Application of Chinese prickly ash extract to preparation of medicament for regulating cholesterol metabolism

A technology of prickly ash extract and cholesterol, applied in metabolic diseases, drug combinations, antipyretics, etc.

Inactive Publication Date: 2014-03-12
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Zanthoxylum bungeanum belongs to the Rutaceae plant. In the two classic works of "Medicine Properties" and "Bie Lu", there are records of Zanthoxylum bungeanum breaking blood, removing old blood and unblocking blood vessels. Modern pharmacological research has found that it has strong antioxidant and anti-inflammatory effects Amides and flavonoids also have anti-platelet aggregation and anti-lipid peroxidation damage in vitro. It has also been reported that volatile oil of peppercorns can improve liver cholesterol and lipoprotein metabolism in guinea pigs, but whether other parts can improve cholesterol metabolism regulation has not yet been established. see the report

Method used

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  • Application of Chinese prickly ash extract to preparation of medicament for regulating cholesterol metabolism
  • Application of Chinese prickly ash extract to preparation of medicament for regulating cholesterol metabolism
  • Application of Chinese prickly ash extract to preparation of medicament for regulating cholesterol metabolism

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of effective parts of Zanthoxylum bungeanum

[0028]Dahongpao Zanthoxylum bungeanum fruit (purchased from Hanyuan City, Sichuan Province) 15kg, put into the extraction tank of the heating extraction and concentration unit, add 3kg each time, add 3 times the volume of 95% ethanol, turn on the heating system of the extraction tank, and heat at 50°C for 30 minutes , so that the soluble components are dissolved in the ethanol in the extraction tank; then the extract is pumped into the concentration tank through the suction filter tube, and the concentration tank system and heating system are turned on to keep the temperature of the concentrated juice at about 60°C and the vacuum degree at - 0.05 to -0.08MPA, the secondary steam generated during concentration passes through the condenser and cooler, becomes condensate and returns to the extraction tank, and is added to the medicine as a new solvent. The new solvent passes through the medicinal material l...

Embodiment 2

[0029] Example 2 Effect of Zanthoxylum bungeanum extract on cholesterol metabolism of HepG2 cells in vitro

[0030] Grouping: After recovery of HepG2 cells, transfer them to culture dishes with 10% FBS-containing DMEM (high glucose) medium, and store them at 37°C, 5% CO 2 Cultured under conditions, the cells were synchronized for 6-12 hours, and randomly divided into 6 groups, namely: ①normal control group; ②model group: cholesterol 10ug / mL+25-hydroxycholesterol 1ug / mL; ③positive control group: simvastatin 0.2ug ④Petroleum ether extract group 0.05mg / ml; ⑤Ethyl acetate extract group 0.05mg / ml; ⑥N-butanol extract group 0.05mg / ml; Treated self-control. Dosing: After changing the serum-free medium and synchronizing for 12 hours, add 5ul of absolute ethanol to the normal control group and the model group, pre-administer 12 hours to the drug group, and then add or not add cholesterol to the model group, positive control group and drug group 10ug / mL + 25-hydroxycholesterol 1ug / mL, ...

Embodiment 3

[0032] Example 3 Effect of Zanthoxylum bungeanum extract on cholesterol metabolism in C57BL\6 mice

[0033] Grouping: 36 C57BL\6 mice were randomly divided into 6 groups: ①normal control group (n=6), ②model group (n=6); ③positive drug group (dexamethasone, 5mg / kg, n=6 ); ④ petroleum ether extract group (400mg / kg, n=6); ⑤ ethyl acetate extract group (400mg / kg, n=6); ⑥ n-butanol extract group (400mg / kg, n=6 ). Administration: Zanthoxylum bungeanum extract was dissolved in 50% soybean oil, mixed evenly to make an emulsion, and administered by intragastric administration once a day. The mice in the model group and the normal control group were intragastrically administered 50% soybean oil emulsion in the same volume. Seven days later, the positive drug group was intraperitoneally injected with 5 mg / kg of dexamethasone, and 2 hours later, all mice except the normal control group were intraperitoneally injected with LPS 0.2 mg / kg. After 2 hours, the eyeballs were removed to take b...

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Abstract

Belonging to the field of pharmacy, the invention relates to application of a Chinese prickly ash extract to preparation of medicaments for regulating cholesterol metabolism. In particular, the invention relates to regulation of cholesterol metabolism by a petroleum ether extract, an ethyl acetate extract and an n-butanol extract in high cholesterol and inflammation states. In vitro experiments show that in high cholesterol condition, the extracts can reduce the content of total cholesterol and secretion of an apolipoprotein B, inhibit the expression of related genes and proteins in a cholesterol biosynthesis pathway in cells, increase the expression of related genes or proteins in a reverse cholesterol transport process in cells. In vivo experiments prove that the ethyl acetate extract and n-butanol extract have anti-inflammatory activity, and improve the accumulation of inflammation-induced cholesterol in the liver by affecting expression of a liver X receptor-alpha and an ATP-binding cassette transporter gene 1. The invention further provides monomer (-)-syringaresinol-4-O-beta-D-glucoside isolated from the n-butanol extract and application thereof to regulation of cholesterol metabolism.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a new medicine application of pepper alcohol extract. In particular, it relates to the use of Zanthoxylum bungeanum extract in preparing drugs for regulating cholesterol metabolism. Background technique [0002] According to reports, the improvement of living conditions and the advancement of urbanization have partly led to the rapid increase in the development rate of cardiovascular diseases in Asia. Studies have shown that high cholesterol often causes atherosclerosis, leading to clinical coronary heart disease, high blood pressure, and later fatal diseases such as myocardial infarction and stroke. With the deepening of research, the role of inflammation in the pathogenesis of atherosclerosis has also been discovered and elucidated. It is believed that both infection and inflammation can cause lipid and lipoprotein metabolism disorders. Therefore, the development of Drugs for cholesterol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/758A61K31/7048A61P3/06A61P29/00
Inventor 朱依谆吴婷婷
Owner FUDAN UNIV
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