^{(From a magazine advertisement for Godiva chocolates. In my opinion, the pose of the woman in this photo just sizzles, with her holding a truffle the size of a testicle and her over-the-shoulder look that says, “And what can YOU do for me, sailor boy?” Wa-Wa-WEE-Wa, it’s SEXY time!)}

Regarding chocolate, what else can you say, what else  need you say, about a concoction derived from a plant whose scientific name, Theobroma cacao, means “Food of the gods”? Carl von Linné, the 18^th century Swedish botanist, who created the system of binomial nomenclature which we use today, was no fool when he assigned that name to the plant which produced chocolate — he deferred to the Mayan belief that, indeed, it was food of the gods.

It is no coincidence that an icon for St. Valentine’s Day is a heart-shaped box of chocolates that the man is expected to give to the woman of interest.  In the animal world, when a male brings a food gift to a female, it is because the male has made considerable progress in the courtship ritual, and now the male expects something from the female in return for his gift of food. 

1  A brief history of cocoa and chocolate

By the time the Spanish Conquistadors came to the New World, they found that the Aztecs had used the cacao beans to prepare a ceremonial drink called chocolatl, made of ground cacao beans, spices, and red pepper.  (Bear in mind that red peppers from Central and South America are hot!)  Montezuma II, who introduced chocolatl to Hernán Cortés in 1519, is reputed to have consumed 50 cups of this beverage every day.

In Aztec culture, this beverage was reserved for royalty, nobility, merchants trading far afield, and warriors. Because of its presumed aphrodisiac quality, women were not permitted to consume it, but they were expected to prepare it for their men, as suggested by the following illustration:

^{Jaguar Claw receives a cup of chocolate from his wife, Flower Snake, in Codex Zouche-Nuttall, Mexico, c.1200-1521. Mexicolore. From https://historycollection.com/20-downright-bizarre-details-about-the-history-of-chocolate-that-we-love-to-sink-our-teeth-into/}

For many years, chocolate was reserved for royalty and clergy, but four  innovations made chocolate the popular beverage and foodstuff that it is today:

1. The replacement of red pepper as a flavoring with sugar;
2. The addition of milk;
3. The invention of the cocoa press, which separates the cocoa butter from cocoa powder; and
4. Dutching, i.e. adding alkalized salts to the cocoa powder, thereby making it more soluble in water.

So this infograph summarizes the steps in producing a modern chocolate bar:

According to the June 2004 Quarterly Bulletin of Cocoa Statistics, published by the International Cocoa Organization, annual production of cocoa beans will exceed 3 million metric tons.

2.  “Addiction” to chocolate

            It is part of the common vernacular for people to refer to themselves as “choco-holics.”  Even if the chemical components of chocolate are in physiologically significant concentrations to stimulate the reward circuitry of the brain, and even if someone can be legitimately diagnosed as a chocolate addict, I do not know of anyone who has been hauled to police headquarters on a DWF (Driving While Fat) charge due to the consumption of chocolate.

            The fact is that chocolate, or cacoa, does not cause a debilitating addiction.  Dallard et. al. (2001) tried to search for eating disorders, DSM III-R mental disorders, personality disorders and addictive behavior among  3 men and 12 women who described themselves as “chocolate addicts”.  These individuals reported feelings of increased energy or concentration ability, and a reduction of anxiety during stress.  Almost half of them reported minor withdrawal symptoms.   Dallard et. al. concluded that the amount of cacoa consumed (an average of 50 grams per day) is moderate, and the subjects under study rarely display other addictive behaviors.

            There is certainly the phenomenon of craving, particularly among women. Whereas only 15% of men admit to chocolate cravings, around 40% of women do.  For many women, the craving for chocolate peaks in the perimenstrual period, beginning a few days before the onset of menses, and then continuing into the first few days of menses (Rozin, Levine and Stoess, 1991).

            3.  Psychoactive compounds in chocolate.

            Nonetheless, there are potent psychoactive compounds in roasted chocolate, including the following:

1. Tetrahydro-beta carbolines are neuroactive alkaloids.  They are also present in beer, wine and liquor;
2. Salsolinol is a tetrahydroisoquinoline (TIQ), which has multiple effects, including binding to D₁, D₂, and D₃ dopamine receptors, inhibiting the formation of cyclic AMP, and inhibiting the release of b-endorphin and ACTH in pituitary cells grown in vitro (Melzig, et. al., 2000).  Concentrations of b-endorphin in the cerebrospinal fluid from alcoholics and other addicts are significantly lower than those of non-addict healthy volunteers (Genazzani, et. al., 1982), so the consumption of chocolate may be an attempt by alcoholics to self-medicate and thereby compensate for the deficiency; 
3. Phenylethylamine is a neuroamine chemically similar to amphetamines.  Like them, phenylethylamine raises blood pressure and blood glucose levels,causes the release of dopamine in the mesolimbic pleasure centers of the brain, and induces a state of well-being and alertness.  Its concentrations peak during orgasm.  There is also evidence that the antidepressant benefits of aerobic exercise is the result of an increase in phenylethylamine production (McConnell, 2001);
4. Anandamide is the endogenous ligand for cannabinoid receptors in the brain.  N-oleoethanolamine and N-linoleoylethanolamine, which inhibit the metabolic breakdown of anandamide, are also found in cacao;
5. Caffeine, is a mild cardiovascular stimulant which increases alertness;
6. Theobromine is chemically similar to caffeine, but is relatively weaker in potency.
7. Serotonin, as we saw in chapter 3,is a neurotransmitter which has clear effects on mood.  It is removed from synapses in a manner similar to that of dopamine removal, by reuptake pumps.  Since clinical symptoms of depression are associated with a deficiency of serotonin, one of the strategies for treatment is the use of selective serotonin reuptake inhibitors, SSRI’s, which target the reuptake pumps.

To estimate possible dosages of the compounds mentioned above, Hetherington and MacDiarmid (2003) state that 50 individuals who identified themselves as “chocoholics” consumed about 12 60-gram bars of chocolate per week, or approximately 100 grams of chocolate daily. 

What does 100 grams of chocolate look like? Voila:

^{About the company that produces this type of chocolate: “The Piura region, located in the foothills of the Andes Mountains in Peru, is known for its “white” cocoa. We were introduced to some wonderful farms in the area by Santiago Paz, who runs a cooperative that helps local farmers develop cocoa varieties. In our first year working with Santiago, our Peru 100% Cocoa chocolate won a gold medal at an international chocolate competition. The cocoa flavors are hinted at by raspberry and toasted pecan.”}

A daily dose of 100 grams yields the following amounts of psychoactive compounds (Table 16.1):

Table 16.1.  Estimated amounts of psychoactive compounds ingested with 100 grams of chocolate bars daily.
Type of compound	Concentration in chocolate	Amount in 100 grams of chocolate bars	Amount required for physiological effect
Tetrahydro-beta carbolines, including 60HMTHbetaC, THCA, 1S-3S MTCA, 1R-3S MTCA, MTHbetaC (Herraiz, T, 2000)	60HMTHbetaC  (0.16 – 3.92 ug/g); THCA (0.01 – 0.85 ug/g); 1S,3S MTCA (0.35 – 2 ug/g); 1R,3S MTCA (0.14-0.88 ug/g); MTHbetaC (nd – 0.21 ug/g)	60HMTHbetaC  (16 – 392 ug/g); THCA (1 – 85 ug/g); 1S,3S MTCA (35 – 200 ug/g); 1R,3S MTCA (14-88 ug/g); MTHbetaC (0 – 21 ug/g)
Salsolinol (a tetrahydro-isoquinolone (TIQ)	5.20 ug/g (Melzig, et. al., 2000)	520	Amount in a 100 gram bar is sufficient.
Phenylethylamine (=BPEA)	.38 – 6.4 ug/gram (that’s micrograms) (Knight, 1999)	38-640 micrograms
Anandamide			Estimates suggest  a 130-pound person would have to eat 25 POUNDS of chocolate at one time to get any marijuana-like effect.
Caffeine	80 mg in 80 g (Rios, et. al., 2003)	100 mg
Theobromine	500 mg in 80 g (Rios, et. al., 2003)	625 mg
Serotonin	6.2 – 58.2 mg/g	62 – 582 mg

            Despite the presence of all these psychoactive compounds, the craving for chocolate seems to have a cultural origin, rather than a physiological one (Zellner, et. al., 2004).  In other words, we learn to associate satiety or the fulfillment of hunger with chocolate because that’s what we were given when we were little, and the association persists into adulthood.

4.The salutary effects of chocolate

The benefits of chocolate center around the presence of antioxidants, including several types of flavonoids and polyphenols, of magnesium.

Antioxidants are compounds which provide cellular protection from free radicals, which are highly reactive forms of oxygen, including singlet oxygen atoms (O), superoxide radicals (O₂^.-), hydrogen peroxide (H₂O₂).

     Each of these free radicals has an unpaired electron, and will seek additional electrons by attacking other compounds, including cell membrane phospholipids and DNA, potentially causing premature cell death or cancer.  We’ve already seen that the damage caused by free radicals is a contributing factor to the liver pathology found in alcoholics.

There are times when taking antioxidant supplements is NOT desirable.  Research suggests that one of the reasons that radiation works to kill cancer cells is because the high-energy electromagnetic waves used in radiation therapy generate free radicals in the exposed tissue.  For that reason, patients undergoing radiation therapy are advised to discontinue their intake of antioxidants until their radiation treatments are completed.

Magnesium is a mineral which, in its ionic form of Mg²⁺, is an activating cofactor for over 300 cellular enzymes.   A dietary deficiency of magnesium can cause serious neurological and cardiac problems, but the reason why women in particular gravitate towards chocolate is because a magnesium deficiency exacerbates the symptoms of premenstrual syndrome (Abraham and Lubran, 1981; Sherwood, et. al. 1986).

The concentrations of these compounds in chocolate are shown in Table 16.3:

Table 16.3.  Concentrations of beneficial compounds in chocolate
Compound	Concentration in chocolate	Amount in 100 grams of chocolate	Amount required for demonstrated beneficial effect, or RDA, Recommended Daily Allowance
Flavonoids	Highly variable, .09 mg to 4 mg	9 to 400 mg	150 mg for rapid antioxidant effect (Kris-Etherton and Keen, 2002).
Polyphenols	439 mg in 80 g (Rios, et. al., 2003)	549 mg
Magnesium	3 mg in a 6-gram wafer (Wardlaw and Insel, 1996), 131 mg/100 g (Hawaiian Vintage Chocolate, 1999)	50 mg, according to Wardlaw and Insel (1996), 131 mg according to Hawaiian Vintage Chocolate	RDAmales = 230-250 mg/day, RDAfemlaes = 200-210 mg/day, from ages 18 – 75+

Research indicates that the protective benefits of antioxidants are most expressed in the cardiovascular and respiratory systems:

1. The cardiovascular system:
2. DARK chocolate, but neither white nor milk chocolate, inhibited collagen-induced platelet aggregation in platelet rich plasma (Innes, et. al., 2003).  Given the fact that cardiovascular disease is a leading cause of death in the United Kingdom, dark chocolate may have an application in the prevention of cardiovascular diseases;
3. In a preliminary study involving 13 elderly individuals with untreated mild hypertension, the ingestion of DARK chocolate, but not white chocolate, resulted in slight, but significant decreases in both systolic and diastolic pressure.  The scientists who conducted this study believe that it is the polyphenols in chocolate which reduced blood pressure (Taubert, et. al., 2003);
4. The respiratory system: Scientists in Australia found that a cocoa-based edible spacer device, dubbed the Chocuhaler, delivered significantly more salbutamol, a bronchodilator, in droplets of a size likely to enter the respiratory tract for asthma management, as compared with to a standard spacer.  No significant bronchodilator response occurred when the spacer was eaten at the end of the study.  These scientists admitted there may be potential drawbacks:  weight gain in some patients, and meltdown of the device in hot climates (Hayden, et. al., 1995);
5. The digestive system: In laboratory studies among rats, cocoa phenols reduced gastric lesions (Osakabe, et. al., 1998).

5. Additional details about the benefits of methylxanthines in cacao, specifically theobromine and caffeine (Franco, et. al., 2013).

There is considerable evidence that cocoa is beneficial to health, because of its higher concentration of phenolic phytochemicals and higher antioxidant capacity than black tea, green tea, or red wine (Lee, .et. al., 2003).

Theobromine in Oral Health

Kargul et. al. (2012) conducted a pilot study in which they applied a 200 mg/L theobromine solution to extracted human third molars. They found a consistent and remarkable protection of the enamel surface of these teeth. While such high levels of theobromine are not found in natural sources, the results suggest the efficacy of supplementing toothpaste and/or mouthwash liquids with theobromine.

Methylxanthines in Respiratory Tract Diseases

Theobromine is able to suppress cough in humans without the side effects caused by other antitussive drugs, such as codeine. Theobromine is now a first-in-class non-codeine non-opioid drug for cough that has successfully completed trails and regularly review in South Korea, where it is sold as AnyCough^TM.

Both theobromine and caffeine improve lung function and produce bronchodilatation in asthma patients. Patients with asthma can safely self-administer coffee or cacao/chocolate to relieve symptoms.

Methylxanthines as psychostimulants

In one study, volunteers took visually identical portions of white chocolate, either containing no methylxanthines, low (8 mg caffeine + 100 mg theobromine) or high amounts (20 mg caffeine + 250 mg theobromine) of methylxanthines. These three forms were formulated to mimic white, milk and dark chocolate respectively. Using a long duration simple reaction time task, a rapid visual information processing task, and a mood questionnaire, the results of this study showed that the psychostimulant effect of chocolate is mainly due to the methylxanthines present.

Methylxanthines and sleep

Whereas caffeine is a psychostimulant, theobromine alone promotes sleep.

Methylxanthines in cardiovascular diseases

Theobromine from cacao consumption significantly increases plasma HDL cholesterol levels, and decreases LDL concentration in plasma, thereby conferring cardiovascular consumption of the theobromine-enriched beverages.

Cacao in insulin resistance and body weight

Short-term administration of dark chocolate is followed by a significant increase in insulin sensitivity and a decrease in blood pressure in healthy persons. Furthermore, studies among high fat-fed mice have shown that dietary cacao ameliorates obesity-related inflammation (Gu, et. al., 2013). Flavonols and methylxanthines appear to be key players in the increase of beneficial gut microbes, e.g. Lactobacilli, and the decrease of less beneficial ones, e.g. Clostridia. Furthermore, cacao and/or chocolate modifies intestinal flora in the same way that prebiotics and probiotics do (Hayek, 2013).

People who regularly eat chocolate have a lower likelihood of developing Type 2 diabetes, according to an article in the Washington Post. (https://www.washingtonpost.com/wellness/2024/12/04/dark-70-chocolate-better-for-you/?utm_campaign=wp_news_alert_revere_trending_now&utm_medium=email&utm_source=alert&location=alert)

In a 30-year study involving over 190,000 health professionals, researchers found that “people who ate at least five ounces of dark chocolate per week — equivalent to five servings — had a 21 percent lower risk of developing Type 2 diabetes compared with people who rarely or never ate dark chocolate. For every ounce of dark chocolate that a person consumed per week, their risk of developing diabetes fell by three percent. The researchers found that this was especially the case for men and for people who were younger than 70 years old, though it’s not entirely clear why.”

Why is that?  “A number of studies have indicated that flavonoids might help protect against Type 2 diabetes by improving how our bodies respond to insulin and break down sugar as well as by protecting the beta cells that produce and release insulin from the pancreas.”

P.S.: The recipe for Xocolatl, according to allrecipes.com

^{Ritual drinking of xocolatl, from Codex Borgia, Mexico, c. 1500}

Xocolatl (Aztec Chocolate)

This bitter, spicy Aztec drink is what modern ‘Hot Chocolate’ is based from. For a more authentic version the way the Aztecs enjoyed, chill the Xocolatl before drinking.

Submitted by Antipex

Prep Time: 5 mins

Cook Time: 15 mins

Total Time: 20 mins

Servings: 2; Yield: 2 servings

Ingredients

Original recipe (1X) yields 2 servings

• 1 ½ cups water
• 1 green chile pepper, sliced
• 4 cups water
• ¼ cup unsweetened cocoa powder
• 2 teaspoons vanilla extract

Directions

1. Bring 1 1/2 cup water to a boil in a pot; add the chili pepper, seeds included, to the boiling water and cook at a boil for 5 to 10 minutes. Strain the chili pepper and seeds from the water; return the water to the pot. Add 4 cups water to the chili pepper-infused water, reduce heat to medium-low, and bring to a slow boil. Stir the cocoa powder and vanilla extract into the boiling water; cook and stir until the powder dissolves completely, 5 to 10 minutes.

Nutrition Facts

Calories46
Total Fat 2g
Saturated Fat 1g
Sodium 24mg
Total Carbohydrate 9g
Dietary Fiber 4g
Total Sugars 2g
Protein 3g
Vitamin C 55mg
Calcium 38mg
Iron 2mg
Potassium 253mg

P.P.S: An appropriate song to end this blog:

https://www.youtube.com/watch?v=kgx5ldWraWY

Abraham, G.E.; Lubran M.M.  (1981). Serum and red cell magnesium levels in patients with premenstrual tension. American Journal of Clinical Nutrition 11:2364-2366.

Dallard, L.; Cathebras, P.; Sauron, C.; Massoubre, C. (2001). Is cacao a psychotropic drug? Psychopathologic study of a population of subjects self-identified as chocolate addicts. Encephale 27(2):181-186.

Franco, R.; Onatibia-Astibia, A.; Martinez-Pinilla, E. (2013). Health Benefits of Methylxanthines in Cacao and Chocolate. Nutrients 5:4159-4173; doi:10.3390/nu5104159.

Genazzani, A.R.; Nappi, G.; Faccinetti, F.; Mazella, G.L.; Parrini, E.; Sinforiani, E.; Petraglia, F.; Sovaldi, F.  (1982).  Central deficiency of b-endorphin in alcohol addicts.  Journal of Clinical Endocrinology and Metabolism 55:583-586.

Gu, Y.; Yu, S.; Lambert, J.D. (2013). Dietary cocoa ameliorates obesity-related inflammation in high fat-fed mice. European Journal of Nutrition, doi:10.1007/s00394-013-0510.1.

Hayden, M.J.; Wildhaber, J.H.; Eber, E.; Devadason, S.G.  (1995).  The Chocuhaler:  sweet deliverance in asthma management.  Medical Journal of Australia
163(11-12):587-588.

Hayek, N. (2013). Chocolate, gut microbiota, and human health. Front. Pharmacol. 4, doi:10.3389/fphar.2013.00011.

Innes, A.J.; Kennedy, G.; McLaren, M.; Bancroft, A.J.; Belch, J.J.  (2003).  Dark chocolate inhibits platelet aggregation in healthy volunteers.  Platelets 14(5):325-327.

Kargul, B.; Ozcan, M.; Peker, S.; Nakamoto, T.; Simmons, W.B.; Falster, A.U. (2012). Evaluation of human enamel surfaces treated with theobromine: A pilot study. Oral Health Prev. Dent. 10, 275–282.

Knight, I.  (1999). Chocolate and Cocoa : Health and Nutrition. Blackwell Science, Malden, Mass.

Lee, K.W.; Kim, Y,J.; Lee, H.J.; Lee, C.Y.  (2003).  Cocoa
has more phenolic phytochemicals and a higher antioxidant capacity than teas and red wine.  Journal of Agricultural Food Chemistry 51(25):7292-7295.

McConnell, H.  (2001). Exercise Levels Of Phenylethylamine May Damp Depression. British Journal of Sports Medicine 35: 342-343.

 Osakabe, N., et. al.  (1998).  Effects of polyphenol substances derived from Theobroma cacao on gastric mucosal lesion induced by ethanol.  Bioscience, Biotechology, Biochemistry 62(8):1535-1538.

Rios, L.Y.; Gonthier, M.P; Remesy, C.; Mila, I.; Lapierre, C.; Lazarus, S.A.; Williamson, G.; Scalbert, A.  (2003).  Chocolate intake increases urinary excretion of polyphenol-derived phenolic acids in health human subjects.  American Journal of Clinical Nutrition 77(4):912-918.

Rozin, P.; Levine, E.; Stoess, C.  1991.  Chocolate craving and liking.  Appetite 17(3):199-212.

Sherwood, R.A.; Rocks, B.F.; Stewart, A.; Saxton, R.S.  (1986). Magnesium and the premenstrual syndrome. Ann Clin Biochem. 23( Pt 6):667-670.

Taubert, D,; Berkels, R.; Roesen, R.; Klaus, W.  (2003). Chocolate and Blood Pressure in Elderly Individuals With Isolated Systolic Hypertension.  Journal of the American Medical Association 290:1029-1030.

Wardlaw G.M.; Insel, P.M.  1996.  Perspectives in Nutrition, Third Edition.  Mosby-Year Book, Inc., St. Louis, MO.