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1.
Nutrients ; 16(13)2024 Jun 26.
Artículo en Inglés | MEDLINE | ID: mdl-38999769

RESUMEN

Caffeine is a well-described ergogenic aid used to enhance athletic performance. Using animal models can greatly increase our understanding of caffeine's mechanisms in performance. Here, we adapted an animal weight-lifting exercise model to demonstrate caffeine's ergogenic effect in rats. Male Wistar rats (315 ± 35 g) were randomly divided into two groups: one group received 5 mg·kg-1 of caffeine (0.5 mL; CEx; n = 5) and the other 0.9% NaCl (0.5 mL; PEx; n = 4) through an orogastric probe (gavage) one hour before exercise. Weight-lifting exercise sessions were performed over three subsequent days, and the number of complete squats performed was counted. Analyses of the area under the curve in all three experiments showed that the CEx group responded more to stimuli, performing more squats (1.7-, 2.0-, and 1.6-fold; p < 0.05) than the control group did. These three days' data were analyzed to better understand the cumulative effect of this exercise, and a hyperbolic curve was fitted to these data. Data fitting from the caffeine-supplemented group, CEx, also showed larger Smax and Kd (2.3-fold and 1.6-fold, respectively) than the PEx group did. Our study demonstrated an acute ergogenic effect of caffeine in an animal weight-lifting exercise model for the first time, suggesting potential avenues for future research.


Asunto(s)
Cafeína , Ratas Wistar , Levantamiento de Peso , Animales , Cafeína/farmacología , Cafeína/administración & dosificación , Masculino , Proyectos Piloto , Ratas , Levantamiento de Peso/fisiología , Condicionamiento Físico Animal/fisiología , Sustancias para Mejorar el Rendimiento/farmacología , Sustancias para Mejorar el Rendimiento/administración & dosificación
3.
Sci Rep ; 14(1): 15571, 2024 Jul 06.
Artículo en Inglés | MEDLINE | ID: mdl-38971848

RESUMEN

The aim of the current study was to investigate the effects of ingesting different dosages of caffeine (CAF) prior to plyometric jump training (PJT) on sport-related performance and physiological parameters in male basketball players. Twenty-four young athletes were randomly divided into 3 groups and performed 6 weeks of PJT while consuming 3 mg·kg-1 of body mass caffeine (CAF3, n = 8), 6 mg·kg-1 body mass caffeine (CAF6, n = 8) or placebo (PL; n = 8) one hour prior to each training session. Before and after the 6-week PJT, the players were evaluated for field-based basketball-specific performance measures (vertical jump, 20-m sprint, Illinois change of direction speed [CODS], and maximal strength) and lab-based physiological (aerobic capacity and anaerobic power) parameters. CAF3, CAF6, and PL groups demonstrated significant improvements in vertical jump (ES = 1.07, 1.45, and 1.1, respectively), 20-m sprint (ES = - 0.50, - 0.61, and - 0.36), change of direction performance (ES = - 1.22, - 1.26, and - 1.09), maximal strength (ES = 1.68, 2.29, and 1.17), maximum oxygen uptake (V̇O2max) (ES = 1.09, 1.59, and 0.92), and peak (ES = 1.82, 1.85, and 0.82) and average power output (ES = 1.39, 1.32, and 1.07) after 6 weeks of training. Comparative analysis of individual adaptive responses to training indicated that the CAF6 led to insignificantly greater effects in vertical jump (ES = 1.45), maximal strength (ES = 2.29), and V̇O2max (ES = 1.59) with lower residuals in individual changes and lower coefficient of variations (CV) in mean group changes. Regarding sprint and CODS performance, both experimental groups indicated similar changes, residuals in individual changes, and CVs in mean group changes. Overall, consuming 6 mg·kg-1 body mass caffeine induces superior adaptations in aerobic fitness, anaerobic power, and sport-specific performance measures, with lower inter-individual variability in the adaptations and more homogenized changes over the training period.


Asunto(s)
Adaptación Fisiológica , Rendimiento Atlético , Baloncesto , Cafeína , Humanos , Baloncesto/fisiología , Cafeína/administración & dosificación , Masculino , Rendimiento Atlético/fisiología , Adaptación Fisiológica/efectos de los fármacos , Ejercicio Pliométrico/métodos , Adolescente , Atletas , Adulto Joven , Fuerza Muscular/efectos de los fármacos
4.
ACS Chem Biol ; 19(7): 1661-1670, 2024 Jul 19.
Artículo en Inglés | MEDLINE | ID: mdl-38975966

RESUMEN

The calcium-sensing receptor (CaSR), abundantly expressed in the parathyroid gland and kidney, plays a central role in calcium homeostasis. In addition, CaSR exerts multimodal roles, including inflammation, muscle contraction, and bone remodeling, in other organs and tissues. The diverse functions of CaSR are mediated by many endogenous and exogenous ligands, including calcium, amino acids, glutathione, cinacalcet, and etelcalcetide, that have distinct binding sites in CaSR. However, strategies to evaluate ligand interactions with CaSR remain limited. Here, we developed a glutathione-based photoaffinity probe, DAZ-G, that analyzes ligand binding to CaSR. We showed that DAZ-G binds to the amino acid binding site in CaSR and acts as a positive allosteric modulator of CaSR. Oxidized and reduced glutathione and phenylalanine effectively compete with DAZ-G conjugation to CaSR, while calcium, cinacalcet, and etelcalcetide have cooperative effects. An unexpected finding was that caffeine effectively competes with DAZ-G's conjugation to CaSR and acts as a positive allosteric modulator of CaSR. The effective concentration of caffeine for CaSR activation (<10 µM) is easily attainable in plasma by ordinary caffeine consumption. Our report demonstrates the utility of a new chemical probe for CaSR and discovers a new protein target of caffeine, suggesting that caffeine consumption can modulate the diverse functions of CaSR.


Asunto(s)
Cafeína , Glutatión , Receptores Sensibles al Calcio , Receptores Sensibles al Calcio/metabolismo , Humanos , Regulación Alostérica/efectos de los fármacos , Cafeína/química , Cafeína/farmacología , Cafeína/metabolismo , Glutatión/metabolismo , Glutatión/química , Calcio/metabolismo , Etiquetas de Fotoafinidad/química , Sitios de Unión , Células HEK293 , Ligandos , Cinacalcet/química , Cinacalcet/farmacología
5.
Diagn. tratamento ; 29(2): 59-66, abr-jun. 2024. tab, quad
Artículo en Portugués | LILACS, SES-SP | ID: biblio-1553890

RESUMEN

Contexto: A associação entre a cafeína e o zumbido é bastante descrita na literatura, mas o papel da cafeína no zumbido não é claramente explicado. A redução no consumo de cafeína ou mesmo sua abolição é recomendada como meio de melhorar o zumbido. Entretanto, há fundamentação nessa orientação? Há evidências científicas que respaldam essa ação? Objetivo: Avaliar as evidências relativas à possível associação entre a ingestão de cafeína e o zumbido. Métodos: Trata-se de sinopse baseada em evidências. Procedeu-se à busca por estudos que associavam cafeína e zumbido em quatro bases de dados: Cochrane - Central de Registros de Ensaios Clínicos - CENTRAL (2023), PubMed (1966-2023), Portal Regional Biblioteca Virtual em Saúde (1982-2023) e Embase (1974-2023). Foram utilizados os descritores "caffeine" e "tinnitus". Dois pesquisadores, independentemente, extraíram os dados e avaliaram a qualidade dos estudos para a síntese. O desfecho primário de análise envolveu a relação entre o consumo de cafeína e o zumbido. Resultados: Foram encontradas 79 referências. Cinco estudos (1 ensaio clínico, 2 coortes e 2 estudos caso-controle) foram incluídos (n = 65.856 participantes). Discussão: A literatura apresenta poucos estudos que buscam a relação entre o consumo de cafeína e o zumbido. Trata-se de estudos com amostragem reduzida e limitações metodológicas. A evidência é baixa e são necessários novos estudos. Conclusões: Não é possível concluir sobre uma possível relação entre a cafeína e o zumbido. Há poucos estudos prospectivos realizados e a evidência é baixa, sendo necessária a realização de novos estudos prospectivos de qualidade para elucidação dessa questão.


Asunto(s)
Acúfeno , Cafeína , Estimulantes del Sistema Nervioso Central
6.
Sensors (Basel) ; 24(12)2024 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-38931814

RESUMEN

Movement-related cortical potential (MRCP) is observed in EEG recordings prior to a voluntary movement. It has been used for e.g., quantifying motor learning and for brain-computer interfacing (BCIs). The MRCP amplitude is affected by various factors, but the effect of caffeine is underexplored. The aim of this study was to investigate if a cup of coffee with 85 mg caffeine modulated the MRCP amplitude and the classification of MRCPs versus idle activity, which estimates BCI performance. Twenty-six healthy participants performed 2 × 100 ankle dorsiflexion separated by a 10-min break before a cup of coffee was consumed, followed by another 100 movements. EEG was recorded during the movements and divided into epochs, which were averaged to extract three average MRCPs that were compared. Also, idle activity epochs were extracted. Features were extracted from the epochs and classified using random forest analysis. The MRCP amplitude did not change after consuming caffeine. There was a slight increase of two percentage points in the classification accuracy after consuming caffeine. In conclusion, a cup of coffee with 85 mg caffeine does not affect the MRCP amplitude, and improves MRCP-based BCI performance slightly. The findings suggest that drinking coffee is only a minor confounder in MRCP-related studies.


Asunto(s)
Interfaces Cerebro-Computador , Cafeína , Electroencefalografía , Movimiento , Humanos , Cafeína/farmacología , Masculino , Electroencefalografía/métodos , Femenino , Movimiento/efectos de los fármacos , Movimiento/fisiología , Adulto , Adulto Joven , Café/química
7.
Yakugaku Zasshi ; 144(7): 715-732, 2024.
Artículo en Japonés | MEDLINE | ID: mdl-38945846

RESUMEN

An aqueous solution of 2,3-cis gallate type catechin (-)-epigallocatechin-3-O-gallate (EGCg) and caffeine afforded a precipitate of Creaming-down Phenomenon, which crystallized slowly for about three months to give a colorless block crystal. By X-ray crystallographic analysis, the crystal was determined to be a 2 : 2 complex of EGCg and caffeine, in which caffeine molecules were captured in a hydrophobic space formed with three aromatic A, B, and B' rings of EGCg. It was considered that the solubility of the 2 : 2 complex in water rapidly decreased and the 2 : 2 complex precipitated from aqueous solution. The hydrophobic spaces of EGCg captured a variety of heterocyclic compounds, and the molecular capture abilities of heterocyclic compounds using EGCg from the aqueous solutions were evaluated. Since the C ring of EGCg has two chiral carbon atoms, C2 and C3, the hydrophobic space of EGCg was a chiral space. EGCg captured diketopiperazine cyclo(Pro-Xxx) (Xxx=Phe, Tyr) and pharmaceuticals with a xanthine skeleton, proxyphylline and diprophylline, in the hydrophobic space, and recognized their chirality.


Asunto(s)
Cafeína , Catequina , Interacciones Hidrofóbicas e Hidrofílicas , Solubilidad , , Catequina/química , Catequina/análogos & derivados , Té/química , Cafeína/química , Cristalografía por Rayos X , Estereoisomerismo , Agua/química , Cristalización , Soluciones , Compuestos Heterocíclicos/química , Xantinas/química
8.
Spectrochim Acta A Mol Biomol Spectrosc ; 320: 124617, 2024 Nov 05.
Artículo en Inglés | MEDLINE | ID: mdl-38870697

RESUMEN

Confocal Raman Spectroscopy is recognised as a potent tool for molecular characterisation of biological specimens. There is a growing demand for In Vitro Permeation Tests (IVPT) in the pharmaceutical and cosmetic areas, increasingly conducted using Reconstructed Human Epidermis (RHE) skin models. In this study, chemical fixation of RHE in 10 % Neutral Buffered Formalin for 24 h has been examined for storing RHE samples at 4 °C for up to 21 days. Confocal Raman Spectroscopy (CRS), combined with Principal Components Analysis, revealed the molecular-level effects of fixation, notably in protein and lipid conformation within the stratum corneum and viable epidermis. IVPT by means of high-performance liquid chromatography, using caffeine as a model compound, showed minimal impact of formalin fixation on the cumulative amount, flux, and permeability coefficient after 12 h. While the biochemical architecture is altered, the function of the model as a barrier to maintain rate-limiting diffusion of active molecules within skin layers remains intact. This study opens avenues for enhanced flexibility and utility in skin model research, promising insights into mitigating the limited shelf life of RHE models by preserving performance in fixed samples for up to 21 days.


Asunto(s)
Epidermis , Formaldehído , Espectrometría Raman , Humanos , Espectrometría Raman/métodos , Epidermis/metabolismo , Epidermis/efectos de los fármacos , Formaldehído/química , Permeabilidad/efectos de los fármacos , Fijación del Tejido/métodos , Cafeína/farmacología , Cafeína/metabolismo , Absorción Cutánea/efectos de los fármacos , Análisis de Componente Principal
9.
Pharmacol Biochem Behav ; 241: 173793, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38823543

RESUMEN

OBJECTIVE: Caffeine and modafinil are used to reverse effects of sleep deprivation. Nicotinic alpha-7 receptor and AMPA receptor positive allosteric modulators (PAM) are also potential substances in this context. Our objective is to evaluate the effects of caffeine, modafinil, AVL-3288 (nicotinic alpha-7 PAM) and CX516 (AMPA receptor PAM) on cognition and mood in a model of sleep deprivation. METHOD: Modified multiple platform model is used to sleep-deprive mice for 24 days, for 8 h/day. Vehicle, Modafinil (40 mg/kg), Caffeine (5 mg/kg), CX516 (10 mg/kg), and AVL3288 (1 mg/kg) were administered intraperitoneally daily. A cognitive test battery was applied every six days for four times. The battery that included elevated plus maze, novel object recognition, and sucrose preference tests was administered on consecutive days. RESULTS: Sleep deprivation decreased novel object recognition skill, but no significant difference was found in anxiety and depressive mood. Caffeine administration decreased anxiety-like behavior in short term, but this effect disappeared in chronic administration. Caffeine administration increased memory performance in chronic period. AVL group showed better memory performance in short term, but this effect disappeared in the rest of experiment. Although, in the modafinil group, no significant change in mood and memory was observed, anhedonia was observed in the chronic period in vehicle, caffeine and modafinil groups, but not in AVL-3288 and CX-516 groups. CONCLUSION: Caffeine has anxiolytic effect in acute administration. The improvement of memory in chronic period may be associated with the neuroprotective effects of caffeine. AVL-3288 had a short-term positive effect on memory, but tolerance to these effects developed over time. Furthermore, no anhedonia was observed in AVL-3288 and CX516 groups in contrast to vehicle, caffeine and modafinil groups. This indicates that AVL-3288 and CX516 may show protective effect against depression.


Asunto(s)
Afecto , Cafeína , Cognición , Modafinilo , Privación de Sueño , Animales , Privación de Sueño/psicología , Privación de Sueño/tratamiento farmacológico , Privación de Sueño/complicaciones , Modafinilo/farmacología , Modafinilo/administración & dosificación , Ratones , Masculino , Cognición/efectos de los fármacos , Cafeína/farmacología , Cafeína/administración & dosificación , Afecto/efectos de los fármacos , Modelos Animales de Enfermedad , Estimulantes del Sistema Nervioso Central/farmacología , Estimulantes del Sistema Nervioso Central/administración & dosificación , Compuestos de Bencidrilo/farmacología , Compuestos de Bencidrilo/administración & dosificación , Factores de Tiempo , Ansiedad/tratamiento farmacológico
10.
Molecules ; 29(12)2024 Jun 19.
Artículo en Inglés | MEDLINE | ID: mdl-38930987

RESUMEN

Peanut shells' adsorption performance in caffeine and triclosan removal was studied. Peanut shells were analyzed for their chemical composition, morphology, and surface functional groups. Batch adsorption and fixed-bed column experiments were carried out with solutions containing 30 mg/L of caffeine and triclosan. The parameters examined included peanut shell particle size (120-150, 300-600, and 800-2000 µm), adsorbent dose (0.02-60 g/L), contact time (up to 180 min), bed height (4-8 cm), and hydraulic loading rate (2.0 and 4.0 m3/m2-day). After determining the optimal adsorption conditions, kinetics, isotherm, and breakthrough curve models were applied to analyze the experimental data. Peanut shells showed an irregular surface and consisted mainly of polysaccharides (around 70% lignin, cellulose, and hemicellulose), with a specific surface area of 1.7 m2/g and a pore volume of 0.005 cm3/g. The highest removal efficiencies for caffeine (85.6 ± 1.4%) and triclosan (89.3 ± 1.5%) were achieved using the smallest particles and 10.0 and 0.1 g/L doses over 180 and 45 min, respectively. Triclosan showed easier removal compared to caffeine due to its higher lipophilic character. The pseudo-second-order kinetics model provided the best fit with the experimental data, suggesting a chemisorption process between caffeine/triclosan and the adsorbent. Equilibrium data were well-described by the Sips model, with maximum adsorption capacities of 3.3 mg/g and 289.3 mg/g for caffeine and triclosan, respectively. In fixed-bed column adsorption tests, particle size significantly influenced efficiency and hydraulic behavior, with 120-150 µm particles exhibiting the highest adsorption capacity for caffeine (0.72 mg/g) and triclosan (143.44 mg/g), albeit with clogging issues. The experimental data also showed good agreement with the Bohart-Adams, Thomas, and Yoon-Nelson models. Therefore, the findings of this study highlight not only the effective capability of peanut shells to remove caffeine and triclosan but also their versatility as a promising option for water treatment and sanitation applications in different contexts.


Asunto(s)
Arachis , Cafeína , Triclosán , Cafeína/química , Cafeína/aislamiento & purificación , Triclosán/química , Triclosán/aislamiento & purificación , Arachis/química , Adsorción , Cinética , Contaminantes Químicos del Agua/química , Contaminantes Químicos del Agua/aislamiento & purificación , Tamaño de la Partícula , Purificación del Agua/métodos
12.
J Food Sci ; 89(7): 4450-4468, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38822553

RESUMEN

A novel style of flavored wine was developed via infusion of either black tea or green tea into Chardonnay wine. The bioaccessibility and bioavailability of phenolic substances in green/black tea-infused Chardonnay wine were investigated. Catechin, caffeine, and epicatechin gallate, originating from the tea, displayed high absorption rates with apparent permeability coefficient values above 10 × 10-6 cm/s in a human Caco-2 intestinal cell model. A paracellular pathway was proposed to drive the transport of catechin and epicatechin gallate, while the possible transport pathway of caffeine is passive transcellular diffusion route. Co-supplementation of flavonoids of quercetin or naringenin (20 µM) could further enhance the uptake of catechin and epicatechin gallate, but reduce the absorption of caffeine. Great in vitro and cellular antioxidant capacities were witnessed in the tea-macerated wine samples. The wine samples also neutralized the negative impact of tert-butyl hydroperoxide (25 µM) on glutathione S-transferase and glutathione levels, apoptosis induction, and intracellular malondialdehyde levels. RNA sequencing with limma method revealed a total of 1473 and 406 differentially expressed genes in the 21-day-old Caco-2 intestinal cells treated with the green and black tea-macerated wines for 5 h respectively, indicating metabolic changes in the cells from the different wines.


Asunto(s)
Antioxidantes , Cafeína , Catequina , , Vino , Humanos , Células CACO-2 , Vino/análisis , Antioxidantes/farmacología , Catequina/análogos & derivados , Catequina/metabolismo , Catequina/farmacología , Té/química , Camellia sinensis/química , Glutatión/metabolismo
13.
Nutrients ; 16(12)2024 Jun 08.
Artículo en Inglés | MEDLINE | ID: mdl-38931158

RESUMEN

Previous studies have reported that TT genotype carriers of the adenosine A2a receptor (ADORA2A) gene rs5751876 polymorphism have better ergogenic and anti-inflammatory responses to caffeine intake compared to C allele carriers. The aim of the present study was twofold: (1) to investigate the association of the ADORA2A rs5751876 polymorphism with acute caffeine supplementation on hormonal (growth hormone and testosterone) response to resistance exercise (RE); (2) to examine the relationship between the rs5751876 polymorphism and the resting levels of growth hormone and testosterone in athletes who are light caffeine consumers. A double-blind, crossover, placebo-controlled study involving 30 resistance-trained men (age 21.7 ± 4.1) was conducted to assess the impact of caffeine supplementation on serum growth hormone (GH) and testosterone (TS) levels before, immediately after, and 15 min post-RE. One hour before engaging in resistance exercise, subjects were randomly administered 6 mg of caffeine per kg of body mass or a placebo (maltodextrin). After a 7-day washout period, the same protocol was repeated. Resting testosterone and growth hormone levels were examined in the sera of 94 elite athletes (31 females, age 21.4 ± 2.8; 63 males, age 22.9 ± 3.8). Caffeine consumption led to significantly greater increases in GH and TS in men with the TT genotype compared to C allele carriers. Furthermore, in the group of athletes, carriers of the TT genotype had significantly higher testosterone (p = 0.0125) and growth hormone (p = 0.0365) levels compared to C allele carriers. In conclusion, the ADORA2A gene rs5751876 polymorphism may modify the effect of caffeine intake on the hormonal response to exercise.


Asunto(s)
Cafeína , Estudios Cruzados , Suplementos Dietéticos , Receptor de Adenosina A2A , Entrenamiento de Fuerza , Testosterona , Humanos , Cafeína/administración & dosificación , Masculino , Método Doble Ciego , Receptor de Adenosina A2A/genética , Adulto Joven , Testosterona/sangre , Adulto , Femenino , Atletas , Polimorfismo de Nucleótido Simple , Genotipo , Hormona de Crecimiento Humana/sangre , Polimorfismo Genético , Ejercicio Físico
14.
Nutrients ; 16(12)2024 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-38931247

RESUMEN

Guarana (GUA), a Brazilian seed extract, contains caffeine and other bioactive compounds that may have psychoactive effects. To assess the acute effects of GUA compared to a low dose of caffeine (CAF) on cognitive and mood parameters, twenty participants completed a double-blind, crossover experiment where they ingested capsules containing the following: (1) 100 mg CAF, (2) 500 mg GUA containing 130 mg caffeine, or (3) placebo (PLA). Cognitive tests (Simon and 2N-Back Task) were performed at the baseline (pre-ingestion) and 60 min after ingestion. The response time for the cognitive tests and heart rate variability were unaffected (p > 0.05) by treatment, although 2N-Back was overall faster (p = 0.001) across time. The accuracy in the 2N-Back Task showed a significant interaction effect (p = 0.029) due to higher post-ingestion versus pre-ingestion levels (p = 0.033), but only with the PLA. The supplements also had no effect on cognitive measures following physical fatigue (n = 11). There was an interaction effect on perceived mental energy, where the pre-ingestion of GUA had lower mental pep ratings compared to post-ingestion (p = 0.006) and post-exercise (p = 0.018) levels. Neither the acute ingestion of GUA nor low dose of CAF influenced cognitive performance or provided consistent benefit on mood or mental workload through vagal modulation. Additional investigations are beneficial to determining the lowest effective dose for CAF or GUA to influence mood and/or cognitive performance.


Asunto(s)
Afecto , Cafeína , Cognición , Estudios Cruzados , Frecuencia Cardíaca , Paullinia , Humanos , Cafeína/administración & dosificación , Cafeína/farmacología , Paullinia/química , Masculino , Método Doble Ciego , Cognición/efectos de los fármacos , Adulto , Adulto Joven , Femenino , Frecuencia Cardíaca/efectos de los fármacos , Afecto/efectos de los fármacos , Nervio Vago/fisiología , Nervio Vago/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/administración & dosificación , Suplementos Dietéticos
15.
Pharmacol Biochem Behav ; 241: 173806, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38878977

RESUMEN

Although previous research has illustrated the effects of the consumption of alcohol and caffeine individually, less research has focused on the popular combination of the two drugs. The increase in alcohol consumption when combined with caffeine has led to the idea that the stimulant effects of caffeine may mask the depressant effects of alcohol, and this may contribute to increased binge drinking as the individual feels more awake and stimulated. Preclinical research has shown various effects of combined alcohol and caffeine where several studies show decreased alcohol consumption and others show increased alcohol consumption and even binge-like drinking. Results from a previous study in our lab indicate that intermittent access (IA) to steady levels of low (0.015 %) but not moderate (0.03 %) caffeine increased alcohol consumption in male C57BL/6J mice. The current studies further investigated the sex and dose differences in adult mice receiving varying concentrations of caffeine on combined alcohol intake. In Experiment 1, adult mice (n = 50, 25 males and 25 females) had IA to one of the following experimental bottles throughout the 4 week period: water, alcohol (10 % v/v), caffeine (0.015 % w/v), or 10 % alcohol +0.015 % caffeine. In Experiment 2, adult mice (n = 70, 35 males and 35 females) were given IA to one of the following experimental bottles: water, alcohol (10 % v/v; steady, maintained throughout the 4 weeks), caffeine (increasing 0.01 % to 0.015 % to 0.02 % to 0.03 % weekly), or 10 % alcohol+increasing caffeine (at the previously mentioned concentrations). When both caffeine and alcohol concentrations remained steady throughout the 4 weeks, there was no change in alcohol consumption. Chronic exposure to IA caffeine led to increased locomotor activity and decreased freezing episodes when tested in the open field test approximately 6 h after removal of the bottles. In Experiment 2, caffeine dose-dependently increased alcohol co-consumption in male mice whereas female mice consumed less alcohol when it was presented in conjunction with caffeine. The results in males are in line with clinical literature suggesting that the combination of alcohol and caffeine may lead to increased stimulation and alcohol drinking. Additionally, these studies provide evidence that the escalation of caffeine is crucial when investigating alcohol and caffeine co-consumption using the IA paradigm.


Asunto(s)
Consumo de Bebidas Alcohólicas , Cafeína , Relación Dosis-Respuesta a Droga , Etanol , Ratones Endogámicos C57BL , Animales , Masculino , Cafeína/farmacología , Cafeína/administración & dosificación , Femenino , Ratones , Etanol/administración & dosificación , Etanol/farmacología , Estimulantes del Sistema Nervioso Central/farmacología , Estimulantes del Sistema Nervioso Central/administración & dosificación , Factores Sexuales , Caracteres Sexuales
16.
Drug Metab Dispos ; 52(8): 911-918, 2024 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-38849209

RESUMEN

Arsenite is an important heavy metal. Some Chinese traditional medicines contain significant amounts of arsenite. The aim of this study was to investigate subacute exposure of arsenite on activities of cytochrome P450 enzymes and pharmacokinetic behaviors of drugs in rats. Midazolam, tolbutamide, metoprolol, omeprazole, caffeine, and chlorzoxazone, the probe substrates for cytochrome P450 (CYP) s3A, 2C6, 2D, 2C11, 1A, and 2E, were selected as probe drugs for the pharmacokinetic study. Significant decreases in areas under the curves of probe substrates were observed in rats after consecutive 30-day exposure to As at 12 mg/kg. Microsomal incubation study showed that the subacute exposure to arsenite resulted in little change in effects on the activities of P450 enzymes examined. However, everted gut sac study demonstrated that such exposure induced significant decreases in intestinal absorption of these drugs by both passive diffusion and carrier-mediated transport. In addition, in vivo study showed that the arsenite exposure decreased the rate of peristaltic propulsion. The decreases in intestinal permeability of the probe drugs and peristaltic propulsion rate most likely resulted in the observed decreases in the internal exposure of the probe drugs. Exposure to arsenite may lead to the reduction of the efficiencies of pharmaceutical agents coadministered resulting from the observed drug-drug interactions. SIGNIFICANCE STATEMENT: Exposure to arsenite may lead to the reduction of the efficiencies of pharmaceutical agents coadministered resulting from the observed drug-drug interactions. The present study, we found that P450 enzyme probe drug exposure was reduced in arsenic-exposed animals (areas under the curve) and the intestinal absorption of the drug was reduced in the animals. Subacute arsenic exposure tends to cause damage to intestinal function, which leads to reduced drug absorption.


Asunto(s)
Arsenitos , Sistema Enzimático del Citocromo P-450 , Interacciones Farmacológicas , Ratas Sprague-Dawley , Animales , Arsenitos/toxicidad , Arsenitos/farmacocinética , Masculino , Ratas , Sistema Enzimático del Citocromo P-450/metabolismo , Absorción Intestinal/efectos de los fármacos , Microsomas Hepáticos/efectos de los fármacos , Microsomas Hepáticos/metabolismo , Omeprazol/farmacología , Omeprazol/farmacocinética , Midazolam/farmacocinética , Cafeína/farmacocinética , Clorzoxazona/farmacocinética , Metoprolol/farmacocinética , Metoprolol/farmacología , Tolbutamida/farmacocinética , Compuestos de Sodio/toxicidad , Compuestos de Sodio/farmacocinética
17.
Eur J Sport Sci ; 24(6): 693-702, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38874987

RESUMEN

We investigated the effect of ischemic preconditioning (IPC) with and without caffeine supplementation on mean power output (MPO) during a 4-min cycling time-trial (TT). In a double-blinded, randomized, crossover-design, 11 trained men performed a TT on 4 days separated by ∼1 week. One hour before TT, participants ingested either caffeine (3 mg kg bw-1) or placebo pills, after which femoral blood-flow was either restricted with occlusion cuffs inflated to ∼180 mmHg (IPC), or sham-restricted (0-10 mmHg; Sham) during 3 × 2-min low-intensity cycling (10% of incremental peak power output). Then, participants performed a standardized warm-up followed by the TT. Plasma lactate and K+ concentrations and ratings of perceived exertion (RPE) were measured throughout trials. TT MPO was 382 ± 17 W in Placebo + Sham and not different from Placebo + IPC (-1 W; 95% CI: -9 to 7; p = 0.848; d: 0.06), whereas MPO was higher with Caffeine + Sham (+6W; 95% CI: -2 to 14; p = 0.115; d: 0.49) and Caffeine + IPC (+8 W; 95% CI: 2-13; p = 0.019; d: 0.79) versus Placebo + Sham. MPO differences were attributed to caffeine (caffeine main-effect: +7 W; 95% CI: 2-13; p = 0.015; d: 0.54. IPC main-effect: 0 W; 95% CI: -6 to 7; p = 0.891; d: 0.03; caffeine × IPC interaction-effect: p = 0.580; d: 0.17). TT RPE and plasma variables were not different between treatments. In conlcusion, IPC with co-ingestion of placebo does not improve short-term high-intensity performance in trained men versus a double-placebo control (Placebo + Sham) and does not additively enhance performance with caffeine. These data do not support IPC as a useful strategy for athletes prior to competition but confirms caffeine's performance-enhancing effect.


Asunto(s)
Rendimiento Atlético , Ciclismo , Cafeína , Estudios Cruzados , Precondicionamiento Isquémico , Humanos , Cafeína/administración & dosificación , Cafeína/farmacología , Masculino , Método Doble Ciego , Rendimiento Atlético/fisiología , Precondicionamiento Isquémico/métodos , Adulto Joven , Ciclismo/fisiología , Adulto , Ácido Láctico/sangre , Potasio/sangre , Sustancias para Mejorar el Rendimiento/administración & dosificación , Sustancias para Mejorar el Rendimiento/farmacología , Esfuerzo Físico/fisiología
18.
Afr J Reprod Health ; 28(5): 84-89, 2024 05 31.
Artículo en Inglés | MEDLINE | ID: mdl-38920287

RESUMEN

Caffeine is one of the most widely consumed pharmacological substances globally, and is known for its potential ergogenic effects. This study examined the impact of caffeine on the blood pressure in athletic and non-athletic women. Caffeine, a CNS stimulant, enhances athletic performance by boosting stamina, alertness, and cognitive speed. The aim of this study was to assess the impact of caffeine on heart rate and blood pressure in both athletic and non-athletic women, and to inform both groups about its effects. The study was conducted in the Kingdom of Saudi Arabia and involved 30 volunteers aged 18-30 years. Participants were equally divided into three groups: athletes who consumed caffeine, non-athletes who consumed caffeine, and a control group (given a placebo). After caffeine ingestion, there were no significant differences in diastolic blood pressure (DBP), systolic blood pressure (SBP), or heart rate between athletes and non-athletes. These findings suggest that caffeine consumption does not significantly affect blood pressure in either athletic or non-athletic women. However, if it raises blood pressure in both groups, it could pose risks, prompting athletes to consider alternative hydration options such as Gatorade.


La caféine est l'une des substances pharmacologiques les plus largement consommées dans le monde, et est connue pour ses effets ergogéniques potentiels. Cette étude a examiné l'impact de la caféine sur la pression artérielle des femmes athlètes et non athlètes. La caféine, un stimulant du système nerveux central, améliore les performances des athlètes en augmentant l'endurance, la vigilance et la vitesse cognitive. L'objectif de cette étude était d'évaluer l'impact de la caféine sur la fréquence cardiaque et la pression artérielle chez les femmes athlètes et non athlètes, et d'informer les deux groupes de ses effets. L'étude a été menée au Royaume d'Arabie saoudite et a impliqué 30 volontaires âgés de 18 à 30 ans. Les participants ont été répartis également en trois groupes : des athlètes qui ont consommé de la caféine, des non-athlètes qui ont consommé de la caféine, et un groupe témoin (ayant reçu un placebo). Après l'ingestion de caféine, il n'y avait pas de différences significatives dans la pression artérielle diastolique (PAD), la pression artérielle systolique (PAS) ou la fréquence cardiaque entre les athlètes et les non-athlètes. Ces résultats suggèrent que la consommation de caféine n'affecte pas significativement la pression artérielle chez les femmes, qu'elles soient athlètes ou non. Cependant, si elle augmente la pression artérielle dans les deux groupes, cela pourrait présenter des risques, incitant les athlètes à envisager des options d'hydratation alternatives, telles que le Gatorade.


Asunto(s)
Atletas , Presión Sanguínea , Cafeína , Frecuencia Cardíaca , Humanos , Femenino , Cafeína/farmacología , Cafeína/administración & dosificación , Presión Sanguínea/efectos de los fármacos , Adulto , Frecuencia Cardíaca/efectos de los fármacos , Adulto Joven , Arabia Saudita , Adolescente , Estimulantes del Sistema Nervioso Central/farmacología , Estimulantes del Sistema Nervioso Central/administración & dosificación , Rendimiento Atlético/fisiología
19.
Braz J Med Biol Res ; 57: e13217, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38896643

RESUMEN

The purpose of this study was to verify the association between angiotensin-converting enzyme (ACE) genotypes DD, DI, and II and caffeine (CAF) ingestion on endurance performance, heart rate, ratio of perceived exertion (RPE), and habitual caffeine intake (HCI) of adolescent athletes. Seventy-four male adolescent athletes (age: DD=16±1.7; DI=16±2.0; II=15±1.7 years) ingested CAF (6 mg/kg) or placebo (PLA) one hour before performing the Yo-Yo Intermittent Recovery level 1 (Yo-Yo IR1) test. No difference was found among groups for HCI. However, CAF increased the maximal distance covered and VO2max in DI and II genotype carriers compared to PLA (DD: Δ=31 m and 0.3 mL·kg-1·min-1; DI: Δ=286 m and 1.1 mL·kg-1·min-1; II: Δ=160 m and 1.4 mL·kg-1·min-1). Heart rate of DI and II genotype carriers increased with CAF compared to PLA, while RPE was higher in the II and lower in the DD genotypes. The correlations between HCI and maximal distance covered or VO2max were significant in the II genotype carriers with CAF. CAF increased endurance capacity, heart rate, and RPE in adolescent athletes with allele I, while endurance performance and aerobic power had a positive correlation to HCI in the II genotype group. These findings suggested that DD genotype were less responsive to CAF and that genetic variations should be taken into account when using CAF supplementation to enhance exercise performance.


Asunto(s)
Atletas , Cafeína , Genotipo , Frecuencia Cardíaca , Peptidil-Dipeptidasa A , Esfuerzo Físico , Humanos , Adolescente , Masculino , Frecuencia Cardíaca/efectos de los fármacos , Cafeína/administración & dosificación , Esfuerzo Físico/fisiología , Peptidil-Dipeptidasa A/genética , Rendimiento Atlético/fisiología , Resistencia Física/efectos de los fármacos , Resistencia Física/genética , Polimorfismo Genético/genética , Brasil , Consumo de Oxígeno/genética , Consumo de Oxígeno/efectos de los fármacos , Sustancias para Mejorar el Rendimiento/administración & dosificación
20.
BMC Pediatr ; 24(1): 401, 2024 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-38898410

RESUMEN

BACKGROUND: With a wide therapeutic index, efficacy, ease of use, and other neuroprotective and respiratory benefits, caffeine citrate(CC) is currently the drug of choice for preterm neonates (PTNs). Caffeine-induced excessive energy expenditure, diuresis, natriuresis, and other CC-associated potential side-effects (CC-APSEs) result in lower daily-weight gain (WG) in premature neonates. This study aimed to evaluate the risk factors for daily-WG in neonates exposed to different dose regimens of caffeine in ICU. METHOD: This retrospective cohort study included neonates of ≤ 36weeks gestational age (GA) and received CC-therapy. The same participants were followed for data analysis in two postnatal phases: 15-28 and 29-42 days of life (DOL). Based on daily CC-dose, formed group-I (received; standard-doses = 5 mg/kg/day), group-II (received;>5-7 mg/kg/day), and group-III (received;>7 mg/kg/day). Prenatal and postnatal clinical characteristics, CC-regimen, daily-WG, CC-APSEs, and concomitant risk-factors, including daily-caloric intake, Parenteral-Nutrition duration, steroids, diuretics, and ibuprofen exposure, were analyzed separately for group-II and group-III using group-I as standard. Regression analysis was performed to evaluate the risk factors for daily-WG. RESULTS: Included 314 PTNs. During 15-28 DOL, the mean-daily-WG(MD-WG) was significantly higher in group-I than group-II [19.9 ± 0.70 g/kg/d vs. 17.7 ± 0.52 p = 0.036] and group-III [19.9 ± 0.70 g/kg/d vs. 16.8 ± 0.73 p < 0.001]. During 29-42 DOL the MD-WG of group-I was only significantly higher than group-III [21.7 ± 0.44 g/kg/d vs. 18.3 ± 0.41 g/kg/d p = 0.003] and comparable with group-II. During 15-28 DOL, observed CC-APSEs was significantly higher in group-II and III but during 29-42 DOL it was only significant in group-III. In the adjusted regression analysis for daily-WG during 15-28DOL, with respect to standard-dose, 5-7 mg/kg/day (ß=-1.04; 95%CI:-1.62,-0.93) and > 7-10 mg/kg/day (ß=-1.36; 95%CI:-1.56,-1.02) were associated with a lower daily-WG. However, during 29-42DOL, this association was present only for > 7-10 mg/kg/day (ß=-1.54; 95%CI:-1.66,-1.42). The GA ≤ 27weeks (ß=-1.03 95%CI:-1.24, -0.88) was associated with lower daily-WG only during 15-28DOL. During both periods of therapy, higher cumulative-caffeine dose and presence of culture proven sepsis, tachypnea, hyponatremia, and feeding intolerance were significantly associated with lower daily-WG. Conversely, daily kcal intake was found to be linked with an increase in daily-WG in both periods. CONCLUSION: In this study cohort exposure to higher caffeine daily and cumulative doses is associated with lower postnatal daily-WG in PTNs than standard-daily doses, which may be due to its catabolic effects and CC-APSEs.


Asunto(s)
Cafeína , Relación Dosis-Respuesta a Droga , Recien Nacido Prematuro , Aumento de Peso , Humanos , Cafeína/administración & dosificación , Cafeína/efectos adversos , Estudios Retrospectivos , Recién Nacido , Femenino , Masculino , Aumento de Peso/efectos de los fármacos , Factores de Riesgo , Unidades de Cuidado Intensivo Neonatal , Citratos/administración & dosificación , Citratos/efectos adversos , Estimulantes del Sistema Nervioso Central/administración & dosificación , Estimulantes del Sistema Nervioso Central/efectos adversos
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