Alteration of the Pharmacokinetics of Theophylline by Paullinia cupana Kunth in Rats

Aims: Paullinia cupana Kunth has been popularly used to prepare different beverages by the Amazonian inhabitants for a long time ago mainly due to its stimulant properties. Although the utilization of this herbal drug has been increasing lately, little is known regarding the possibility of drug interactions. Therefore, this research tried to investigate the effects of the aqueous extract of P. cupana on the pharmacokinetics of theophylline (TPH), a CYP1A marker in rats. Methodology: The extract was prepared according to the popular recipe and subjects received different once daily doses of extract (vehicle, 82.1 mg/Kg and 821 mg/Kg) by oral gavage during two weeks. Non-compartimental analysis was carried out to obtain the pharmacokinetic parameters. Results: Animals treated with P. cupana (AUC: 1,197.2 ± 284.4 and 346.6 ± 37.0 µg.h/mL for 82.1 and 821 mg/Kg, respectively) had lower exposition to TPH than controls (3,539.48 ± 278.4 µg.h/mL). On the other hand, drug clearance was higher in treated subjects (2.44 ± 0.4 and 7.27 ± 0.7 L/h/kg for 82.1 and 821 mg/Kg, respectively) than controls (0.71 ± 0.0 L/h/kg). Conclusion: Therefore, the multiple oral administration of an aqueous extract of P. cupana caused a significant effect on the pharmacokinetics of TPH in rats.

AVALIAÇÃO DE DESENVOLVIMENTO DE CULTURA SIMBIÓTICA DE BACTÉRIAS E LEVEDURAS ATIVAS (SCOBY) EM KOMBUCHA COM DIFERENTES FONTES DE CAFEÍNA.

O SCOBY refere-se a um biofilme celulósico de leveduras e bactérias de alta cristalinidade, resistência à tração, insolubilidade, moldabilidade, polimerização, retenção de água e fibras mais finas que as de celulose vegetal. O presente trabalho teve como objetivo desenvolver e caracterizar crescimento e desenvolvimento do biofilme flutuante em amostras de Kombucha produzidas em diferentes fontes de cafeína: Camellia sinensis, Ilex paragauiensis, Coffea, Paullinia cupana e Theobroma cacao. EMBASA, em Barreiras-BA. O experimento foi conduzido em delineamento inteiramente casualizado, com cinco tratamentos (T1, chá verde, T2, chá mate, T3, café, T4, guaraná e T5, cacau 100%) e quatro repetições, no conjunto de 20 parcelas, realizadas em triplicata, totalizando 60 unidades experimentais. Os substratos de fermentação foram eficientes para a produção de um novo biofilme. O fator pH não variou com os teores de cafeína, diferente do crescimento da película bacteriana, que se multiplicou em maiores teores da substância. O tratamento 5 obteve maiores índices de crescimento, rendimento, quantidade de matéria seca, e menor teor de umidade em relação aos demais, seguindo pelos tratamentos 1 e 3, com rendimento de biofilme mediano e valores aproximados de teor de umidade 65% e 60% respectivamente. Os tratamentos com menores desempenhos foram o 2, com 80% de umidade, e 4, com 75,17%. Conclui-se que para produção de biofilmes com objetivo de obtenção de biocelulose, o cacau 100% torna-se a melhor opção como fonte de inoculo para as bactérias e leveduras microbiologicamente ativas presentes na Kombucha.

ACTIVIDAD ENZIMÁTICA Y PROCESO DE INFECCIÓN INICIAL DE LA PLANTA DE GUARANÁ (Paullinia cupana) POR CEPAS PATOGÉNICAS Y ENDOFÍTICAS DE Colletotrichum guaranicola

Anthracnose of the guarana plant (Paullinia cupana) is a disease caused by Colletotrichum guaranicola Albuq. Few studies have analyzed the origin, the form of penetration and the colonization of endophytic fungi in the guarana plant. This study aimed to determine differences in the enzymatic activities of endophytic and pathogenic strains of C. guaranicola during the initial infection process in leaves of clones sensitive to guarana anthracnose. Fourteen pathogenic and nine endophytic strains of C. guaranicola were isolated from guarana leaves with and without anthracnose symptoms, respectively. The enzymatic activities of protease, amylase, polyphenol oxidase, lipase, pectinase, and cellulolytic activities were evaluated for each fungal strain. The experimental design for each enzymatic assay was completely randomized with five replicates. The enzymatic evaluation was based on the measurement of halo produced by the enzyme reaction in each assay. Conidia were evaluated during germination and appressoria formation. Results did not detect enzymatic difference between pathogenic and endophytic strains. Data prior to germination showed differences between endophytic and pathogenic strains. Colonization of plant tissues by pathogenic strain was evidenced after the appearance of disease symptoms 48 hours after inoculation (hai), while for endophytic strains the presence of appressoria was observed on the surface of the epidermis 48 hai, and colonization of cells was not observed.

Heterologous expression of methylxanthine synthesis enzymes in mammalian cells and their use as reporter proteins

This work demonstrates the reconstitution of active methylxanthine synthesis enzymes in human cells and their potential use as inducible reporter enzymes. A variety of plant enzymes involved in caffeine synthesis have been characterized in vitro and several of these methylxanthine synthesis enzymes have been heterologously-expressed in yeast or bacteria. In this work, enzymes from Coffea arabica, Camellia sinensis, and Paullinia cupana have been heterologously-expressed in human cells. We demonstrate that the enzymes tested exhibit similar patterns of activity with a set of xanthine substrates in human cells when compared to previous reports of in vitro activity. We demonstrate that the activity of these enzymes can be used as a reporter for juxtacrine signaling using synNotch-induced expression in the presence of an appropriate substrate. When used in combination with synthetic caffeine receptors, this work has potential for use as an in vivo reporter (e.g. enabling non-invasive monitoring of cell-cell interactions after a cellular transplant) or in synthetic intercellular signaling a methylxanthine, such as caffeine, acting as a synthetic paracrine hormone.