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. 2013 Oct 18;5(10):4159-73.
doi: 10.3390/nu5104159.

Health Benefits of Methylxanthines in Cacao and Chocolate

Free PMC article

Health Benefits of Methylxanthines in Cacao and Chocolate

Rafael Franco et al. Nutrients. .
Free PMC article


One may wonder why methylxanthines are so abundant in beverages used by humans for centuries, or in cola-drinks that have been heavily consumed since their appearance. It is likely that humans have stuck to any brew containing compounds with psychoactive properties, resulting in a better daily life, i.e., more efficient thinking, exploring, hunting, etc., however, without the serious side effects of drugs of abuse. The physiological effects of methylxanthines have been known for a long time and they are mainly mediated by the so-called adenosine receptors. Caffeine and theobromine are the most abundant methylxanthines in cacao and their physiological effects are notable. Their health-promoting benefits are so remarkable that chocolate is explored as a functional food. The consequences of adenosine receptor blockade by natural compounds present in cacao/chocolate are here reviewed. Palatability and health benefits of methylxanthines, in general, and theobromine, in particular, have further contributed to sustain one of the most innocuous and pleasant habits: chocolate consumption.


Figure 1
Figure 1
(A) Xanthine as an intermediate of GTP and nucleic acid anabolism and catabolism. Rectangles in compounds highlight the xanthine unit; (B) Structures of methylxanthines, adenosine, and adenosine receptor antagonists structurally related to methylxanthines. Rectangles in compounds highlight the xanthine unit.

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