, toxicity assessment, and predictive bioactive properties, using human samples in in vitro tests. In silico analysis suggested that Pg-1 presents a good absorption index for penetrating biological membranes (for oral bioavailability), while also suggesting potential antimutagenic, anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic, and apoptosis agonist bioactivities. Assessment of hemolytic and genotoxic effects revealed low hemolysis rates in red blood cells with no cellular toxicity in oral mucosa cells. The reduced cytotoxic activity suggested the safety of the concentrations used (500-1000 µg/mL), and demonstrated the varied interactions of Pg-1 with the analyzed cells. The data obtained in the present study suggested potential therapeutic application, and the non-toxic profile indicated viability for future studies.
Asunto(s)
Flavonoides , Extractos Vegetales , Antioxidantes/farmacología , Apoptosis , Simulación por Computador , Flavonoides/farmacología , HumanosRESUMEN
Tiliroside is a glycosidic flavonoid present in many plants species including Helicteres velutina K. Schum (Malvaceae sensu lato), commonly known in Brazil as "pitó". This molecule has been shown to have many biological activities, however no study has been carried out to investigate the toxicity of this substance. The present work aimed to evaluate the possible cellular toxicity in silico, in vitro and ex-vivo of the kaempferol-3-O-ß-D-(6"-E-p-coumaroyl) glucopyranoside (tiliroside), through chemical structure analysis, toxicity assessment and predictive bioactive properties, using human samples for in vitro and ex-vivo tests. The in silico analysis suggests that tiliroside exhibited great absorption index when penetrating biological membranes. In addition, it also displayed considerable potential for cellular protection against free radicals, and anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and antithrombotic activities. The assessment of the hemolytic and genotoxic effects of tiliroside showed low hemolysis rates in red blood cells and absence of cellular toxicity in the oral mucosa cells. The data obtained indicate that this molecule could be a promising therapeutic approach as a possible new drug with biotechnological potential.
Asunto(s)
Quempferoles , Extractos Vegetales , Brasil , Simulación por Computador , Flavonoides , Humanos , Quempferoles/toxicidadRESUMEN
Phytochemical studies of the species Pavonia glazioviana were performed. Quercetin, kaempferol, acacetin, and trimethoxylated flavonoid compounds (which present biological activity) were isolated. We aimed to evaluate the in silico, in vitro, and ex vivo toxicity of flavonoid 5,7-dihydroxy-3,8,4'-trimethoxy (Pg-1) obtained from P. glazioviana through chemical structure analyses, toxicity assessment, and predictive bioactive properties, using human samples in in vitro tests. In silico analysis suggested that Pg-1 presents a good absorption index for penetrating biological membranes (for oral bioavailability), while also suggesting potential antimutagenic, anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic, and apoptosis agonist bioactivities. Assessment of hemolytic and genotoxic effects revealed low hemolysis rates in red blood cells with no cellular toxicity in oral mucosa cells. The reduced cytotoxic activity suggested the safety of the concentrations used (500-1000 µg/mL), and demonstrated the varied interactions of Pg-1 with the analyzed cells. The data obtained in the present study suggested potential therapeutic application, and the non-toxic profile indicated viability for future studies.
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Humanos , Flavonoides/farmacología , Extractos Vegetales , Simulación por Computador , Apoptosis , Antioxidantes/farmacologíaRESUMEN
Parkinson's disease (PD) is mostly known as a dopamine deficiency syndrome due the structural and functional changes in striatal projection neurons. However, studies have considered this pathology as a multi-systemic disease in which the neurodegenerative process extends beyond the dopaminergic system. Therefore, the purpose of the present study was to investigate the morphological and immunohistochemical changes associated with behavioral and cognitive alterations in a model of parkinsonism induced by low dose of reserpine. Animals showed anxiety-like behavior and deficits in short-term recognition memory. Besides, Tyrosine Hydroxylase (TH) immunoreactive cells decreased in reserpine (RES) group in CA1 and serotonin (5-HT) immunoreactive cells decreased in RES group in CA1, CA3 and medial prefrontal cortex (mPFC). Moreover, an increase in the area (µm2) of 5 H T labeled ultrastructure (axon terminal) was observed in RES group only in CA1 and mPFC. The evidence of alterations in 5-HT immunoreactive in the premotor phase of model of parkinsonism highlights the importance of looking beyond the nigrostriatal system to elucidate the underling mechanisms and deficits in other neurotransmitters systems. This provides vital information regarding novel interventions for the management of non-motor symptoms. Additionally, the low-dose reserpine treatment has an early effect on axonal ultrastructure. As the axonopathy in PD has been increasingly recognized, the focus on axonal neurobiology is noteworthy for both neuroprotective and restorative therapeutics, and the progressive reserpine rat model can be a useful tool in this search.
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Trastornos Parkinsonianos/fisiopatología , Neuronas Serotoninérgicas/metabolismo , Neuronas Serotoninérgicas/patología , Animales , Ansiedad/fisiopatología , Encéfalo/metabolismo , Región CA1 Hipocampal/efectos de los fármacos , Cognición/fisiología , Cuerpo Estriado/metabolismo , Modelos Animales de Enfermedad , Dopamina/metabolismo , Dopamina/farmacología , Inmunohistoquímica/métodos , Masculino , Memoria a Corto Plazo/fisiología , Actividad Motora/efectos de los fármacos , Enfermedad de Parkinson/patología , Trastornos Parkinsonianos/inducido químicamente , Trastornos Parkinsonianos/metabolismo , Corteza Prefrontal/metabolismo , Ratas , Ratas Wistar , Reserpina/farmacología , Serotonina/metabolismo , Tirosina 3-Monooxigenasa/metabolismoRESUMEN
The main purpose of this study was to investigate the effects of 12 weeks of resistance training (RT) on phase angle (PhA), inflammatory and oxidative stress biomarkers, and to evaluate whether these RT-induced adaptations are related to PhA changes. Fifty-one older women (70.6 ± 5.1 years; 26.9 ± 4.2 kg/m2 ) were randomly allocated into a training group (TG) that performed 12-week RT or a nonexercising control group (CG). The PhA (Xitron), body composition (DXA), and blood sample measurements (after a 12 hours fast) were performed before and after the intervention. The TG showed a significant (P < .05) increase in PhA (TG: +7.4±5.9% vs CG: -3.6 ± 8.8%), and interleukin-10 (IL-10; TG: +51.8 ± 71.1% vs CG: -46.6 ± 38.0%), and a decrease in tumor necrosis factor alpha (TNF-α; TG: -15.2 ± 11.1% vs CG: +6.9±17.7%), interleukin-6 (IL-6; TG: -17.9 ± 17.8% vs CG: +6.1 ± 24.8%), and C-reactive protein (CRP; TG: -24.1 ± 19.9% vs CG: +43.8 ± 31.1%). Moreover, TG upregulated catalase (TG: +11.4 ± 15.0% vs CG: -6.7 ± 10.2%). Changes in TNF-α (r = -.71), CRP (r = -.65), lower advanced oxidation protein products (r = -.55), and catalase (r = +.73) after RT were correlated with changes in PhA (P < .05). These results suggest that RT improves PhA, inflammatory and oxidative stress biomarkers, and the changes in inflammatory and oxidative damage markers are correlated with changes in PhA.
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Biomarcadores/sangre , Inflamación/sangre , Estrés Oxidativo , Entrenamiento de Fuerza , Absorciometría de Fotón , Anciano , Composición Corporal , Proteína C-Reactiva/análisis , Impedancia Eléctrica , Femenino , Humanos , Interleucina-10/sangre , Interleucina-6/sangre , Persona de Mediana Edad , Factor de Necrosis Tumoral alfa/sangreRESUMEN
Phase angle (PhA) is an angular-derived bioelectrical impedance parameter based on resistance and reactance that has been widely used in different populations as an objective indicator of cellular health. The purpose of this study was to analyze the effect of resistance training (RT) on PhA in older women. Forty-one older women (67.2 ± 4.5 years, 64.0 ± 12.3 kg, 154.7 ± 5.2 cm, and 26.6 ± 4.8 kg/m2 ) were randomly assigned to one of two groups: a training group (TG, n = 19) that underwent progressive RT for 12 weeks (eight exercises, three sets of 10-15 repetitions maximum, three times per week) or a control group (CG, n = 22) that did not perform any type of exercise during the intervention period. Resistance, reactance, PhA, total body water (TBW), intracellular (ICW) and extracellular (ECW) water were assessed by spectral bioelectrical impedance. There was a significant group by time interaction (P < 0.05) for PhA, TBW, and ICW in which only the TG increased their scores after the intervention period (PhA = +6.5%, TBW = +2.8%, and ICW = +5.1%). The results suggest that progressive RT promotes an increase in PhA in older women. Therefore, the PhA seems to be a good parameter to assess changes in cellular health during RT intervention.
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Impedancia Eléctrica , Entrenamiento de Fuerza , Anciano , Composición Corporal , Agua Corporal , Femenino , Humanos , Persona de Mediana Edad , Fuerza MuscularRESUMEN
Aedes aegypti (L.) has become an efficient vector of important arboviruses due to its anthropophilic and domiciliary behaviors. Since the 1980s, dengue affects thousands of people every year in Brazil; in Fernando de Noronha (FN), a touristic archipelago, dengue cases have occurred since 2001. Once Ae. aegypti populations are well established in the inhabited areas of FN, the threat of dengue or another arbovirus epidemic is continuously imminent. This study aimed to monitor the DENV serotypes in mosquito samples collected in FN, where at least one resident was clinically diagnosed as dengue patient. Entomological surveillance was conducted in 2011 and 2012. Mosquitoes were sorted by sex and location and were stored in pools. DENV detection was performed using polymerase chain reaction with reverse transcription (RT-PCR) and the Platelia Dengue NS1 Ag. RNA integrity was checked by RT-PCR using rpL8 primers, and the minimum infection rate (MIR) was calculated. In total, 339 pools were analyzed, and only one was positive (DENV-1) by Multiplex RT-PCR (MIR = 1.53). When considering only pools with RNA integrity, the MIR was 2.92. Using the Platelia kit, the MIR was 9.18 (considering all the pools) and 17.54 (only 140 pools with RNA integrity). Our results showed the importance of a constant entomological surveillance in that area, the need to improve storage and transportation protocols, and an endogenous control in the RT-PCR to avoid false-negative results. Finally, our study indicated that the NS1-Ag detection was the most sensitive method and should be used routinely for DENV surveillance in mosquitoes if the serotype identification is not required.
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Aedes/virología , Virus del Dengue/aislamiento & purificación , Dengue/virología , Aedes/fisiología , Animales , Brasil/epidemiología , Dengue/epidemiología , Dengue/transmisión , Virus del Dengue/clasificación , Virus del Dengue/genética , Virus del Dengue/fisiología , Femenino , Humanos , Insectos Vectores/fisiología , Insectos Vectores/virología , Masculino , Vigilancia de Guardia , SerogrupoRESUMEN
Cocaine sensitization is a marker for some facets of addiction, is greater in female rats, and may be influenced by their sex hormones. We compared the modulatory effects of endogenous or exogenous estradiol and progesterone on cocaine-induced behavioral sensitization in 106 female rats. Ovariectomized female rats received progesterone (0.5 mg/mL), estradiol (0.05 mg/mL), progesterone plus estradiol, or the oil vehicle. Sham-operated control females received oil. Control and acute subgroups received injections of saline, while the repeated group received cocaine (15 mg/kg, ip) for 8 days. After 10 days, the acute and repeated groups received a challenge dose of cocaine, after which locomotion and stereotypy were monitored. The estrous cycle phase was evaluated and blood was collected to verify hormone levels. Repeated cocaine treatment induced overall behavioral sensitization in female rats, with increased locomotion and stereotypies. In detailed analysis, ovariectomized rats showed no locomotor sensitization; however, the sensitization of stereotypies was maintained. Only females with endogenous estradiol and progesterone demonstrated increased locomotor activity after cocaine challenge. Estradiol replacement enhanced stereotyped behaviors after repeated cocaine administration. Cocaine sensitization of stereotyped behaviors in female rats was reduced after progesterone replacement, either alone or concomitant with estradiol. The behavioral responses (locomotion and stereotypy) to cocaine were affected differently, depending on whether the female hormones were of an endogenous or exogenous origin. Therefore, hormonal cycling appears to be an important factor in the sensitization of females. Although estradiol increases the risk of cocaine sensitization, progesterone warrants further study as a pharmacological treatment in the prevention of psychostimulant abuse.
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Sensibilización del Sistema Nervioso Central/efectos de los fármacos , Cocaína/farmacología , Estradiol/sangre , Actividad Motora/efectos de los fármacos , Progesterona/sangre , Conducta Estereotipada/efectos de los fármacos , Análisis de Varianza , Animales , Cocaína/administración & dosificación , Estradiol/farmacología , Ciclo Estral/sangre , Femenino , Terapia de Reemplazo de Hormonas , Ovariectomía , Progesterona/farmacología , Ratas Wistar , Factores SexualesRESUMEN
Cocaine sensitization is a marker for some facets of addiction, is greater in female rats, and may be influenced by their sex hormones. We compared the modulatory effects of endogenous or exogenous estradiol and progesterone on cocaine-induced behavioral sensitization in 106 female rats. Ovariectomized female rats received progesterone (0.5 mg/mL), estradiol (0.05 mg/mL), progesterone plus estradiol, or the oil vehicle. Sham-operated control females received oil. Control and acute subgroups received injections of saline, while the repeated group received cocaine (15 mg/kg, ip) for 8 days. After 10 days, the acute and repeated groups received a challenge dose of cocaine, after which locomotion and stereotypy were monitored. The estrous cycle phase was evaluated and blood was collected to verify hormone levels. Repeated cocaine treatment induced overall behavioral sensitization in female rats, with increased locomotion and stereotypies. In detailed analysis, ovariectomized rats showed no locomotor sensitization; however, the sensitization of stereotypies was maintained. Only females with endogenous estradiol and progesterone demonstrated increased locomotor activity after cocaine challenge. Estradiol replacement enhanced stereotyped behaviors after repeated cocaine administration. Cocaine sensitization of stereotyped behaviors in female rats was reduced after progesterone replacement, either alone or concomitant with estradiol. The behavioral responses (locomotion and stereotypy) to cocaine were affected differently, depending on whether the female hormones were of an endogenous or exogenous origin. Therefore, hormonal cycling appears to be an important factor in the sensitization of females. Although estradiol increases the risk of cocaine sensitization, progesterone warrants further study as a pharmacological treatment in the prevention of psychostimulant abuse.
Asunto(s)
Animales , Femenino , Sensibilización del Sistema Nervioso Central/efectos de los fármacos , Cocaína/farmacología , Estradiol/sangre , Actividad Motora/efectos de los fármacos , Progesterona/sangre , Conducta Estereotipada/efectos de los fármacos , Análisis de Varianza , Cocaína/administración & dosificación , Estradiol/farmacología , Ciclo Estral/sangre , Terapia de Reemplazo de Hormonas , Ovariectomía , Progesterona/farmacología , Ratas Wistar , Factores SexualesRESUMEN
The present study is pioneer in analyzing the chemical composition of the essential oil from aerial parts of Turnera subulata Sm. and evaluates their antibacterial activity against a panel of drug-resistant strains of Staphylococcus aureus. The aerial parts were kiln-dried and then powdered in mechanical mill, and was subjected to hydrodistillation in a Clevenger-type apparatus. The components were analyzed using a mass spectrometrycoupled gas chromatography (GC-MS), and the identification of substances was performed by comparison of the mass spectra obtained with the mass spectra of the database of the GC-MS and retention indices . The essential oil was evaluated using the method of broth dilution at concentrations ranging from 3.125µg/mL to 3200µg/mL. It was possible to identify 45 substances (92.1%) of the essential oils, and the major components were trans-caryophyllene (6.7%), citronellol (5.6%), sphatulenol (5.3%), α-cadinol (4.3%), n-tricosano (4.3%), geraniol (4.1%) and trans-geranilacetone (3.7%), n-pentacosano (3.5%), globulol (3.4%), caryophyllene oxide (3.2%). The essential oil of T. subulata Sm. showed effective antibacterial activity for the various strains of S. aureus tested, with the MIC values between 25 µg/mL and 1600 µg/mL. The study of the essential oil of Turnera subulata Sm. showed that it consists of a complex mixture of several classes of compounds having the sesquiterpenes as major constituents followed by monoterpenes, and showed an antibacterial activity significant front the strains tested.
O presente estudo é pioneiro em analisar a composição química dos óleos essenciais das partes aéreas de Turnera subulata Sm. e sua atividade antibacteriana frente à Staphylococcus aureus resistentes a antibióticos. As partes aéreas da planta foram secas em estufa, pulverizadas em moinho mecânico e submetidas à hidrodestilaçao em aparato tipo Clevenger. A composição dos óleos essenciais foi analisada por cromatografia gasosa acoplada a espectrometria de massas (CG-EM), e a identificação realizada por comparação dos espectros de massas com a biblioteca do CG-EM e índices de retenção. A atividade antimicrobiana do óleo essencial foi avaliada usando o método de diluição em caldo, em concentrações que variaram de 3.125µg/mL to 3200µg/mL. Foi possível identificar 45 substâncias (92,1%) do óleo essencial, sendo os componentes majoritários: trans-cariofileno (6,7%), citronelol (5,6%), espatulenol (5,3%), α-cadinol (4,3%), n-tricosano (4,3%), geraniol (4,1%) e trans-geranilacetona (3,7%), n-pentacosano (3,5%), globulol (3,4%) e óxido de cariofileno (3,2%). O óleo essencial de T. subulata Sm. mostrou atividade antibacteriana eficaz para as várias cepas de S. aureus testadas, com valores de CIM entre 25 µg/mL e 1600 µg/mL. O estudo do óleo essencial de Turnera subulata Sm. evidenciou sua complexa mistura, contendo várias classes de substâncias, tendo os sesquiterpenos como constituintes majoritários seguido dos monoterpenos, e mostrou significativa atividade antibacteriana frente as cepas testadas.
Asunto(s)
Infecciones Estafilocócicas/tratamiento farmacológico , Aceites Volátiles/química , Turnera/metabolismo , Espectrometría de Masas/instrumentación , Staphylococcus aureus/patogenicidad , Cromatografía de Gases/instrumentación , Componentes Aéreos de las Plantas/metabolismoRESUMEN
The objective of this paper was to study the effect of four levels of organic fertilization (0, 3, 6 and 9 kg m-2) to produce the essential oil of Lippia sidoides Cham. (Verbenacea) and its pests. A higher number of red mite Tetranychus sp. (Acari: Tetranychiidae) was observed on the abaxial face of the median and basal leaves of L. sidoides plants with eight weeks of age cultivated with 6 kg m-2 of organic fertilization. On the other hand, the smallest number of this mite was noted in control (0 kg m-2). L. sidoides cultivated with 6 kg m-2 of organic fertilization produced a greater quantity of essential oil. The highest number of mealy bug Phenacoccus sp. (Hemiptera: Pseudococcidae) was observed on the apical leaves (both leaf surfaces) of L. sidoides plants with nine and ten weeks of age cultivated with 3 kg m-2 of organic fertilization. No significant effect of the organic fertilization on Aphis gossypii Glover (Hemiptera: Aphididae) was detected. However, a greater number of this aphid and of its predator Scymnus sp. (Coleoptera: Coccinelidae) was observed on the abaxial face of the bottom leaves of L. sidoides plants with eight weeks of age. The dose of organic fertilization recommended for the production of essential oil of L. Sidoides is 6 kg m-2, however, one must pay attention to the fact this dosage favors the attack by Tetranychus sp.. And, when needed, pulverization must always be directed to the lower surface of the leaf.
O objetivo deste trabalho foi avaliar o efeito de quatro níveis de adubação orgânica (0, 3, 6, e 9 kg m-2) na produção de óleo essencial de Lippia sidoides Cham. (Verbenacea) e de suas pragas. Observou-se maior número de ácaro vermelho Tetranychus sp. (Acari: Tetranychiidae) na face inferior das folhas dos terços medianos e basais das plantas de L. sidoides com oito semanas de idade cultivadas com 6 kg m-2 de adubo orgânico. Por outro lado, a menor quantidade deste ácaro foi notada na testemunha (0 kg m-2). L. sidoides cultivada com 6 kg m-2 de adubo orgânico produziu maior quantidade de óleo essencial. Observou-se maior número de cochonilhas Phenacoccus sp. (Hemiptera: Pseudococcidae) nas folhas apicais, sem distinção de face foliar, das plantas de L. sidoides com nove e 10 semanas de idade cultivadas com 3 kg m-2 de adubo orgânico. Não se detectou efeito significativo de adubo orgânico sobre Aphis gossypii Glover (Hemiptera: Aphididae). Contudo, observou-se maior número desse pulgão bem como de seu predador Scymnus sp. (Coleoptera: Coccinelidae) nas faces abaxiais das folhas basais das plantas de L. sidoides com oito semanas de idade. A dose de adubo orgânico recomendada para produção de óleo essencial de L. sidoides é de 6 kg m-2. Contudo, essa dosagem favorece o ataque de Tetranychus sp. e, quando necessário, deve-se dirigir a pulverização sempre para a face inferior da folha, local preferencial de ataque dos artrópodes.
Asunto(s)
Plantas Medicinales/clasificación , Aceites Volátiles/análisis , Plagas Agrícolas , Lippia/metabolismo , Insectos , ÁcarosRESUMEN
BACKGROUND: Poor semen quality of pedigree bulls has major economic implications in cattle breeding. AIMS: To evaluate the effect of homeopathy on the semen of bulls with reproductive disorders. METHODS: The behavioral, clinical and spermatic characteristics of four Nelore bulls were evaluated. The bulls received individualized homeopathic treatment mixed into the feed and administered once per day. Semen was collected using an artificial vagina. Successful collection, freezing, effective doses, and the number of doses of semen per collection were compared before and after homeopathic treatment. RESULTS: The bulls were treated with Sulphur, Phosphorus, Lycopodium and Argentum nitricum all in 30CH dilution. The rates of successful collection were 97.14%, 100%, 96.67% and 30.77% pretreatment and 95.45%, 100%, 94.67% and 96.77% at post-treatment for bulls A, B, C and D, respectively. The average number of doses per ejaculate pre and post-treatment were 102.67 (SD 74.41) vs. 300.08 (SD 180.58), 0 vs. 234.78 (SD 96.12), 0 vs. 105.12 (SD 54.98), 0 ± vs. 107.37 (SD 52.12) respectively. Many of these differences were statistically significant. CONCLUSION: The use of homeopathy apparently improved the production of viable doses of semen from bulls with previous freezing problems and poor semen quality. Controlled studies should be conducted.
Asunto(s)
Cruzamiento/métodos , Enfermedades de los Bovinos/tratamiento farmacológico , Homeopatía/métodos , Infertilidad Masculina/tratamiento farmacológico , Infertilidad Masculina/veterinaria , Materia Medica/uso terapéutico , Semen/efectos de los fármacos , Animales , Bovinos , Relación Dosis-Respuesta a Droga , Femenino , Masculino , Análisis de Semen , Recuento de Espermatozoides/veterinaria , Medicina Veterinaria/métodosRESUMEN
Methylphenidate (MPD) is a psychostimulant that is prescribed to treat attention-deficit/hyperactivity disorder (ADHD) and has been used as a recreational drug. In animal models, repetitive exposure to methylphenidate can induce a behavioral sensitization. Stimulants are able to change neuronal circuits in the mesolimbic pathway, and the GABA system is one of the most involved neurotransmitter systems in this process. Women represent a risk group for psychostimulant abuse because they respond more strongly, which is probably due to the influence of sex hormones. The objective of the present study was to investigate the influence of sex hormones on behavioral sentsitization and changes to glutamic acid decarboxylase (GDA65 and GDA67) isoenzymes and α2 GABAA receptor subunit mRNA expression in the prefrontal cortex and the striatum of rats, as induced by methylphenidate administration (2.5 mg/kg, i.p.). Female rats were divided into 2 hormonal conditions: ovariectomized and intact group. Repeated methylphenidate treatment led to behavioral sensitization, which was stronger in females with circulating hormones (intact group). The analysis of mRNA levels in the striatum, in both groups, showed a decline in GAD65, but not GAD67, transcription after repeated methylphenidate treatment. In the prefrontal cortex, both GAD65 and GAD67 showed an increase in transcription with repeated methylphenidate treatment. There was no change in the transcription level of α2 GABAA receptor subunits. In conclusion, it was shown that sex hormones were able to modify behavioral sensitization to methylphenidate and the drug affected the GABA system in brain areas known to be involved in the development of drug dependence.
Asunto(s)
Conducta Animal/efectos de los fármacos , Encéfalo/efectos de los fármacos , Sensibilización del Sistema Nervioso Central/efectos de los fármacos , Estimulantes del Sistema Nervioso Central/farmacología , Metilfenidato/farmacología , Ácido gamma-Aminobutírico/metabolismo , Animales , Encéfalo/metabolismo , Femenino , Glutamato Descarboxilasa/metabolismo , Actividad Motora/efectos de los fármacos , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Ovariectomía , RatasRESUMEN
O alecrim-pimenta, espécie nativa do nordeste brasileiro, é uma planta medicinal de porte arbustivo, com folhas aromáticas, que possuem óleo essencial rico em timol e carvacrol. Essas substâncias conferem grande importância à planta, uma vez que apresentam atividades farmacológicas comprovadas cientificamente. Desta forma, o estudo das condições de cultivo da espécie é essencial para obtenção de maiores produtividades. O espaçamento entre plantas destaca-se como um dos fatores mais importantes relativos ao cultivo, de forma que a produtividade e o rendimento da cultura são afetados pela densidade de plantas. Dada a necessidade de otimizar técnicas de cultivo do alecrim-pimenta (Lippia sidoides Cham.), objetivou-se avaliar a produção de fitomassa e óleo essencial em quatro espaçamentos de plantio. O trabalho foi realizado em campo, no Instituto de Ciências Agrárias da Universidade Federal de Minas Gerais (ICA/UFMG), no município de Montes Claros/MG. Utilizou-se o delineamento em blocos casualizados, com quatro tratamentos e cinco repetições. Os tratamentos foram definidos pelos espaçamentos de plantio: 1,0 x 0,5 m; 1,0 x 1,0 m; 1,5 x 1,0 m; e fileiras duplas (1,0 x 0,8 x 0,5m), sendo 1,0 m entre fileiras duplas, 0,8 m entre fileiras simples e 0,5 m entre plantas na fileira. Após 150 dias do plantio no campo, foram avaliadas as variáveis produção de fitomassa fresca e seca das folhas, a produção e o teor de óleo essencial. Observou-se que o espaçamento de 1,0 x 0,5 m possibilitou uma maior produção de fitomassa e de óleo essencial, sendo, portanto, o mais indicado para o cultivo do alecrim-pimenta (Lippia sidoides Cham.).
Native to Northeastern Brazil, pepper-rosmarin (Lippia sidoides Cham.) is a shrubby medicinal plant with aromatic leaves and essential oil rich in thymol and carvacrol. These components have great importance to the species since they present scientifically proven pharmacological activities. Thus, the study of cultivation conditions for this species is essential to obtain higher productivity. Spacing between plants is one of the most important factors related to cultivation, since crop productivity and yield are affected by plant density. Based on the need of optimizing pepper-rosmarin cultivation techniques, this work aimed to evaluate the phytomass production and the essential oil yield in four planting spacings. The experiment was carried out under field conditions in the Agricultural Sciences Institute, Federal University of Minas Gerais (ICA/UFMG), Montes Claros Municipality, Minas Gerais State, Brazil. Experimental design was in randomized blocks, with four treatments and five replicates. Treatments consisted of the planting spacings 1.0 x 0.5 m; 1.0 x 1.0 m; 1.5 x 1.0 m; and double rows (1.0 x 0.8 x 0.5 m), with 1.0m between double rows, 0.8m between single rows and 0.5m between plants in the row. After 150 days of planting in the field, leaf fresh and dry phytomass production and essential oil yield were evaluated. The spacing 1.0 x 0.5 m led to higher phytomass production and essential oil yield, being therefore the most recommended for pepper-rosmarin cultivation.