Health benefits of methylxanthines in cacao and chocolate

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


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.

Publication types

  • Review

MeSH terms

  • Beverages / analysis*
  • Cacao / chemistry*
  • Caffeine / pharmacology
  • Candy / analysis*
  • Humans
  • Purinergic P1 Receptor Antagonists / pharmacology
  • Randomized Controlled Trials as Topic
  • Theobromine / pharmacology
  • Xanthines / pharmacology*


  • Purinergic P1 Receptor Antagonists
  • Xanthines
  • methylxanthine
  • Caffeine
  • Theobromine