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1.
Braz J Med Biol Res ; 54(4): e10346, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33624730

RESUMO

The main movements of artistic swimming demand various physical capacities such as flexibility, strength, power, and muscular endurance. The use of ergogenic resources to potentialize performance in this sport, however, is underexplored and deserves investigation. In the present study, we tested whether caffeine ingestion would improve the execution of movements that are essential in a typical figure competition or routines in artistic swimming (i.e., amplitude in the Ariana, height in the Boost and Barracuda, and time maintained in the Stationary Scull techniques). Sixteen experienced female athlete artistic swimmers (17.4±3.2 years of age, 5.6±2.8 years of artistic swimming practice) performed several movements of artistic swimming after having ingested a capsule containing caffeine (5 mg/kg body mass) or cellulose (placebo). Compared to the placebo, caffeine improved latero-lateral amplitude during the Ariana (P=0.035), the height of the Boost and Barracuda (P=0.028 and 0.009), and maintained duration in Stationary Sculling (P=0.012). Bayes factor analysis, however, indicated substantial evidence of a positive effect of caffeine only on the Barracuda and Stationary Scull techniques. These findings indicated that caffeine improved performance during specific artistic swimming movements. Coaches and athletes should consider caffeine ingestion in their supplementation plans.


Assuntos
Desempenho Atlético , Cafeína , Teorema de Bayes , Cafeína/farmacologia , Criança , Pré-Escolar , Ingestão de Alimentos , Feminino , Humanos , Natação
2.
Eur J Pharmacol ; 887: 173561, 2020 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-32946870

RESUMO

COVID-19 pandemic presents an unprecedented challenge to identify effective drugs for treatment. Despite multiple clinical trials using different agents, there is still a lack of specific treatment for COVID-19. Having the potential role in suppressing inflammation, immune modulation, antiviral and improving respiratory symptoms, this review discusses the potential role of methylxanthine drugs like pentoxifylline and caffeine in the management of COVID-19 patients. COVID-19 pathogenesis for clinical features like severe pneumonia, acute lung injury (ALI) / acute respiratory distress syndrome (ARDS), and multi-organ failures are excessive inflammation, oxidation, and cytokine storm by the exaggerated immune response. Drugs like pentoxifylline have already shown improvement of the symptoms of ARDS and caffeine has been in clinical use for decades to treat apnea of prematurity (AOP) in preterm infants and improve respiratory function. Pentoxifylline is well-known anti-inflammatory and anti-oxidative molecules that have already shown to suppress Tumor Necrosis Factor (TNF-α) as well as other inflammatory cytokines in pulmonary diseases, and this may be beneficial for better clinical outcomes in COVID-19 patients. Pentoxifylline enhances blood flow, improves microcirculation and tissue oxygenation, and caffeine also efficiently improves tissue oxygenation, asthma, decreases pulmonary hypertension and an effective analgesic. There are significant shreds of evidence that proved the properties of pentoxifylline and caffeine against virus-related diseases as well. Along with the aforementioned evidences and high safety profiles, both pentoxifylline and caffeine offer a glimpse of considerations for future use as a potential adjuvant to COVID-19 treatment. However, additional clinical studies are required to confirm this speculation.


Assuntos
Infecções por Coronavirus/tratamento farmacológico , Pandemias , Pentoxifilina/uso terapêutico , Pneumonia Viral/tratamento farmacológico , Xantinas/farmacologia , Xantinas/uso terapêutico , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/uso terapêutico , Cafeína/farmacologia , Cafeína/uso terapêutico , Infecções por Coronavirus/complicações , Humanos , Recém-Nascido , Recém-Nascido Prematuro , Inflamação/tratamento farmacológico , Inflamação/etiologia , Pentoxifilina/farmacologia , Pneumonia Viral/complicações
3.
Life Sci ; 261: 118364, 2020 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-32866516

RESUMO

AIMS: Prenatal hypoxia (PH) could affect peripheral vascular tone of the offspring, thus increasing the risk of cardiovascular diseases in adult. However, it's still unknown whether functions of coronary arteries (COA) in adult offspring would be influenced by PH. The present study aimed at effects of PH on vascular tone of COA and its related mechanisms. METHODS: Coronary arteries of adult offspring exposed to hypoxic or normoxic circumstances during gestational day 5 to 21 were collected. Wire myograph system, whole-cell patch clamp technique, IonOptix MyoCam system, PCR, and western blot were used to detect vascular function of adult offspring COA. KEY FINDINGS: PH significantly attenuated serotonin- and phorbol 12, 13-dibutyrate (PDBu)-induced constriction. Iberiotoxin potentiated PDBu-induced constriction and the effect was augmented by PH, however, no significant differences were found in whole-cell BKCa channel currents and its protein expression. Nifedipine inhibited PDBu-mediated constriction and the inhibitory effect was reduced in PH group, and whole-cell calcium channel current was decreased in offspring COA. Besides, PH reduced the capability of calcium release from the endoplasmic reticulum in COA. The phosphorylated PKCß protein expression at Ser660 site, not Thr641 site, was significantly decreased in PH offspring. Chronic hypoxia during pregnancy attenuated PDBu-mediated constriction in offspring COA, presumably through decreased phosphorylated PKCß at serine660 sites and decreased intracellular calcium-related weaker PKC activation. SIGNIFICANCE: The findings provided new information on the influence of prenatal hypoxia on COA, and suggested potential use of PKCß-serine660 for early prevention of coronary heart diseases in developmental origins.


Assuntos
Cálcio/metabolismo , Vasos Coronários/fisiopatologia , Hipóxia/complicações , Espaço Intracelular/metabolismo , Fosfosserina/metabolismo , Efeitos Tardios da Exposição Pré-Natal/fisiopatologia , Proteína Quinase C beta/metabolismo , Vasoconstrição , Animais , Peso Corporal/efeitos dos fármacos , Cafeína/farmacologia , Canais de Cálcio/metabolismo , Vasos Coronários/efeitos dos fármacos , Vasos Coronários/patologia , Retículo Endoplasmático/efeitos dos fármacos , Retículo Endoplasmático/metabolismo , Feminino , Miocárdio/patologia , Tamanho do Órgão/efeitos dos fármacos , Fosforilação/efeitos dos fármacos , Gravidez , Ratos Sprague-Dawley , Serotonina/metabolismo , Acetato de Tetradecanoilforbol
4.
PLoS One ; 15(8): e0236592, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32790792

RESUMO

Caffeine improves cycling time trial performance through enhanced motor output and muscle recruitment. However, it is unknown if caffeine further increases power output entropy. To investigate the effects of caffeine effects on cycling time trial performance and motor output entropy (MOEn), nine cyclists (VO2MAX of 55 ± 6.1 mL.kg.-1min-1) performed a 4 km cycling time trial (TT4km) after caffeine and placebo ingestion in a counterbalanced order. Power output data were sampled at a 2 Hz frequency, thereafter entropy was estimated on a sliding-window fashion to generate a power output time series. A number of mixed models compared performance and motor output entropy between caffeine and placebo every 25% of the total TT4km distance. Caffeine ingestion improved power output by 8% (p = 0.003) and increased MOEn by 7% (p = 0.018). Cyclists adopted a U-shaped pacing strategy after caffeine ingestion. MOEn mirrored power output responses as an inverted U-shape MOEn during the time trial. Accordingly, a strong inverse correlation was observed between MOEn and power output responses over the last 25% of the TT4km (p < 0.001), regardless of the ingestion, likely reflecting the end spurt during this period (p = 0.016). Caffeine ingestion improved TT4km performance and motor output responses likely due to a greater power output entropy.


Assuntos
Desempenho Atlético , Cafeína/farmacologia , Estimulantes do Sistema Nervoso Central/farmacologia , Resistência Física/efeitos dos fármacos , Adulto , Ciclismo , Entropia , Humanos , Masculino , Efeito Placebo
5.
Mol Pharmacol ; 98(4): 351-363, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32764093

RESUMO

Ryanodine receptor (RYR) mutations confer stress-triggered malignant hyperthermia (MH) susceptibility. Dietary caffeine (CAF) is the most commonly consumed psychoactive compound by humans. CAF-triggered Ca2+ release and its influences on skeletal muscle contractility are widely used as experimental tools to study RYR function/dysfunction and diagnose MH susceptibility. We hypothesize that dietary CAF achieving blood levels measured in human plasma exacerbates the penetrance of RYR1 MH susceptibility mutations triggered by gaseous anesthetic, affecting both central and peripheral adverse responses. Heterozygous R163C-RYR1 (HET) MH susceptible mice are used to investigate the influences of dietary CAF on both peripheral and central responses before and after induction of halothane (HAL) maintenance anesthesia under experimental conditions that maintain normal core body temperature. HET mice receiving CAF (plasma CAF 893 ng/ml) have significantly shorter times to respiratory arrest compared with wild type, without altering blood chemistry or displaying hyperthermia or muscle rigor. Intraperitoneal bolus dantrolene before HAL prolongs time to respiratory arrest. A pilot electrographic study using subcutaneous electrodes reveals that dietary CAF does not alter baseline electroencephalogram (EEG) total power, but significantly shortens delay to isoelectric EEG, which precedes respiratory and cardiac arrest. CAF ± HAL are studied on RYR1 single-channel currents and HET myotubes to define molecular mechanisms of gene-by-environment synergism. Strong pharmacological synergism between CAF and HAL is demonstrated in both single-channel and myotube preparations. Central and peripheral nervous systems mediate adverse responses to HAL in a HET model of MH susceptibility exposed to dietary CAF, a modifiable lifestyle factor that may mitigate risks of acute and chronic diseases associated with RYR1 mutations. SIGNIFICANCE STATEMENT: Dietary caffeine at a human-relevant dose synergizes adverse peripheral and central responses to anesthesia in malignant hyperthermia susceptible mice. Synergism of these drugs can be attributed to their actions at ryanodine receptors.


Assuntos
Cafeína/efeitos adversos , Dantroleno/efeitos adversos , Halotano/efeitos adversos , Hipertermia Maligna/fisiopatologia , Fibras Musculares Esqueléticas/fisiologia , Mutação , Canal de Liberação de Cálcio do Receptor de Rianodina/genética , Animais , Cafeína/farmacologia , Dantroleno/administração & dosagem , Modelos Animais de Doenças , Sinergismo Farmacológico , Eletroencefalografia/instrumentação , Feminino , Halotano/administração & dosagem , Heterozigoto , Humanos , Injeções Intraperitoneais , Masculino , Hipertermia Maligna/genética , Camundongos , Canal de Liberação de Cálcio do Receptor de Rianodina/metabolismo
6.
AAPS PharmSciTech ; 21(7): 243, 2020 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-32856144

RESUMO

The objective of this work was to develop taste-masked donut-shaped tablet formulations utilizing fused filament fabrication three-dimensional printing paired with hot-melt extrusion techniques. Caffeine citrate was used as the model drug for its bitter taste, and a 3-point bend test was performed to assess the printability of filaments. The stiffness constant was calculated to represent the printability by fitting the breaking distances and stress data into Hooke's law. The formulations without Eudragit E PO (F6) and with Eudragit E PO (F7) filaments exhibited the desired hardness with a "k" value of 48.30 ± 3.52 and 45.47 ± 3.51 g/mm3 (n = 10), respectively, and were successfully printed. The donut-shaped tablets were 3D printed with 10, 50, and 100% infill densities. In vitro dissolution studies were performed in simulated salivary fluid (pH 6.8, artificial saliva) to evaluate the taste-masking efficiency of the printed donuts. In the first minute, the concentrations of caffeine citrate observed in the dissolution media from all the printed donuts were less than the bitter threshold of caffeine citrate (0.25 mg/mL). Formulation F7, which contained Eudragit E PO copolymer, demonstrated better taste-masking efficiency than formulation F6. Furthermore, both formulations F6 and F7 demonstrated immediate drug release profiles in gastric medium (10% infill, > 80% release within 1 h). Taste-masked caffeine citrate formulations were successfully developed with donut shapes, which will enhance appeal in pediatric populations and increase compliance and patient acceptance of the dosage form.


Assuntos
Composição de Medicamentos/métodos , Tecnologia de Extrusão por Fusão a Quente/métodos , Impressão Tridimensional , Paladar/efeitos dos fármacos , Cafeína/química , Cafeína/farmacologia , Citratos/química , Citratos/farmacologia , Liberação Controlada de Fármacos/efeitos dos fármacos , Liberação Controlada de Fármacos/fisiologia , Excipientes/química , Excipientes/farmacologia , Humanos , Ácidos Polimetacrílicos/química , Ácidos Polimetacrílicos/farmacologia , Comprimidos , Paladar/fisiologia
8.
Am J Physiol Regul Integr Comp Physiol ; 319(2): R233-R242, 2020 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-32579854

RESUMO

Continuous infusion of prostaglandin E1 (PGE1) is used to maintain ductus arteriosus patency in infants with critical congenital heart disease, but it can also cause central apnea suggesting an effect on respiratory neural control. In this study, we investigated whether 1) PGE1 inhibits the various phases of the acute hypoxic ventilatory response (HVR; an index of respiratory control dysfunction) and increases apnea incidence in neonatal rats; and 2) whether these changes would be reversible with caffeine pretreatment. Whole body plethysmography was used to assess the HVR and apnea incidence in neonatal rats 2 h following a single bolus intraperitoneal injection of PGE1 with and without prior caffeine treatment. Untreated rats exhibited a biphasic HVR characterized by an initial increase in minute ventilation followed by a ventilatory decline of the late phase (~5th minute) of the HVR. PGE1 had a dose-dependent effect on the HVR. Contrary to our hypothesis, the lowest dose (1 µg/kg) of PGE1 prevented the ventilatory decline of the late phase of the HVR. However, PGE1 tended to increase postsigh apnea incidence and the coefficient of variability (CV) of breathing frequency, suggesting increased respiratory instability. PGE1 also decreased brainstem microglia mRNA and increased neuronal nitric oxide synthase (nNOS) and platelet-derived growth factor-ß (PDGF-ß) gene expression. Caffeine pretreatment prevented these effects of PGE1, and the adenosine A2A receptor inhibitor MSX-3 had similar preventative effects. Prostaglandin appears to have deleterious effects on brainstem respiratory control regions, possibly involving a microglial-dependent mechanism. The compensatory effects of caffeine or MSX-3 treatment raises the question of whether prostaglandin may also operate on an adenosine-dependent pathway.


Assuntos
Alprostadil/farmacologia , Tronco Encefálico/efeitos dos fármacos , Cafeína/farmacologia , Ventilação Pulmonar/efeitos dos fármacos , Respiração/efeitos dos fármacos , Animais , Tronco Encefálico/metabolismo , Microglia/efeitos dos fármacos , Microglia/metabolismo , Óxido Nítrico Sintase Tipo I/metabolismo , Pletismografia Total , Proteínas Proto-Oncogênicas c-sis/genética , Proteínas Proto-Oncogênicas c-sis/metabolismo , Antagonistas de Receptores Purinérgicos P1/farmacologia , Ratos , Ratos Sprague-Dawley
9.
PLoS One ; 15(6): e0229806, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32555600

RESUMO

The A2 adenosine receptors play an important role, among others, in the regulation of inflammatory process and glucose homeostasis in diabetes and obesity. Thus, the presented project evaluated of influence of the selective antagonist of A2A adenosine receptor-KD-64 as compared to the known non-selective antagonist-caffeine on these two particular processes. Two different inflammation models were induced namely local and systemic inflammation. Obesity was induced in mice by high-fat diet and the tested compounds (KD-64 and caffeine) were administrated for 21 days. KD-64 showed anti-inflammatory effect in both tested inflammation models and administered at the same dose as ketoprofen exerted stronger effect than this reference compound. Elevated levels of IL-6 and TNF-α observed in obese control mice were significantly lowered by the administration of KD-64 and were similar to the values observed in control non-obese mice. Interestingly, caffeine increased the levels of these parameters. In contrast to caffeine which had no influence on AlaT activity, KD-64 administration significantly lowered AlaT activity in the obese mice. Although, contrary to caffeine, KD-64 did not reduce diet-induced obesity in mice, it improved glucose tolerance. Thus, the activity of the selective adenosine A2A receptor antagonist was quite different from that of the non-selective.


Assuntos
Antagonistas do Receptor A2 de Adenosina/farmacologia , Anti-Inflamatórios/farmacologia , Dieta/efeitos adversos , Antagonistas do Receptor A2 de Adenosina/uso terapêutico , Animais , Anti-Inflamatórios/uso terapêutico , Peso Corporal/efeitos dos fármacos , Cafeína/farmacologia , Permeabilidade Capilar/efeitos dos fármacos , Dieta Hiperlipídica/efeitos adversos , Resistência à Insulina , Interleucina-6/sangue , Locomoção/efeitos dos fármacos , Masculino , Camundongos , Obesidade/induzido quimicamente , Obesidade/tratamento farmacológico , Peritônio/efeitos dos fármacos , Fator de Necrose Tumoral alfa/sangue
10.
PLoS One ; 15(4): e0228350, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32320391

RESUMO

Dosimetry is an important tool for triage and treatment planning following any radiation exposure accident, and biological dosimetry, which estimates exposure dose using a biological parameter, is a practical means of determining the specific dose an individual receives. The cytokinesis-blocked micronucleus assay (CBMN) is an established biodosimetric tool to measure chromosomal damage in mitogen-stimulated human lymphocytes. The CBMN method is especially valuable for biodosimetry in triage situations thanks to simplicity in scoring and adaptability to high-throughput automated sample processing systems. While this technique produces dose-response data which fit very well to a linear-quadratic model for exposures to low linear energy transfer (LET) radiation and for doses up for 5 Gy, limitations to the accuracy of this method arise at larger doses. Accuracy at higher doses is limited by the number of cells reaching mitosis. Whereas it would be expected that the yield of micronuclei increases with the dose, in many experiments it has been shown to actually decrease when normalized over the total number of cells. This variation from a monotonically increasing dose response poses a limitation for retrospective dose reconstruction. In this study we modified the standard CBMN assay to increase its accuracy following exposures to higher doses of photons or a mixed neutron-photon beam. The assay is modified either through inhibitions of the G2/M and spindle checkpoints with the addition of caffeine and/or ZM447439 (an Aurora kinase inhibitor), respectively to the blood cultures at select times during the assay. Our results showed that caffeine addition improved assay performance for photon up to 10 Gy. This was achieved by extending the assay time from the typical 70 h to just 74 h. Compared to micronuclei yields without inhibitors, addition of caffeine and ZM447439 resulted in improved accuracy in the detection of micronuclei yields up to 10 Gy from photons and 4 Gy of mixed neutrons-photons. When the dose-effect curves were fitted to take into account the turnover phenomenon observed at higher doses, best fitting was achieved when the combination of both inhibitors was used. These techniques permit reliable dose reconstruction after high doses of radiation with a method that can be adapted to high-throughput automated sample processing systems.


Assuntos
Citogenética , Doses de Radiação , Radiometria , Adulto , Benzamidas/farmacologia , Cafeína/farmacologia , Células Cultivadas , Relação Dose-Resposta à Radiação , Feminino , Humanos , Linfócitos/efeitos dos fármacos , Linfócitos/efeitos da radiação , Masculino , Testes para Micronúcleos , Pessoa de Meia-Idade , Nêutrons , Prótons , Quinazolinas/farmacologia
11.
Int J Mol Sci ; 21(7)2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-32244616

RESUMO

Triple-negative tumor cells, a malignant subtype of breast cancer, lack a biologically targeted therapy. Given its DNA repair inhibiting properties, caffeine has been shown to enhance the effectiveness of specific tumor chemotherapies. In this work, we have investigated the effects of caffeine, cisplatin, and a combination of the two as potential treatments in energy metabolism for three cell lines, triple-negative breast cancer (MDA-MB-231), estrogen-receptor lacking breast cancer (MCF7) and breast epithelial cells (MCF10A) using a sensitive label-free approach, phasor-fluorescence lifetime imaging microscopy (phasor-FLIM). We found that solely using caffeine to treat MDA-MB-231 shifts their metabolism towards respiratory-chain phosphorylation with a lower ratio of free to bound NADH, and a similar trend is seen in MCF7. However, MDA-MB-231 cells shifted to a higher ratio of free to bound NADH when cisplatin was added. The combination of cisplatin and caffeine together reduced the survival rate for MDA-MD231 and shifted their energy metabolism to a higher fraction of bound NADH indicative of oxidative phosphorylation. The FLIM and viability results of MCF10A cells demonstrate that the treatments targeted cancer cells over the normal breast tissue. The identification of energy metabolism alteration could open up strategies of improving chemotherapy for malignant breast cancer.


Assuntos
Cafeína/farmacologia , Cisplatino/farmacologia , Metabolismo Energético/efeitos dos fármacos , Microscopia de Fluorescência/métodos , Fosforilação Oxidativa/efeitos dos fármacos , Neoplasias de Mama Triplo Negativas/metabolismo , Antineoplásicos/farmacologia , Linhagem Celular , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Estimulantes do Sistema Nervoso Central/farmacologia , Relação Dose-Resposta a Droga , Feminino , Humanos , Células MCF-7 , NAD/metabolismo , Neoplasias de Mama Triplo Negativas/patologia
12.
Artigo em Inglês | MEDLINE | ID: mdl-32260589

RESUMO

Caffeine is the most consumed psychostimulant worldwide. Its use among children is controversial. Although it produces an increase in brain activity, it could hamper growth and development in young consumers. Therefore, the aim of this review was to recognize changes produced by caffeine in children under 12 years of age and to identify the relevant alterations and the conditions of their occurrence. A systematic review of the literature was carried out using PRISMA. Initially, 5468 articles were found from the EBSCO, ScienceDirect, PubMed, and Clarivate Analytics databases. In this review, were retained 24 published articles that met the inclusion criteria. The results obtained showed that caffeine consumption hampers children's growth and development. In contrast, it supports the activation of the central nervous system and brain energy management.


Assuntos
Encéfalo , Cafeína , Estimulantes do Sistema Nervoso Central , Encéfalo/efeitos dos fármacos , Cafeína/efeitos adversos , Cafeína/farmacologia , Estimulantes do Sistema Nervoso Central/efeitos adversos , Estimulantes do Sistema Nervoso Central/farmacologia , Criança , Desenvolvimento Infantil , Humanos
13.
J Pediatr ; 222: 244-247, 2020 07.
Artigo em Inglês | MEDLINE | ID: mdl-32143932

RESUMO

Infants born very preterm have a variable baseline risk of bronchopulmonary dysplasia (BPD). Using the example of evidence-based drug therapies to prevent BPD, we designed a visual aid that displays the "number needed to treat" with CIs for caffeine, vitamin A, and hydrocortisone over a range of baseline risks.


Assuntos
Displasia Broncopulmonar/prevenção & controle , Cafeína/farmacologia , Medicina Baseada em Evidências/métodos , Glucocorticoides/farmacologia , Hidrocortisona/farmacologia , Recém-Nascido Prematuro , Vitamina A/farmacologia , Anti-Inflamatórios/farmacologia , Humanos , Recém-Nascido , Inibidores de Fosfodiesterase/farmacologia , Vitaminas/farmacologia
14.
J Pharmacol Sci ; 143(2): 83-88, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32178942

RESUMO

Spontaneous locomotor activity (SLA) is a useful parameter reflecting physical and mental status of experimental animals. Here we aimed to establish a novel and simple method to assess mouse SLA using motion picture. Movement of C57BL/6 mice was continuously recorded by an infrared video camera connected with a single board computer. The geometric center of mouse outline in each frame was calculated using an image processing library, OpenCV in a programming language Python. Moving distance of the geometric center every second was utilized as an index of mouse SLA. Twenty-four hours assessment of SLA showed that mice repeated active and resting phase. Mice moved more actively during the dark period compared with the light period. Time-frequency analysis of SLA followed by unsupervised clustering classified their active and resting phase. Administration of a sedative, chlorpromazine (5 mg/kg) abolished mouse SLA for 8 h. In contrast, administration of a central nervous stimulant, caffeine (25 mg/kg) increased SLA for 3 h. In conclusion, we here established the automatic measurement system of mouse SLA using motion picture. This system is composed of common equipment and analysis software written in freely available programming language. We also confirmed that it is applicable for drug assessment.


Assuntos
Locomoção/fisiologia , Camundongos Endogâmicos C57BL/fisiologia , Camundongos Endogâmicos C57BL/psicologia , Filmes Cinematográficos , Atividade Motora/fisiologia , Animais , Cafeína/farmacologia , Estimulantes do Sistema Nervoso Central/farmacologia , Clorpromazina/farmacologia , Hipnóticos e Sedativos/farmacologia , Locomoção/efeitos dos fármacos , Masculino , Atividade Motora/efeitos dos fármacos
15.
Acta Biochim Pol ; 67(1): 79-84, 2020 Mar 19.
Artigo em Inglês | MEDLINE | ID: mdl-32191411

RESUMO

BACKGROUND: Energy Drinks (EDs) and Soft Drinks (SDs) are widely consumed among adolescents and young adults. These drinks contain variable amounts of caffeine which is a central nervous system stimulator; in addition to sugar, taurine, vitamins and herbal extracts. Several adverse effects have been reported for the excessive consumption of caffeine and sugar. AIM: This work aimed at providing a comparison between the effect of chronic consumption of both drinks on metabolism biochemically as well as at the histopathological level. METHODS: Adult albino rats were randomly divided into three groups and treated for 4 weeks. Animals received water (control, group 1), 12.5 ml/kg/day of either Pepsi® (SD, group 2) or Power Horse® (ED, group 3). All animals had free access to water and standard animal chow. RESULTS: ED and SD groups showed a significant weight gain compared to control. ED animals showed a significant increase in serum urea, hyperlipidemia and hyperglycemia in comparison to control and SD groups. Serum uric acid significantly increased in ED and SD groups. ED group showed congestion and inflammation in their renal tissues in addition to splenomegaly and increased phagocyte infiltration. CONCLUSION: The high caffeine-sugar content in ED exerts a more significant influence on the metabolic pathways than SDs. Both increase the incidence of cardiovascular diseases and tissue inflammation due to their effect on lipid profile and blood glucose. The other ingredients in EDs may play a role in the observed metabolic disturbances. Chronic use of EDs should be especially discouraged to avoid these negative effects.


Assuntos
Bebidas Gaseificadas/efeitos adversos , Bebidas Energéticas/efeitos adversos , Doenças Metabólicas/etiologia , Animais , Glicemia/efeitos dos fármacos , Cafeína/farmacologia , Doenças Cardiovasculares/etiologia , Rim/patologia , Lipídeos/sangue , Doenças Metabólicas/induzido quimicamente , Ratos , Esplenomegalia/etiologia , Açúcares/farmacologia , Ganho de Peso/efeitos dos fármacos
16.
Behav Processes ; 174: 104108, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32198089

RESUMO

OBJECTIVE: This study is aimed at comparing the relative reinforcing efficacy (RRE) of nicotine though CPT performance in function of alcohol and coffee consumption of treatment-seeking smokers. MATERIAL AND METHODS: A total of 88 treatment-seeking smokers (60.2 % female) completed the CPT. A multivariate analysis of variance (MANOVA) was used to compare alcohol (consumers and abstainers of alcohol) and coffee intake (high coffee consumers and low coffee consumers) on CPT indices. RESULTS: Univariate effects of coffee × alcohol use interaction were significant for elasticity [F (1, 83) = 4.9435, p = .038, η2 = .051] and intensity [F (1, 83) = 6.972, p = .01, η2 = .077]. CONCLUSIONS: Alcohol and coffee use is associated with an elevated cigarette demand among treatment-seeking smokers. This finding suggests the need for specific interventions to reduce alcohol and coffee use in order to increase the effectiveness of treatments for smoking cessation.


Assuntos
Consumo de Bebidas Alcoólicas/psicologia , Viés de Atenção/efeitos dos fármacos , Fumar Cigarros/psicologia , Café , Reforço Psicológico , Fumantes/psicologia , Adulto , Cafeína/farmacologia , Etanol/farmacologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Nicotina/farmacologia
17.
DNA Repair (Amst) ; 88: 102805, 2020 04.
Artigo em Inglês | MEDLINE | ID: mdl-32062581

RESUMO

This study was initiated to examine the effects of caffeine on the DNA damage response (DDR) and homologous recombination (HR) in mammalian cells. A 5 mM caffeine treatment caused the cell cycle to stall at G2/M and cells eventually underwent apoptosis. Caffeine exposure also induced a strong DDR along with subsequent activation of wildtype p53 protein. An unexpected observation was the caffeine-induced depletion of Rad51 (and Brca2) proteins. Consequently, caffeine-treated cells were expected to be inefficient in HR. However, a dichotomy in the HR response of cells to caffeine treatment was revealed. Caffeine treatment rendered cells significantly better at performing the nascent DNA synthesis that accompanies the early strand invasion steps of HR. Additionally, caffeine treatment increased chromatin accessibility and elevated the efficiency of illegitimate recombination. Conversely, the increase in nascent DNA synthesis did not translate into a higher number of gene targeting events. Thus, prolonged caffeine exposure stalls the cell cycle, induces a p53-mediated apoptotic response and a down-regulation of critical HR proteins, and for reasons discussed, stimulates early steps of HR, but not the formation of complete recombination products.


Assuntos
Cafeína/farmacologia , Recombinação Homóloga/efeitos dos fármacos , Apoptose/efeitos dos fármacos , Apoptose/genética , Proteína BRCA2/metabolismo , Proteínas de Ligação ao Cálcio , Proteínas de Ciclo Celular , Linhagem Celular Tumoral , Cromatina/efeitos dos fármacos , Cromatina/metabolismo , Dano ao DNA , Relação Dose-Resposta a Droga , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Pontos de Checagem da Fase G2 do Ciclo Celular/genética , Humanos , Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos , Pontos de Checagem da Fase M do Ciclo Celular/genética , Proteínas Nucleares , Rad51 Recombinase/metabolismo
18.
Food Funct ; 11(2): 1826-1834, 2020 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-32057057

RESUMO

This study evaluated the effects of polysaccharides from Spirulina platensis (PSP) on endurance during treadmill exercise; levels of some biochemical indicators including hemoglobin (Hb), lactic acid (LA), creatine kinase (CK), and blood urea nitrogen (BUN); concentrations of 5-hydroxytryptamine (5-HT); and expressions of second isoforms of tryptophan hydroxylase (TPH2) and serotonergic type 1B inhibitory autoreceptor (5-HT1B) in the caudate putamen of exercising rats. Sixty Sprague-Dawley male rats were randomly divided into six groups: control group, exercise group, exercise and PSP (50, 100, or 200 mg kg-1)-treated groups, and exercise and caffeine (10 mg kg-1)-treated group (positive control). In the exercise groups, rats were put on a treadmill and forced to run for 30 min once a day for 6 consecutive days. On the 7th day of the experiment, time to exhaustion during the treadmill exercise was determined for the trained groups. Immediately after determination of the exhaustion time, all rats were sacrificed. Levels of Hb and LA were tested by the HiCN (Hemoglobin ferricyanide) colorimetry method and a colorimetric assay, respectively. Levels of CK and BUN were determined by automatic biochemical analyzer. 5-HT concentrations were detected by HPLC analysis. TPH2 and 5-HT1B expressions were measured by western blotting and real-time PCR. The results demonstrated that PSP prolonged the time to exhaustion during the treadmill exercise; increased Hb levels; decreased LA, BUN, and CK levels in the blood; suppressed the exercise-induced increase of 5-HT concentrations and TPH2 expression; and prevented the exercise-induced decrease of 5-HT1B expression in the caudate putamen. The most potent effects were observed at the PSP dose of 200 mg kg-1. These results suggest that the mechanism of promotion of physical performance by PSP might be related to increase in Hb levels; decrease in LA, BUN, and CK levels in the blood; inhibition of the exercise-induced 5-HT and TPH2 expressions; and the increase in the 5-HT1B expression in the caudate putamen of exercised rats.


Assuntos
Comportamento Animal/efeitos dos fármacos , Resistência Física/efeitos dos fármacos , Polissacarídeos/farmacologia , Serotonina/metabolismo , Spirulina/química , Animais , Cafeína/farmacologia , Fadiga/metabolismo , Masculino , Condicionamento Físico Animal , Ratos , Ratos Sprague-Dawley
19.
Int J Mol Sci ; 21(4)2020 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-32070054

RESUMO

Bacterial nanocellulose (BNC) membranes have enormous potential as systems for topical drug delivery due to their intrinsic biocompatibility and three-dimensional nanoporous structure, which can house all kinds of active pharmaceutical ingredients (APIs). Thus, the present study investigated the long-term storage stability of BNC membranes loaded with both hydrophilic and lipophilic APIs, namely, caffeine, lidocaine, ibuprofen and diclofenac. The storage stability was evaluated under accelerated testing conditions at different temperatures and relative humidity (RH), i.e., 75% RH/40 °C, 60% RH/25 °C and 0% RH/40 °C. All systems were quite stable under these storage conditions with no significant structural and morphological changes or variations in the drug release profile. The only difference observed was in the moisture-uptake, which increased with RH due to the hydrophilic nature of BNC. Furthermore, the caffeine-loaded BNC membrane was selected for in vivo cutaneous compatibility studies, where patches were applied in the volar forearm of twenty volunteers for 24 h. The cutaneous responses were assessed by non-invasive measurements and the tests revealed good compatibility for caffeine-loaded BNC membranes. These results highlight the good storage stability of the API-loaded BNC membranes and their cutaneous compatibility, which confirms the real potential of these dermal delivery systems.


Assuntos
Materiais Biocompatíveis/farmacologia , Celulose/farmacologia , Sistemas de Liberação de Medicamentos , Nanopartículas/química , Administração Tópica , Bactérias/química , Materiais Biocompatíveis/química , Cafeína/química , Cafeína/farmacologia , Celulose/química , Diclofenaco/química , Diclofenaco/farmacologia , Portadores de Fármacos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Humanos , Ibuprofeno/química , Ibuprofeno/farmacologia , Lidocaína/química , Lidocaína/farmacologia
20.
Life Sci ; 246: 117420, 2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-32050085

RESUMO

PURPOSE: We intend to assess the effect of the conditioned medium of Caffeine pulsed MSCS in the amelioration of rheumatoid arthritis (RA)-afflicted rats. METHODS: MSCs were incubated with 0, 0.1, 0.5 or 1 mM Caffeine for 2 weeks. RA was induced by the injection of complete Freund's adjuvant (CFA) into the base of the tail of Wistar rats. According to in vitro studies, RA rats were intraperitoneally treated with MSCs, Caffeine (0.5 mM) pulsed MSCs or vehicle on day 14 when all rats had shown signs of RA. RESULTS: Our results suggest that the least effective dose concentration of Caffeine that can induce potent anti-inflammatory property in the MSC population is 0.5 mM. Without any significant impact on the vitality or MScs' marker, Caffeine at this concentration could induce lower levels of IFN-γ, IL-6, and IL-1ß and a higher level of IDO, TGF-ß, and IL-10 compared to other groups. Therefore, MSCs pulsed with Caffeine at 0.5 mM concentration was selected for in vitro studies. Caffeine pulsed MSCs could reduce the severity of the disease and improve weight-gaining more profoundly than treatment with MSCs alone. Furthermore, Caffeine pulsed MSCs caused a significant reduction in the serum levels C-reactive protein, Nitric oxide, Myeloperoxidase, TNF-α and conversely led a significant increase in the levels of IL-10 more prominent than the similar findings brought about by MSCs alone. CONCLUSION: In general, caffeine-treated MSCs may be a promising strategy for cell-based therapy of RA.


Assuntos
Artrite Reumatoide/terapia , Cafeína/farmacologia , Transplante de Células-Tronco Mesenquimais/métodos , Células-Tronco Mesenquimais/efeitos dos fármacos , Animais , Artrite Experimental/imunologia , Artrite Experimental/terapia , Artrite Reumatoide/imunologia , Relação Dose-Resposta a Droga , Imunomodulação , Masculino , Ratos , Ratos Wistar
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