Cocao (Theobroma cacao)

The following information is directly pulled from the National Institutes of Health database. The National Institutes of Health (NIH) is a biomedical research facility primarily located in Bethesda, Maryland. An agency of the United States Department of Health and Human Services, it is the primary agency of the United States government responsible for biomedical and health-related research.

Health Benefits of Methylxanthines in Cacao and Chocolate


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. Read More.

Keywords: adenosine, adenosine receptors, adenosine receptor antagonist, caffeine, theobromine

Health benefits of cocoa.



In modern society, cocoa is being eaten as a confectionery, contrary to its medicinal use in the past. However, since the last decade, there has been a revival of talks about cocoa‘s health beneficial effects. Development has been made at the molecular level recently. This review discusses the recent progresses on potential health benefits of cocoa and/or its derivatives, with a focus on the areas that have been paid little attention so far, such as the role of cocoa in immune regulation, inflammation, neuroprotection, oxidative stress, obesity, and diabetes control.


Thanks to the advancement in analytical technologies, the cocoa‘s metabolic pathways have now been properly mapped providing essential information on its roles. Cocoa helps in weight loss by improving mitochondrial biogenesis. It increases muscle glucose uptake by inserting glucose transporter 4 in skeletal muscles membrane. Because of its antioxidant properties, cocoaoffers neuron protection and enhances cognition and positive mood. It lowers immunoglobulin E release in allergic responses. It can affect the immune response and bacterial growth at intestinal levels. It reduces inflammation by inhibiting nuclear factor-κB.


Keeping in view the pleiotropic health benefits of cocoa, it may have the potential to be used for the prevention/treatment of allergies, cancers, oxidative injuries, inflammatory conditions, anxiety, hyperglycemia, and insulin resistance. Read More.

The relevance of theobromine for the beneficial effects of cocoa consumption


Cocoa consumption began in America and in the mid sixteenth Century it quickly spread to Europe. Beyond being considered a pleasant habit due to its rich sweet lingering taste, chocolate was considered a good nutrient and even a medicine. Traditionally, health benefits of cocoa have been related with the high content of antioxidants of Theobroma cocoa beans. However, the direct psychoactive effect due to methylxanthines in cocoa is notable. Theobromine and caffeine, in the proportions found in cocoa, are responsible for the liking of the food/beverage. These compounds influence in a positive way our moods and our state of alertness. Theobromine, which is found in higher amounts than caffeine, seems to be behind several effects attributed to cocoa intake. The main mechanisms of action are inhibition of phosphodiesterases and blockade of adenosine receptors. Further mechanisms are being explored to better understand the health benefits associated to theobromine consumption. Unlike what happens in other mammals -pets- included, theobromine is safe for humans and has fewer unwanted effects than caffeine. Therefore, theobromine deserves attention as one of the most attractive molecules in cocoa.

Keywords: caffeine, theobromine, cocoa, adenosine receptor, neurological disease, receptor antagonist


Caffeine present in coffee and in cola beverages is heavily consumed worldwide. The reason of such high consumption relates to its benefits for day-life activities. Caffeine actions in the central nervous system (CNS) are fundamental to understand the interest of the intake of caffeine-containing beverages. Beneficial actions range from alertness to reducing the risk of neurodegenerative diseases. Although the highest concentration of caffeine is present in coffee, cocoa also contains this methylxanthine (Figure (Figure1)1) but at doses that probably are not enough to activate neural mechanisms. However, cocoa has elevated concentrations of a structurally similar component, theobromine. The effects of theobromine have been less studied than those of caffeine but it is known that this molecule exerts some positive effects in different human pathologies. The combination of caffeine and theobromine in cocoa may have the expected methylxanthine-derived benefits without the side effects reported for caffeine. Interestingly, the main action mechanism of caffeine and theobromine consists of blocking adenosine receptors and inhibiting phosphodiesterases. The present paper takes data of novel studies that point toward alternative modes of action of theobromine. Further research is, however, required to fully understand the health benefits of cocoa consumption. Read More.


Chemical structure of xanthine, caffeine, theobromine, and adenosine.


Over the last decades, a remarkable progress has allowed understanding some of the molecular mechanisms that are behind the proved health benefits of cacao consumption in man. Apart from the high content of antioxidants, solid evidence points to methylxanthines as key players in the beneficial effects. Caffeine has been classically considered with higher potential than other methylxanthines. Recent studies have highlighted the potential of theobromine, which may act as antitumoral, anti-inflammatory or cardiovascular protector molecule without the undesirable side effects described for caffeine. The main mechanisms of action of theobromine are inhibition of phosphodiesterases and blockade of adenosine receptors but, interestingly, it exhibits other important adenosine receptor-independent effects as the reduction of cellular oxidative stress or regulation of gene expression. In this sense, theobromine could be considered a safe and natural alternative in the treatment of some human diseases and may serve as lead compound for the development of novel drugs.

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