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Novel hypolipidemic effect of piperine

A technology of piperine and blood lipid lowering, which is applied in the field of medicine, can solve the problem that the blood lipid lowering activity has not yet been reported, and achieve the effect of inhibiting the formation of atherosclerotic plaques.

Inactive Publication Date: 2019-03-01
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Modern pharmacological studies have shown that piperine has the effect of preventing atherosclerosis, but the blood lipid-lowering activity of piperine targeting calpain has not been reported

Method used

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  • Novel hypolipidemic effect of piperine
  • Novel hypolipidemic effect of piperine
  • Novel hypolipidemic effect of piperine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Serum levels of total TC, total TG, HDL-C and LDL-C in ICR mice under the action of piperine.

[0020] Experimental materials: 8-week-old ICR mice were purchased from Beijing Weitong Lihua Company; TC, TG, HDL-C and LDL-C assay kits were purchased from Nanjing Jiancheng Bioengineering Institute; piperine was purchased from Sigma Aldrich Company.

[0021] Experimental method: Mice were fed high-fat diet (10% lard, 3% cholesterol, 0.5% pig bile salt) for 3 weeks to establish a stable fat-bearing mouse model. The mice were randomly divided into 4 groups, namely: normal diet-control group, normal diet-piperine group, high-fat diet-control group and high-fat diet-piperine group. The piperine group was given 25 mg / kg of piperine, and the control group was given the corresponding solvent. After feeding the mice for 8 weeks, they were sacrificed and serum was collected. The levels of total TC, total TG, HDL-C and LDL-C in serum were measured respectively.

[0022]...

Embodiment 2

[0023] Example 2: Piperine regulates THP-1 macrophage cholesterol efflux.

[0024] Experimental materials: THP-1 monocytes were purchased from the National Experimental Cell Resource Sharing Service Platform (Beijing Headquarters); NBD-cholesterol was purchased from Shanghai Aibison Company; PMA was purchased from Sigma Aldrich Company.

[0025] Experimental method: take THP-1 mononuclear cells in the logarithmic growth phase, and count them to a concentration of 0.2×10 6 Cells / mL were seeded on 24-well plates, and the cells were cultured with 200nM PMA to differentiate into macrophages. After 72 hours, the RPMI-1640 cell culture medium was removed, and administered according to different experimental groups such as the control group (solvent), the positive control group (pioglitazone), and the administration group (piperine 5, 10, 25, 50, 100 μM). At the same time, cells were labeled with NBD-cholesterol. After culturing for 24 hours, the culture medium was removed and the ...

Embodiment 3

[0028] Example 3: Effect of piperine on cell viability of human THP-1 macrophages.

[0029] Experimental materials: resazurin and digitonin were purchased from Sigma Aldrich Company.

[0030] Experimental method: the concentration is 0.2×10 6 THP-1 mononuclear cells / mL in logarithmic growth phase were seeded on 96-well plates, cultured for 72 h under the induction of 200 nM PMA, and differentiated into macrophages. The RPMI-1640 cell culture medium was removed, and administered according to different experimental groups such as the control group (solvent), the positive control group (digitonin 50 μg / mL), and the administration group (piperine 50 and 100 μM). After culturing for 24 h, remove the culture medium and continue culturing with 0.1% resazurin for 4 h, then measure the absorbance in each well.

[0031] Experimental results: piperine does not affect the viability of human THP-1 macrophages at working concentrations (50 and 100 μM), and has no toxicity to cells, indica...

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Abstract

The invention discloses a novel hypolipidemic effect of piperine. The piperine significantly reduces serum total cholesterol TC, total triglyceride TG and low density lipoprotein cholesterol LDL-C levels in lipid-loaded ICR mice; the piperine concentration-dependently increases cholesterol efflux from human THP-1 macrophages, specifically upregulates ABCA1 protein levels, and acts similarly to calpeptin, a calpain inhibitor. The upregulation of the protein levels of ABCA1 by the piperine is achieved by inhibiting the activity of total calpain in cells. The piperine has the beneficial effect ofproviding a theoretical basis for further development of the piperine as a blood fat reducing medicament or a health food.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to a novel blood lipid-lowering effect of piperine. Background technique [0002] Hyperlipidemia (Hyperlipoidemia) refers to excessive blood lipid levels, which can cause atherosclerosis, coronary heart disease and other diseases that seriously endanger human health. The main manifestation of hyperlipidemia is that the content of high-density lipoprotein cholesterol (HDL-C) in serum decreases, while the content of lipids such as total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) Abnormally increased and deposited on the arterial intima, resulting in thickening and hardening of the arterial wall, narrowing of the lumen, and a decrease in the blood supply level of the blood supplying organs. Accompanied by the high incidence of myocardial infarction and cerebral thrombosis caused by dyslipidemia, especially hypercholesterolemia, the family and s...

Claims

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Application Information

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IPC IPC(8): A61K31/4525A61P3/06
CPCA61K31/4525A61P3/06
Inventor 王李梅王克威侯兴明
Owner QINGDAO UNIV
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