Pharmaceutical application of quercetin-3-O-(6''-O-alpha-L-rhamnose)-beta-D-glucose-O-beta-D-glucoside

A technology of glucoside and quercetin, which is applied in the directions of drug combination, pharmaceutical formula, medical preparation containing active ingredients, etc., can solve the problems such as the lack of lipid-lowering regulating substances in Zanthoxylum bungeanum

Inactive Publication Date: 2017-01-11
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there are few research reports on lip...

Method used

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  • Pharmaceutical application of quercetin-3-O-(6''-O-alpha-L-rhamnose)-beta-D-glucose-O-beta-D-glucoside
  • Pharmaceutical application of quercetin-3-O-(6''-O-alpha-L-rhamnose)-beta-D-glucose-O-beta-D-glucoside
  • Pharmaceutical application of quercetin-3-O-(6''-O-alpha-L-rhamnose)-beta-D-glucose-O-beta-D-glucoside

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1, Lipid regulation experiment of compound ZYZ-772 in hyperlipidemia animal model

[0032] 28 apoE gene knockout mice were randomly and equally divided into model group, positive drug group (simvastatin 1mg / kg / d), compound ZYZ-772 low dose group (10mg / kg / d), high dose group (20mg / kg / d) kg / d), and given high-fat diet, intraperitoneal administration for 38 days; 7 C57BL / 6 mice were used as normal group, given normal diet, and intraperitoneal injection of equal volume of normal saline for 38 days; 38 days later, serum total cholesterol, Triglyceride, HDL-c, LDL-c, alanine aminotransferase and aspartate aminotransferase levels, liver tissue was stained with H&E and oil red, and the expression of liver tissue proteins SREBP-2, LDLR, PCSK9, ABCG5 and ABCG8 were detected;

[0033] The results show that the compound ZYZ-772 can well regulate the blood lipid level and has a protective effect on fatty liver.

Embodiment 2

[0034] Embodiment 2, ZYZ-772 cytotoxicity assay and cell proliferation situation

[0035] HepG2 cells in the logarithmic growth phase were digested, diluted with DMEM high-glucose medium containing 10% FBS, and seeded in 96-well plates (1×10 4 In each well), control group, model group, simvastatin group and different concentration administration groups were set. After 12 hours, each different concentration administration group was replaced with 1% FBS high-sugar DMEM medium and 0.1 μM , 0.5 μM, 2.5 μM, 5.0 μM, 25 μM, 50 μM, and 100 μM ZYZ-772, the simvastatin group was replaced with 1% FBS high-glucose DMEM medium containing 1 μM simvastatin, and the control and model groups were only replaced with 1 %FBS high-glucose DMEM medium, after pretreatment for 24 hours, the model group, simvastatin group and each administration group were replaced with a modeling solution containing 50 μg / ml cholesterol + 5 μg / ml 25-hydroxycholesterol, and the control group was replaced with DMEM hi...

Embodiment 3

[0037] Example 3, Cholesterol Modulating Activity of Compound ZYZ-772 at the Cellular Level

[0038] HepG2 cells in the logarithmic growth phase were digested, diluted with DMEM high-glucose medium containing 10% FBS, and seeded in 24-well plates (8×10 4 per hole), set up the control group, model group, simvastatin group, administration groups of different concentrations, and administration groups of quercetin (the mother core structure of ZYZ-772), and after 12h, administration of different concentrations The group was replaced with 1% FBS high-sugar DMEM medium, and 0.1 μM, 0.5 μM, 2.5 μM, 5.0 μM ZYZ-772 were added respectively, and the groups administered with various concentrations of quercetin were replaced with 1% FBS high-sugar DMEM medium 0.1 μM, 1.0 μM, and 5.0 μM quercetin were added respectively, the simvastatin group was replaced with 1% FBS high-sugar DMEM medium containing 1 μM simvastatin, and the control and model groups were only replaced with 1% FBS high-suga...

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Abstract

The invention belongs to the field of pharmacy, and relates to an application of quercetin-3-O-(6''-O-alpha-L-rhamnose)-beta-D-glucose-O-beta-D-glucoside (ZYZ-772) in lipid metabolism regulation, especially an application in the preparation of drugs for treating diseases related with lipid metabolism. The results of in-vivo and in-vitro experiments show that the lipid metabolism adjusting effect of the provided compound is better than that of quercetin with a mother nucleus structure of the compound; and the results show that the provided compound can adjust the blood lipid level, reduces the aggregation of lipid in the liver so as to prevent fatty liver, and can adjust the lipid through increasing the activity of low density lipoprotein receptor (LDLR) and promoting the expression of cholesterol adjusting element binding protein-2 (SREBP-2). The compound ZYZ has a prominent adjusting effect on lipid metabolism, and can be used to prepare drugs for treating diseases related with lipid metabolism.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a new pharmaceutical use of quercetin-3-O-(6"-O-α-L-rhamnose)-β-D-glucose-7-O-β-D-glucoside , specifically related to quercetin-3-O-(6”-O-α-L-rhamnose)-β-D-glucose-7-O-β-D-glucoside (ZYZ-772) in lipid The application in metabolic regulation, especially the application in the preparation of medicines for preventing and treating diseases related to lipid metabolism. Background technique [0002] According to literature reports, cardiovascular disease is currently one of the important factors causing mortality in the world. In 2002, a report by the World Health Organization (WHO) pointed out that about 50% of global disability and death were caused by heart disease or stroke. Studies have shown that one of the main pathogenic factors of cardiovascular diseases is lipid metabolism disorder. Therefore, regulating lipid metabolism and reducing blood lipid levels have important practical significa...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P3/06A61P1/16
Inventor 朱依谆钟亮解郭薇王莹
Owner FUDAN UNIV
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