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Application of gentiopicroside in preparation of medicines for treating hyperlipidemia

A technology of gentiopicroside and hyperlipidemia, which is applied in the field of biomedicine, can solve the problem of unreported blood lipid-lowering activity, and achieves the effect of relieving lipid accumulation and increasing the level.

Inactive Publication Date: 2020-04-28
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Gentiopicroside has a variety of biological activities and a wide range of pharmacological effects, and its effects mainly include choleretic, stomach invigorating, anti-inflammatory, liver protection, etc. However, its blood lipid-lowering activity has not been reported

Method used

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  • Application of gentiopicroside in preparation of medicines for treating hyperlipidemia
  • Application of gentiopicroside in preparation of medicines for treating hyperlipidemia
  • Application of gentiopicroside in preparation of medicines for treating hyperlipidemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Determination of TG content in embodiment 1HepG2 cells

[0034] experimental method:

[0035] (1) HepG2 cells were seeded in a six-well plate with a density of 1×10 per well. 6 cells. The formula of the cell culture medium is DMEM medium with 4.5g / L glucose, 10% fetal bovine serum and 1% penicillin and streptomycin. Cells were cultured in 5% CO 2 and in a cell culture incubator at 37°C for 12 hours.

[0036] (2) Remove the original culture medium and replace it with DMEM with only 4.5g / L glucose as the culture medium to culture the cells, and starve the HepG2 cells for 3 hours.

[0037] (3) Incubate HepG2 cells with 200 μM gentiopicroside for 1 hour and then co-incubate the cells with 1000 μM free fatty acid (oleic acid:palmitic acid=2:1) ​​for 24 hours; among them, divide into blank group (DMEM medium), model group (1000 μM free fatty acid), control group (200 μM gentiopicroside), experimental group (200 μM gentiopicroside + 1000 μM free fatty acid).

[0038] (4)...

Embodiment 2

[0041] Example 2 HepG2 Cell Oil Red O Staining Experiment

[0042] experimental method:

[0043] (1)-(3) Experimental procedures are the same as in Example 1.

[0044] (4) Remove the cell culture medium, wash the cells 2-3 times with PBS, and then fix with 4% paraformaldehyde for 20-30 minutes.

[0045] (5) Formaldehyde was discarded, cells were washed 3 times with distilled water, and soaked with 60% isopropanol for 5 minutes.

[0046] (6) Stain with 0.5% Oil Red O staining solution for 10-20 minutes.

[0047] (7) Discard the staining solution, wash the cells 3-5 times with distilled water, and then stain with hematoxylin for 1-2 minutes.

[0048] (8) Observing lipid droplets with an optical microscope, the observation magnification is 1000 times.

[0049] (9) The experimental results are attached figure 2 .

[0050] attached figure 2 Oil red O staining results showed that the model group could increase the formation of lipid droplets in HepG2 cells, and the experime...

Embodiment 3

[0051] The mensuration of TC, TG, LDL, HDL content in the mouse serum of embodiment 3

[0052] experimental method:

[0053] (1) Raise the mice in an SPF environment with a temperature of 24±1° C. and a relative humidity of 40%-80%.

[0054](2) Before the experiment, the mice were fasted for 12 hours, then injected intraperitoneally with 40 mg / kg gentiopicroside for 1 hour, and then injected intraperitoneally with 500 mg / kg tyloxapol for 12 hours. The mice were randomly divided into five groups: control group (normal saline), model group (500 mg / kg tyloxapol), control group (40 mg / kg gentiopicroside), experimental group (40 mg / kg gentiopicrin Glycoside + 500 mg / kg Tyloxapol), drug positive control group (100 mg / kg fenofibrate + 500 mg / kg Tyloxapol).

[0055] (3) The mouse blood was obtained by taking blood from the eyeball, and left at room temperature. After the serum was precipitated, it was centrifuged at 3000 rpm for 5 minutes, and the upper layer of serum was absorbed. ...

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Abstract

The invention discloses application of gentiopicroside in preparation of a medicines for treating hyperlipidemia. According to the invention, it is proven by pharmacological experiments for the firsttime that the gentiopicroside has good therapeutic effects on hyperlipidemia mouse models and hepatic cell lipid accumulation models. The invention relates to detection of antilipidemic ability of gentiopicroside compounds, as well as study on the mechanism of action. Test results show that the gentiopicroside compounds can reduce TC, TG and LDL, as well as raise HDL and SOD, in serum of mice withthe hyperlipidemia; and the mechanism of action of the gentiopicroside compounds is related to up-regulation of PPAR[alpha] and down-regulation of SREBP-1c. Thus, the antilipidemic ability of the gentiopicroside is proven with the mechanism of action of the gentiopicroside in blood lipid reduction discovered.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of gentiopicroside in the preparation of drugs for treating hyperlipidemia. Background technique [0002] Hyperlipidemia often induces atherosclerosis, hypertension, diabetes, fatty liver and other metabolic diseases, which seriously threaten the health of humans and livestock. Most of the causes of hyperlipidemia are caused by disorder or abnormality of blood lipid metabolism due to poor eating habits and lack of exercise. The typical features of dyslipidemia are elevated total cholesterol (TC) and triglyceride (TG), with or without increased “bad cholesterol” low-density lipoprotein (LDL), and “good cholesterol” high-density lipoprotein (HDL). )reduce. Hyperlipidemia can be manifested as intravascular cholesterol transport disorder, so that intravascular apolipoprotein cannot perform its normal transport function, resulting in blockage of reverse cholesterol transpo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P3/06
CPCA61K31/7048A61P3/06
Inventor 冯海华金美玉覃海燕王齐沈冰玉严斯如李金霞阚兴池王建锋邱家章
Owner JILIN UNIV
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