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Application of dammarane-type triterpenoid saponins in Gynostemma Gynostemma total glycosides in the preparation of drugs for inhibiting pcsk9 and exerting lipid-lowering effect

A technology of triterpenoid saponins and dammarane type, which is applied in the field of natural medicinal chemistry, can solve the problems of increasing PCSK9 and reducing lipid-lowering activity, and achieves the enhancement of lipid-lowering effect, blood lipid-lowering activity and drug safety guarantee. Effect

Active Publication Date: 2022-07-15
湖南华宝通制药有限公司
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  • Abstract
  • Description
  • Claims
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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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  • Application of dammarane-type triterpenoid saponins in Gynostemma Gynostemma total glycosides in the preparation of drugs for inhibiting pcsk9 and exerting lipid-lowering effect
  • Application of dammarane-type triterpenoid saponins in Gynostemma Gynostemma total glycosides in the preparation of drugs for inhibiting pcsk9 and exerting lipid-lowering effect
  • Application of dammarane-type triterpenoid saponins in Gynostemma Gynostemma total glycosides in the preparation of drugs for inhibiting pcsk9 and exerting lipid-lowering effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 The preparation method of monomer compound in Gynostemma pentaphyllum from Hunan origin and Guangxi origin

[0029] The medicinal materials of Gynostemma japonica from the two origins were taken separately, extracted twice by decocting method, extracted with 8 times the amount of water for 2 hours each time, the extracts were combined, filtered and concentrated to obtain the total Gynostemma saponin extract. The total saponin extract of Gynostemma pentaphyllum was taken, and ultrasonically extracted with 8 times the amount of methanol for 5 times for 20 min each time. The filtrates were combined and concentrated under reduced pressure to obtain the methanol-soluble fraction. An appropriate amount of methanol-soluble extract was subjected to deactivated silica gel column chromatography, eluted with a gradient of chloroform-methanol-water (100:0:0→0:100:0), checked by TLC, and 5 fractions were combined. (Fr.a~Fr.i). Then repeat silica gel, ODS, Sephadex LH-2...

Embodiment 2

[0055] Example 2 Some monomeric compounds in Gynostemma pentaphyllum from Hunan origin and Guangxi origin have significant PCSK9 reducing activity on HepG2 cells under the condition of 20 μM drug concentration

[0056] Human hepatoma cells (HepG2) were divided into several groups, each group had three parallel wells, and 1*10 cells were inoculated in each well. 5 Cells were inserted into 12-well plates and cultured in DMEM low-glucose medium containing 10% fetal bovine serum in 5% CO. 2 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-deficient serum (LPDS), and the subsequent groups were the administration groups (20 μM) of different monomer compounds, which were cultured with DMEM low-glucose medium containing 5% LPDS. Cultur...

Embodiment 3

[0058] Example 3 Some monomeric compounds in Gynostemma pentaphyllum from Hunan origin and Guangxi origin have significant PCSK9 reducing activity on HepG2 cells under the condition of 10 μM drug concentration and total Gynostemma glycosides

[0059] Human hepatoma 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, and cultured in DMEM low-glucose medium containing 10% fetal bovine serum. %CO2 in a 37°C incubator; after inoculation, these groups of cells were treated as follows: the first group was a blank group, cultured with DMEM low-glucose medium containing 5% FBS, and the second group was a model group, Cultured with DMEM low-glucose medium containing 5% LPDS, and then several groups were respectively treated with different monomer compounds (10 μM) or total glycosides (50 μg / mL) were cultured with DMEM low-sugar medium containing 5% LPDS, The blank group was treated for 48...

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Abstract

The invention relates to the technical field of natural medicinal chemistry, in particular to dammarane-type triterpenoid saponin compounds separated from Gynostemma pentaphyllum from Hunan and Guangxi origin, and the preparation of dammarane-type triterpenoid saponins for inhibiting PCSK9 from exerting lipid-lowering effects applications in . Part of the monomeric compounds in Gynostemma pentaphyllum from Hunan origin and Guangxi origin of the present invention have different degrees of inhibitory activity on the secretion of PCSK9 by hepatocytes, so as to achieve the purpose of lowering lipids alone or synergistically with statins to enhance the lipid-lowering effect.

Description

technical field [0001] The invention relates to the technical field of natural medicinal chemistry, in particular to a dammarane-type triterpenoid saponin compound isolated from Gynostemma pentaphyllum from Hunan and Guangxi and its application in the preparation of a drug for inhibiting PCSK9 and exerting 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] Over the past 20 years, statin use has successfully reduced the risk of cardiovascular events. Statins are inhibitors of 3-hydroxy-3-methyl-glutaryl coenzym...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K31/704A61P3/06C07H15/256C07H17/07C07H1/08C07J17/00C07J71/00
CPCA61P3/06A61K31/7048C07H1/08C07H17/07A61K31/704C07H15/256C07J17/005C07J71/0005
Inventor 姜新宇刘朝辉张增勤
Owner 湖南华宝通制药有限公司
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