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A kind of natural medicine and its application for reducing the secretion of pcsk9 from liver cells

A liver cell and drug technology, applied in the field of natural medicinal chemistry, can solve the problems of lowering lipid-lowering activity and increasing PCSK9, and achieve the effect of blood-lipid-lowering activity guarantee, enhanced lipid-lowering effect, and drug safety guarantee

Active Publication Date: 2022-02-22
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problem that the first-line drug for the treatment of hyperlipidemia—statin drugs, the increase of PCSK9 leads to the reduction of lipid-lowering activity, the present invention provides an application of a natural drug that reduces the secretion of PCSK9 by liver cells

Method used

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  • A kind of natural medicine and its application for reducing the secretion of pcsk9 from liver cells
  • A kind of natural medicine and its application for reducing the secretion of pcsk9 from liver cells
  • A kind of natural medicine and its application for reducing the secretion of pcsk9 from liver cells

Examples

Experimental program
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Effect test

Embodiment 1

[0030] The preparation method of monomer compound in Gynostemma pentaphyllum of Fujian origin 1

[0031] Take Gynostemma pentaphylla from Fujian, extract it twice by decocting, and extract with 8 times the amount of water for 2 hours each time, combine the extracts, filter, and concentrate to obtain the total saponins extract of Gynostemma pentaphyllum from Fujian. Take the total saponins extract of Gynostemma pentaphylla from Fujian, and ultrasonically extract it with 8 times the amount of methanol for 5 times, each time for 20 minutes, combine the filtrates, concentrate under reduced pressure, and obtain the methanol-soluble fraction. Appropriate amount of methanol-soluble extract was subjected to deactivated silica gel column chromatography, gradient elution with chloroform-methanol-water (100:0:0→0:100:0), TLC inspection, combined to obtain 9 fractions (Fr.a~Fr.i). Then repeated silica gel, ODS, Sephadex LH-20 column chromatography, Flash rapid preparation and semi-prepar...

Embodiment 2

[0057] Example 2 Some monomers in Gynostemma pentaphyllum from Fujian origin have significant PCSK9-reducing activity on HepG2 cells under the condition of 20 μM drug concentration

[0058] Human liver cancer cells (HepG2) were divided into several groups, each group had three parallel wells, and 1*10 5 Cells were inserted into a 12-well plate and cultured in DMEM low-glucose medium containing 10% fetal bovine serum in 5% CO 2 It was carried out in a 37°C incubator; after the cells were inoculated, these groups of cells were treated as follows: the first group was a blank group, cultured with DMEM low-glucose medium containing 5% fetal bovine serum (FBS), and the second group was The model group was cultured with DMEM low-glucose medium containing 5% lipoprotein-poor serum (LPDS), and the following groups were respectively administered with different monomer compounds (20 μM), cultured with DMEM low-sugar medium containing 5% LPDS Cultivate, the blank group was treated for 48...

Embodiment 3

[0060] Example 3 Some monomers in Gynostemma pentaphylla from Fujian origin have significant PCSK9-reducing activity on HepG2 cells at a concentration of 10 μM

[0061] Human liver cancer cells (HepG2) were divided into several groups, each group had three parallel wells, and 1*105 cells were inoculated into 12-well plates in each well, cultured with DMEM low-glucose medium containing 10% fetal bovine serum, and incubated at 5 %CO2 in a 37°C incubator; after the cells were inoculated, these groups of cells were treated as follows: the first group was a blank group, which was cultured with DMEM low-glucose medium containing 5% FBS, and the second group was a model group. Cultivate with DMEM low-sugar medium containing 5% LPDS, and then several groups are administration groups (10 μ M) of different monomer compounds respectively, cultivate with DMEM low-sugar medium containing 5% LPDS, blank group is treated for 48h, model group Add simvastatin (1 μ M) after culturing 23 h with ...

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Abstract

The invention relates to the technical field of natural medicinal chemistry, in particular to a monomer compound isolated from Gynostemma pentaphyllum produced in Fujian and its application in the preparation of a drug that inhibits PCSK9 and exerts a lipid-lowering effect, that is, a natural drug that reduces the secretion of PCSK9 by liver cells and its application. The novel dammarane-type saponins compound of the present invention is obtained by extracting, separating and purifying from the whole plant of Gynostemma pentaphyllum produced in Fujian. Some monomeric compounds in Gynostemma pentaphyllum produced in Fujian of the present invention have different degrees of inhibitory activity on hepatic cell secretion of PCSK9, so as to achieve the purpose of reducing lipid alone or synergistically with statin drugs to enhance its lipid-lowering effect.

Description

technical field [0001] The invention relates to the technical field of natural medicinal chemistry, in particular to a monomer compound isolated from Gynostemma pentaphyllum produced in Fujian and its application in the preparation of a drug that inhibits PCSK9 and exerts a lipid-lowering effect. Background technique [0002] Atherosclerosis (AS (arteriosclerosis)) and cardiovascular disease (CVD (cardiovascular disease)) have extremely high morbidity and mortality rates worldwide, and are the main causes of death in my country. Hypercholesterolemia is a major risk factor for atherosclerosis and heart disease, and low-density lipoprotein cholesterol (LDL-C) has been identified as an independent and most potent modifiable risk factor for the development of cardiovascular disease. [0003] The use of statins has successfully reduced the risk of cardiovascular events over the past 20 years. Statins are inhibitors of 3-hydroxy-3-methyl-glutaryl coenzyme (HMGCR) (the rate-limiti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J17/00A61P3/06A61K31/366A61K31/704A61K31/7048
CPCC07J17/005A61P3/06A61K31/366A61K31/704A61K31/7048
Inventor 殷志琦黄亚萍王云杉姜新宇
Owner CHINA PHARM UNIV
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