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Methylxanthines and Human Health: Epidemiological and Experimental Evidence

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Methylxanthines

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 200))

Abstract

When considering methylxanthines and human health, it must be recognized that in many countries most caffeine is consumed as coffee. This is further confounded by the fact that coffee contains many bioactive substances in addition to caffeine; it is rich in phenols (quinides, chlorogenic acid, and lactones) and also has diterpenes (fatty acid esters), potassium, niacin, magnesium, and the vitamin B3 precursor trigonelline. There is a paradox as consumption of either caffeine or caffeinated coffee results in a marked insulin resistance and yet habitual coffee consumption has repeatedly been reported to markedly reduce the risk for type 2 diabetes. There is strong evidence that caffeine reduces insulin sensitivity in skeletal muscle and this may be due to a combination of direct antagonism of A1 receptors and indirectly β-adrenergic stimulation as a result of increased sympathetic activity. Caffeine may also induce reduced hepatic glucose output. With the exception of bone mineral, there is little evidence that caffeine impacts negatively on other health issues. Coffee does not increase the risk of cardiovascular diseases or cancers and there is some evidence suggesting a positive relationship for the former and for some cancers, particularly hepatic cancer.

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Abbreviations

AUC:

Area under the curve

cAMP:

Cyclic AMP

CGA:

Chlorogenic acid

CNS:

Central nervous system

CVD:

Cardiovascular disease

CYP1A2:

Cytochrome P450 1A2

FFA:

Free fatty acid

GIP:

Glucose-dependent insulinotropic polypeptide

GLP-1:

Glucagon-like peptide-1

ISI:

Insulin sensitivity index

OGTT:

Oral glucose tolerance test

SNS:

Sympathetic nervous system

T2D:

Type 2 diabetes

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Acknowledgements

The work by the authors was supported by the Natural Science and Engineering Research Council of Canada (NSERC). M.-S.B. received an Ontario Graduate Scholarship.

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  1. Department of Human Health and Nutritional Sciences, University of Guelph, 50 Stone Road East, Guelph, ON, Canada, N1G 2W1

    Marie-Soleil Beaudoin & Terry E. Graham

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Correspondence to Terry E. Graham .

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Beaudoin, MS., Graham, T.E. (2011). Methylxanthines and Human Health: Epidemiological and Experimental Evidence. In: Methylxanthines. Handbook of Experimental Pharmacology, vol 200. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-13443-2_21

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