Original scientific paper

https://doi.org/10.17113/ftb.55.04.17.5138

In vitro Inhibition of Pancreatic Lipase by Polyphenols: A Kinetic, Fluorescence Spectroscopy and Molecular Docking Study

Alejandra I. Martinez-Gonzalez ; Department of Chemical Biological Sciences, Institute for Biomedical Sciences, Autonomous University of Juarez City, 1210 Plutarco Elias Calles Ave., MX-32310 Juarez, Chihuahua, Mexico
Emilio Alvarez-Parrilla orcid.org/0000-0002-6162-8139 ; Department of Chemical Biological Sciences, Institute for Biomedical Sciences, Autonomous University of Juarez City, 1210 Plutarco Elias Calles Ave., MX-32310 Juarez, Chihuahua, Mexico
Ángel G. Díaz-Sánchez ; Department of Chemical Biological Sciences, Institute for Biomedical Sciences, Autonomous University of Juarez City, 1210 Plutarco Elias Calles Ave., MX-32310 Juarez, Chihuahua, Mexico
Laura A. de la Rosa ; Department of Chemical Biological Sciences, Institute for Biomedical Sciences, Autonomous University of Juarez City, 1210 Plutarco Elias Calles Ave., MX-32310 Juarez, Chihuahua, Mexico
José A. Núñez-Gastélum ; Department of Chemical Biological Sciences, Institute for Biomedical Sciences, Autonomous University of Juarez City, 1210 Plutarco Elias Calles Ave., MX-32310 Juarez, Chihuahua, Mexico
Alma A. Vazquez-Flores ; Department of Chemical Biological Sciences, Institute for Biomedical Sciences, Autonomous University of Juarez City, 1210 Plutarco Elias Calles Ave., MX-32310 Juarez, Chihuahua, Mexico
Gustavo A. Gonzalez-Aguilar ; Research Center for Food and Development, A.C. (CIAD), Carretera a Ejido La Victoria, Km. 0.6, MX-83304 Hermosillo, Sonora, Mexico

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.

Keywords

polyphenolic compounds; pancreatic lipase; enzymatic inhibition; molecular docking; anti-obesity effect

Hrčak ID:

192345

URI

https://hrcak.srce.hr/192345

Publication date:

29.12.2017.

Article data in other languages: croatian

Visits: 3.688 *