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Plant Source Foods
Published in Chuong Pham-Huy, Bruno Pham Huy, Food and Lifestyle in Health and Disease, 2022
Chuong Pham-Huy, Bruno Pham Huy
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.
Dietary Substances Not Required in Human Metabolism
Published in Luke Bucci, Nutrients as Ergogenic Aids for Sports and Exercise, 2020
Caffeine has been used since the Stone Age as a stimulant.807 Major dietary sources are coffee, tea, chocolate, colas, and several herbs which constitute important dietary items for most cultures.807–809 Theophylline and theobromine are other methylxanthines found in significant amounts in teas and chocolates.807–811 Caffeine is also present in many nonprescription medications.808,809 Daily intake of caffeine from dietary sources can range from 0 to over 1 g/d.808–810 Widespread availability, low cost, and social acceptance have allowed caffeine to be well studied. Caffeine has been shown to stimulate neurons, the central nervous system, cardiac muscles, diuresis, epinephrine release and actions, lipolysis of adipose tissue increasing serum FFA levels, relaxation of smooth muscle, and gastric acid secretion.807,809 Several of these effects have been postulated to improve physical performance.
Sympathomimetics
Published in Frank A. Barile, Barile’s Clinical Toxicology, 2019
The predominant CNS stimulant properties of caffeine and the respiratory relaxation produced by theophylline are well documented. Caffeine stimulates cerebral activity, skeletal and cardiac muscle contraction, and general basal metabolic rate, while theophylline has less central stimulation but significant bronchial smooth muscle relaxation properties. Caffeine and theophylline enhance cardiac muscle contraction, induce coronary vasodilation, and promote diuresis. Caffeine is available in combination with ergotamine, belladonna alkaloids, or pentobarbital for the treatment of migraine headaches (Wigraine® tablets, Cafergot® suppositories), for its synergistic action with ephedrine for weight loss, and as an aid to wakefulness and restoring mental alertness. In combination with sodium benzoate (injectable), caffeine is used in the treatment of drug-induced respiratory depression, and as caffeine citrate (injectable) for the short-term treatment of apnea in premature infants. Theophylline (Elixophyllin®, Theolair®, Theo-Dur®, and various others) is employed in the treatment of bronchial asthma and other respiratory-related disorders. The calcium and sodium salicylate salts of theobromine are available for use as mild diuretics, vasodilators, smooth muscle relaxants, and cardiac stimulants.
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).
Urinary caffeine and caffeine metabolites, asthma, and lung function in a nationwide study of U.S. adults
Published in Journal of Asthma, 2022
Yueh-Ying Han, Erick Forno, Juan C. Celedón
Caffeine (1,3,7-trimethylxanthine) can be absorbed within 45 min after ingestion. Caffeine is primarily metabolized by CYP1A2 in the liver, where it undergoes successive demethylations and oxidations (9). The half-life of caffeine in adults is typically 2.5 to 5 h (9). The main products of the first steps in caffeine metabolism through demethylations are paraxanthine (1,7-dimethylxanthine), theobromine (3,7-dimethylxanthine), and theophylline (1,3-dimethylxanthine)(9). Caffeine and these primary metabolites are methylxanthines, a purine derived group of pharmacologic agents with bronchodilator properties (10). Caffeine has been used to treat apnea of prematurity (AOP) in infants (11) and shown to slightly improve lung function up to four hours post-ingestion in adults with mild to moderate asthma (12). While theophylline is a mild bronchodilator that has been used to treat asthma (13,14), there is limited and inconclusive evidence of any bronchodilator effects of theobromine (10). Although paraxanthine is the major caffeine metabolite, little is known about paraxanthine and asthma or lung function (9).
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
Presently, the majority of therapies available for myopia have scarce benefits that last for a relatively short period or have significant side effects, like reduced accommodation and dilation of the pupil. Furthermore, there is no effective treatment available that could manage the progression of myopia without inflicting side effects (Polkinghorne and Craig 2004). Amongst them, topically applied muscarinic acetylcholine antagonists, such as atropine (non-selective antagonist), and pirenzepine (Muscarinic receptor type 1 selective antagonist) are available and act by reducing the progression of myopia and axial eye growth (Saw et al. 2002, Siatkowski et al. 2008). Amid these challenges, a new molecule, 7-methylxanthine (7-MX) being instigated for the treatment of myopia. It is a purine analog and a metabolic product of methylxanthines (caffeine, theophylline, and theobromine). CYP1A2 and xanthine oxidase primarily catalyzes the metabolism of caffeine into 14 different metabolites, including 7-MX as one of them (Safranow and Machoy 2005).