Cacao supplement pill benefit and side effects, antioxidant content, health benefit of supplements by Ray Sahelian, M.D.
March 26 2014

The cacao bean, and tasty products derived from the cacao bean such as chocolate, and the beverage cacao, popular with many people worldwide, is rich in specific antioxidants, with the basic structure of catechins and epicatechin, and especially the polymers procyanidins, polyphenols similar to those found in vegetables and tea. The alkaloids theobromine and caffeine are responsible for the stimulant effect of cacao and chocolate and contribute to the bitter cacao flavor. Cacao is the raw unprocessed form closest to the cacao bean. Cocoa is the processed form of cacao.
   Additional supplements to consider with beneficial properties include curcumin (an extract from turmeric), acai berry extract, pomegranate fruit, resveratrol, and noni. Cacoa powders, beverages, and dark chocolate are best consumed that are not alkalized. Alkalization is a process used to mellow the flavor of cocoa, but it also destroys the polyphenolic compounds.

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CACAO - FRONT.jpgThe cacao bean, and tasty products derived from it such as chocolate, and the beverage cacao, popular with many people worldwide, is rich in specific antioxidants, with the basic structure of catechins and epicatechin, and especially the polymers procyanidins, polyphenols similar to those found in vegetables and tea. The alkaloids theobromine and caffeine are responsible for the stimulant effect of cacao and chocolate and contribute to bitter cacao flavor.

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Benefits of cacao
Metabolic epidemiological studies indicate that regular intake increases the plasma level of antioxidants, a desirable attribute as a defense against reactive oxygen species (ROS). The antioxidants in cacao can prevent the oxidation of LDL-cholesterol, related to the mechanism of protection in heart disease. Likewise, a few studies show that ROS associated with the carcinogenic processes is also inhibited, although there have not been many studies on a possible lower risk of various types of cancer either in humans or in animal models consuming cacao butter or chocolates. Adding boiling water is not known to reduce the antioxidant effects.
   Eating dark chocolate may help lower blood pressure, boost normal responses to insulin to keep blood sugar levels down, and improve blood vessel function in patients with high blood pressure. All of these effects would be expected to decrease the risk of heart attack and stroke. However, the sugar content of chocolate can reduce these benefits.

The information on the benefits of cacao focuses mostly on preventive benefits, but how about therapeutic benefits if some damage has already occurred in the cardiovascular system?
    As of 2014, I have not seen enough data on the therapeutic benefits of cacao supplement ingestion to know how well it benefits those with existing heart disease, heart failure or other forms of cardiovascular disease.

Alzheimer's disease
Epicatechin and catechin in cacao inhibit amyloid beta protein induced apoptosis.
J Agric Food Chem. 2005.
Cacao may have anti-neurodegenerative effect in addition to other known chemopreventive effects.

Antioxidant
Cacao can be a rich source of antioxidants including the flavan-3-ols, epicatechin and catechin, and their oligomers (procyanidins).

Blood pressure lowering
The benefits would be reduced when sugar is part of the product you are ingesting>

Short-term administration of dark chocolate is followed by a significant increase in insulin sensitivity and a decrease in blood pressure in healthy persons.
Am J Clin Nutr. 2005.
The objective was to compare the effects of either dark or white chocolate bars on blood pressure and glucose and insulin responses to an oral-glucose-tolerance test in healthy subjects. After a 7-d cacao -free run-in phase, 15 healthy subjects were randomly assigned to receive for 15 d either 100 g dark chocolate bars, which contained approximately 500 mg polyphenols, or 90 g white chocolate bars, which presumably contained no polyphenols. Successively, subjects entered a further cacao -free washout phase of 7 d and then were crossed over to the other condition. Although within normal values, systolic blood pressure was lower after dark than after white chocolate ingestion. Dark, but not white, chocolate decreases blood pressure and improves insulin sensitivity in healthy persons.

Heart disease
A few squares of dark chocolate every day might cut the risk of serious heart disease by helping to stave off the hardening of arteries. Researchers from University Hospital in Zurich studied 20 male smokers, who are at greater risk of hardening arteries characteristic of coronary heart disease, to see the effects of dark and white chocolate on arterial blood flow. The subjects, who were asked to abstain from eating foods rich in antioxidants for 24 hours, were given 40 grams (2 ounces) of chocolate to eat. After two hours, ultrasound scans revealed that dark chocolate -- made up of 74 percent cacao solids -- significantly improved the smoothness of arterial flow, whilst white chocolate, with four percent cocoa, had no effect.

Epidemiological studies suggest that high flavonoid intake found in cacao confers a benefit on cardiovascular outcome.  Researchers examined the effects of flavonoid-rich cacao in dark chocolate on blood-vessel function in 17 young, healthy volunteers over a 3-hour period after they consumed 100 grams of a commercially available dark chocolate. The investigators saw that an artery in the arm dilated significantly more in response to an increase in bloodflow. Cacao consumption also led to a significant 7-percent decrease in aortic stiffness. The predominant mechanism appears to be dilation of small and medium-sized peripheral arteries and arterioles. The team didn't detect any change in antioxidant levels, so they suggest other possible explanations. The dilatory effect of chocolate under resting conditions can be attributed to improved nitric oxide bioavailability, prostacyclin increase, direct effect of cacao in smooth muscle cells, or activation of central mechanisms. SOURCE: American Journal of Hypertension, June 2005.

History of the cacao tree
The cacao tree (Theobroma cacao) originated in the Amazon rain forest and then later it moved to Central America. The Mayan tribes in Central America cultivated the cocoa tree about 1500 BC.  Late, the Aztecs made a sacred beverage called "chocolatl," where we get the word chocolate.  Cocoa was exported to Europe in the late 16th century but the first chocolate bar was not made until the mid 1800s.

Availability
Cacao bean is available in hot drink, tea, powder, and in chocolate bars. Try to find a chocolate bar that is at least 50% cacao. There are some that are as high as 80%.

Research study
Cacao polyphenols and inflammatory mediators.
Am J Clin Nutr. 2005.
Because intake of flavonoid-rich chocolate by human subjects decreases the plasma concentrations of proinflammatory cysteinyl leukotrienes, we assessed whether cacao polyphenols inhibited human 5-lipoxygenase, the key enzyme of leukotriene synthesis. Epicatechin and other cacao flavan-3-ols proved to be inhibitory at the enzyme level. In a double-blind crossover study, 20 individuals at risk for cardiovascular diseases received cacao beverages with high or low contents of flavan-3-ols. NO-dependent, flow-mediated dilation of the brachial artery and concentrations of nitroso compounds in plasma were measured, and it was shown that ingestion of the high-flavanol coca drink but not the low-flavanol cacao drink significantly increased plasma concentrations of nitroso compounds and flow-mediated dilation of the brachial artery. Therefore, ingested flavonoids may reverse endothelial dysfunction through enhancement of NO bioactivity. Oxidative modification of LDL appears to be crucial for atherogenesis, and one of the mediators is the proinflammatory proatherogenic enzyme myeloperoxidase. Micromolar concentrations of epicatechin or other flavonoids were found to suppress lipid peroxidation in LDL induced by myeloperoxidase in the presence of physiologically relevant concentrations of nitrite, an NO metabolite. Adverse effects of NO metabolites, such as nitrite and peroxynitrite, were thus attenuated.

Methylxanthines are the psycho-pharmacologically active constituents of chocolate.
Psychopharmacology. 2004.
Liking, cravings and addiction for chocolate "chocoholism" are often explained through the presence of pharmacologically active compounds. Studies measured the effects on cognitive performance and mood of the amounts of cacao powder and methylxanthines found in a 50 g bar of dark chocolate. In study 1, participants completed a test battery once before and twice after treatment administration. Treatments included 11.6 g cacao powder and a caffeine and theobromine combination (19 and 250 mg, respectively). Study 2 comprised three post-treatment test batteries and investigated the effects of "milk" and "dark" chocolate levels of these methylxanthines. The test battery consisted of a long duration simple reaction time task, a rapid visual information processing task, and a mood questionnaire. Identical improvements on the mood construct "energetic arousal" and cognitive function were found for cacao powder and the caffeine+theobromine combination versus placebo. In chocolate, both "milk chocolate" and "dark chocolate" methylxanthine doses improved cognitive function compared with "white chocolate". The effects of white chocolate did not differ significantly from those of water. A normal portion of chocolate exhibits psychopharmacological activity. The identical profile of effects exerted by cacao powder and its methylxanthine constituents shows this activity to be confined to the combination of caffeine and theobromine. Methylxanthines may contribute to the popularity of chocolate; however, other attributes are probably much more important in determining chocolate's special appeal and in explaining related self-reports of chocolate cravings and "chocoholism".

Polyphenols of cacao: inhibition of mammalian 15-lipoxygenase.
Biol Chem. 2001.
Some cacaos and chocolates are rich in epicatechin and its related oligomers, the procyanidins. Fractions of these compounds, isolated from the seeds of Theobroma cacao, caused dose-dependent inhibition of isolated rabbit 15-lipoxygenase-1 with the larger oligomers being more active. These observations suggest general lipoxygenase-inhibitory potency of flavanols and procyanidins that may contribute to their putative beneficial effects on the cardiovascular system in man. Thus, they may provide a plausible explanation for recent literature reports indicating that procyanidins decrease the leukotriene / prostacyclin ratio in humans and human aortic endothelial cells.

Cacao tree
Theobroma cacao is an evergreen tree found in South America. It grows well in a humid climate with lots of rainfall. The cacao fruit pods grow directly from the trunk and older branches, turning orange when ripe. The seeds are then used to make cocoa and chocolate. The fermented seeds are roasted, cracked, and ground into a powder from which fat is extracted, resulting in cocoa butter. The cacao fruit is about the size of a mango and contains edible white pulp but full of the seeds. The seeds can be eaten raw. The white pulp is used to make cacao juice, In Brazil it is called suco de cacao.

Emails
Can you tell me about Chocamine, the benefits?
   Chocamine is a proprietary cacao extract with methylxanthines (theobromine, caffeine, and theophylline), biogenic amines (phenylethylamine, tyramine, and according to one source, synephrine), amino acids (phenylalanine, tryptophan, tyrosine, others), minerals (with a high content of magnesium), and numerous beneficial antioxidantss. Promotional literature makes many positive claims about Chocamine, including increased energy, appetite suppression, increased lipolysis (fat burning), improved mood, improved concentration, increased alertness, improved physical performance, aphrodisiac properties, and health benefits. We have not seen any studies specifically on Chocamine, but the health benefits of cacao are well known.

I read somewhere that the anti-oxidants are only released under heat. So why make cacao capsules?
   As far as we know, the polyphenol antioxidants in cacao powder are well absorbed and utilized by the body.

Is cacao any different from cocoa powder? I assume it's not processed with alkali, which supposedly removes a lot of the antioxidants from the cacao seed, based upon what I've read. Another question; can cacao be used to make your own skin products? If so, what is it soluble in...water, propylene glycol, ethanol? I regularly visit websites on skincare, and with the astronomical prices of skincare products on the market, making your own skin products is becoming more popular. The latest info is that cacao extract when applied to the skin topically( or also taken internally) can be even more beneficial to the skin than green tea extract, since it contains even more antioxidants than green tea extract and has the same types of flavonoids (catechins) that presumably make green tea extract beneficial for the skin.
   Cacao bean is the raw bean from which after processing cocoa powder is created. We are not familiar with it used in skin care products.

There is a buzz out there on cacao beans, in tea, etc. Does this have a lot of caffeine?
    When used in reasonable amounts, cacao beans are healthy but they should be avoided late in the day due to possible insomnia or shallow sleep.

I am wondering if you can have too much cacao powder? Since it has one of the highest amounts of ORAC units/value of any food, can too much be bad for you? I mean if it has a very high orac value how can they advertise to mix a couple tablespoons into a smoothie, for example? Sounds like it would be way too much and might cause you a problem?
    Too much of anything can cause problems but cacao is quite safe since many people eat large amounts of dark chocolate without problems. It is good to consume a variety of natural herbs and plants rather than too much of just one or two.