Cacao

• Cardiovascular support
• Cognitive function
• Antioxidant protection
• Mood enhancement

• Blood pressure regulation
• Blood flow improvement
• Anti-inflammatory
• Insulin sensitivity
• Skin health
• Gut microbiome support
• Exercise performance

Cacao (Theobroma cacao) exerts its diverse therapeutic effects through a complex array of bioactive compounds, with flavanols (particularly epicatechin, catechin, and procyanidins) being the most well-studied active constituents. Additional bioactive compounds include theobromine, caffeine, phenylethylamine (PEA), anandamide, magnesium, and various other minerals and phytochemicals. The cardiovascular benefits of cacao stem from multiple mechanisms. Its flavanols enhance nitric oxide (NO) bioavailability by activating endothelial nitric oxide synthase (eNOS), leading to vasodilation and improved blood flow.

Research has demonstrated that cacao flavanols inhibit angiotensin-converting enzyme (ACE), similar to certain blood pressure medications, contributing to its antihypertensive effects. Additionally, cacao compounds reduce platelet aggregation and adhesion, potentially decreasing the risk of thrombus formation. The cognitive benefits of cacao are attributed to several pathways. The improved cerebral blood flow resulting from flavanol-induced vasodilation enhances oxygen and nutrient delivery to brain tissues.

Cacao flavanols have demonstrated the ability to cross the blood-brain barrier and directly protect neuronal cells from oxidative damage. Research suggests that epicatechin and other flavanols may enhance brain-derived neurotrophic factor (BDNF) levels, supporting neurogenesis and synaptic plasticity. Additionally, cacao’s modest caffeine and theobromine content provides mild stimulant effects that can enhance alertness and cognitive function. The antioxidant properties of cacao are among the most potent of any food source.

Its flavanols directly scavenge free radicals and reactive oxygen species, while also enhancing endogenous antioxidant defenses by activating nuclear factor erythroid 2-related factor 2 (Nrf2), which regulates the expression of antioxidant enzymes. This dual antioxidant action provides comprehensive protection against oxidative stress implicated in aging and various chronic diseases. The mood-enhancing effects of cacao involve multiple neurotransmitter systems. Phenylethylamine (PEA) and anandamide in cacao may stimulate the release of endorphins and other ‘feel-good’ neurotransmitters.

Cacao also contains compounds that inhibit monoamine oxidase (MAO), potentially increasing levels of serotonin and dopamine in the brain. The theobromine and caffeine content provides mild stimulant effects that can improve mood and energy levels. For blood sugar regulation, cacao flavanols have demonstrated the ability to enhance insulin sensitivity in peripheral tissues and protect pancreatic beta cells from oxidative damage. Some research suggests that cacao may slow carbohydrate digestion and absorption by inhibiting digestive enzymes like alpha-amylase and alpha-glucosidase.

The anti-inflammatory properties of cacao stem from multiple pathways. Its flavanols inhibit nuclear factor-kappa B (NF-κB) activation, a master regulator of inflammatory responses, and reduce the production of pro-inflammatory cytokines. Cacao also inhibits the activity of pro-inflammatory enzymes including cyclooxygenase-2 (COX-2) and lipoxygenase. For skin health, cacao’s flavanols protect against UV damage through antioxidant effects and may enhance skin blood flow, hydration, and elasticity.

Some research suggests cacao compounds may inhibit collagenase and elastase enzymes that break down skin structural proteins. The gut microbiome benefits of cacao are attributed to its fiber content and polyphenols, which serve as prebiotics, supporting the growth of beneficial bacteria like Bifidobacteria and Lactobacilli. Cacao polyphenols may also inhibit the growth of pathogenic bacteria. For exercise performance, cacao’s nitric oxide-enhancing effects may improve oxygen and nutrient delivery to muscles during exercise.

Its epicatechin content has demonstrated the ability to enhance mitochondrial biogenesis and function in muscle tissue, potentially improving endurance. Additionally, cacao’s theobromine provides mild stimulant effects that may enhance energy and focus during physical activity.

200-900 mg of flavanols daily, which translates to approximately: 20-40 grams of high-quality dark chocolate (70-85% cacao); or 2-4 tablespoons (10-20 grams) of raw cacao powder; or 1-2 tablespoons (10-15 grams) of cacao nibs. For standardized extracts, follow manufacturer recommendations, typically 500-1000 mg daily standardized to 5-10% flavanols.

Moderate to variable; the flavanols in cacao have variable absorption rates, with monomers like epicatechin showing relatively good absorption (approximately 25-30%)

while larger procyanidins have much lower bioavailability (less than 10%). Epicatechin reaches peak plasma concentration within 2-3 hours after consumption. Theobromine and caffeine have excellent bioavailability (over 80%) and reach peak plasma levels within 1-2 hours. The overall bioavailability of cacao’s bioactive compounds is influenced by food matrix, processing methods, and individual factors like gut microbiota composition.

Consuming with fat increases absorption of fat-soluble components; traditional preparations often include cacao butter or other healthy fats, Fermentation of cacao beans enhances bioavailability of flavanols by breaking down larger polyphenols into more absorbable forms, Combining with black pepper extract (piperine) may increase absorption by inhibiting certain metabolic enzymes, Consuming with dairy may reduce absorption of some polyphenols due to protein binding; plant-based milks may be preferable for maximum flavanol absorption, Alkalization (Dutch processing) significantly reduces flavanol content and should be avoided when seeking maximum health benefits, Micronized or finely ground cacao powder increases surface area, potentially improving dissolution and absorption, Liposomal delivery systems can significantly enhance bioavailability of cacao flavanols, Consuming with prebiotics or probiotics may enhance biotransformation of larger polyphenols by gut microbiota, Standardized extracts with higher flavanol content generally provide more consistent bioavailability than variable whole food sources

For cardiovascular benefits, consistent daily consumption is more important than specific timing, though some research suggests morning consumption may align better with circadian rhythms of vascular function. For cognitive enhancement, consuming 1-2 hours before mentally demanding tasks may provide optimal acute benefits due to the timing of peak blood levels of flavanols, theobromine, and caffeine. For exercise performance, consuming 1-2 hours before activity allows time for nitric oxide-enhancing effects to develop. Taking with or shortly after meals containing moderate fat content (10-15g fat) enhances absorption of fat-soluble compounds, though very high-fat meals may delay gastric emptying and slow overall absorption.

For sleep quality, avoid consumption within 6 hours of bedtime if sensitive to caffeine or theobromine, which can have half-lives of 5-10 hours in some individuals. The flavanols in cacao have relatively short half-lives (approximately 3-4 hours for epicatechin), suggesting that divided dosing (2 times daily) may provide more consistent blood levels for cardiovascular benefits. However, some metabolites and effects may persist longer, and consistent daily consumption appears more important than multiple daily doses for most health benefits. Cacao is traditionally consumed in ceremonial settings in the morning or early afternoon, which aligns with modern understanding of its stimulant properties and potential sleep disruption if consumed late in the day.

• Insomnia or sleep disturbances due to caffeine and theobromine content (common with evening consumption or in sensitive individuals)
• Increased heart rate or palpitations (occasional, particularly with higher doses)
• Headache (uncommon, typically with very high consumption or during withdrawal)
• Gastrointestinal discomfort including acid reflux, nausea, or diarrhea (occasional, particularly with higher doses)
• Anxiety or jitteriness in caffeine-sensitive individuals (occasional)
• Allergic reactions (rare, more common in individuals with allergies to other beans or nuts)
• Migraine triggering in susceptible individuals (occasional)
• Heartburn or acid reflux (occasional)
• Increased urination due to mild diuretic effect (common)

• Severe caffeine sensitivity (due to caffeine and theobromine content)
• Gastroesophageal reflux disease (GERD) exacerbation in some individuals
• Migraine susceptibility in some individuals (cacao can be a trigger)
• Severe anxiety disorders (stimulant effects may exacerbate symptoms in some individuals)
• Severe insomnia (stimulant effects may worsen sleep issues)
• Certain heart arrhythmias that may be sensitive to stimulants (consult healthcare provider)
• Known allergy to cacao or chocolate products
• Severe kidney stones (high oxalate content may be problematic in very large amounts)
• Irritable bowel syndrome (may exacerbate symptoms in some individuals)

• MAO inhibitors (potential interaction with phenylethylamine and other amines in cacao)
• Stimulant medications (potential additive effects with caffeine and theobromine)
• Certain antidepressants (potential mild interaction with mood-active compounds)
• Beta-blockers (theobromine may counteract some effects)
• Anticoagulant and antiplatelet drugs (potential mild additive effects on blood clotting)
• Certain antibiotics like ciprofloxacin (may slow caffeine metabolism)
• Medications metabolized by cytochrome P450 1A2 (CYP1A2) enzymes (potential competition for metabolism)
• Blood pressure medications (may enhance or interfere with effects)
• Medications for GERD or acid reflux (cacao may reduce effectiveness)

No established upper limit for cacao flavanols; clinical studies have safely used up to 2000 mg flavanols daily without significant adverse effects. For theobromine, up to 1000 mg daily appears well-tolerated in most healthy adults (approximately 50-70g of dark chocolate). For caffeine, general recommendations suggest limiting to 400 mg daily from all sources combined (approximately 200g of dark chocolate would reach this limit). Practical upper limits are typically determined by caloric content and potential side effects like insomnia or gastrointestinal discomfort rather than toxicity concerns.

Individuals with specific health conditions or sensitivities may need to consume less. Children should consume significantly lower amounts due to their smaller body size and potentially greater sensitivity to theobromine and caffeine.

Cacao (Theobroma cacao) is generally recognized as safe (GRAS) by the FDA as a food ingredient. Cacao products like cocoa powder, cocoa butter, and chocolate are regulated as conventional foods rather than dietary supplements. However, concentrated cacao extracts marketed specifically for their health benefits may be regulated as dietary supplements. The FDA has not approved any specific health claims for cacao or its components, though qualified health claims related to flavanols and cardiovascular health have been proposed.

As with other foods and supplements, manufacturers are responsible for ensuring their products are safe before marketing and that product labels are truthful and not misleading.

Eu: In the European Union, cacao is primarily regulated as a food ingredient. The European Food Safety Authority (EFSA) has evaluated several health claims related to cocoa flavanols. In 2012, EFSA approved a health claim stating that ‘cocoa flavanols help maintain the elasticity of blood vessels, which contributes to normal blood flow.’ This claim can be used for products providing at least 200 mg of cocoa flavanols daily. The EU has established standards for chocolate products, including minimum cacao content requirements for various chocolate categories. Cacao extracts marketed as food supplements must comply with the EU Food Supplements Directive (2002/46/EC).

Canada: Health Canada regulates cacao primarily as a food ingredient. Concentrated cacao extracts marketed for health purposes fall under Natural Health Products Regulations. Health Canada has not approved specific health claims for cacao products, though products meeting certain requirements can make structure-function claims with appropriate disclaimers. The Canadian Food Inspection Agency enforces standards for chocolate products, including minimum cacao content requirements.

Australia: The Food Standards Australia New Zealand (FSANZ) regulates cacao primarily as a food ingredient. Concentrated cacao extracts marketed for health purposes are regulated as complementary medicines by the Therapeutic Goods Administration (TGA). Australia has established standards for chocolate products, including minimum cacao content requirements for various chocolate categories.

Japan: In Japan, cacao is regulated primarily as a food ingredient. Certain cacao products with standardized flavanol content may qualify for Foods for Specified Health Uses (FOSHU) status if they meet strict requirements for scientific evidence of health benefits. Several cacao-based products have received FOSHU approval for claims related to blood pressure management.

Who: The World Health Organization (WHO) recognizes the potential health benefits of moderate cacao consumption, particularly related to cardiovascular health, though it has not issued specific recommendations regarding cacao intake. WHO’s Codex Alimentarius Commission has established international standards for cocoa products and chocolate to ensure quality and safety.

Low to medium

Raw cacao nibs: $0.30-0.80 per day; Cacao powder: $0.20-0.60 per day; Dark chocolate (70%+ cacao): $0.50-1.50 per day; Standardized cacao extract: $0.70-1.80 per day; Ceremonial grade cacao: $1.00-2.50 per day

Cacao offers excellent value for its diverse health benefits, particularly for cardiovascular and cognitive support. The relatively low cost of basic forms like cacao powder makes it one of the more accessible functional foods with substantial research backing. For cardiovascular health, cacao represents a high-value option compared to many supplements targeting similar mechanisms. The cost of achieving clinically significant flavanol intake (500-900 mg daily) through cacao powder ($0.20-0.60 per day) is substantially lower than many specialized cardiovascular supplements, while providing additional benefits for mood, cognition, and overall wellbeing.

When comparing different forms, cacao powder offers the best value in terms of flavanol content per dollar, though it requires more preparation effort. Dark chocolate provides convenience but at a higher cost per dose of active compounds, with additional calories from sugar and fat. Standardized extracts provide more consistent active compound content and convenience, justifying their higher cost for those seeking therapeutic effects without the calories of whole cacao products. The value proposition varies significantly based on quality and processing method.

Mass-produced, alkalized (Dutch-processed) cacao products are less expensive but contain dramatically reduced flavanol content, significantly diminishing their health value despite the lower price. Organic certification typically adds 20-40% to the cost but reduces exposure to pesticides and often indicates higher quality processing that preserves more active compounds. Fair trade or direct trade certification adds a similar premium but ensures ethical sourcing, which many consumers consider an important aspect of value. Single-origin and specialty cacao products command premium prices (often 2-3 times higher than conventional products) but may offer unique phytochemical profiles and flavor experiences that justify the cost for some users.

Ceremonial grade cacao used for traditional cacao ceremonies represents the highest price point but offers a unique combination of high flavanol content, ethical sourcing, and cultural connection that many practitioners find worthwhile. When considering the versatility of cacao – its applications spanning cardiovascular health, cognitive function, mood enhancement, and culinary enjoyment – the overall value proposition is excellent, particularly for minimally processed, high-flavanol products. The substantial research backing cacao’s health benefits further enhances its value proposition compared to many supplements with less scientific support. Overall, cacao represents one of the more cost-effective functional foods available, with the best value found in high-quality, minimally processed cacao powder for those willing to incorporate it into their daily routine.

Raw cacao beans: 2-3 years when properly stored; Cacao nibs: 1-2 years; Cacao powder: 1-2 years; Dark chocolate (70%+ cacao): 1-2 years; Cacao butter: 2-3 years; Standardized extracts: 2-3 years; Cacao capsules/tablets: 2-3 years when properly stored

Store in airtight, opaque containers protected from light, heat, moisture, and strong odors. Cacao beans, nibs, and powder should be kept in dark glass containers or opaque packaging. Dark chocolate should be stored at cool temperatures (15-20°C/59-68°F) but not refrigerated, as temperature fluctuations can cause ‘bloom’ (separation of cocoa butter). Cacao butter should be stored in a cool, dark place in an airtight container.

Avoid exposure to direct sunlight or high temperatures, which can accelerate degradation of flavanols and other active compounds. Traditional storage methods in producing regions often involve keeping cacao beans in breathable natural fiber bags in cool, dry places. For long-term storage of cacao beans or nibs, some producers use vacuum sealing to prevent oxidation. Cacao products readily absorb odors from their environment, so store away from strong-smelling foods or substances.

Exposure to light, particularly UV light, accelerates degradation of flavanols and other photosensitive compounds, High temperatures (above 30°C/86°F) significantly increase the rate of degradation of most active compounds, Moisture promotes hydrolysis of various compounds and increases risk of microbial growth and mycotoxin formation, Oxidation occurs gradually with air exposure, affecting flavanols and other polyphenols, Alkalization (Dutch processing) dramatically reduces flavanol content by 60-90% and should be avoided for maximum health benefits, Enzymatic degradation can occur in improperly dried or stored cacao products, Microbial contamination can lead to degradation of active compounds and production of potentially harmful mycotoxins, pH extremes affect stability of flavanols; neutral to slightly acidic conditions are most stable, Metal ions, particularly iron and copper, can catalyze oxidation reactions, Repeated temperature fluctuations (as in moving between refrigeration and room temperature) can accelerate degradation and cause undesirable textural changes, Long-term storage gradually reduces potency even under optimal conditions due to slow oxidation and molecular rearrangement of unstable compounds

Synthesis Methods

Natural Sources

Quality Considerations

Cacao (Theobroma cacao) has one of the richest and most fascinating histories of any medicinal plant, with evidence of its use dating back over 5,000 years. The name ‘Theobroma’ itself means ‘food of the gods,’ reflecting the reverence ancient cultures had for this remarkable plant. Archaeological evidence indicates that cacao was first domesticated by the Olmec civilization in Mesoamerica (present-day Mexico) around 1500 BCE, though wild harvesting likely predated cultivation by centuries. The earliest documented medicinal use appears in ancient Mayan texts from around 600 CE, where cacao was described as a sacred medicine with diverse applications.

The Mayans prepared cacao as a bitter, frothy drink called ‘xocolatl,’ often mixed with chili peppers, vanilla, and various herbs. This preparation was used ceremonially and medicinally rather than as a sweet treat. Mayan physicians prescribed cacao for a wide range of conditions including fatigue, fever, respiratory issues, digestive problems, and to enhance strength and vitality. The Aztec civilization, which rose to prominence after the Mayans, similarly revered cacao as a divine gift with powerful medicinal properties.

Aztec emperor Montezuma II reportedly consumed large quantities of cacao daily for its energizing and aphrodisiac effects. Cacao beans were so valuable in Aztec society that they were used as currency, with 100 beans able to purchase a turkey or a slave. When Spanish conquistadors encountered cacao in the early 16th century, they initially found the bitter drink unpalatable. However, they quickly recognized its medicinal value and began shipping it back to Europe, where it was initially used primarily as a medicine rather than a food.

By the 17th century, European physicians were prescribing cacao for conditions including angina, heart pain, anemia, fever, low virility, fatigue, gout, kidney stones, and poor appetite. The addition of sugar to cacao, which began in Spanish monasteries, transformed it into a more palatable beverage that gradually gained popularity throughout Europe. By the 18th century, ‘chocolate houses’ had become fashionable gathering places for the European elite, where cacao was consumed both for pleasure and for its perceived health benefits. In traditional Mesoamerican medicine, different parts of the cacao plant were used for various conditions.

The beans were used for heart conditions, fatigue, and as a general tonic; the fat (cacao butter) was applied topically for skin conditions and burns; and the bark was used for intestinal infections. Cacao was often combined with other medicinal plants in complex formulations tailored to specific conditions. Beyond physical ailments, cacao played a crucial role in spiritual and psychological healing traditions. It was used in sacred ceremonies to facilitate connection with the divine, enhance meditation, open the heart, and foster community bonding.

This spiritual dimension of cacao use has experienced a revival in recent decades with the emergence of ‘cacao ceremonies’ in various parts of the world. The modern scientific understanding of cacao’s health benefits began to emerge in the late 20th century, with research focusing on its cardiovascular effects, antioxidant properties, and impact on mood and cognition. This research has largely validated many of the traditional uses of cacao, providing a scientific basis for what ancient healers understood through centuries of observation and experience. Today, cacao continues to be used both as a beloved food and as a medicine, bridging ancient wisdom and modern science in a way few other plants have achieved.

Hooper L, Kay C, Abdelhamid A, Kroon PA, Cohn JS, Rimm EB, Cassidy A. Effects of chocolate, cocoa, and flavan-3-ols on cardiovascular health: a systematic review and meta-analysis of randomized trials. American Journal of Clinical Nutrition. 2012;95(3):740-751., Lin X, Zhang I, Li A, Manson JE, Sesso HD, Wang L, Liu S. Cocoa Flavanol Intake and Biomarkers for Cardiometabolic Health: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Journal of Nutrition. 2016;146(11):2325-2333., Ried K, Sullivan TR, Fakler P, Frank OR, Stocks NP. Effect of cocoa on blood pressure. Cochrane Database of Systematic Reviews. 2017;4:CD008893.

COcoa Supplement and Multivitamin Outcomes Study (COSMOS) – large-scale, long-term clinical trial examining effects of cocoa flavanol supplements on cardiovascular health and cancer risk (ClinicalTrials.gov: NCT02422745), Cocoa Flavanols and Vascular Health in Patients with Coronary Artery Disease (COVASC) – examining effects of cocoa flavanols on vascular function in patients with coronary artery disease (ClinicalTrials.gov: NCT02876887), Cocoa Flavanols and Exercise Study (CFES) – investigating combined effects of cocoa flavanols and exercise on cardiometabolic health (ClinicalTrials.gov: NCT03041961)