Abstract
The inhibitory activity and binding characteristics of caffeic acid, p-coumaric acid, quercetin and capsaicin, four phenolic compounds found in hot pepper, against porcine pancreatic lipase activity were studied and compared to hot pepper extract. Quercetin was the strongest inhibitor (IC50=(6.1±2.4) µM), followed by p-coumaric acid ((170.2±20.6) µM) and caffeic acid ((401.5±32.1) µM), while capsaicin and a hot pepper extract had very low inhibitory activity. All polyphenolic compounds showed a mixed-type inhibition. Fluorescence spectroscopy studies showed that polyphenolic compounds had the ability to quench the intrinsic fluorescence of pancreatic lipase by a static mechanism. The sequence of Stern-Volmer constant was quercetin, followed by caffeic and p-coumaric acids. Molecular docking studies showed that caffeic acid, quercetin and p-coumaric acid bound near the active site, while capsaicin bound far away from the active site. Hydrogen bonds and π-stacking hydrophobic interactions are the main pancreatic lipase-polyphenolic compound interactions observed.
Highlights
Obesity is a global public health concern that has been described as a risk factor for diseases such as cardiovascular, hypertension, type II diabetes, and some forms of cancer [1]
The effect of four compounds: caffeic acid, p-coumaric acid, quercetin and capsaicin (Fig. 1), commonly found in hot pepper, and the hot pepper extract, on the activity of pancreatic lipase were monitored at saturation conditions, using 62.1 μM pNPL
We found that only quercetin had a higher content than its IC50 value, whereas phenolic acids had lower content than their IC50 values
Summary
Obesity is a global public health concern that has been described as a risk factor for diseases such as cardiovascular, hypertension, type II diabetes, and some forms of cancer [1]. Several strategies have been developed to overcome this problem, among them the use of drugs and surgeries, or most frequently changes in alimentary habits These changes include diets low in caloric intake, and inclusion of foods rich in bioactive compounds that exert specific beneficial effects, such as polyphenolic compounds. Several mechanisms may explain the anti-obesity actions of polyphenolic compounds, including the interaction and inhibition of digestive enzymes like pancreatic. Quercetin has been reported as one of the best pancreatic lipase inhibitors, while phenolic acids have shown low inhibitory activity [1,10]. Polyphenolic compounds extracted from hot peppers are recognized for their antioxidant activity [13], and anti-obesity properties, related to an increase in energy expenditure [14]; no information about its possible inhibitory activity against pancreatic lipase has been reported. In the case of phenolic acids such as caffeic acid, p-coumaric acid and capsaicin, as far as we know there are no reports describing the mechanism of their inhibition of pancreatic lipase
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