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Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells
(1) Background: Obesity, a complex metabolic disease resulting from an imbalance between food consumption and energy expenditure, leads to an increase in adipocytes and chronic inflammatory conditions. The aim of this paper was to synthesize a small series of carvacrol derivatives (CD1-3) that are a...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10055808/ https://www.ncbi.nlm.nih.gov/pubmed/36986440 http://dx.doi.org/10.3390/ph16030340 |
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author | Cacciatore, Ivana Spalletta, Sonia Di Rienzo, Annalisa Flati, Vincenzo Fornasari, Erika Pierdomenico, Laura Del Boccio, Piero Valentinuzzi, Silvia Costantini, Erica Toniato, Elena Martinotti, Stefano Conte, Carmela Di Stefano, Antonio Robuffo, Iole |
author_facet | Cacciatore, Ivana Spalletta, Sonia Di Rienzo, Annalisa Flati, Vincenzo Fornasari, Erika Pierdomenico, Laura Del Boccio, Piero Valentinuzzi, Silvia Costantini, Erica Toniato, Elena Martinotti, Stefano Conte, Carmela Di Stefano, Antonio Robuffo, Iole |
author_sort | Cacciatore, Ivana |
collection | PubMed |
description | (1) Background: Obesity, a complex metabolic disease resulting from an imbalance between food consumption and energy expenditure, leads to an increase in adipocytes and chronic inflammatory conditions. The aim of this paper was to synthesize a small series of carvacrol derivatives (CD1-3) that are able to reduce both adipogenesis and the inflammatory status often associated with the progression of the obesity disease. (2) Methods: The synthesis of CD1-3 was performed using classical procedures in a solution phase. Biological studies were performed on three cell lines: 3T3-L1, WJ-MSCs, and THP-1. The anti-adipogenic properties of CD1-3 were evaluated using western blotting and densitometric analysis by assessing the expression of obesity-related proteins, such as ChREBP. The anti-inflammatory effect was estimated by measuring the reduction in TNF-α expression in CD1-3-treated THP-1 cells. (3) Results: CD1-3—obtained through a direct linkage between the carboxylic moiety of anti-inflammatory drugs (Ibuprofen, Flurbiprofen, and Naproxen) and the hydroxyl group of carvacrol—have an inhibitory effect on the accumulation of lipids in both 3T3-L1 and WJ-MSCs cell cultures and an anti-inflammatory effect by reducing TNF- α levels in THP-1 cells. (4) Conclusions: Considering the physicochemical properties, stability, and biological data, the CD3 derivative—obtained by a direct linkage between carvacrol and naproxen—resulted in the best candidate, displaying anti-obesity and anti-inflammatory effects in vitro. |
format | Online Article Text |
id | pubmed-10055808 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-100558082023-03-30 Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells Cacciatore, Ivana Spalletta, Sonia Di Rienzo, Annalisa Flati, Vincenzo Fornasari, Erika Pierdomenico, Laura Del Boccio, Piero Valentinuzzi, Silvia Costantini, Erica Toniato, Elena Martinotti, Stefano Conte, Carmela Di Stefano, Antonio Robuffo, Iole Pharmaceuticals (Basel) Article (1) Background: Obesity, a complex metabolic disease resulting from an imbalance between food consumption and energy expenditure, leads to an increase in adipocytes and chronic inflammatory conditions. The aim of this paper was to synthesize a small series of carvacrol derivatives (CD1-3) that are able to reduce both adipogenesis and the inflammatory status often associated with the progression of the obesity disease. (2) Methods: The synthesis of CD1-3 was performed using classical procedures in a solution phase. Biological studies were performed on three cell lines: 3T3-L1, WJ-MSCs, and THP-1. The anti-adipogenic properties of CD1-3 were evaluated using western blotting and densitometric analysis by assessing the expression of obesity-related proteins, such as ChREBP. The anti-inflammatory effect was estimated by measuring the reduction in TNF-α expression in CD1-3-treated THP-1 cells. (3) Results: CD1-3—obtained through a direct linkage between the carboxylic moiety of anti-inflammatory drugs (Ibuprofen, Flurbiprofen, and Naproxen) and the hydroxyl group of carvacrol—have an inhibitory effect on the accumulation of lipids in both 3T3-L1 and WJ-MSCs cell cultures and an anti-inflammatory effect by reducing TNF- α levels in THP-1 cells. (4) Conclusions: Considering the physicochemical properties, stability, and biological data, the CD3 derivative—obtained by a direct linkage between carvacrol and naproxen—resulted in the best candidate, displaying anti-obesity and anti-inflammatory effects in vitro. MDPI 2023-02-22 /pmc/articles/PMC10055808/ /pubmed/36986440 http://dx.doi.org/10.3390/ph16030340 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Cacciatore, Ivana Spalletta, Sonia Di Rienzo, Annalisa Flati, Vincenzo Fornasari, Erika Pierdomenico, Laura Del Boccio, Piero Valentinuzzi, Silvia Costantini, Erica Toniato, Elena Martinotti, Stefano Conte, Carmela Di Stefano, Antonio Robuffo, Iole Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells |
title | Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells |
title_full | Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells |
title_fullStr | Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells |
title_full_unstemmed | Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells |
title_short | Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells |
title_sort | anti-obesity and anti-inflammatory effects of novel carvacrol derivatives on 3t3-l1 and wj-mscs cells |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10055808/ https://www.ncbi.nlm.nih.gov/pubmed/36986440 http://dx.doi.org/10.3390/ph16030340 |
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