Recent advances in caffeine and theobromine toxicities: a review



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.
Key words: Biosynthesis, Caffeine, Theobromine, Toxicity

Prof Mbeh Eteng

Mbeh Eteng is a Professor of Biochemistry in the Faculty of University of Calabar. He holds a Ph.D from the University of Calabar (2000). He was Dean of Faculty of Basic Medical Science (2012-2016) and Chairman Committee of Deans (2014-2015). Member Governing Board UCTH, Calabar (2018 -till date). Fellow, Institute of Co-operate Administration. His current area of research is on malaria/prostrate hyperplaxia and medicinal plants research and use in management. He has successfully supervised 25 Ph.Ds.
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