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吉普萨烯醇 A-脂质体通过激活 FXR 受体有效改善肝细胞脂质积累。

Gypensapogenin A-Liposomes Efficiently Ameliorates Hepatocellular Lipid Accumulation via Activation of FXR Receptor.

机构信息

Guizhou Engineering Research Center of Industrial Key-Technology for Dendrobium Nobile, Zunyi Medical University, Zunyi 563000, China.

Joint International Research Laboratory of Ethnomedicine of Ministry of Education, Zunyi Medical University, Zunyi 563000, China.

出版信息

Molecules. 2024 Aug 28;29(17):4080. doi: 10.3390/molecules29174080.

Abstract

Non-alcoholic fatty liver disease (NAFLD) is one of the most common metabolic diseases encountered in clinical practice, which is characterized by the excessive accumulation of triglycerides (steatosis), and a variety of metabolic abnormalities including lipid metabolism and bile acid metabolism are closely related to NAFLD. In China, is used as functional food and Chinese medicine to treat various diseases, especially NAFLD, for a long time. However, the active components that exert the main therapeutic effects and their mechanisms remain unclear. In this study, Gypensapogenin A was isolated from the total saponins of and prepared as a liposomal delivery system. Gypensapogenin A liposomes could activate FXR, inhibit the expression of CYP7A1 and CYP8B1, increase the expression of CYP27A1, modulate the ratio of CA and CDCA, decrease the content of CA, and increase the content of CDCA, thus forming a virtuous cycle of activating FXR to play a role in lowering blood lipid levels.

摘要

非酒精性脂肪性肝病(NAFLD)是临床实践中最常见的代谢性疾病之一,其特征为甘油三酯(脂肪变性)过度积累,多种代谢异常,包括脂质代谢和胆汁酸代谢与 NAFLD 密切相关。在中国, 长期以来一直被用作功能性食品和中药来治疗各种疾病,尤其是 NAFLD。然而,发挥主要治疗作用的活性成分及其机制仍不清楚。在这项研究中,从 总皂苷中分离得到了 ,并将其制备成脂质体传递系统。 皂甙 A 脂质体可以激活 FXR,抑制 CYP7A1 和 CYP8B1 的表达,增加 CYP27A1 的表达,调节 CA 和 CDCA 的比值,降低 CA 的含量,增加 CDCA 的含量,从而形成激活 FXR 以降低血脂水平的良性循环。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5df9/11397205/8908922765c6/molecules-29-04080-g001.jpg

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