CORD, University of Kashmir, Hazratbal, Srinagar, 190006, Jammu & Kashmir, India.
Proteomics Laboratory, Division of Plant Biotechnology, Sher-e-Kashmir University of Agricultural Sciences & Technology of Kashmir, Shalimar, Srinagar, 190025, Jammu & Kashmir, India.
Mol Biol Rep. 2024 Jun 14;51(1):759. doi: 10.1007/s11033-024-09695-z.
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.
本研究旨在阐明荞麦中一种生物活性化合物的降胆固醇作用,并阐明其对胆固醇代谢调节机制的影响。研究的化合物被鉴定为槲皮素。
在体外实验中,用荞麦中提取的生物活性化合物槲皮素处理 HepG2 细胞,发现细胞内胆固醇积累显著减少。通过评估参与胆固醇生物合成和代谢的关键基因的转录活性,对这一现象进行了严格的定量。观察到 HMG-CoA 还原酶 (HMGCR) 的表达显著降低,表明内源性胆固醇合成减少。相反,胆固醇 7α-羟化酶 (CYP7A1) 的表达上调,提示胆固醇向胆汁酸的代谢增强。此外,该研究还探讨了槲皮素和辛伐他汀(一种临床应用的他汀类药物)联合作用的效果,结果表明在不同剂量下,两者在调节胆固醇水平方面具有协同作用。
本研究提供了关于荞麦中提取的生物活性化合物槲皮素发挥降胆固醇作用的机制途径的全面见解。此外,观察到槲皮素和辛伐他汀之间的协同相互作用为开发联合治疗策略来管理高脂血症开辟了新途径。