Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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
_version_ 1785015964333506560
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
work_keys_str_mv AT cacciatoreivana antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT spallettasonia antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT dirienzoannalisa antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT flativincenzo antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT fornasarierika antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT pierdomenicolaura antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT delbocciopiero antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT valentinuzzisilvia antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT costantinierica antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT toniatoelena antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT martinottistefano antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT contecarmela antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT distefanoantonio antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells
AT robuffoiole antiobesityandantiinflammatoryeffectsofnovelcarvacrolderivativeson3t3l1andwjmscscells