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Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin
(1) Background: Capsaicin, a chief ingredient of natural chili peppers, enhances metabolism and energy expenditure and stimulates the browning of white adipose tissue (WAT) and brown fat activation to counter diet-induced obesity. Although capsaicin and its nonpungent analogs are shown to enhance en...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321193/ https://www.ncbi.nlm.nih.gov/pubmed/30518154 http://dx.doi.org/10.3390/molecules23123198 |
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author | Baskaran, Padmamalini Covington, Kyle Bennis, Jane Mohandass, Adithya Lehmann, Teresa Thyagarajan, Baskaran |
author_facet | Baskaran, Padmamalini Covington, Kyle Bennis, Jane Mohandass, Adithya Lehmann, Teresa Thyagarajan, Baskaran |
author_sort | Baskaran, Padmamalini |
collection | PubMed |
description | (1) Background: Capsaicin, a chief ingredient of natural chili peppers, enhances metabolism and energy expenditure and stimulates the browning of white adipose tissue (WAT) and brown fat activation to counter diet-induced obesity. Although capsaicin and its nonpungent analogs are shown to enhance energy expenditure, their efficiency to bind to and activate their receptor—transient receptor potential vanilloid subfamily 1 (TRPV1)—to mediate thermogenic effects remains unclear. (2) Methods: We analyzed the binding efficiency of capsaicin analogs by molecular docking. We fed wild type mice a normal chow or high fat diet (± 0.01% pungent or nonpungent capsaicin analog) and isolated inguinal WAT to analyze the expression of thermogenic genes and proteins. (3) Results: Capsaicin, but not its nonpungent analogs, efficiently binds to TRPV1, prevents high fat diet-induced weight gain, and upregulates thermogenic protein expression in WAT. Molecular docking studies indicate that capsaicin exhibits the highest binding efficacy to TRPV1 because it has a hydrogen bond that anchors it to TRPV1. Capsiate, which lacks the hydrogen bond, and therefore, does not anchor to TRPV1. (4) Conclusions: Long-term activation of TRPV1 is imminent for the anti-obesity effect of capsaicin. Efforts to decrease the pungency of capsaicin will help in advancing it to mitigate obesity and metabolic dysfunction in humans. |
format | Online Article Text |
id | pubmed-6321193 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-63211932019-01-14 Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin Baskaran, Padmamalini Covington, Kyle Bennis, Jane Mohandass, Adithya Lehmann, Teresa Thyagarajan, Baskaran Molecules Article (1) Background: Capsaicin, a chief ingredient of natural chili peppers, enhances metabolism and energy expenditure and stimulates the browning of white adipose tissue (WAT) and brown fat activation to counter diet-induced obesity. Although capsaicin and its nonpungent analogs are shown to enhance energy expenditure, their efficiency to bind to and activate their receptor—transient receptor potential vanilloid subfamily 1 (TRPV1)—to mediate thermogenic effects remains unclear. (2) Methods: We analyzed the binding efficiency of capsaicin analogs by molecular docking. We fed wild type mice a normal chow or high fat diet (± 0.01% pungent or nonpungent capsaicin analog) and isolated inguinal WAT to analyze the expression of thermogenic genes and proteins. (3) Results: Capsaicin, but not its nonpungent analogs, efficiently binds to TRPV1, prevents high fat diet-induced weight gain, and upregulates thermogenic protein expression in WAT. Molecular docking studies indicate that capsaicin exhibits the highest binding efficacy to TRPV1 because it has a hydrogen bond that anchors it to TRPV1. Capsiate, which lacks the hydrogen bond, and therefore, does not anchor to TRPV1. (4) Conclusions: Long-term activation of TRPV1 is imminent for the anti-obesity effect of capsaicin. Efforts to decrease the pungency of capsaicin will help in advancing it to mitigate obesity and metabolic dysfunction in humans. MDPI 2018-12-04 /pmc/articles/PMC6321193/ /pubmed/30518154 http://dx.doi.org/10.3390/molecules23123198 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Baskaran, Padmamalini Covington, Kyle Bennis, Jane Mohandass, Adithya Lehmann, Teresa Thyagarajan, Baskaran Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin |
title | Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin |
title_full | Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin |
title_fullStr | Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin |
title_full_unstemmed | Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin |
title_short | Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin |
title_sort | binding efficacy and thermogenic efficiency of pungent and nonpungent analogs of capsaicin |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321193/ https://www.ncbi.nlm.nih.gov/pubmed/30518154 http://dx.doi.org/10.3390/molecules23123198 |
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