The invention also discloses application of dammarane triterpenoid saponin compound in preparation of drugs for inhibiting PCSK9 from playing role in lowering lipid

A technology of triterpene saponins and dammarane, which is applied in the field of natural medicinal chemistry, can solve the problems of lowering lipid-lowering activity and increasing PCSK9, and achieves the effect of guaranteeing blood-lipid-lowering activity and drug safety

Active Publication Date: 2021-01-29
湖南华宝通制药有限公司
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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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  • The invention also discloses application of dammarane triterpenoid saponin compound in preparation of drugs for inhibiting PCSK9 from playing role in lowering lipid
  • The invention also discloses application of dammarane triterpenoid saponin compound in preparation of drugs for inhibiting PCSK9 from playing role in lowering lipid
  • The invention also discloses application of dammarane triterpenoid saponin compound in preparation of drugs for inhibiting PCSK9 from playing role in lowering lipid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation method of the monomer compound in the Gynostemma pentaphylla of the place of origin of embodiment 1 Hunan and Guangxi

[0029] Take Gynostemma pentaphyllum medicinal materials from two producing areas respectively, extract twice by decoction, 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. Take the total saponin extract of Gynostemma pentaphyllum, 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, eluted with chloroform-methanol-water (100:0:0→0:100:0) gradient, TLC inspection, combined to obtain 5 fractions (Fr.a~Fr.i). Then repeated silica gel, ODS, Sephadex LH-20 col...

Embodiment 2

[0054] Example 2 Some monomeric compounds in Gynostemma pentaphyllum from Hunan and Guangxi have significant PCSK9-reducing activity on HepG2 cells at a concentration of 20 μM

[0055] 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 48h, th...

Embodiment 3

[0057] Example 3 Some monomeric compounds in Gynostemma pentaphyllum from Hunan and Guangxi production areas have significant PCSK9-reducing activity on HepG2 cells under the condition of 10 μM drug concentration and total gypenosides

[0058] 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, cultured with DMEM low-sugar medium containing 5% FBS, the second group was a model group, Cultivate with DMEM low-sugar medium containing 5% LPDS, and then several groups are the administration groups (10 μ M) of different monomer compounds or total glycosides (50 μ g / mL) and cultivate with DMEM low-sugar medium containing 5% LPDS, The blank...

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Abstract

The invention relates to the technical field of natural medicinal chemistry and particularly relates to a dammarane type triterpenoid saponin compound separated from gynostemma pentaphylla in Hunan and Guangxi production places, and application of the dammarane type triterpenoid saponin compound in preparation of a medicine for inhibiting PCSK9 from playing a role in lowering lipid. Part of monomeric compounds in gynostemma pentaphylla in Hunan and Guangxi places of origin have different degrees of inhibitory activity on PCSK9 secreted by hepatocytes, so the purpose of independently lowering lipid or enhancing the lipid lowering effect of gynostemma pentaphylla in Hunan and Guangxi places of origin is achieved.

Description

technical field [0001] The invention relates to the technical field of natural medicine chemistry, in particular to a dammarane-type triterpene saponin compound isolated from Gynostemma pentaphyllum in Hunan and Guangxi 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 coenzy...

Claims

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Application Information

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