Abstract

Coffee is one of the most widely consumed beverages worldwide. It is usually identified as a stimulant because of a high content of caffeine. However, caffeine is not the only coffee bioactive component. The coffee beverage is in fact a mixture of a number of bioactive compounds such as polyphenols, especially chlorogenic acids (in green beans) and caffeic acid (in roasted coffee beans), alkaloids (caffeine and trigonelline), and the diterpenes (cafestol and kahweol). Extensive research shows that coffee consumption appears to have beneficial effects on human health. Regular coffee intake may protect from many chronic disorders, including cardiovascular disease, type 2 diabetes, obesity, and some types of cancer. Importantly, coffee consumption seems to be also correlated with a decreased risk of developing some neurodegenerative conditions such as Alzheimer’s disease, Parkinson’s disease, and dementia. Regular coffee intake may also reduce the risk of stroke. The mechanism underlying these effects is, however, still poorly understood. This review summarizes the current knowledge on the neuroprotective potential of the main bioactive coffee components, i.e., caffeine, chlorogenic acid, caffeic acid, trigonelline, kahweol, and cafestol. Data from both in vitro and in vivo preclinical experiments, including their potential therapeutic applications, are reviewed and discussed. Epidemiological studies and clinical reports on this matter are also described. Moreover, potential molecular mechanism(s) by which coffee bioactive components may provide neuroprotection are reviewed.

Highlights

  • The genus Coffea L. includes at least 125 species which naturally occur in Tropical and East Africa, Tropical Asia, and Australia and in the Comoros, Madagascar, and the Mascarenes [1]

  • Higher Cmax, Cmin, Cavg, AUC0-24 values as well as the 24-h total excretion concentrations for trigonelline were detected in subjects that drank three cups of espresso coffee per day when compared to volunteers drinking only one cup of espresso coffee with or without two cocoa-based products containing coffee [91]

  • Impairments in the blood–brain barrier as well as changes in the brain vascular system are observed in epilepsy. It has not been determined whether microvessel proliferation and disruption in the blood–brain barrier are the causative factors of seizures or they occur as a consequence of seizures [179,180]

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Summary

Introduction

The genus Coffea L. (family: Rubiaceae, subfamily: Ixoroideae, tribe: Coffeeae) includes at least 125 species which naturally occur in Tropical and East Africa, Tropical Asia, and Australia and in the Comoros, Madagascar, and the Mascarenes [1]. Caffeine fromCthafefesitnoemfriasocmhra.CptAhaidefcfclesyoitnroadembinsiasogcrrhbta.oepAdAid–crplcnyoroiramudbdiasnro[gi4rlybt0oe]f,dArto–hrpmenroiptmuhedaeakr[si4lmpy0l]aa,flsrtlmohimenatpcetehosatneikncseepmn,ltaabrslualmttiinoaantlcesosoontfipcnceaeanr,ftftbieraauilntltiyeoanlsoofpcaarftfieailnlye (4–5 mg/kg) i(s4–o5bsmergv/ekdg)wiisthoibnse3r0v–e1d20wmithinina3ft0e–r1a2d0mmiinnisatrftaetrioandmwiitnhishtraaltfi-olinvews iuthsuhaalllfy-lives usually ranged between 2.5 and 5 h It seems that caffeine absorption is not influenced by age, gender, genetics, undergoing disease, concomitant drugs, or stimulants such as alcohol. In caffeine metabolism were observed during pregnancy or in smoking women taking oral contraceptives [55] Pharmacokinetics of this methylxanthine may be affected by genetic determinants [56], specific diet (grapefruit juice, quercetin, brassica vegetables, apiaceous vegetables, large quantities of vitamin C, curcumin, turmeric) [57,58,59,60,61] and lifestyle (i.e., smoking) [62], environmental factors, diseases ( liver conditions) [63,64] or concurrent drugs (i.e., clozapine, rofecoxib, quinolones, calcium antagonists, and antiarrhythmics) [65,66,67,68]. 0.5–2% of caffeine is excreted in an unchanged form [71]

Chlorogenic Acids
Caffeic Acid
Trigonelline
Kahweol and Cafestol
Neurodegenerative Diseases
Parkinson’s Disease
Ischemic Stroke
Epilepsy
Neuroprotective Effects of Coffee Bioactive Compounds
Neuroprotective Effects of Caffeine
Neuroprotective Effects of Chlorogenic Acid
Neuroprotective Effects of Caffeic Acid
Neuroprotective Effects of Trigonelline
Findings
Neuroprotective Effects of Kahweol and Cafestol

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