Alkaloids are vitally important ingredients for energy drinks; research continually discloses news about the mechanisms for caffeine in particular and other related substances for providing usable energy. One of those ‘new’ related ingredients is theacrine which has excited interest in recent years.

Caffeine is an extraordinary ergogenic ingredient for maximal endurance exercise as well as high-intensity exercise. The continuing interest in caffeine for sports related studies has now moved onto its role in stimulating the central nervous system (CNS), for improving alertness especially during sleep deprivation and helping with performance during extreme exercise.

The latest research looks at dosages of between 3 and 6 mg of caffeine per kg body weight which enhances sports performance, and it has a greater ergogenic effect when consumed in its crystalline state as opposed to just being found in coffee. A recent review has looked at coffee-based, pre-workout shots as the preferred means of obtaining caffeine for athletes (Ganio et al., 2009).

A number of research reports that have been subjected to meta-analysis describe how coffee that provides between 3 to 8.1 mg/kg bodyweight of caffeine can reduce feelings of perceived exertion and improve endurance performance during time-to-exhaustion trials (Doherty and Smith, 2005), and influence body lipid distribution (Cai et al., 2012). In addition, more recent research found low doses of caffeine (<3mg/kg body weight, or about 200 mg) can also improve subjective feelings like vigilance, alertness, mood, and cognitive processes during and after exercise, with few side-effects (Ganio et al., 2009; Warren et al., 2010). The need for an ingredient which does not trigger heart problems or stroke is a major factor for many exercising, especially as they enter later life.

However, caffeine isn’t the only ingredient on the market that improves feelings of alertness. A purine alkaloid attracting considerable research interest is theacrine (1,3,7,9-tetramethyluric acid). Theacrine is found in coffee plants too, as well as fruits and an unusual Chinese tea called kucha (Camellia assamica var. kucha)  and in the chocolate analog, cupuaçu (Theobroma grandiflorum).  The chemical structure is similar to other methylxanthines but it is probably synthesised from caffeine in a three way step with 1,3,7-methyluric acid as an intermediate (Zheng et al., 2002). It appears to inhibit adenosine, preventing dopamine from binding as caffeine does. It also stimulates the dopamine pathway.

Early data shows that theacrine when ingested in doses of about 2.8 to 3.2 mg/kg (~200mg), improves feelings of energy, focus, and mood, while reducing fatigue (Kuhman et al., 2015). Unlike caffeine, theacrine isn’t habit-forming and technically is not classed as a stimulant. When combined with caffeine, the optimal dose is closer to ~0.75 to 2 mg/kg or about ~50mg to 125mg.

One study has found that theacrine in humans does not alter heart rate, blood pressure or any blood measures associated with clinical safety, yet it lowers low-density lipoprotein (LDL) and total cholesterol. It may be because of the high polyphenol content. It has no effect on body composition. There is also another randomised double-blind crossover study looking at the effect of 200 mg of theacrine on healthy individuals which has led to significant improvements in subjective measures of energy, reduced fatigue, and improvement across some indices of mental performance. Additionally, in a subset of six subjects, a 200mg dose, open-label, repeated-dose study over a seven-day period improved subjective measures of energy, fatigue, concentration, anxiety, motivation to exercise and libido (Habowski et al., 2014; Ziegenfuss et al., 2016).

Theacrine appears to be a novel innovation for improving the function of the CNS and energy metabolism, without the more disconcerting side effects associated with caffeine. It could be a viable substitute in formulation for caffeine, which is avoided by some consumers avoid due to side effects that include energy crashes, raised heart rate and hypertension, and some of the habit-forming aspects. There is a need for non-caffeinated solutions especially for sports enthusiasts to take their game to the next level.

References

Cai, L., Ma, D., Zhang, Y., Liu, Z., & Wang, P. (2012). The effect of coffee consumption on serum lipids: a meta-analysis of randomized controlled trials. Eur. J. Clin. Nutr., 66(8), pp. 872-877.

Doherty, M., & Smith, P. M. (2005). Effects of caffeine ingestion on rating of perceived exertion during and after exercise: a meta‐analysis. Scand. J Med. Sci. Sports. 15(2), pp. 69-78

Ganio, M. S., Klau, J. F., Casa, D. J., Armstrong, L. E., & Maresh, C. M. (2009). Effect of caffeine on sport-specific endurance performance: a systematic review. J. Strength & Conditioning Research, 23(1), pp. 315-324

Habowski, S.M., Sandrock, J. E., Kedia, A.W., Ziegenfuss, T.N. (2014) The effects of Teacrine™, a nature-identical purine alkaloid, on subjective measures of cognitive function, psychometric and hemodynamic indices in healthy humans: a randomized, double-blinded crossover pilot trial. J. International Society of Sports Nutrition, 11,(1), P49

Kuhman, D. J., Joyner, K. J., & Bloomer, R. J. (2015). Cognitive performance and mood following ingestion of a theacrine-containing dietary supplement, caffeine, or placebo by young men and women. Nutrients, 7(11), pp. 9618-9632.

Warren, G. L., Park, N. D., Maresca, R. D., McKibans, K. I., & Millard-Stafford, M. L. (2010). Effect of caffeine ingestion on muscular strength and endurance: a meta-analysis. Med. Sci. Sports Exerc., 42(7), pp. 1375-87.

Zheng, X. Q., Ye, C. X., Kato, M., Crozier, A., & Ashihara, H. (2002). Theacrine (1, 3, 7, 9-tetramethyluric acid) synthesis in leaves of a Chinese tea, kucha (Camellia assamica var. kucha). Phytochemistry, 60(2), pp. 129-134

Ziegenfuss, T. N., Habowski, S. M., Sandrock, J. E., Kedia, A. W., Kerksick, C. M., & Lopez, H. L. (2016). A Two-Part Approach to Examine the Effects of Theacrine (TeaCrine®) Supplementation on Oxygen Consumption, Hemodynamic Responses, and Subjective Measures of Cognitive and Psychometric Parameters. J. Dietary Supplements, pp. 1-15.