Absorption and pharmacokinetics of green tea catechins in beagles

The present study evaluates for the first time in dogs, the kinetics of green tea catechins and their metabolic forms in plasma and urine. Ten beagles were administered 173 mg (12·35 mg/kg body weight) of catechins as a green tea extract, in capsules. Blood samples were collected during 24 h after intake and urine samples were collected during the following periods of time: 0-2, 2-6, 6-8 and 8-24 h. Two catechins with a galloyl moiety and three conjugated metabolites were detected in plasma. Most of the detected forms in plasma reached their maximum plasma concentration (Cmax) at around 1 h. Median Cmax for (2)-epigallocatechin-3-gallate (EGCG), (2)-epicatechin-3-gallate (ECG), (2)-epigallocatechin glucuronide (EGCglucuronide), (2)-epicatechin glucuronide (EC-glucuronide), (2)-epicatechin sulphate (EC sulphate) were 0·3 (range 0·1-1·9), 0·1 (range 0-0·4), 0·8 (range 0·2-3·9), 0·2 (range 0·1 1·7) and 1 (range 0·3-3·4) mmol/l, respectively. The areas under the plasma concentration v. time curves (AUC0!24) were 427 (range 102-1185) mmol/l £ min for EGC-glucuronide, 112 (range 53-919) mmol/l £ min for EC-sulphate, 71 (range 26-306) mmol/l £ min for EGCG, 40 (range 12-258) mmol/l £ min for EC-glucuronide and 14 (range 0·1-124) mmol/l £ min for ECG. The values of mean residence time (MRT0!24) were 5 (range 2-16), 2 (range 1-11), 10 (range 2-13), 3 (range 2-16) and 2·4 (range 1-18) h for EGCG, ECG, EGC-glucuronide, EC-glucuronide and EC sulphate, respectively. In urine, catechins were present as conjugated forms, suggesting bile excretion of EGCG and ECG. Green tea catechins are absorbed following an oral administration and EGC-glucuronide is the metabolic form that remains in the organism for a longer period of time, suggesting that this compound could suffer an enterohepatic cycle.

An integrated pharmacokinetic and pharmacodynamic study of a new drug of abuse, methylone, a synthetic cathinone sold as 'bath salts'

Material and methods. Methylone was administered to male Sprague-Dawley rats intravenously (10 mg/kg) and orally (15 and 30 mg/kg). Plasma concentrations and metabolites were characterized by LC/MS and LC-MS/MS fragmentation patterns. Locomotor activity was monitored for 180-240 min. Results. Oral administration of methylone induced a dose-dependent increase in locomotor activity in rats. The plasma concentrations after i.v. administration were described by a two-compartment model with distribution and terminal elimination phases of α = 1.95 h− 1 and β = 0.72 h− 1. For oral administration, peak methylone concentrations were achieved between 0.5 and 1 h and fitted to a flip-flop model. Absolute bioavailability was about 80% and the percentage of methylone protein binding was of 30%. A relationship between methylone brain levels and free plasma concentration yielded a ratio of 1.42 ± 0.06, indicating access to the central nervous system. We have identified four Phase I metabolites after oral administration. The major metabolic routes are N-demethylation, aliphatic hydroxylation and O-methylation of a demethylenate intermediate. Discussion. Pharmacokinetic and pharmacodynamic analysis of methylone showed a correlation between plasma concentrations and enhancement of the locomotor activity. A contribution of metabolites in the activity of methylone after oral administration is suggested. Present results will be helpful to understand the time course of the effects of this drug of abuse in humans.

Dose and time-dependent selective neurotoxicity induced by mephedrone in mice.

Mephedrone is a drug of abuse marketed as 'bath salts'. There are discrepancies concerning its long-term effects. We have investigated the neurotoxicity of mephedrone in mice following different exposition schedules. Schedule 1: four doses of 50 mg/kg. Schedule 2: four doses of 25 mg/kg. Schedule 3: three daily doses of 25 mg/kg, for two consecutive days. All schedules induced, in some animals, an aggressive behavior and hyperthermia as well as a decrease in weight gain. Mephedrone (schedule 1) induced dopaminergic and serotoninergic neurotoxicity that persisted 7 days after exposition. At a lower dose (schedule 2) only a transient dopaminergic injury was found. In the weekend consumption pattern (schedule 3), mephedrone induced dopamine and serotonin transporter loss that was accompanied by a decrease in tyrosine hydroxylase and tryptophan hydroxylase 2 expression one week after exposition. Also, mephedrone induced a depressive-like behavior, as well as a reduction in striatal D2 density, suggesting higher susceptibility to addictive drugs. In cultured cortical neurons, mephedrone induced a concentration-dependent cytotoxic effect. Using repeated doses for 2 days in an elevated ambient temperature we evidenced a loss of frontal cortex dopaminergic and hippocampal serotoninergic neuronal markers that suggest injuries at nerve endings.

An integrated pharmacokinetic and pharmacodynamic study of a new drug of abuse, methylone, a synthetic cathinone sold as 'bath salts'

Material and methods. Methylone was administered to male Sprague-Dawley rats intravenously (10 mg/kg) and orally (15 and 30 mg/kg). Plasma concentrations and metabolites were characterized by LC/MS and LC-MS/MS fragmentation patterns. Locomotor activity was monitored for 180-240 min. Results. Oral administration of methylone induced a dose-dependent increase in locomotor activity in rats. The plasma concentrations after i.v. administration were described by a two-compartment model with distribution and terminal elimination phases of α = 1.95 h− 1 and β = 0.72 h− 1. For oral administration, peak methylone concentrations were achieved between 0.5 and 1 h and fitted to a flip-flop model. Absolute bioavailability was about 80% and the percentage of methylone protein binding was of 30%. A relationship between methylone brain levels and free plasma concentration yielded a ratio of 1.42 ± 0.06, indicating access to the central nervous system. We have identified four Phase I metabolites after oral administration. The major metabolic routes are N-demethylation, aliphatic hydroxylation and O-methylation of a demethylenate intermediate. Discussion. Pharmacokinetic and pharmacodynamic analysis of methylone showed a correlation between plasma concentrations and enhancement of the locomotor activity. A contribution of metabolites in the activity of methylone after oral administration is suggested. Present results will be helpful to understand the time course of the effects of this drug of abuse in humans.

Mephedrone pharmacokinetics after intravenous and oral administration in rats: relation to pharmacodynamics

Rationale Mephedrone (4-methylmethcathinone) is a still poorly known drug of abuse, alternative to ecstasy or cocaine. Objective The major aims were to investigate the pharmacokineticsa and locomotor activity of mephedrone in rats and provide a pharmacokinetic/pharmacodynamic model. Methods Mephedrone was administered to male Sprague-Dawley rats intravenously (10 mg/kg) and orally (30 and 60 mg/kg). Plasma concentrations and metabolites were characterized using LC/MS and LC-MS/MS fragmentation patterns. Locomotor activity was monitored for 180-240 min. Results Mephedrone plasma concentrations after i.v. administration fit a two-compartment model (α=10.23 h−1, β=1.86 h−1). After oral administration, peak mephedrone concentrations were achieved between 0.5 and 1 h and declined to undetectable levels at 9 h. The absolute bioavailability of mephedrone was about 10 % and the percentage of mephedrone protein binding was 21.59±3.67%. We have identified five phase I metabolites in rat blood after oral administration. The relationship between brain levels and free plasma concentration was 1.85±0.08. Mephedrone induced a dose-dependent increase in locomotor activity, which lasted up to 2 h. The pharmacokinetic-pharmacodynamic model successfully describes the relationship between mephedrone plasma concentrations and its psychostimulant effect. Conclusions We suggest a very important first-pass effect for mephedrone after oral administration and an easy access to the central nervous system. The model described might be useful in the estimation and prediction of the onset, magnitude,and time course of mephedrone pharmacodynamics as well as to design new animal models of mephedrone addiction and toxicity.

Absorption and pharmacokinetics of green tea catechins in beagles

The present study evaluates for the first time in dogs, the kinetics of green tea catechins and their metabolic forms in plasma and urine. Ten beagles were administered 173 mg (12·35 mg/kg body weight) of catechins as a green tea extract, in capsules. Blood samples were collected during 24 h after intake and urine samples were collected during the following periods of time: 0-2, 2-6, 6-8 and 8-24 h. Two catechins with a galloyl moiety and three conjugated metabolites were detected in plasma. Most of the detected forms in plasma reached their maximum plasma concentration (Cmax) at around 1 h. Median Cmax for (2)-epigallocatechin-3-gallate (EGCG), (2)-epicatechin-3-gallate (ECG), (2)-epigallocatechin glucuronide (EGCglucuronide), (2)-epicatechin glucuronide (EC-glucuronide), (2)-epicatechin sulphate (EC sulphate) were 0·3 (range 0·1-1·9), 0·1 (range 0-0·4), 0·8 (range 0·2-3·9), 0·2 (range 0·1 1·7) and 1 (range 0·3-3·4) mmol/l, respectively. The areas under the plasma concentration v. time curves (AUC0!24) were 427 (range 102-1185) mmol/l £ min for EGC-glucuronide, 112 (range 53-919) mmol/l £ min for EC-sulphate, 71 (range 26-306) mmol/l £ min for EGCG, 40 (range 12-258) mmol/l £ min for EC-glucuronide and 14 (range 0·1-124) mmol/l £ min for ECG. The values of mean residence time (MRT0!24) were 5 (range 2-16), 2 (range 1-11), 10 (range 2-13), 3 (range 2-16) and 2·4 (range 1-18) h for EGCG, ECG, EGC-glucuronide, EC-glucuronide and EC sulphate, respectively. In urine, catechins were present as conjugated forms, suggesting bile excretion of EGCG and ECG. Green tea catechins are absorbed following an oral administration and EGC-glucuronide is the metabolic form that remains in the organism for a longer period of time, suggesting that this compound could suffer an enterohepatic cycle.

Corruption scandals, press reporting, and accountability. Evidence from Spanish mayors.

[spa] En este trabajo se analiza con datos de España los efectos de la corrupción local sobre los resultados electorales. En base a las noticias publicadas entre 1996 y 2009, se construye una nueva base de datos que recoge los casos de corrupción y noticias relativas a cambios en los planes urbanísticos que no han seguido el procedimiento legal. La base de datos muestra que los primeros escándalos de corrupción urbanística surgieron durante el mandato electoral de 1999-2003, pero que éstos alcanzaron sus niveles máximos justo antes de las elecciones de 2007. Se estima una ecuación del porcentaje de voto obtenido por el partido en el poder en estas elecciones locales y se encuentra que la pérdida media de voto después de un caso de corrupción se sitúa alrededor del 4%. Este efecto es más elevado (del 9%) si el caso de corrupción ha recibido una amplia cobertura por los diarios. Los efectos estimados para las elecciones de 2003 son significativamente inferiores. Cuando se consideran los casos en que los políticos han tenido cargas judiciales por corrupción y amplia cobertura por los diarios, la pérdida de voto asciende hasta el 12%. No obstante, la cobertura por los diarios genera un efecto negativo en el voto incluso cuando no hay cargas judiciales.

Corruption scandals, press reporting, and accountability. Evidence from Spanish mayors.

[spa] En este trabajo se analiza con datos de España los efectos de la corrupción local sobre los resultados electorales. En base a las noticias publicadas entre 1996 y 2009, se construye una nueva base de datos que recoge los casos de corrupción y noticias relativas a cambios en los planes urbanísticos que no han seguido el procedimiento legal. La base de datos muestra que los primeros escándalos de corrupción urbanística surgieron durante el mandato electoral de 1999-2003, pero que éstos alcanzaron sus niveles máximos justo antes de las elecciones de 2007. Se estima una ecuación del porcentaje de voto obtenido por el partido en el poder en estas elecciones locales y se encuentra que la pérdida media de voto después de un caso de corrupción se sitúa alrededor del 4%. Este efecto es más elevado (del 9%) si el caso de corrupción ha recibido una amplia cobertura por los diarios. Los efectos estimados para las elecciones de 2003 son significativamente inferiores. Cuando se consideran los casos en que los políticos han tenido cargas judiciales por corrupción y amplia cobertura por los diarios, la pérdida de voto asciende hasta el 12%. No obstante, la cobertura por los diarios genera un efecto negativo en el voto incluso cuando no hay cargas judiciales.

Anàlisi de competències en el Pràcticum de Pedagogia de la Universitat de Barcelona

El procés de convergència vers l"Espai Europeu d"Educació Superior (EEES), iniciat a partir de la declaració de Bolonya, col·loca l"assignatura del Pràcticum en una situació fonamental dins dels plans d"estudi de les titulacions. Això ens obliga a repensar-lo a partir dels nous paràmetres didàctics i organitzatius de l"EEES. El projecte de recerca Millora i reorientació del Pràcticum de Pedagogia vers l"EEES s"ha proposat una revisió del Pràcticum de Pedagogia de la UB des de diferents angles: l"estudi de l"ocupabilitat i la inserció laboral dels titulats de Pedagogia, la gestió i l"organització virtual de les tasques relacionades amb la coordinació del Pràcticum, així com l"elaboració d"un pla docent i un dossier de recursos per als tutors i tutores. En aquest article ens centrem exclusivament en el treball realitzat en relació a l"anàlisi de les competències que el Pràcticum de Pedagogia ha de permetre desenvolupar entre els estudiants. Aquest treball té especial vinculació amb l"elaboració d"un pla docent, però a la vegada és transversal als altres eixos esmentats.

Draft genome sequence of Aeromonas molluscorum strain 848TT, isolated from bivalve molluscs

We report here the draft genome sequence of Aeromonas molluscorum 848T, the type strain of this Aeromonas species, which was isolated from wedge shells (Donax trunculus) obtained from a retail market in Barcelona, Spain, in 1997.

Cambio climático y diversidad de la flora vascular en las montañas tabulares de Guayana.

Una de las posibles consecuencias del calentamiento global es la extinción de especies de alta montaña por migración ascendente de las condiciones ambientales y pérdida de hábitat, fenómeno que, por el momento, ha sido considerado únicamente en montañas templadas y boreales. Este trabajo analiza la misma situación en montañas tropicales y estima el grado de amenaza de la flora vascular de las cimas de las montañas neotropicales de Guayana, al norte de Sudamérica. Del estudio basado en una muestra de 83 especies, entre aproximadamente el 8 y el 33% de las mismas se encuentran en peligro de extinguirse debido a la desaparición de su hábitat. La mayoría de estas especies son endémicas de Guayana, por lo que su desaparición afectaría a la biodiversidad global.

Local perception and use of the multifunctionality of water tanks in two villages of Tamil Nadu, South India

Using data from free listings and a survey in two villages of Tamil Nadu, India, we discuss local perceptions and uses of water tanks, a traditional irrigation infrastructure. We hypothesize that both farmers and nonfarmers perceive and use water tanks for purposes other than irrigation. We found that informants recognized the importance of water tanks for irrigation, but also acknowledged other socioeconomic uses and ecological functions. Marginal sectors (i.e., Scheduled Castes) use tank resources in more diverse ways than other sectors of the population. Findings are relevant for development. International organizations working on the revival of water tanks aim to transfer water management to farmers for the purpose of irrigation. By recognizing that tanks benefit people other than farmers and in ways other than providing irrigation water, organizations working on tank rejuvenation could achieve a more equitable management of tank resources.

Sistemas agrarios sustentables y transiciones en el metabolismo agrario: desigualdad social, cambios institucionales y transformaciones del paisaje en Catalunya (1850-2010)

How did farmers maintain soil fertility as they cultivated the same land over decades and centuries? How did they transfer energy and nutrients (nitrogen, potassium, phosphorous) across the landscape to fertilize crops? How did farmers structure landscapes (field, pasture, woodland) to sustain communities, ensure long-term productivity, and produce profits? We summarize in this article the results of the ongoing research on the last stage of organic agriculture in Catalonia carried out by our project. We also outline the forthcoming steps to continue our research.

Heteromeric nicotinic receptors are involved in the sensitization and addictive properties of MDMA in mice

We have investigated the effect of nicotinic receptor ligands in the behavioral sensitization (hyperlocomotion) and rewarding properties (conditioned place preference paradigm, CPP) of 3,4-methylenedioxy-methamphetamine (MDMA) in mice. Each animal received intraperitoneal pretreatment with either saline, dihydro-β-erythroidine (DHβE, 1 mg/kg) or varenicline (VAR, 0.3 mg/kg), 15 min prior to subcutaneous saline or MDMA (5 mg/kg), for 10 consecutive days. On day 1, both DHβE and VAR inhibited the MDMA-induced hyperlocomotion. After 10 days of treatment, MDMA induced a hyperlocomotion that was not reduced (rather enhanced) in antagonist-pretreated animals. This early hyperlocomotion was accompanied by a significant increase in heteromeric nicotinic receptors in cortex that was not blocked by DHβE or VAR. Behavioral sensitization to MDMA was highest 2 weeks after the discontinuation of MDMA treatment. This additional increase in sensitivity was prevented in animals pretreated with DHβE or VAR. At this time, MDMA-treated mice showed a significant increase in heteromeric receptors in cortex that was prevented by DHβE and VAR. An involvement of α7 nicotinic receptors in this effect is ruled out. MDMA (10 mg/kg) induced positive CPP that was abolished by DHβE (2 mg/kg) and VAR (2 mg/kg). Moreover, chronic nicotine pretreatment (2 mg/kg, ip, b.i.d., for 14 days) caused MDMA, administered at a low dose (3 mg/kg), to induce CPP, which would otherwise not occur. Finally, present results point out that heteromeric nicotinic receptors are involved in locomotor sensitization and addictive potential induced by MDMA. Thus, varenicline might be a useful drug to treat both tobacco and MDMA abuse at once.

Lletra de Dona. Una eina per a l'avaluació continuada en assignatures de l'àmbit de les humanitats.

Des de 2004, un equip de professorat de l"àrea de Filologia (literatura) i ara també de Filosofia de la Universitat de Barcelona treballa en una experiència d"innovació docent anomenada Lletra de Dona. Es tracta de potenciar un tipus de tasques ressenya o comentari que faciliten l"avaluació continuada en aquests àmbits. Aquesta eina avaluadora serveix de base també per a una publicació en línia que inicia l"alumnat en el món de la crítica literària i treballa competències ètiques (responsabilitat d"autoria, visibilitat de la producció literària i filosòfica femenina) i professionalitzadores.