Goodman and Gilman's the Pharmacological Basis of Therapeutics, 8th ed

It has been over 10 years since the first mention in a medical journal about cocoa and chocolate as potential sources of antioxidants for health. During this time, cocoa has been found to improve antioxidant status, reduce inflammation and correlate with reduced heart disease risk; with these results, and its popularity, it has received wide coverage in the press. However, after 10 years of research, what is known about the potential health benefits of cocoa and what are the important next steps in understanding this decadent source of antioxidants?

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Cocoa and health: a decade of research

Caffeine, widely consumed in beverages, and many xanthine analogs have had a major impact on biomedical research. Caffeine and various analogs, the latter designed to enhance potency and selectivity toward specific biological targets, have played key roles in defining the nature and role of adenosine receptors, phosphodiesterases, and calcium release channels in physiological processes. Such xanthines and other caffeine-inspired heterocycles now provide important research tools and potential therapeutic agents for intervention in Alzheimer’s disease, asthma, cancer, diabetes, and Parkinson’s disease. Such compounds also have activity as analgesics, antiinflammatories, antitussives, behavioral stimulants, diuretics/natriuretics, and lipolytics. Adverse effects can include anxiety, hypertension, certain drug interactions, and withdrawal symptoms.

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Caffeine analogs: biomedical impact

Role of plant alkaloids on human health: A review of biological activities

One may wonder why methylxanthines are so abundant in beverages used by humans for centuries, or in cola-drinks that have been heavily consumed since their appearance. It is likely that humans have stuck to any brew containing compounds with psychoactive properties, resulting in a better daily life, i.e., more efficient thinking, exploring, hunting, etc., however, without the serious side effects of drugs of abuse. The physiological effects of methylxanthines have been known for a long time and they are mainly mediated by the so-called adenosine receptors. Caffeine and theobromine are the most abundant methylxanthines in cacao and their physiological effects are notable. Their health-promoting benefits are so remarkable that chocolate is explored as a functional food. The consequences of adenosine receptor blockade by natural compounds present in cacao/chocolate are here reviewed. Palatability and health benefits of methylxanthines, in general, and theobromine, in particular, have further contributed to sustain one of the most innocuous and pleasant habits: chocolate consumption.

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Health Benefits of Methylxanthines in Cacao and Chocolate

SPECIFIC AIMSCough is a condition that affects the vast majority of people at some point in their lives and is the most common complaint for which medical attention is sought. Currently, no effective treatment exists. The aim of this study was to investigate the utility of a novel antitussive called theobromine, a methylxanthine derivative present in cocoa and chocolate, on cough and airway sensory nerve function in humans.PRINCIPAL FINDINGS1. Theobromine as a potential antitussiveSeveral synthetic antitussives are characterized by the presence of a 1,2,4-oxadiazole ring in their chemical structure. With the renaissance of the methylxanthine theophylline to treat asthma in the 1970s, a series of novel compounds with an oxadiazolylalkyl substituent at the N7 atom on the basic xanthine skeleton was synthesized and investigated as potential antiasthmatic and antitussive agents.With two of these compounds selected for preclinical testing, 3,7-dihydro-3-methyl-7-/(5-methyl-1,2,4-oxadiazol-3yl)methyl/-1H-purine...

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Dezső Korbonits

Papers

Theobromine inhibits sensory nerve activation and cough