Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss

Peripheral targets like pancreatic-lipase appear to be the most suitable pharmacological alternative for obesity, as with orlistat, although its adverse effects limit its use. Therefore, the aim of this work was to identify new natural compounds able to inhibit pancreatic-lipase in an in vitro model...

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Main Authors: Teresa Del Castillo-Santaella, Juan José Hernández-Morante, Jesús Suárez-Olmos, Julia Maldonado-Valderrama, Jorge Peña-García, Carlos Martínez-Cortés, Horacio Pérez-Sánchez
Format: Article
Language:English
Published: Elsevier 2021-08-01
Series:Journal of Functional Foods
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S1756464621001286
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spelling doaj-745571ae5e374360bda13cf227863eb92021-06-19T04:53:18ZengElsevierJournal of Functional Foods1756-46462021-08-0183104479Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight lossTeresa Del Castillo-Santaella0Juan José Hernández-Morante1Jesús Suárez-Olmos2Julia Maldonado-Valderrama3Jorge Peña-García4Carlos Martínez-Cortés5Horacio Pérez-Sánchez6Department of Applied Physics, University of Granada (UGR), Campus de Fuentenueva, sn, 18071 Granada, SpainEating Disorders Research Unit, Universidad Católica de Murcia (UCAM), 30107 Murcia, SpainDepartment of Applied Physics, University of Granada (UGR), Campus de Fuentenueva, sn, 18071 Granada, Spain; Molecular Cancer Therapeutics, Hospital del Mar Medical Research Institute (IMIM) Pg Marítim, 25-29, 08003 Barcelona, Spain1Department of Applied Physics, University of Granada (UGR), Campus de Fuentenueva, sn, 18071 Granada, Spain; Excellence Research Unit “Modeling Nature” (MNat), University of Granada, Granada, SpainStructural Bioinformatics and High Performance Computing Research Group (BIO-HPC), Computer Engineering Department, Universidad Católica de Murcia (UCAM), 30107 Murcia, SpainStructural Bioinformatics and High Performance Computing Research Group (BIO-HPC), Computer Engineering Department, Universidad Católica de Murcia (UCAM), 30107 Murcia, SpainStructural Bioinformatics and High Performance Computing Research Group (BIO-HPC), Computer Engineering Department, Universidad Católica de Murcia (UCAM), 30107 Murcia, Spain; Corresponding author at: Bioinformatics and High Performance Computing Research Group (BIO-HPC), Campus de Guadalupe, s/n, 30107 Murcia, Spain.Peripheral targets like pancreatic-lipase appear to be the most suitable pharmacological alternative for obesity, as with orlistat, although its adverse effects limit its use. Therefore, the aim of this work was to identify new natural compounds able to inhibit pancreatic-lipase in an in vitro model. The DrugBank database was used to perform docking calculations. The best fitting-score compounds were further evaluated in vitro. Our data revealed that glutathione-disulphide (GSSG) and silibinin(A) inhibit pancreatic-lipase. This was confirmed by measuring hydrolysis in an emulsion model, obtaining that the suppression of lipid digestion by silibinin(A) was higher than that of GSSG and close to the effect of orlistat. Combined analysis established the existence of different inhibition mechanisms for each compound. In summary, silibinin(A) and GSSG inhibited pancreatic-lipase and, therefore, may be served as promise natural compounds to face with obesity. Further studies comprise the next step to fully validate the suitability of these compounds.http://www.sciencedirect.com/science/article/pii/S1756464621001286Pancreatic lipaseSilibinin(A)ObesityLipolysisEmulsionInterfacial tension
collection DOAJ
language English
format Article
sources DOAJ
author Teresa Del Castillo-Santaella
Juan José Hernández-Morante
Jesús Suárez-Olmos
Julia Maldonado-Valderrama
Jorge Peña-García
Carlos Martínez-Cortés
Horacio Pérez-Sánchez
spellingShingle Teresa Del Castillo-Santaella
Juan José Hernández-Morante
Jesús Suárez-Olmos
Julia Maldonado-Valderrama
Jorge Peña-García
Carlos Martínez-Cortés
Horacio Pérez-Sánchez
Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss
Journal of Functional Foods
Pancreatic lipase
Silibinin(A)
Obesity
Lipolysis
Emulsion
Interfacial tension
author_facet Teresa Del Castillo-Santaella
Juan José Hernández-Morante
Jesús Suárez-Olmos
Julia Maldonado-Valderrama
Jorge Peña-García
Carlos Martínez-Cortés
Horacio Pérez-Sánchez
author_sort Teresa Del Castillo-Santaella
title Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss
title_short Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss
title_full Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss
title_fullStr Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss
title_full_unstemmed Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss
title_sort identification of the thistle milk component silibinin(a) and glutathione-disulphide as potential inhibitors of the pancreatic lipase: potential implications on weight loss
publisher Elsevier
series Journal of Functional Foods
issn 1756-4646
publishDate 2021-08-01
description Peripheral targets like pancreatic-lipase appear to be the most suitable pharmacological alternative for obesity, as with orlistat, although its adverse effects limit its use. Therefore, the aim of this work was to identify new natural compounds able to inhibit pancreatic-lipase in an in vitro model. The DrugBank database was used to perform docking calculations. The best fitting-score compounds were further evaluated in vitro. Our data revealed that glutathione-disulphide (GSSG) and silibinin(A) inhibit pancreatic-lipase. This was confirmed by measuring hydrolysis in an emulsion model, obtaining that the suppression of lipid digestion by silibinin(A) was higher than that of GSSG and close to the effect of orlistat. Combined analysis established the existence of different inhibition mechanisms for each compound. In summary, silibinin(A) and GSSG inhibited pancreatic-lipase and, therefore, may be served as promise natural compounds to face with obesity. Further studies comprise the next step to fully validate the suitability of these compounds.
topic Pancreatic lipase
Silibinin(A)
Obesity
Lipolysis
Emulsion
Interfacial tension
url http://www.sciencedirect.com/science/article/pii/S1756464621001286
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