Inhibition of Key Digestive Enzymes by Cocoa Extracts and Procyanidins

Gu, Yeyi; Hurst, W. Jeffrey; Stuart, David A.; Lambert, Joshua D.

doi:10.1021/jf200180n

Cited by 150 publications

(129 citation statements)

References 32 publications

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“…Therefore they were mixed type inhibitors of lipase, which means that they were able to bind both free enzyme and an enzyme--substrate complex. The same conclusions were presented by Gu et al [2011], who studied the effect of cocoa extract on lipase activity. However, the authors attributed the inhibitory effect to procyanidins contents only and did not comment the role of theobromine in this process.…”

Section: Studies Of Inhibition Typessupporting

confidence: 76%

Methylxanthine Drugs Are Human Pancreatic Lipase Inhibitors

Wikiera¹,

Mika²,

Żyła³

2012

Pol. J. Food Nutr. Sci.

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Methylxanthines such as caffeine, theobromine and theophylline are intensively consumed as food components by large proportion of human population all over the world. This class of compounds show various biological activities and have been found to act as broad specifi city inhibitors towards numerous enzymes. However, their action on digestive enzymes have not been yet investigated. In this paper we aimed to evaluate the effects of methylxanthines on the human pancreatic lipase activity in vitro. Emulsions of short-and long-chain triglycerides (tributyrin and tripalmitate, respectively) were used as substrates. The concentrations of methylxanthines in the reaction mixtures covered the range between 0.015 mmol/L to 15 mmol/L. We demonstrated that all three tested substances, caffeine, theophylline and theobromine inhibited the hydrolysis of tributyrin and tripalmitate catalysed by human pancreatic lipase in dose-dependent fashion. The highest lipase inhibition ratios during tripalmitate and tributyrin hydrolysis were 25.74% and 79.54% respectively in the presence of caffeine, 29.89% and 62.79% respectively with theophylline and 21.08% and 67.74% respectively in the presence of theobromine. All the tested methylxanthines exert stronger inhibition in the short-chain triglyceride lipolysis comparing to long-chain substrates. Their mechanism of action involves most likely the interaction with enzyme protein but not substrate emulgation. In case of tripalmitate lipolysis all the methylxanthines showed mixed type of inhibition. Interestingly, during tributyrin lipolysis theophylline behaved as classical noncompetitive inhibitor.

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Section: Studies Of Inhibition Typessupporting

confidence: 76%

Methylxanthine Drugs Are Human Pancreatic Lipase Inhibitors

Wikiera¹,

Mika²,

Żyła³

2012

Pol. J. Food Nutr. Sci.

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“…The ability of flavonoids to inhibit lipid digestion and absorption (Gu et al 2011), to reduce fat deposition ; Min et al, 2013;Cherniack, 2011;Faisal et al 2015) and/or to down-regulate the expression of genes involved in lipid metabolism (unpublished own data from current analysis) are proposed mechanisms by which cocoa intake may affect body weight gain. Another possible mechanism is the effects of polyphenols on the gut microbiota composition.…”

Section: Discussionmentioning

confidence: 98%

Prebiotic effects of cocoa fibre on rats

Massot-Cladera

Costabile

Childs

et al. 2015

Journal of Functional Foods

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The impact of cocoa on microbiota composition, its crosstalk with the immune system and the SCFA production, focusing on the involvement of cocoa fibre were investigated Wistar rats were fed for 3-weeks a standard diet, a diet containing 10%-cocoa (C10), cocoa fibre (CF) or inulin (I).Faecal and serum samples were collected before and after the intervention and caecal content and colon sample were collected at the end. Microbiota composition and IgA-coated bacteria and the SCFA content was quantified. The colonic expression of immune-related genes was studied. The CF diet increased Bifidobacterium and Lactobacillus counts, the proportion of IgA-coated bacteria, the SCFA concentrations and the TLR2, TLR5, TLR7 and occludin expression. With the exception on Lactobacillus counts, the I diet modified the other variables in a more modest way than the CF diet. The CF, unlike from the C10 diet, has prebiotic effects and modulates intestinal immune markers.

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“…Distinct mechanisms of action may be involved in the prevention of obesity and insulin resistance vs. the amelioration of existing obesity and insulin resistance 124 . Furthermore, flavanols may improve insulin and blood glucose levels by distinct mechanisms in the acute post-prandial (gut mechanisms such as inhibiting macronutrient digestion/absorption, increased GLP-1 and insulin secretion) 30,120 vs. chronic effects in the fasted state (peripheral tissue mechanisms such as decreased insulin secretion, improved insulin sensitivity, etc.). It should also be noted that, while all three flavanol fractions effectively inhibited hyperinsulinemia (Figure 4.7), only the oligomer-rich fraction effectively improved glucose tolerance compared to the HF diet (Figure 4.6B), inhibited increases in 4 h fasting glucose compared to the LF control (Figure 4.6C), and inhibited the development of insulin resistance (Figure 4.6D).…”

Section: Discussionmentioning

confidence: 99%

Oligomeric Cocoa Procyanidins Possess Enhanced Bioactivity Compared to Monomeric and Polymeric Cocoa Procyanidins for Preventing the Development of Obesity, Insulin Resistance, and Impaired Glucose Tolerance during High-Fat Feeding

Dorenkott

Griffin

Goodrich

et al. 2014

J. Agric. Food Chem.

134

102

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Cocoa is a major source of these flavanols. However, research on the potential anti-obesity and anti-diabetic health benefits of cocoa flavanols is lacking in the literature. Furthermore, the effect that the size of these flavanols has on the extent of its beneficial properties is also unclear. The objective of this study was to evaluate the dietary effects of cocoa flavanols on the onset of obesity, insulin resistance and impaired glucose tolerance and to determine the impact that the size of these compounds has on the magnitude of this effect. Cocoa extract was fractionated into a monomer-, an oligomer-, and a polymer-rich fraction. Six groups (n=9) of C57BL/6J mice were fed either a control low-fat diet, a control high-fat diet, or a high-fat diet supplemented with 25 mg/kg*BW of cocoa extract or one of the three cocoa fractions. After 12 weeks on these diets, the oligomer-rich fraction proved to be most effective in preventing weight gain, fat mass accumulation, elevated fasting blood glucose and impaired glucose tolerance in diet-induced obese mice. This is the first long-term feeding study to examine the relative activities of cocoa constituents on diet-induced obesity and insulin resistance.iii Acknowledgements

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Inhibition of Key Digestive Enzymes by Cocoa Extracts and Procyanidins

Cited by 150 publications

References 32 publications

Methylxanthine Drugs Are Human Pancreatic Lipase Inhibitors

Methylxanthine Drugs Are Human Pancreatic Lipase Inhibitors

Prebiotic effects of cocoa fibre on rats

Oligomeric Cocoa Procyanidins Possess Enhanced Bioactivity Compared to Monomeric and Polymeric Cocoa Procyanidins for Preventing the Development of Obesity, Insulin Resistance, and Impaired Glucose Tolerance during High-Fat Feeding

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