What Foods Contain Theophylline and What Are Its Benefits?

Learn all about this phytonutrient

You’ve probably heard about the phytonutrient beta-carotene, but have you heard of theophylline? (Pronounced thee-aa-fuh-luhn or theo-fye-lin.)

Theophylline is in the alkaline family of phytonutrients.[1] It is sometimes called a xanthine or methylxanthine too.[2] Theophylline has been used in medications, but we are interested in its whole food form, not extracted or synthetically made. Many nutrients—including vitamins, minerals, and phytochemicals—are often isolated or synthetic. These don’t even come close to natural nutrients in their whole food state; they are not the same. We believe in the synergistic effect of all phytonutrients.

Read our helpful resource about how they are different and why natural nutrients, as opposed to isolated or synthetic, are safer and much more beneficial. Theophylline is found naturally in black and green tea, green coffee, unsweetened natural cocoa, and mate (sometimes called Yerba mate, Jesuits’ tea, or Paraguayan tea)[3].

Theophylline can stimulate the central nervous system, relax bronchial smooth muscle, improve the diaphragm’s contraction, lower blood pressure, fight inflammation, affect heart rate, and inhibit phosphodiesterase (an enzyme involved in cell function). Phosphodiesterase inhibitors have been used to treat heart failure, inflammatory airways disease, and erectile dysfunction.[4] Theophylline in particular has been used to treat people with asthma and chronic obstructive pulmonary diseases.[5]

For drug use, it is isolated from the plants Camellia sinensis (tea) and Coffea arabica. In terms of chemical safety, unnatural theophylline has acute toxicity and is classified as an irritant.[6] Tachycardia, anorexia, nausea, vomiting, diarrhea, insomnia, irritability, restlessness, headache, agitated maniacal behavior, extreme thirst, slight fever, tinnitus, palpitation, arrhythmia, delirium, muscle twitching, severe dehydration, albuminuria, emesis of a "coffee ground" material, hyperthermia, profuse diaphoresis, and seizures could all be signs of toxicity from high serum concentrations or rapid injection of isolated theophylline.[7] Its use has decreased due to the development of other pharmacologic agents and concern about its toxicity.[8]

Foods

Xanthines are contained in cocoa, tea, and coffee. These are believed to help protect the heart and brain, improve physical performance, boost metabolism, and more.[9]

Specifically, the consumption of unsweetened natural cocoa powder could be beneficial for asthmatics.

According to the International Journal of Immunopathology and Pharmacology, “Anecdotal reports indicate that regular consumption of unsweetened natural cocoa powder . . . has the potential to reduce the tendency of asthmatic episodes” because it contains the anti-asthamitc compounds theobromine and theophylline.[10]

In addition to xanthines, cocoa also contains polyphenols and flavonoids, which have antioxidant and anti-inflammatory properties. Eating cocoa has also been tied to managing oxidative stress, providing cardiovascular protection, and protecting against tumor and carcinogenic processes. Cocoa that goes under certain chemical processes like sweetening and heat isn’t nearly as beneficial. Raw, unheated, unsweetened, unadulterated cocoa is best in terms of potency.

Theophylline is also found in tea, green coffee, and mate but at very low levels. Nevertheless, its natural form is a lot safer than its synthetic forms.[11]

Green tea in particular may contribute to many health benefits involving cancer, heart disease, liver disease, diabetes, skin disorders, and more.[12] A lot of this has to do with green tea’s antioxidant properties. Though, the amount of theophylline and its isomer, theobromine, in a cup of tea is very small. Opposed to black tea, green tea has not been fermented at all.[13]

Mate is a drink made from the leaves of the plant Ilex paraguariensis. The dry leaves were found to contain theophylline in addition to other methylxanthines, albeit a small amount. It’s important to note that, in Uruguay, mate drinking has been associated with increased risk of squamous cell carcinoma of the larynx and oesophageal cancer.[14]

More Facts

Theophylline can be absorbed rapidly and is metabolized in the liver.

In general, alkaloids can help improve immune function. Theophylline and its isomers are natural metabolites of caffeine in the human body. As mentioned, cocoa is a major source of this alkaloid.[15]

With in vitro treatment, theophylline reduced free radical production in monocytes by inhibiting phosphodiesterase and more. Theophylline also reduced production of certain leukotrienes.

Looking at in vivo studies, people with chronic obstructive pulmonary disease were treated with theophylline. They showed the ability of theophylline to act as an immunomodulator (affecting function of the immune system) at therapeutic concentrations.

The Last Bite

Theophylline is used in medications to treat breathing conditions like asthma. Current drugs that use theophylline use a synthetic, industrially made form of theophylline that can come with many side effects and a certain level of toxicity. Getting nutrients through whole food is always best. Small amounts of theophylline naturally occur in tea, cocoa, and mate. Theophylline can act as a stimulant, help relax airways, affect immune system function, and more. This phytochemical is an alkaloid but often referred to as a methylxanthine or xanthine.

[1] “Theophylline,” Phytochemicals (Phytochemicals.info), accessed July 15, 2020, https://www.phytochemicals.info/phytochemicals/theophylline.php.

[2] Rafael Franco, Ainhoa Oñatibia-Astibia, and Eva Martínez-Pinilla, “Health Benefits of Methylxanthines in Cacao and Chocolate,” Nutrients (MDPI, October 18, 2013), https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3820066/.

[3] IARC Working Group on the Evaluation of Carcinogenic Risks to Humans, “MATE,” Coffee, Tea, Mate, Methylxanthines and Methylglyoxal. (U.S. National Library of Medicine, January 1, 1991), https://www.ncbi.nlm.nih.gov/books/NBK507022/.

[4] Victoria Boswell-Smith, Domenico Spina, and Clive P Page, “Phosphodiesterase Inhibitors,” NCBI (British Journal of Pharmacology, January 2006), https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1760738/.

[5] Peter J. Barnes, “Theophylline,” ATSJournals (American Journal of Respiratory and Critical Care Medicine, May 3, 2013), https://www.atsjournals.org/doi/full/10.1164/rccm.201302-0388PP.

[6] “Theophylline,” National Center for Biotechnology Information. PubChem Compound Database (U.S. National Library of Medicine), accessed July 15, 2020, https://pubchem.ncbi.nlm.nih.gov/compound/Theophylline.

[7] “Theophylline: Toxicity Data,” National Center for Biotechnology Information. PubChem Compound Database (U.S. National Library of Medicine), accessed July 15, 2020, https://pubchem.ncbi.nlm.nih.gov/compound/Theophylline.

[8] Miles Weinberger and Leslie Hendeles, “Theophylline in Asthma,” The New England Journal of Medicine (The New England Journal of Medicine, May 23, 1996), https://www.nejm.org/doi/full/10.1056/nejm199605233342107.

[9] Aleksa Ristic, “7 Methyl-Xanthines Benefits, Side Effects & Sources,” SelfHacked (SelfHacked, April 16, 2020), https://selfhacked.com/blog/xanthines/.

[10] C. Awortwe et al., “PDF” (Accra, Ghana, May 9, 2014).

[11] IARC Working Group on the Evaluation of Carcinogenic Risks to Humans, “Theophylline,” Coffee, Tea, Mate, Methylxanthines and Methylglyoxal. (International Agency for Research on Cancer, January 1, 1991), https://www.ncbi.nlm.nih.gov/books/NBK507021/.

[12] V. R. Sinija and H. N. Mishra, “Green Tea: Health Benefits,” Taylor & Francis (Journal of Nutritional & Environmental Medicine, July 13, 2009), https://www.tandfonline.com/doi/abs/10.1080/13590840802518785.

[13] Nancy Lowry, “PDF” (Amherst, MA, n.d.).

[14] IARC Working Group on the Evaluation of Carcinogenic Risks to Humans, “MATE,” Coffee, Tea, Mate, Methylxanthines and Methylglyoxal. (U.S. National Library of Medicine, January 1, 1991), https://www.ncbi.nlm.nih.gov/books/NBK507022/.

[15] David S. Senchina et al., “PDF” (Iowa, 2014).