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Review
. 2023 Nov 22;12(2):734-764.
doi: 10.1002/fsn3.3848. eCollection 2024 Feb.

Bioactive compounds in coffee and their role in lowering the risk of major public health consequences: A review

Affiliations
Review

Bioactive compounds in coffee and their role in lowering the risk of major public health consequences: A review

Markos Urugo Makiso et al. Food Sci Nutr. .

Abstract

This article addresses the bioactive components in coffee aroma, their metabolism, and the mechanism of action in lowering the risk of various potential health problems. The main bioactive components involved in the perceived aroma of coffee and its related health benefits are caffeine, chlorogenic acid (CGA), trigonelline, diterpenes, and melanoids. These compounds are involved in various physiological activities. Caffeine has been shown to have anticancer properties, as well as the ability to prevent the onset and progression of hepatocellular carcinoma and to be anti-inflammatory. CGA exhibits antioxidant action and is implicated in gut health, neurodegenerative disease protection, type 2 diabetes, and cardiovascular disease prevention. Furthermore, together with diterpenes, CGA has been linked to anticancer activity. Trigonelline, on the other side, has been found to lower oxidative stress by increasing antioxidant enzyme activity and scavenging reactive oxygen species. It also prevents the formation of kidney stones. Diterpenes and melanoids possess anti-inflammatory and antioxidant properties, respectively. Consuming three to four cups of filtered coffee per day, depending on an individual's physiological condition and health status, has been linked to a lower risk of several degenerative diseases. Despite their health benefits, excessive coffee intake above the recommended daily dosage, calcium and vitamin D deficiency, and unfiltered coffee consumption all increase the risk of potential health concerns. In conclusion, moderate coffee consumption lowers the risk of different noncommunicable diseases.

Keywords: caffeine; chlorogenic acid; coffee aroma; health benefits; trigonelline.

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Conflict of interest statement

The authors declare that they do not have any conflict of interest.

Figures

FIGURE 1
FIGURE 1
A schematic diagram detailing the article search and selection.
FIGURE 2
FIGURE 2
Chemical structure of caffeine and its metabolites (Anastasiadi et al., 2021).
FIGURE 3
FIGURE 3
Chemical structure of chlorogenic acids and its derivatives (Hernandez‐Estrada, 1985).
FIGURE 4
FIGURE 4
Structure of trigonelline and related nicotinic acid metabolites (Ashihara et al., 2015).
FIGURE 5
FIGURE 5
Chemical structure of common lipids in coffee (Silva et al., ; Vandeponseele et al., 2020).
FIGURE 6
FIGURE 6
Schematic representation of melanoid formation due to Maillard reaction (Tamanna & Mahmood, 2015).
FIGURE 7
FIGURE 7
Chemical structure of melanoids (Moreira et al., 2012).
FIGURE 8
FIGURE 8
Chemical structures of adenosine receptor and caffeine.
FIGURE 9
FIGURE 9
Schematic representation of the antagonistic interactions between adenosine A2A and dopamine D2 receptors in striato‐Gpe projection neurons. At the plasma membrane level, stimulation of A2A receptors results in decreased affinity of the dopamine D2 receptor for agonists. At the cytoplasmic level, A2A receptors stimulate, whereas D2 receptors inhibit the production of cAMP. This results in opposite regulation of the state of phosphorylation of DARPP‐32 and downstream target proteins involved in the control of the activity of striato‐Gpe neurons. In the nucleus, the opposite regulation of the cAMP/PKA pathway results in the opposite regulation of CREB phosphorylation and IEG expression. Green and red arrows indicate positive and negative regulations, respectively (Fisone et al., 2004).
FIGURE 10
FIGURE 10
Antioxidant activity mechanism of action of CGA (Rashidi et al., 2022).
FIGURE 11
FIGURE 11
A model of the proposed mechanism of chlorogenic acid (CGA)‐attenuated intestinal inflammation and injury induced by oxidative stress CGA protects the intestinal epithelium against oxidative stress‐induced injury via regulating the phosphatidylinositol‐3‐kinase (PI3K)/protein kinase B (Akt)/nuclear factor erythroid‐derived‐related factor 2 (Nrf2) signaling pathway; CGA attenuates the intestinal inflammation by coregulating the PI3K/Akt/heme oxygenase‐1 (HO‐1) and NF‐kappa‐B inhibitor alpha (Iκ‐Bα)/nuclear factor‐κB (NF‐κB) signaling pathway (Chen et al., 2021).
FIGURE 12
FIGURE 12
Cardiovascular vascular disease prevention mechanism of action of CGA (Li et al., 2020).
FIGURE 13
FIGURE 13
Anticancer effect mechanism of action of CGA (Wang, Pan, et al., ; Wang, Wang, et al., 2022).
FIGURE 14
FIGURE 14
Diagram showing bioactivities and targets of cafestol and kahweol. Cafestol and kahweol raise human serum lipid level and show extensive anti‐inflammatory, anticancer, and potential antidiabetic activities (Ren et al., 2019).

References

    1. Abrankó, L. , & Clifford, M. N. (2017). An unambiguous nomenclature for the acyl‐quinic acids commonly known as chlorogenic acids. Journal of Agricultural and Food Chemistry, 65(18), 3602–3608. 10.1021/acs.jafc.7b00729 - DOI - PubMed
    1. Acikalin, B. , & Sanlier, N. (2021). Coffee and its effects on the immune system. Trends in Food Science and Technology, 114(June), 625–632. 10.1016/j.tifs.2021.06.023 - DOI
    1. Addicott, M. A. , Yang, L. L. , Peiffer, A. M. , Burnett, L. R. , Burdette, J. H. , Chen, M. Y. , Hayasaka, S. , Kraft, R. A. , Maldjian, J. A. , & Laurienti, P. J. (2009). The effect of daily caffeine use on cerebral blood flow: How much caffeine can we tolerate? Human Brain Mapping, 30(10), 3102–3114. 10.1002/hbm.20732 - DOI - PMC - PubMed
    1. Adronikos, B. S. (2019). Coffee a worldwide trend with health benefits. Acta Scientific Nutrition Health, 3(3), 70–73.
    1. Al‐Ansari, M. M. , & Aboussekhra, A. (2014). Caffeine mediates sustained inactivation of breast cancer‐associated myofibroblasts via up‐regulation of tumor suppressor genes. PLoS One, 9(3), e90907. 10.1371/journal.pone.0090907 - DOI - PMC - PubMed