Cholesterol-lowering effects of rhubarb free anthraquinones and their mechanism of action

被引：2
作者：
Wang, Lifang [1 ,2 ]
Wang, Haijiao [1 ,2 ]
Niu, Jingjing [1 ,2 ]
Chen, Honggang [3 ]
Wang, Meng [1 ,2 ]
Yang, Zhigang [1 ,2 ,4 ]
Wang, Shaohua [1 ,2 ,4 ]
Sun, Xiuxia [1 ,2 ]
Shi, Yanbin [1 ,2 ,4 ]
机构：
[1] Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China
[2] Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China
[3] Gansu Univ Chinese Med, Coll Pharm, Lanzhou 730000, Peoples R China
[4] Lanzhou Univ, Collaborat Innovat Ctr Northwestern Chinese Med, Lanzhou 730000, Peoples R China
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 2024年 / 966卷
关键词：
Rhubarb free anthraquinones; Hypercholesterolemia; Cholesterol synthesis; Mechanism of action; Liposomes; METABOLISM; INHIBITION;
D O I：
10.1016/j.ejphar.2024.176348
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Rhubarb free anthraquinones (RhA) have significant lipid-regulating activity. However, whether RhA monomers have a role in lipid-regulating and their mechanism of action remains unclear. Based on the cholesterol accumulated HepG2 cell model, the cholesterol-regulating effect of RhA monomers and their combinations was investigated. The expression of sterol-regulatory element binding protein 2 (SREBP2), 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HMGCR) and squalene monooxygenase (SQLE) of the model cells was analyzed to preliminarily explore the mechanism of action. After that, the liposomes of each active RhA monomer were separately prepared with the same lipid materials and the same preparation method so that each monomer has similar or equal bioavailability after oral administration to rats. Finally, the hypercholesterolemic rat model was established, and the effect of active RhA monomers loaded liposomes as well as their combinations on cholesterol-regulating was investigated and their mechanism of action was analyzed. The results showed that aloe-emodin, rhein and emodin were the main cholesterol-regulating components of RhA, and the combination of rhein and emodin showed significant cholesterol-lowering effect, which may be related to the expression of SREBP2, HMGCR and SQLE in the rat liver.
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页数：13
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