Structure-Bioactivity Relationships of Methylxanthines: Trying to Make Sense of All the Promises and the Drawbacks
Open Access
- 27 July 2016
- Vol. 21 (8), 974
- https://doi.org/10.3390/molecules21080974
Abstract
Methylxanthines are a group of phytochemicals derived from the purine base xanthine and obtained from plant secondary metabolism. They are unobtrusively included in daily diet in common products as coffee, tea, energetic drinks, or chocolate. Caffeine is by far the most studied methylxanthine either in animal or epidemiologic studies. Theophylline and theobromine are other relevant methylxanthines also commonly available in the aforementioned sources. There are many disseminated myths about methylxanthines but there is increased scientific knowledge to discuss all the controversy and promise shown by these intriguing phytochemicals. In fact, many beneficial physiologic outcomes have been suggested for methylxanthines in areas as important and diverse as neurodegenerative and respiratory diseases, diabetes or cancer. However, there have always been toxicity concerns with methylxanthine (over)consumption and pharmacologic applications. Herein, we explore the structure-bioactivity relationships to bring light those enumerated effects. The potential shown by methylxanthines in such a wide range of conditions should substantiate many other scientific endeavors that may highlight their adequacy as adjuvant therapy agents and may contribute to the advent of functional foods. Newly designed targeted molecules based on methylxanthine structure may originate more specific and effective outcomes.Keywords
Funding Information
- Fundação para a Ciência e a Tecnologia (SFRH/BPD/80451/2011, SFRH/BPD/108837/2015)
This publication has 326 references indexed in Scilit:
- Caffeine Inhibits Acetylcholinesterase, But Not ButyrylcholinesteraseInternational Journal of Molecular Sciences, 2013
- Delayed caffeine treatment prevents nigral dopamine neuron loss in a progressive rat model of Parkinson's diseaseExperimental Neurology, 2012
- Methylxanthines and the KidneyHandbook of Experimental Pharmacology, 2010
- Association of the Anxiogenic and Alerting Effects of Caffeine with ADORA2A and ADORA1 Polymorphisms and Habitual Level of Caffeine ConsumptionNeuropsychopharmacology, 2010
- Increased caffeine consumption is associated with reduced hepatic fibrosisJournal of Hepatology, 2009
- Systemic 7-methylxanthine in retarding axial eye growth and myopia progression: a 36-month pilot studyJournal of Ocular Biology, Diseases, and Informatics, 2008
- Caffeine protects against MPTP‐induced blood‐brain barrier dysfunction in mouse striatumJournal of Neurochemistry, 2008
- Caffeine analogs: biomedical impactCellular and Molecular Life Sciences, 2007
- The enigmatic effects of caffeine in cell cycle and cancerCancer Letters, 2007
- Effect of reducing caffeine intake on birth weight and length of gestation: randomised controlled trialBMJ, 2007