Plant Source Foods
Chuong Pham-Huy, Bruno Pham Huy in Food and Lifestyle in Health and Disease, 2022
Cocoa is a rich source of polyphenolic antioxidants with high amounts of flavonoids such as epicatechin, catechin, and procyanidins (277–279). Dark chocolate contains considerably higher amounts of flavonoids than milk chocolate. Moreover, the milk may slow down the intestinal absorption of flavonoids (277, 279). Due to their high amounts of polyphenol antioxidants, cocoa and chocolate increase the production or bioavailability of endothelial nitric oxide (NO). Nitric oxide regulates vasodilation and the environment of the blood vessel wall. Therefore, cocoa and chocolate may be useful for the prevention of hypertension and atherosclerosis. In addition, cocoa contains theobromine (2–3%) and caffeine (0.2%) (277). Theobromine is a purine alkaloid. It stimulates heart muscle and relaxes bronchial smooth muscles for the treatment of asthma. In addition, theobromine has antioxidant activity and may be used for depression therapy (278). Chocolate and cacao bean are rich in essential minerals like magnesium, copper, potassium, and iron – mostly magnesium (277–279). These minerals may enhance the activities of some polyphenol antioxidants.
Catalog of Herbs
James A. Duke in Handbook of Medicinal Herbs, 2018
Toxicity — Classed as a narcotic stimulant.54 As a long-term drinker of 5 to 10 cups of coffee a day, I do not think I do myself any favors by drinking coffee. Tyler37 cites “some evidence linking coffee and cancer of the pancreas . . . Caffeine ... in large amounts produces many undesirable side effects — from nervousness and insomnia to rapid and irregular heartbeats, elevated blood sugar and cholesterol levels, excess stomach acid, and heartburn. It is definitely a teratogen in rats.”37 At 100 mg/kg theophylline is fetotoxic to rats, but no teratogenic abnormalities were noted. In therapeutics, theobromine has been used as a diuretic, as a cardiac stimulant, and for dilation of arteries. But at 100 mg, theobromine is fetotoxic and teratogenic.137 Leung reports a fatal dose in man at 10,000 mg, with 1000 mg or more capable of inducing headache, nausea, insomnia, restlessness, excitement, mild delirium, muscle tremor, tachycardia, and extrasystoles. Leung also adds “caffeine has been reported to have many other activities including mutagenic, teratogenic, and carcinogenic activities; . . to cause temporary increase in intraocular pressure, to have calming effects on hyperkinetic children ... to cause chronic recurring headache . . . Coffee drinking has also been linked to myocardial infarction . . . cancer of the lower urinary tract (e.g., bladder), ovaries, prostate, and others.”
Biochemistry of Caffeine's Influence On Exercise Performance
Peter M. Tiidus, Rebecca E. K. MacPherson, Paul J. LeBlanc, Andrea R. Josse in The Routledge Handbook on Biochemistry of Exercise, 2020
Caffeine metabolism is not altered by the route of administration but can be negatively affected by the presence of disease or environmental factors. For example, barbiturates and nicotine are known to induce the CYP1A2 enzyme and result in enhanced metabolism of caffeine (50). Likewise, caffeine may act as a competitive inhibitor and slow drug metabolism if significant amounts are ingested. Upon metabolism, each of the three primary caffeine metabolites are also metabolically active. Paraxanthine, comprising the majority of caffeine breakdown, is wake promoting (20). Theophylline is not ergogenic, but has been used as a bronchodilator in asthma and is an immune mediator (79). Lastly, theobromine has vasodilatory properties and can be used as a cardiac inducer, but levels resulting from caffeine consumption are very minor and are thought to have little physiological impact.
Changes in endothelial function, arterial stiffness and blood pressure in pregnant women after consumption of high-flavanol and high-theobromine chocolate: a double blind randomized clinical trial
Published in Hypertension in Pregnancy, 2018
Asma Babar, Emmanuel Bujold, Vicky Leblanc, Élise Lavoie-Lebel, Joalee Paquette, Laurent Bazinet, Simone Lemieux, Isabelle Marc, Belkacem Abdous, Sylvie Dodin
Our pilot study performed in a group of 54 pregnant normotensive women (21 weeks gestation) without risk of PE evaluated the impacts of high flavanol chocolate (HF) with similar theobromine concentrations in both the experimental and low flavanol chocolate, on plasma flavanol and methylxanthines concentrations, FMD, SBP and DBP (30). Acute consumption of HF chocolate resulted in increased epicatechin and increased theobromine. Acute and chronic consumption was not associated with significant within or in between group changes in FMD, SBP or DBP. Although many of the results of the present study were concordant with our pilot study, the use of a different measurement technique for the evaluation of endothelial function, a small study population providing insufficient power and most importantly a different chocolate composition complicate the comparison of results.
A Proprietary Herbal Blend Containing Extracts of Punica granatum Fruit Rind and Theobroma cocoa Seeds Increases Serum Testosterone Level in Healthy Young Males: A Randomized, Double-Blind Placebo-Controlled Study
Published in Journal of Dietary Supplements, 2023
Poorna Gopal Azad Sreeramaneni, Amulya Yalamanchi, Manikyeswara Rao Konda, Sree Harsha Varma Cherukuri, Joseph C. Maroon
LN18178 is standardized with two major bioactive phytochemicals, viz. punicalagin, and theobromine. The polyphenol punicalagin (combined A and B isomers) is reported as a potent anti-oxidant (32). Rao et al. demonstrated in a mouse model that punicalagin mitigated testicular damage and improved reproductive capacity in oxidative stress-induced male animals (33). In males, oxidative stress-induced reactive oxygen species (ROS) disrupts hypothalamic-pituitary-gonadal (HPG) cross-talk and reduces productions of the sex hormones, including testosterone from the gonads (34, 35). Polyphenols enhance mitochondrial function and biogenesis through AMP-activated protein kinase (AMPK) activation and modulation of peroxisome proliferator-activated receptor coactivator 1 alpha (PGC1α) protein expression in the muscle cells (36). Theobromine inhibits phosphodiesterase activity, increasing intracellular cyclic AMP (cAMP) level (37). Enhanced cAMP signaling increases cholesterol transport into the mitochondria and promotes steroidogenesis in the Leydig cells (28).
Sub-chronic and chronic toxicity evaluation of 7-methylxanthine: a new molecule for the treatment of myopia
Published in Drug and Chemical Toxicology, 2022
Harjeet Singh, Harmanpreet Singh, Nikhil Shri Sahajpal, Surinder Paul, Inderjit Kaur, Subheet Kumar Jain
In the sub-chronic and chronic toxicity study, there was no mortality, no signs of toxicity (tremor, convulsion, salivation, diarrhea, lethargy, or coma) and unscheduled deaths were observed at any dose of 7-MX. Whereas, 10% and 40% mortality was observed in caffeine and theobromine treated groups, respectively. Mild toxicity of caffeine and theobromine are well reported in animal models. As per the review of literature, Bolignano et al. 2007 also reported the mild nephrotoxic effects of caffeine on chronic treatment in rats. Many other studies have also reported that the chronic treatment of caffeine and theobromine leads to mild nephrotoxicity (Sellman et al. 1984, Belibi et al. 2002, Rieg et al. 2005, Osswald and Schnermann 2011).