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: 02, 26, 68 and 824 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 0·11·9), 0·1 (range 00·4), 0·8 (range 0·23·9), 0·2 (range 0·1 1·7) and 1 (range 0·33·4) mmol/l, respectively. The areas under the plasma concentration v. time curves (AUC0!24) were 427 (range 1021185) mmol/l £ min for EGC-glucuronide, 112 (range 53919) mmol/l £ min for EC-sulphate, 71 (range 26306) mmol/l £ min for EGCG, 40 (range 12258) mmol/l £ min for EC-glucuronide and 14 (range 0·1124) mmol/l £ min for ECG. The values of mean residence time (MRT0!24) were 5 (range 216), 2 (range 111), 10 (range 213), 3 (range 216) and 2·4 (range 118) 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.

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.

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.

Female stick insects mate multiply to find compatible mates

Why females of many species mate multiply in the absence of direct benefits remains an open question in evolutionary ecology. Interacting and mating with multiple males can be costly to females in terms of time, resources, predation risk, and disease transmission. A number of indirect genetic benefits have been proposed to explain such behaviors, but the relative importance of these mechanisms in natural systems remains unclear. We tested for several direct and indirect benefits of polyandry in the walking stick Timema cristinae. We found no evidence of direct benefits with respect to longevity or fecundity. However, male x female genotypic interactions affected egg-hatching success and offspring production independent of relatedness, suggesting that mating with certain males benefits females and that the best male may differ for each female. Furthermore, multiply mated females biased paternity toward one or few males, and the extent of this bias was positively correlated to egg-hatching success. Our data, therefore, provide evidence for indirect benefits through compatibility effects in this species. By mating multiply, females may improve their chances of mating with a compatible male if compatibility cannot be assessed before mating. Such compatibility effects can explain the evolution and maintenance of polyandry in Timema and many other species.

La intervenció psicomotriu educativa com estratègia per afavorir la inclusió d'alumnes amb trastorn de l'espectre autista (TEA) dins l'aula ordinària: Anàlisi d'un cas

Des de la inclusió es pretén aconseguir una societat més justa per tothom, on els infants per molt diferents que siguin puguin estar i participar en una escola ordinària, gaudint de les mateixes oportunitats i els mateixos drets. Amb la diversitat ens enriquim els uns amb els altres i aquest fet dóna sentit a l’educació. Amb aquest marc referencial, el present treball d’investigació tracta sobre la millora de la inclusió d’un infant amb TEA (Trastorn de l’Espectre Autista) a través de la pràctica psicomotriu educativa i vivencial, és a dir, una educació més lliure, donant lloc a l’experiència i a uns espais relacionals per dur a terme una activitat espontània psicomotriu. De fet, tracta de demostrar, de manera més específica, que la pràctica psicomotriu millora la capacitat d’interacció social de l’infant amb TEA, és a dir, la relació amb els altres, així com assegurar que aquesta pràctica vivencial aporta més beneficis en la implicació del joc dels infants amb TEA, que una intervenció psicomotriu més funcional.

Green tea catechin inhibits fatty acid synthase without stimulating carnitine Palmitoyltransferase-1 or inducing weight loss in experimental animals

Background: The enzyme fatty acid synthase (FASN) is highly expressed in many human carcinomas and its inhibition is cytotoxic to human cancer cells. The use of FASN inhibitors has been limited until now by anorexia and weight loss, which is associated with the stimulation of fatty acid oxidation. Materials and Methods: The in vitro effect of (-)-epigallocatechin-3-gallate (EGCG) on fatty acid metabolism enzymes, on apoptosis and on cell signalling was evaluated. In vivo, the effect of EGCG on animal body weight was addressed. Results: EGCG inhibited FASN activity, induced apoptosis and caused a marked decrease of human epidermal growth factor receptor 2 (HER2), phosphatidylinositol 3-kinase (PI3K)/AKT and extracellular (signal)-regulated kinase (ERK) 1/2 proteins, in breast cancer cells. EGCG did not induce a stimulatory effect on CPT-1 activity in vitro (84% of control), or on animal body weight in vivo (99% of control). Conclusion: EGCG is a FASN inhibitor with anticancer activity which does not exhibit cross-activation of fatty acid oxidation and does not induce weight loss, suggesting its potential use as an anticancer drug.

Variação anual de metilxantinas totais em amostras de Ilex paraguariensis A. St. - Hil. (erva-mate) em Ijuí e Santa Maria, Estado do Rio Grande do Sul

Ilex paraguariensis is a native plant in Southern Brazil, whose leaves are utilized in beverages such as chimarrão and tererê. This study investigated variations of total methylxanthines in leaves from two Ilex populations collected at one-month intervals over the course of one year. The levels varied from 1.92 to 10.37 mg/g (Ijuí) and 1.77 to 9.17 mg/g (Santa Maria). Statistical analysis indicated a significative variation in the contents of all samples analysed, confirming seasonal fluctuations. These results show that the period of harvest might decisively influence the organoleptic characteristics of raw material used in industry and therefore in commercial products.

Influência do método de extração nos teores de metilxantinas em erva-mate (Ilex paraguariensis a. St.-Hil., aquifoliaceae)

Ilex paraguariensis A. St. -Hil. is a native species of southern South America. The caffeine content in Ilex paraguariensis leaves has been considered an important quality parameter for maté-derived products. In this work different extraction methods for the determination of these methylxantines are compared. The influence of the extraction conditions on the methylxanthine yields was evaluated. Extraction by decoction with acidic aqueous solution (H2SO4 4N) presented the higher efficiency in the theobromine extraction. The extraction in a Soxhlet with acidic aqueous solution and decoction with acidic aqueous solution showed the highest caffeine yield. For the concomitant theobromine and caffeine quantification, the decoction with acidic aqueous solution is suggested.

Determinação do perfil de compostos voláteis e avaliação do sabor e aroma de bebidas produzidas a partir da erva-mate (Ilex paraguariensis)

Volatile compounds from green and roasted yerba mate were analyzed by gas chromatography/mass spectrometry and the flavor profile from yerba mate beverages was determined by descriptive quantitative analyses. The main compounds tentatively identified in green mate were linalool, alpha-terpineol and trans-linalool oxide and in roasted mate were (E,Z)-2,4-heptadienal isomers and 5-methylfurfural. Green mate infusion was qualified as having bitter taste and aroma as well as green grass aroma while roasted mate was defined as having a smooth, slightly burnt aroma. The relationship between the tentatively identified compounds and flavor must be determined by olfatometric analysis.

Determinação de compostos fenólicos por cromatografia líquida de alta eficiência isocrática durante estacionamento da erva-mate

Different phenolic compound, 5- caffeoylquinic acid (5-CQA), caffeic acid (AC) and rutin (Ru) contents of yerba-mate (Ilex paraguariensis) Brazilian samples of 06 different regions of São Mateus - Paraná, during natural and accelerated industrial storage, were evaluated. For quantification, a reverse phase HPLC isocratic method was developed and validated using methanol:water (35:65 v/v) acidified with 0.5% acetic acid as mobile phase and a photodiode array detector. The six sample global average contents were (34.90 and 36.10 mg g-1) for 5-CQA, (0.18 mg g-1 and 0.23 mg g-1) for AC and (7.12 and 7.18 mg g-1) for Ru, respectively, for the natural and accelerated storage systems. The results showed that the 5-CQA and Ru content are kept constant during the storage while AC content increase only during accelerated storage.

Foam-forming properties of Ilex paraguariensis (mate) saponin: foamability and foam lifetime analysis by Weibull equation

Saponins are natural soaplike foam-forming compounds widely used in foods, cosmetic and pharmaceutical preparations. In this work foamability and foam lifetime of foams obtained from Ilex paraguariensis unripe fruits were analyzed. Polysorbate 80 and sodium dodecyl sulfate were used as reference surfactants. Aiming a better data understanding a linearized 4-parameters Weibull function was proposed. The mate hydroethanolic extract (ME) and a mate saponin enriched fraction (MSF) afforded foamability and foam lifetime comparable to the synthetic surfactants. The linearization of the Weibull equation allowed the statistical comparison of foam decay curves, improving former mathematical approaches.

Green tea in transdermal formulation: HPLC method for quality control and in vitro drug release assays

RP-HPLC based analytical method for use in both quality control of green tea in a semisolid formulation and for in vitro drug release assays was developed and validated. The method was precise (CV < 5%), accurate (recovery between 98% and 102%), linear (R² > 0.99), robust, and specific for the determination of epigallocatechin 3-gallate (EGCG), caffeine (CAF), and gallic acid (GA). In a diffusion cell chamber, the release rate of EGCG was 8896.01 µg cm-2. This data showed that EGCG will be able to exert its systemic activity when delivered though the transdermal formulation, due to its good flux rates with the synthetic membrane.

Estudo comparativo de dellineamentos experimentais para estimativas de parâmetros genéticos em erva-mate (Ilex paraguariensis A. St. - Hil.)

O presente trabalho teve por objetivo comparar a eficiência do látice em relação aos delineamentos em blocos casualizados (DBC) e inteiramente casualizados (DIC) quanto aos caracteres altura e produção de massa verde em erva-mate (Ilex paraguariensis A. St. - Hil.). O experimento, conduzido na Fazenda Experimental do Canguiri, da Universidade Federal do Paraná, em Pinhais, PR, foi composto de cinco procedências, quatro com 13 e uma com 12 progênies de meias-irmãs. Cada progênie continha 54 plantas (nove parcelas de seis plantas). O experimento seguiu o modelo látice 8 x 8 com nove repetições balanceadas. As análises foram conduzidas usando-se tanto este modelo quanto os modelos DBC e DIC. Com relação ao caráter altura, a estimativa da eficiência do DBC em relação ao DIC (Êb/i) foi de 48,6%; do látice em relação ao DBC (Êl/b), de 61%; e do látice em relação ao DIC (Êl/i), de 139%. A estimativa da correlação intraclasse entre plantas dentro das parcelas (c²) foi de 9,4% para o DBC e zero para o látice. Para o caráter produção de massa verde, Êb/i, Êl/b e Êl/i foram de 14,3; 81,7; e 108%, respectivamente; e c², 16,9% para o DBC e 3,1% para o látice. Essas estimativas, associadas a uma estimativa de F de Snedecor altamente significativa dos dois caracteres, permitiram concluir que a capacidade de teste do DBC foi satisfatória para o caráter altura de plantas, mas insatisfatória para o caráter produção de massa verde.

Distribuição espacial e tamanho de amostra para o ácaro-do bronzeado da erva-mate

O ácaro Dichopelmus notus Keifer (Acari, Eriophyidae) provoca o bronzeamento e queda de folhas da erva-mate, reduzindo a produção e a qualidade de seus produtos. O acompanhamento dos níveis populacionais dessa espécie é importante para aprimorar seu manejo em plantios comerciais. Este trabalho teve por objetivos identificar a distribuição espacial e determinar o número de plantas e de folhas por planta que devem ser inspecionadas em cultivos comerciais de erva-mate em programas de monitoramento do ácaro-do-bronzeado. O estudo foi conduzido no Município de Chapecó, Santa Catarina, no período de janeiro de 2004 a janeiro de 2005. As avaliações foram realizadas quinzenalmente em um erval de 10 anos, dividido em três talhões com cerca de 2.500 m²cada, em que foram selecionadas 10 plantas ao acaso e em cada planta foi observado o número de ácaros em 18 folhas maduras. As inspeções foram executadas diretamente nos ervais com lentes com aumento de 10 vezes e 1 cm² de campo fixo. Constatou-se a distribuição espacial agregada para o ácaro, bem como a necessidade de inspecionar três folhas por planta, em 29 delas ao acaso e por hectare, de fevereiro a abril, para estimar a população com nível de precisão de 15%.

EFEITO DA ADIÇÃO DE RESÍDUOS DE PODA DA ERVA-MATE EM PAINÉIS AGLOMERADOS

O objetivo deste trabalho foi avaliar a viabilidade técnica da utilização de resíduos da poda de erva-mate na produção de painéis aglomerados. Foram produzidos painéis de aglomerados nas seguintes composições: 100% de pinus (T1), 100% de resíduos de erva-mate com casca (T2), 100% de resíduos de erva-mate sem casca (T3), 50% de pinus com 50% de resíduos de erva-mate com casca (T4) e 50% de pinus com 50% de resíduos de erva-mate sem casca (T5). Os painéis foram produzidos com o adesivo ureia-formaldeído a um teor de 8%, com ciclo de prensagem de 8 min, a 170 ºC e 30 kgf.cm-2. Os painéis produzidos com os resíduos de erva-mate apresentaram menor umidade de equilíbrio higroscópico (UEH), assim como menor absorção de água após 24 h de imersão (AA 24 h). Não houve diferença estatística entre os tratamentos quanto às propriedades de compressão, arrancamento de parafusos, dureza Janka e ligação interna. Os painéis produzidos com resíduos de erva-mate, assim como as misturas deles com partículas de pinus, apresentaram valores de módulo de ruptura à flexão estática inferiores aos estipulados pela norma brasileira NBR 14810-2 (ABNT, 2002). Como não atenderam a um dos requisitos mínimos, painéis produzidos com resíduos de erva-mate não devem ser utilizados em substituição aos painéis de madeira aglomerada.