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Abstract

Caffeine and theobromine are purine alkaloids widely consumed as stimulants and snacks in coffee and cocoa based foods and most often as part of ingredients in drugs. Man has enjoyed a long history of consumption of caffeine and theobromine. Recent interest in these two alkaloids, however, is centered on their potential reproductive toxicities. Caffeine and theobromine are now known to cross the placental and blood brain barrier thus potentially inducing fetal malformation by affecting the expression of genes vital in development. The developing fetus may not have developed enzymes for detoxification of these methylxanthine alkaloids via demethylation. There is a need, therefore, to protect the conceptus against 'insults' from teratogens of this nature. Apart from its reproductive toxicity, the presence of caffeine and theobromine in cocoa could limit its potentials as a nourishing food. This is an issue that needs to be addressed by nutritionists and the food industry at large. This paper discusses the natural sources, consumption and uses, toxicity and the major advances in the reproductive toxicology of caffeine and theobromine. The biosynthesis of these compounds in plants, metabolism in mammalian systems and the involvement of cytochrome P450 are reviewed and summarized. Evidence in favor of the toxicity of these compounds in experimental animals is presented with emphasis on the implications of these findings in humans. The paper concludes with a call for caution in the use of caffeine and theobromine pending further and more elaborate investigations.

Thermochemical study of two anhydrous polymorphs of caffeine

“…The wide academic and industrial importance of the caffeine molecule [5] contrasts with the lack of reliable experimental values for the standard enthalpy of combustion and standard enthalpy of formation for the two anhydrous polymorphic forms. The present work is precisely a contribution to the thermodynamic characterisation of the pure phases of anhydrous caffeine, using combustion calorimetry and solution calorimetry.…”

Rapid analysis of caffeine in various coffee samples employing direct analysis in real-time ionization–high-resolution mass spectrometry

“…Caffeine (3,7-dihydro-1,3,7-trimethyl-1H-purine-2,6,-dione or 1,3,7-trimethylxanthine) is a biologically active xanthine alkaloid naturally occurring in coffee, tea, cacao, and guarana plant parts [1]. Among various types of beverages containing caffeine, coffee represents the traditional source for the adult population.…”

Determination of methylxanthines in urine by liquid chromatography with diode array UV detection

“…Paraxanthine (1,7-dimethylxanthine) is not found in foods but is the main metabolite [4] of caffeine. These substances show various physiological effects [5] on various body systems, including the central nervous, cardiovascular, gastrointestinal, respiratory and renal systems. There is also a general consensus by sport investigators that methylxanthines are in some respect ergogenic.…”