Abstract
Methylxanthines, purine alkaloids found in plants, are found in beverages (coffee, tea, cocoa) and foods (chocolate and other cocoa-containing foods) commonly consumed worldwide. Members of this family include caffeine, theophylline and theobromine. Methylxanthines have a variety of pharmacological effects, and caffeine and theophylline are used as pharmaceuticals. Methylxanthines are metabolized in the liver predominantly by the enzyme CYP1A2. Their co-administration with CYP1A2 inhibitors may lead to pharmacokinetic interactions. Little is known about the possible drug interactions between caffeine and substrates of other CYP450 enzymes. In our study, methylxanthine fractions inhibited CYP3A4 in a concentration-dependent manner. Concomitant consumption of green tea with CYP3A4 substrates could increase the possibility of interactions, and this requires further clarification. The inhibition of CYP3A4 is not only due to the presence of catechin derivatives but methylxanthines may also contribute to this effect.
Highlights
Tea is one of the most commonly consumed beverages in the world, and it has many beneficial health effects
Methylxanthines are extensively metabolized in the liver by the cytochrome P450 (CYP450) oxidase enzyme system, mainly by demethylation, and they are excreted in human urine in the form of metabolites with less than 2% of administered caffeine being excreted unchanged[9,10]
The aim of the present study was to analyse the methylxanthine fractions isolated from Pu-erh and Bancha tea leaves and to evaluate their potential to modulate the activity of human recombinant CYP3A4 in vitro
Summary
Tea is one of the most commonly consumed beverages in the world, and it has many beneficial health effects They are harvested from the same plant, Camellia sinensis, there are many different types of tea depending on the manufacturing process, and they contain different biologically active substances. Concomitant consumption of caffeine with CYP1A2 substrates (certain drugs used for cardiovascular, CNS, gastrointestinal, infectious, and other disorders) may lead to pharmacokinetic interactions at the CYP1A2 enzyme level. This may result in side effects or may hinder the treatment[13]. The aim of the present study was to analyse the methylxanthine fractions isolated from Pu-erh and Bancha tea leaves and to evaluate their potential to modulate the activity of human recombinant CYP3A4 in vitro
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