CAFFEINE AND OTHER PHARMACOLOGICALLY ACTIVE INGREDIENTS CONTAINED IN COFFEE BEANS
DOI:
https://doi.org/10.56782/pps.11Keywords:
kawa, kofeina, trygonelina, kwas chlorogenowy, kafestol, kahweolAbstract
Coffee (a decoction of coffee seeds), which is one of the most frequently consumed beverages, contains numerous substances with various pharmacological effects and a diverse chemical structure. The main ones include caffeine (purine alkaloids), chlorogenic acid (phenolic acids), kahweol and cafestol (diterpenes) and trigonelline (pyridine alkaloids). This article presents a review of the scientific literature on the properties of active substances contained in coffee beans, with particular emphasis on the pharmacological action and potential side effects of its main component — caffeine.
Downloads
References
Ogita S., Uefuji H. et al., Metabolic engineering of caffeine production, Plant Biotechnology, 2005, 22, 461-468. DOI: https://doi.org/10.5511/plantbiotechnology.22.461
Sereshti H., Samadi S., A rapid and simple determination of caffeine in teas, coffees and eight beverages, Food Chemistry, 2014, 158, 8-13. DOI: https://doi.org/10.1016/j.foodchem.2014.02.095
Waldvogel S.R., Caffeine — A drug with a surprise, Angewandte Chemie — International Edition, 2003, 42, 604-605. DOI: https://doi.org/10.1002/anie.200390173
Siwek R., Witkowska-Banaszczak E., Szumański M., Kofeina w lekach i suplementach diety — znaczenie w lecznictwie, Farmacja Polska, 2013, 69(9), 541-549.
Lovett-Doust J., Plant strategies, vegetation processes, and ecosystem properties, 2002. DOI: https://doi.org/10.1658/1100-9233(2002)013[0294:PSVPAE]2.0.CO;2
Vignoli J.A., Viegas M.C. et al., Roasting process affects differently the bioactive compounds and the antioxidant activity of arabica and robusta coffees, Food Research International, 2014, 61, 279-285. DOI: https://doi.org/10.1016/j.foodres.2013.06.006
Dąbrowska-Molenda M., Szwedziak K., Zabłudowska Ż., Analiza zawartości kofeiny w wybranych rodzajach kawy, Postępy Techniki Przetwórstwa Spożywczego, 2019, 68-71.
Ameca G.M., Cerrilla M.E.O. et al., Chemical composition and antioxidant capacity of coffee pulp, Ciencia e Agrotecnologia, 2018, 42, 307-313. DOI: https://doi.org/10.1590/1413-70542018423000818
Farah A., Coffee Constituents. Coffee: emerging health effects and disease prevention, 2012, 21-58. DOI: https://doi.org/10.1002/9781119949893.ch2
Gross G., Jaccaud E. et al., Analysis of the content of the diterpenes cafestol and kahweol in coffee brews, Food and Chemical Toxicology, 1997, 35, 547-554. DOI: https://doi.org/10.1016/S0278-6915(96)00123-8
Tajik N., Tajik M., et al., The potential effects of chlorogenic acid, the main phenolic components in coffee, on health: a comprehensive review of the literature, European Journal of Nutrition, 2017, 56, 2215-2244. DOI: https://doi.org/10.1007/s00394-017-1379-1
Mohamadi N., Sharififar F. et al., A review on biosynthesis, analytical techniques, and pharmacological activities of trigonelline as a plant alkaloid, Journal of Dietary Supplements, 2018, 15, 207-222. DOI: https://doi.org/10.1080/19390211.2017.1329244
Riedel A., Lang R. et al., Structure-dependent effects of pyridine derivatives on mechanisms of intestinal fatty acid uptake: Regulation of nicotinic acid receptor and fatty acid transporter expression, Journal of Nutritional Biochemistry, 2014, 25, 750-777. DOI: https://doi.org/10.1016/j.jnutbio.2014.03.002
Sharma L., Lone N.A. et al., Trigonelline prevents high cholesterol and high fat diet induced hepatic lipid accumulation and lipo-toxicity in C57BL/6J mice, via restoration of hepatic autophagy, Food and Chemical Toxicology, 2018, 121, 283-296. DOI: https://doi.org/10.1016/j.fct.2018.09.011
Yoshinari O., Sato H. et al., Anti-diabetic effects of pumpkin and its components, trigonelline and nicotinic acid, on goto-kakizaki rats, Bioscience, Biotechnology and Biochemistry, 2009, 73, 1033-1041. DOI: https://doi.org/10.1271/bbb.80805
Rendón M.Y., dos Santos Scholz M.B. et al., Physical characteristics of the paper filter and low cafestol content filter coffee brews, Food Research International, 2018, 108, 280-285. DOI: https://doi.org/10.1016/j.foodres.2018.03.041
Urgert .R., Essed N. et al., Separate effects of the coffee diterpenes cafestol and kahweol on serum lipids and liver aminotransferases, American Journal of Clinical Nutrition, 1997, 65, 519-524. DOI: https://doi.org/10.1093/ajcn/65.2.519
Post S.M., De Wit E.C.M. et al., Cafestol, the cholesterol-raising factor in boiled coffee, suppresses bile acid synthesis by downregulation of cholesterol 7α-hydroxylase and sterol 27-hydroxylase in rat hepatocytes, Arteriosclerosis, Thrombosis, and Vascular Biology, 1997, 17, 3064-3070. DOI: https://doi.org/10.1161/01.ATV.17.11.3064
Lima C.S., Spindola D.G. et al. Cafestol, a diterpene molecule found in coffee, induces leukemia cell death, Biomedicine and Pharmacotherapy, 2017, 92, 1045-1054. DOI: https://doi.org/10.1016/j.biopha.2017.05.109
Mellbye F.B., Jeppesen P.B. et al., Cafestol, a bioactive substance in coffee, has antidiabetic properties in KKAy mice, Journal of Natural Products, 2017, 80, 2353-2259. DOI: https://doi.org/10.1021/acs.jnatprod.7b00395
Shokouh P., Jeppesen P.B. et al., A combination of coffee compounds shows insulin-sensitizing and hepatoprotective effects in a rat model of diet-induced metabolic syndrome, Nutrients, 2018; 10, 1-15. DOI: https://doi.org/10.3390/nu10010006
van Cruchten S.T.J., Cafestol : a multi-faced compound kinetics and metabolic effects of cafestol in mice, PhD Thesis, 2010.
Baek J.H., Kim N.J. et al., Kahweol inhibits lipid accumulation and induces glucose-uptake through activation of AMP-activated protein kinase (AMPK), BMB Reports, 2017, 50, 566-571. DOI: https://doi.org/10.5483/BMBRep.2017.50.11.031
Lee K.J., Jeong H.G., Protective effects of kahweol and cafestol against hydrogen peroxide-induced oxidative stress and DNA damage, Toxicology Letters, 2007, 173, 80-87. DOI: https://doi.org/10.1016/j.toxlet.2007.06.008
Oh S.H., Hwang Y.P. et al. Kahweol inhibits proliferation and induces apoptosis by suppressing fatty acid synthase in HER2-overexpressing cancer cells, Food and Chemical Toxicology, 2018, 121, 326-335. DOI: https://doi.org/10.1016/j.fct.2018.09.008
Yoon J.J., Danesh-Meyer H.V., Caffeine and the eye, Survey of Ophthalmology, 2019, 64, 334-344. DOI: https://doi.org/10.1016/j.survophthal.2018.10.005
Echeverri D., Montes F.R. et al., Caffeine’s vascular mechanisms of action, International Journal of Vascular Medicine, 2010, Article ID 834060. DOI: https://doi.org/10.1155/2010/834060
Schuster J., Mitchell E.S., More than just caffeine: psychopharmacology of methylxanthine interactions with plantderived phytochemicals, Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2019, 89, 263-274. DOI: https://doi.org/10.1016/j.pnpbp.2018.09.005
Sheriffdeen M.M., Alehaideb Z.I. et al., Caffeine/Angelica dahurica and caffeine/Salvia miltiorrhiza metabolic inhibition in humans: In vitro and in vivo studies. Complementary Therapies in Medicine, 2019, 46, 87-94. DOI: https://doi.org/10.1016/j.ctim.2019.07.024
Voskoboinik A., Koh Y. et al., Cardiovascular effects of caffeinated beverages, Trends in Cardiovascular Medicine, 2019, 29, 345-350. DOI: https://doi.org/10.1016/j.tcm.2018.09.019
Voskoboinik A., Kalman J.M. et al., Caffeine and Arrhythmias: Time to Grind the Data, JACC: Clinical Electrophysiology 2018, 4, 425-432. DOI: https://doi.org/10.1016/j.jacep.2018.01.012
Strubelt O., Diederich K.W., Experimental treatment of the acute cardiovascular toxicity of caffeine, Journal of Toxicology — Clinical Toxicology, 1999, 37, 29-33. DOI: https://doi.org/10.1081/CLT-100102405
Abdelfattah R., Kamran H. et al., Does caffeine consumption increase the risk of new-onset atrial fibrillation?, Cardiology (Switzerland), 2018, 140, 106-114. DOI: https://doi.org/10.1159/000489843
Zuchinali P., Ribeiro P.A.B. et al., Effect of caffeine on ventricular arrhythmia: A systematic review and meta-analysis of experimental and clinical studies, Europace, 2016, 18, 257-266. DOI: https://doi.org/10.1093/europace/euv261
Richardson T., Baker J. et al., Randomized control trial investigating the influence of coffee on heart rate variability in patients with STsegment elevation myocardial infarction, Qjm, 2009, 102, 555-561. DOI: https://doi.org/10.1093/qjmed/hcp072
Akash M.S.H., Rehman K. et al., Effects of coffee on type 2 diabetes mellitus, Nutrition 2014, 30, 755-763. DOI: https://doi.org/10.1016/j.nut.2013.11.020
Lavie C.J., DiNicolantonio J.J. et al., Editorial commentary: Coffee, tea, and cardiovascular morbidity and mortality, Trends in Cardiovascular Medicine, 2019, 29, 351-352. DOI: https://doi.org/10.1016/j.tcm.2018.11.016
Akash M.S.H., Rehman K. et al., Sustained delivery of IL-1Ra from PF127-gel reduces hyperglycemia in diabetic GK-rats, PLoS ONE, 2013, 8, 1-12. DOI: https://doi.org/10.1371/journal.pone.0055925
Trexler E.T., Smith-Ryan A.E. et al., International society of sports nutrition position stand: Beta-Alanine., Journal of the International Society of Sports Nutrition, 2015, 12, 1-16. DOI: https://doi.org/10.1186/s12970-015-0090-y
Yamaji T., Mizoue T. et al., Coffee consumption and glucose tolerance status in middle-aged Japanese men, Diabetologia, 2004, 47, 2145-2151. DOI: https://doi.org/10.1007/s00125-004-1590-5
Wu T., Willett W.C. et al., Caffeinated coffee, decaffeinated coffee, and caffeine in relation to plasma C-peptide levels, a marker of insulin secretion, in U.S. women, Diabetes Care, 2005, 28, 1390-1396. DOI: https://doi.org/10.2337/diacare.28.6.1390
Smith B., Wingard D.L. et al., Does coffee consumption reduce the risk of type 2 diabetes in individuals with impaired glucose?, Diabetes Care, 2006, 29, 2385-2390. DOI: https://doi.org/10.2337/dc06-1084
van Dam R.M., Feskens E.J.M., Coffee consumption and risk of type 2 diabetes mellitus, Lancet, 2002, 360(9344), 1477-1478. DOI: https://doi.org/10.1016/S0140-6736(02)11436-X
Tuomilehto J., Hu G. et al.,Coffee consumption and risk of type 2 diabetes mellitus among middle-aged Finnish men and women, JAMA, 2004, 291, 1213-1239. DOI: https://doi.org/10.1001/jama.291.10.1213
Agardh E.E., Carlsson S. et al., Coffee consumption, type 2 diabetes and impaired glucose tolerance in Swedish men and women, Journal of Internal Medicine, 2004, 255, 645-652. DOI: https://doi.org/10.1111/j.1365-2796.2004.01331.x
Muley A., Muley P. et al., Coffee to reduce risk of type 2 diabetes? : A systematic review, Current Diabetes Reviews, 2012, 8, 162-168. DOI: https://doi.org/10.2174/157339912800564016
Shearer J., Farah A. et al., Quinides of roasted coffee enhance insulin action in conscious rats, The Journal of Nutrition, 2003, 133, 3529-3532. DOI: https://doi.org/10.1093/jn/133.11.3529
Santos R.M.M., Lima D.R.A., Coffee consumption, obesity and type 2 diabetes: a mini-review, European Journal of Nutrition, 2016, 55, 1345-1358. DOI: https://doi.org/10.1007/s00394-016-1206-0
Choi B.K., Park S.B. et al., Green coffee bean extract improves obesity by decreasing body fat in high-fat diet-induced obese mice, Asian Pacific Journal of Tropical Medicine, 2016, 9, 635-643. DOI: https://doi.org/10.1016/j.apjtm.2016.05.017
Farias-Pereira R., Oshiro J. et al., Green coffee bean extract and 5-O-caffeoylquinic acid regulate fat metabolism in Caenorhabditis elegans, Journal of Functional Foods, 2018, 48, 586-593. DOI: https://doi.org/10.1016/j.jff.2018.07.049
Huang K., Liang X. et al., 5-Caffeoylquinic acid decreases dietinduced obesity in rats by modulating PPARα and LXRα transcription, Journal of the Science of Food and Agriculture, 2015, 95, 1903-1910. DOI: https://doi.org/10.1002/jsfa.6896
Ong K.W., Hsu A. et al., Anti-diabetic and anti-lipidemic effects of chlorogenic acid are mediated by ampk activation, Biochemical Pharmacology, 2013, 85, 1341-1351. DOI: https://doi.org/10.1016/j.bcp.2013.02.008
Jia H., Aw W. et al. Coffee intake mitigated inflammation and obesity-induced insulin resistance in skeletal muscle of high-fat dietinduced obese mice, Genes and Nutrition, 2014, 9, 389-395. DOI: https://doi.org/10.1007/s12263-014-0389-3
Murase T., Misawa K. et al., Coffee polyphenols suppress dietinduced body fat accumulation by downregulating SREBP-1c and related molecules in C57BL/6J mice, American Journal of Physiology — Endocrinology and Metabolism, 2011, 300, 122-133. DOI: https://doi.org/10.1152/ajpendo.00441.2010
Sudeep H.V., Venkatakrishna K. et. al., Biomechanism of chlorogenic acid complex mediated plasma free fatty acid metabolism in rat liver, BMC Complementary and Alternative Medicine, 2016, 16, 4-8. DOI: https://doi.org/10.1186/s12906-016-1258-y
Zheng G., Qiu Y. et al., Chlorogenic acid and caffeine in combination inhibit fat accumulation by regulating hepatic lipid metabolismrelated enzymes in mice, British Journal of Nutrition, 2014, 112, 1034-1040. DOI: https://doi.org/10.1017/S0007114514001652
Proença A.R.G., Sertié R.A.L. et al. New concepts in white adipose tissue physiology, Brazilian Journal of Medical and Biological Research, 2014, 47, 192-205. DOI: https://doi.org/10.1590/1414-431X20132911
Wang Z., Lam K.L. et al., Chlorogenic acid alleviates obesity and modulates gut microbiota in high-fat-fed mice, Food Science and Nutrition, 2019, 7, 579-588. DOI: https://doi.org/10.1002/fsn3.868
Egawa T., Hamada T. et al. Caffeine activates preferentially α1-isoform of 5′AMP-activated protein kinase in rat skeletal muscle, Acta Physiologica, 2011, 201, 227-238. DOI: https://doi.org/10.1111/j.1748-1716.2010.02169.x
Mathew T.S., Ferris R.K. et al., Caffeine promotes autophagy in skeletal muscle cells by increasing the calcium-dependent activation of AMP-activated protein kinase, Biochemical and Biophysical Research Communications, 2014, 453, 411-418. DOI: https://doi.org/10.1016/j.bbrc.2014.09.094
Ong K.W., Hsu A. et al., Chlorogenic acid stimulates glucose transport in skeletal muscle via AMPK activation: A contributor to the beneficial effects of coffee on diabetes, PLoS ONE 2012, 7, e32718. DOI: https://doi.org/10.1371/journal.pone.0032718
Zhang S.J., Li Y.F. et al., Caffeine ameliorates high energy dietinduced hepatic steatosis: Sirtuin 3 acts as a bridge in the lipid metabolism pathway, Food and Function, 2015, 6, 2578-2587. DOI: https://doi.org/10.1039/C5FO00247H
Zheng X., Dai W. et al., Caffeine reduces hepatic lipid accumulation through regulation of lipogenesis and ER stress in zebrafish larvae, Journal of Biomedical Science, 2015, 22, 1-12. DOI: https://doi.org/10.1186/s12929-015-0206-3
Ma Y., Gao M. et al., Chlorogenic acid improves high fat diet-induced hepatic steatosis and insulin resistance in mice, Pharmaceutical Research, 2015, 32, 1200-1209. DOI: https://doi.org/10.1007/s11095-014-1526-9
Ontawong A., Boonphang O. et al., Hepatoprotective effect of coffee pulp aqueous extract combined with simvastatin against hepatic steatosis in high-fat diet-induced obese rats, Journal of Functional Foods, 2019, 54, 568-577. DOI: https://doi.org/10.1016/j.jff.2019.02.011
Schnuck J.K., Gould L.M. et al., Metabolic effects of physiological levels of caffeine in myotubes, Journal of Physiology and Biochemistry, 2018, 74, 35-45. DOI: https://doi.org/10.1007/s13105-017-0601-1
Ontawong A., Duangjai A. et al., Lipid-lowering effects of Coffea arabica pulp aqueous extract in Caco-2 cells and hypercholesterolemic rats, Phytomedicine, 2019, 52, 187-197. DOI: https://doi.org/10.1016/j.phymed.2018.06.021
Flanagan J., Bily A. et al., Lipolytic activity of svetol®, a decaffeinated green coffee bean extract, Phytotherapy Research, 2014, 28, 946-948. DOI: https://doi.org/10.1002/ptr.5085
Vandenberghe C., St-Pierre V. et al., Caffeine intake increases plasma ketones: An acute metabolic study in humans, Canadian Journal of Physiology and Pharmacology, 2017, 95, 455-458. DOI: https://doi.org/10.1139/cjpp-2016-0338
Carrageta D.F., Dias T.R. et al., Anti-obesity potential of natural methylxanthines, Journal of Functional Foods, 2018, 43, 84-94. DOI: https://doi.org/10.1016/j.jff.2018.02.001
Qian J., Zhang Y. et al. Caffeine consumption during early pregnancy impairs oviductal embryo transport, embryonic development and uterine receptivity in mice, Biology of Reproduction, 2018,99, 1266-1275. DOI: https://doi.org/10.1093/biolre/ioy155
Qian J., Chen Q. et al., Impacts of caffeine during pregnancy, Trends in Endocrinology and Metabolism 2019, 31, 218-227. DOI: https://doi.org/10.1016/j.tem.2019.11.004
Silva C.G., Métin C. et al., Adenosine receptor antagonists including caffeine alter fetal brain development in mice., Science Translational Medicine, 2013, 5, 104-116. DOI: https://doi.org/10.1126/scitranslmed.3006258
Fazeli W., Zappettini S. et al. Early-life exposure to caffeine affects the construction and activity of cortical networks in mice, Experimanetal Neurology, 2017, 295, 88-103. DOI: https://doi.org/10.1016/j.expneurol.2017.05.013
Zappettini S., Faivre E.et al., Caffeine consumption during pregnancy accelerates the development of cognitive deficits in offspring in a model of tauopathy, Frontiers in Cellular Neuroscience, 2019, 13, Article No 438. DOI: https://doi.org/10.3389/fncel.2019.00438
Galéra C., Bernard J.Y. et al. Prenatal caffeine exposure and child IQ at age 5.5 years: The EDEN — Mother-Child Cohort, Biological Psychiatry ,2016, 80, 720-726. DOI: https://doi.org/10.1016/j.biopsych.2015.08.034
Ward R.M., Bates B.A., et al., The transfer of drugs and other chemicals into human milk, Pediatrics 2001, 108, 776-789. DOI: https://doi.org/10.1542/peds.108.3.776
EFSA Journal, Scientific opinion on the safety of caffeine, 2015.
Rudolph T., Knudsen K., A case of fatal caffeine poisoning, Acta Anaesthesiologica Scandinavica, 2010, 54, 521-523. DOI: https://doi.org/10.1111/j.1399-6576.2009.02201.x
Kato Y., Kuriyama A.et al., Extracorporeal membrane oxygenation for hypokalemia and refractory ventricular fibrillation associated with caffeine intoxication, Journal of Emergency Medicine, 2019, 5, 1-4. DOI: https://doi.org/10.1016/j.jemermed.2019.09.023
Juliano L.M., Griffiths R.R., A critical review of caffeine withdrawal: Empirical validation of symptoms and signs, incidence, severity, and associated features, Psychopharmacology, 2004, 176, 1-29. DOI: https://doi.org/10.1007/s00213-004-2000-x
Lara D.R., Caffeine, mental health, and psychiatric disorders, Journal of Alzheimer’s Disease, 2010, 20, 1-4. DOI: https://doi.org/10.3233/JAD-2010-1378
Grant S.S., Magruder K.P. et al., Controlling for caffeine in cardiovascular research: A critical review, International Journal of Psychophysiology, 2018, 133, 193-201. DOI: https://doi.org/10.1016/j.ijpsycho.2018.07.001
Alstadhaug K.B., Andreou A.P., Caffeine and primary (migraine) headaches — friend or foe?, Frontiers in Neurology, 2019, 10, 1-13. DOI: https://doi.org/10.3389/fneur.2019.01275
Lane J.D., Effects of brief caffeinated-beverage deprivation on mood, symptoms, and psychomotor performance, Pharmacology Biochemistry and Behavior, 1997, 58, 203-208. DOI: https://doi.org/10.1016/S0091-3057(97)00007-5
Downloads
Published
Issue
Section
License

This work is licensed under a Creative Commons Attribution 4.0 International License.
For all articles published in Prospects in Pharmaceutical Sciences copyright is retained by the authors. The journal publishes articles in the Open Access policy, within the CC BY 4.0 licence.
This is a human-readable summary of (and not a substitute for) the license. Disclaimer.
You are free to:
Share — copy and redistribute the material in any medium or format
Adapt — remix, transform, and build upon the material for any purpose, even commercially.
The licensor cannot revoke these freedoms as long as you follow the license terms.
Under the following terms:
Attribution — You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
No additional restrictions — You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits.
Notices:
You do not have to comply with the license for elements of the material in the public domain or where your use is permitted by an applicable exception or limitation.
No warranties are given. The license may not give you all of the permissions necessary for your intended use. For example, other rights such as publicity, privacy, or moral rights may limit how you use the material.