Unravelling effects of phytochemicals from buckwheat on cholesterol metabolism and lipid accumulation in HepG2 cells and its validation through gene expression analysis.
Humans
Fagopyrum
/ chemistry
Hep G2 Cells
Cholesterol
/ metabolism
Quercetin
/ pharmacology
Lipid Metabolism
/ drug effects
Phytochemicals
/ pharmacology
Hydroxymethylglutaryl CoA Reductases
/ metabolism
Cholesterol 7-alpha-Hydroxylase
/ metabolism
Anticholesteremic Agents
/ pharmacology
Simvastatin
/ pharmacology
Plant Extracts
/ pharmacology
Gene Expression Profiling
/ methods
Gene Expression Regulation
/ drug effects
Buckwheat
CYP7A1
HMGCR
Quercetin
Journal
Molecular biology reports
ISSN: 1573-4978
Titre abrégé: Mol Biol Rep
Pays: Netherlands
ID NLM: 0403234
Informations de publication
Date de publication:
14 Jun 2024
14 Jun 2024
Historique:
received:
21
03
2024
accepted:
31
05
2024
medline:
14
6
2024
pubmed:
14
6
2024
entrez:
14
6
2024
Statut:
epublish
Résumé
The objective of this research was to elucidate the hypocholesterolemic effects of a bioactive compound extracted from buckwheat, and to delineate its influence on the regulatory mechanisms of cholesterol metabolism. The compound under investigation was identified as quercetin. In vitro experiments conducted on HepG2 cells treated with quercetin revealed a significant reduction in intracellular cholesterol accumulation. This phenomenon was rigorously quantified by assessing the transcriptional activity of key genes involved in the biosynthesis and metabolism of cholesterol. A statistically significant reduction in the expression of HMG-CoA reductase (HMGCR) was observed, indicating a decrease in endogenous cholesterol synthesis. Conversely, an upregulation in the expression of cholesterol 7 alpha-hydroxylase (CYP7A1) was also observed, suggesting an enhanced catabolism of cholesterol to bile acids. Furthermore, the study explored the combinatory effects of quercetin and simvastatin, a clinically utilized statin, revealing a synergistic action in modulating cholesterol levels at various dosages. The findings from this research provide a comprehensive insight into the mechanistic pathways through which quercetin, a phytochemical derived from buckwheat, exerts its hypocholesterolemic effects. Additionally, the observed synergistic interaction between quercetin and simvastatin opens up new avenues for the development of combined therapeutic strategies to manage hyperlipidemia.
Sections du résumé
BACKGROUND
BACKGROUND
The objective of this research was to elucidate the hypocholesterolemic effects of a bioactive compound extracted from buckwheat, and to delineate its influence on the regulatory mechanisms of cholesterol metabolism. The compound under investigation was identified as quercetin.
MATERIAL AND RESULTS
RESULTS
In vitro experiments conducted on HepG2 cells treated with quercetin revealed a significant reduction in intracellular cholesterol accumulation. This phenomenon was rigorously quantified by assessing the transcriptional activity of key genes involved in the biosynthesis and metabolism of cholesterol. A statistically significant reduction in the expression of HMG-CoA reductase (HMGCR) was observed, indicating a decrease in endogenous cholesterol synthesis. Conversely, an upregulation in the expression of cholesterol 7 alpha-hydroxylase (CYP7A1) was also observed, suggesting an enhanced catabolism of cholesterol to bile acids. Furthermore, the study explored the combinatory effects of quercetin and simvastatin, a clinically utilized statin, revealing a synergistic action in modulating cholesterol levels at various dosages.
CONCLUSIONS
CONCLUSIONS
The findings from this research provide a comprehensive insight into the mechanistic pathways through which quercetin, a phytochemical derived from buckwheat, exerts its hypocholesterolemic effects. Additionally, the observed synergistic interaction between quercetin and simvastatin opens up new avenues for the development of combined therapeutic strategies to manage hyperlipidemia.
Identifiants
pubmed: 38874818
doi: 10.1007/s11033-024-09695-z
pii: 10.1007/s11033-024-09695-z
doi:
Substances chimiques
Cholesterol
97C5T2UQ7J
Quercetin
9IKM0I5T1E
Phytochemicals
0
Hydroxymethylglutaryl CoA Reductases
EC 1.1.1.-
Cholesterol 7-alpha-Hydroxylase
EC 1.14.14.23
HMGCR protein, human
EC 1.1.1.-
Anticholesteremic Agents
0
Simvastatin
AGG2FN16EV
CYP7A1 protein, human
EC 1.14.14.23
Plant Extracts
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
759Informations de copyright
© 2024. The Author(s), under exclusive licence to Springer Nature B.V.
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