Use of stilbene compounds derived from hemp leaves in preparation of lipid-lowering drugs

A technology of stilbenes and compounds, which can be used in pharmaceutical combinations, medical preparations containing active ingredients, pharmaceutical formulations, etc., and can solve problems such as unreported lipid-lowering activity.

Inactive Publication Date: 2018-12-18
NORTHWEST UNIV(CN)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the lipid-lowering activity of stilbene compounds in hemp

Method used

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  • Use of stilbene compounds derived from hemp leaves in preparation of lipid-lowering drugs
  • Use of stilbene compounds derived from hemp leaves in preparation of lipid-lowering drugs
  • Use of stilbene compounds derived from hemp leaves in preparation of lipid-lowering drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0028] Lipid-lowering effects of stilbene compounds 1-3 (HM1-HM3) derived from hemp leaves

[0029] 1. Macrophage cholesterol efflux assay

[0030] Raw264.7 mouse macrophages were placed in a 24-well plate at a final density of 5×10 per well 4 cells. After 6 hours, the medium was discarded and the cells were gently washed 3 times with phosphate buffered saline (PBS). Add 1 µCi / mL to 600 µL of Dulbecco's Modified Eagle (DMEM) medium containing 1% fetal bovine serum [ 3 H]-cholesterol calculation[ 3 H]- total cholesterol, and then added to each well, incubated for 24 hours.

[0031] Wash 3 times with PBS, incubate in 500 μL DMEM medium containing 1% fetal bovine serum for 4 hours in the presence or absence of 1.0 mg / L test sample, then add 100 μL high-density lipoprotein medium, the final concentration is 20 μg / mL , and continue to incubate for 6 hours. Collect the medium in a 1.5 mL microfluidic tube and centrifuge at 14,000 rpm for 10 min at room temperature to remove ce...

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Abstract

The invention discloses a use of stilbene compounds derived from hemp leaves in preparation of lipid-lowering drugs. The results of the Raw264.7 mouse macrophage and hepatoma cell HepG2 tests show that the cytotoxicity of three stilbene compounds is higher than 1 mg/L. Through improvement of ABCG1 and SR-B1 protein expression, discharge of [3H]-cholesterol of RAW264.7 macrophages is improved to high-density lipoprotein, at 1 mg/L, the significant difference from fenofibrate is produced, the expression of ABCA1, LDLR, SR-B1 and CYP7A1 proteins is significantly improved and the influence on PCSK9 is avoided. The above results show that the three stilbene compounds have low cytotoxicity and high activity to RCT-related protein expression. Through improvement of SR-B1 and LDLR protein expression and increasing of CYP7A1 protein expression, bile acid is synthesized so that the transfer of cholesterol to liver cells is improved. The stilbene compounds can be used as novel lipid-lowering drugs.

Description

technical field [0001] The invention relates to the application of stilbene compounds derived from hemp leaves in the preparation of lipid-lowering drugs. Background technique [0002] As a natural plant resource, hemp has been planted in my country for thousands of years, and it is widely used in textiles, medicine, food and other fields. So far, more than 700 monomeric compounds have been isolated from hemp plants, divided into cannabinoids and non-cannabinoids, including cannabinoids (divided into 10 main structural types and other types) , a total of more than 70 monomeric compounds), flavonoids (more than 20 monomeric compounds), stilbene compounds, triterpenoids, alkaloids and quinones, etc. It is precisely because of the rich chemical components in the hemp plant that it has many pharmacological activities. Studies on the biological activity of chemical components in hemp plants have shown that cannabinoids have anti-cancer, anti-emetic, anti-inflammatory, anti-edem...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/085A61P3/06
CPCA61K31/085A61P3/06
Inventor 刘庆超白乃生郭甜甜刘浪浪李国林刘甜韩稳荣卢英辉
Owner NORTHWEST UNIV(CN)
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