Psychoactive compounds in Chocolate

A few months ago came by our lab a friend, chef Arnaud Hauchon (@chefarnaudhauchon), and tasted some of our cacao. After having two roasted beans he looked at his fingertips, then up at me said “oh my. I think I’m high.”

How is this possible?

Well, the good/bad news is that this is a rare experience, and while chocolate of cacao which was cultivated, fermented and roasted very well naturally carries stimulating compounds, to feel their effect as viscerally as my friend you will need to have a high metabolism, a high sensitivity to these compounds and probably an empty stomach. Arnaud’s lifestyle and diet are very clean without frequent exposure to drugs like caffeine, and very mindful making him highly aware of change in sensations in the brain hence his access to this feeling. But you may be able to simulate these conditions in other ways.

The ancient Mayans were situated in some proximity to areas of South America where the coca plant (known worldwide for its psychoactive alkaloid cocaine) was cultivated, and found their own stimulants in cacao. They believed that consumption of cacao can offer a powerful supernatural effect and thus in parts of history only warriors and royalty had access to its consumption.

Caffeine

Only two types of methylxanthines can be found in cacao: caffeine and theobromine. Caffeine is in a very small concentration, with quite a bit more theobromine. At times when your system is more sensitive, for example on an empty stomach (especially after a fast or detox) or post-exercise, or simply as someone who does not regularly consume caffeine, you will be more acutely aware of their effects.

Theobromine

Theobromine is the primary bitter-tasting alkaloid found in cacao and chocolate. Chocolate contains 0.5–2.7% theobromine and about 0.4% caffeine, according to Stephen T Beckett, The Science of Chocolate (The Royal Society of Chemistry, 2018).

Both of these compounds can be damaged or diminished by heat, meaning over-roasted chocolate (most commodity-cacao made chocolate, which is most chocolate available today) will carry a much lesser effect if at all. To enjoy them you will also want to target high cacao-concentration chocolate, ideally 70% and above.

Theobromine’s softer effect on the body and caffeine’s low concentration make an excellent balance for chocolate to work as a “pick me up” for energy in the day, or a natural pre-workout. At this low impact you can also enjoy the benefits of stimulants such as sharper focus, increased motivation and improved mood and blood flow, without the jittery and sleep-depriving effects of a cup of coffee or tea.

Beside Theobromine and Caffeine, cacao beans produce further compounds during fermentation (according to this review of research papers on whether theobromine is a cognitive modulator) including phenylethylamine which increases

Serotonin

attention and relieves depression and serotonin, a neurotransmitter that at normal levels makes you feel more focused, emotionally stable, happier and calmer (according to this clinic in the US).

Theobromine

Theobromine’s name is derived from Theobroma, the name of the genus of the cacao plant, Greek for “food of the gods” with the suffix “ine” given to alkaloids and other basic nitrogen-containing compounds.

Like Caffeine, it crosses the blood-brain barrier and binds to adenosine receptors.

Theobromine’s elimination half-life is between 6-8 hours. This is the time it takes concentration in the blood to go from full to half.

It is also a bronchodilator, meaning a substance that dilates the bronchi and bronchioles, increasing airflow to the lungs.

It is far weaker than caffeine, and unlike caffeine has no impact on the central nervous system meaning it should not negatively impact sleep even if consumed late in the day. In a study comparing it with caffeine it was shown to decrease blood pressure (while caffeine increases it) and impart no strong alerting effect (while caffeine does).

Authors of this study also found a significant decrease of age-related cognitive impairment in mice supplied with a diet rich in theobromine, polyphenols, and polyunsaturated fatty acid (LMN diet).

Lastly, in another study on mice who’s diet was also rich in theobromine, they found significant improvement in motor learning, such as sequence, skill, adaptation, and reversal learning compared with normal nourished mice.

There is more evidence of positive effects of theobromine on brain health but for the sake of not making this into a list, if you’re curious I recommend reading inside the linked studies, especially this review.

Caffeine

Caffeine exists in cacao in a relatively low ratio, about 1:5 compared with Theobromine (according to this study). In Human culture it is much more common and studied than theobromine. Compared with other sources of caffeine, it is present in cacao at a very low level, almost negligible, especially to an average coffee drinker.

Unlike most other psychoactive substances, caffeine remains largely unregulated and legal in nearly all parts of the world. Caffeine is also an outlier as its use is seen as socially acceptable in most cultures and even encouraged in others.

Beside cacao, caffeine is found in coffee, tea, and the seeds, fruit, nuts or leaves of a few other plants, as well as man-made soft drinks and energy drinks.

A cup of coffee contains 80-175mg of caffeine depending on the bean and extraction method, while a 50g bar of chocolate contains around 22mg, and is often not consumed by one person in one sitting.

Thanks to this low concentration all of the effects described here are extremely mild in chocolate if present at all, relative to your caffeine tolerance.

When metabolised by humans caffeine breaks down to three other molecules including theobromine.

Caffeine famously stimulates (increases activity of) the brain and nervous system. While it is a drug, it is not an intoxicant. It is mainly used recreationally as a cognitive enhancer, increasing alertness and attentional performance, or to relieve or prevent drowsiness.

It works by blocking binding of adenosine (a molecule associated with sleepiness) to the adenosine A1 receptor, due to having a similar three dimensional structure to that of adenosine.

In nature this compound protects its plant in two ways: in its bitter taste deterring herbivores (animals or insects who eat plants) from eating it, and in its function by preventing the germination of nearby seeds, thus avoiding competition. It also encourages consumption by select species such as honey bees.

In terms of health, it seems to go both ways as an honest champion of the “everything at moderation” mantra. I don’t personally believe this mantra is fit for everything health related, but it seems to be the best consensus on caffeine among doctors.

Caffeine is known for both positive and negative health impacts; preventing or protecting from certain diseases, mood enhancing, and enhancing focus and ability to exert energy. It has also been reported to help with exercise or deep cognitive work. On the other hand excessive consumption, especially late in the day, risks disturbed sleep, anxiety and mild drug dependence. At high consumption it’s short-term implications such as increased blood pressure and heart rate seem to be reduced via tolerance.

Coffee cherries

Both the US Food and Drug Administration and the European Food Safety Authority agree that moderate consumption of caffeine (400mg/day according to EFSA - about 19 bars of chocolate) does not raise safety concerns for non-pregnant adults and low consumption (200mg/day by EFSA) in pregnant or breastfeeding adults does not raise safety concerns for babies or foetuses.

Is chocolate good or bad for my brain?

The amount of chocolate you will need to eat for negative health implications on the brain appears to be very high, higher than you would naturally want to eat of one thing anyway, and negligible compared with other sources of caffeine.

As I mention all over this blog - I am not a doctor and all of this advice is the result of secondary research. If you feel you are at risk, consult with your doctor before taking anything written on the internet for a fact relevant to your situation.

Taiwanese cacao I de-podded in '21

Good quality dark chocolate which was made well carries small amounts of psychoactive compounds which can enhance your experience and maybe even performance in the short and long term. It also appears that lifestyle plays a major role in the perception of this effect.

I personally have chocolate much more often than coffee and find its effect far more pleasant and less disruptive. I am definitely on the extreme side with a daily consumption of 200-500g of chocolate, due to the nature of my job. Its nutritional benefits to my life are only enhanced by these psychoactive compounds, but I am also conscious not to eat excessive (100g+) quantities late in the evening to avoid disrupted sleep (although, as an entrepreneur.. What is sleep?)

There is a lot more to chocolate’s positive long term effect on our health, especially in nutrition, not touched in this article but detailed in my other articles as well as our health page and I invite you to check them out as well in your exploration of healthy ingredients, snacks, and lifestyle.