The relevance of theobromine for the beneficial effects of cocoa consumption

Abstract

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.

Chocolate Consumption is Associated with a Lower Risk of Cognitive Decline

“…Interestingly, contrary to what is observed for humans, theobromine appears to be toxic in some mammals [33]. The reasons for this different profile of toxicity are not well established but this might suggest that in humans the pharmacodynamic properties of theobromine may be different from other mammals [37]. It should be kept in mind that methylxanthines are metabolized in humans by demethylation by the enzyme superfamily cytochrome P450, especially its member CYP1A2 which is responsible for more than 95% of the primary metabolism of caffeine [43].…”

“…In fact, while theobromine displays a longer half-life compared to caffeine (7.2 h against 4.1 h) [41], theobromine seems to be 2-to 3-fold less active than caffeine as an antagonist of the adenosine A 1 receptors in rat brain and at least 10-fold less active than caffeine as an antagonist of A 2A receptors [42]. However, theobromine may have other actions, independent on adenosine receptors blockade, as gene inducer or repressor [37]. Interestingly, contrary to what is observed for humans, theobromine appears to be toxic in some mammals [33].…”

“…Caffeine has been more widely explored, showing a protective effect against cognitive impairment and cognitive decline [35] and a possible preventive effect on the development of Alzheimer's disease (AD) [36]. On the other hand, the effects of theobromine have been less studied than those of caffeine, and the potential neurobiological effects of theobromine are still poorly understood [33,37], partially due to the prevalent idea that it is a weak central nervous system stimulant [38,39], and has only been showed to produce very minor subjective effects compared to caffeine [40]. In fact, while theobromine displays a longer half-life compared to caffeine (7.2 h against 4.1 h) [41], theobromine seems to be 2-to 3-fold less active than caffeine as an antagonist of the adenosine A 1 receptors in rat brain and at least 10-fold less active than caffeine as an antagonist of A 2A receptors [42].…”

The colonic metabolites dihydrocaffeic acid and dihydroferulic acid are more effective inhibitors of in vitro platelet activation than their phenolic precursors

“…Our results suggest that the beneficial effects of YMPE are only present at lower concentrations, which may be observed in the blood stream, and that higher, pro- cardiovascular protector effects. 50,51,52 In this study we show, for the first time, an important role of methylxanthines on modulation of platelet function. Previous studies have evaluated the effect of 300 -600 mg orally administered caffeine on human platelet function.…”

Effectiveness of some herbals on initial enamel caries lesion

“…Most plants used for preparation of beverages on human consumption are enriched in methylxanthines [14] . The antioxidants of Theobroma cacao beans have psychoactive effects at high amounts because of methylxanthines [15] . Besides, theobromine could show protective effect on enamel surface of human molars as shown by a pilot study [16] .…”