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Anti-insulin resistance adenosine monophosphate-activated protein kinase agonist

A technology of Aralis saponin and Aralia taibai, applied in the field of biomedicine, can solve problems such as difficulty, and achieve the effects of low price, strong AMPK agonistic activity, and few adverse reactions

Inactive Publication Date: 2012-12-12
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, Metformin's side effects on the digestive system, blood system, etc. make the decision of physicians to prescribe more difficult

Method used

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  • Anti-insulin resistance adenosine monophosphate-activated protein kinase agonist
  • Anti-insulin resistance adenosine monophosphate-activated protein kinase agonist
  • Anti-insulin resistance adenosine monophosphate-activated protein kinase agonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Effect of araloside on C2C12 muscle cell AMPK and its target protein ACC

[0024] The differentiated C2C12 muscle cells were randomly divided into 5 groups: (1) control group (0min group), C2C12 muscle cells; (2) 15min group, C2C12 muscle cells were collected with 1 μg / ml araloside for 15 minutes; (3 ) 30min group, C2C12 muscle cells were given 1μg / ml araloside for 30min to collect; (4) 60min group, C2C12 muscle cells were given 1μg / ml aralin for 60min to collect; (5) 120min group, C2C12 muscle cells were given 1μg / ml ml of araloside was collected in 120min.

[0025] Cells were washed with PBS (pH 7.4) pre-cooled to 0°C and transferred to pre-cooled lysate [Tris HCl 20, NaCl 50, NaF 50, NaF 4 P 2 o 7 50, Sucrose 250, Na 3 VO 42, DTT 1 (mmol / l) and 1% compound protease inhibitor]. BSA protein quantification kit for protein quantification. The samples were subjected to SDS-PGEA electrophoresis, and the proteins were transferred to polyvinylidene fluorid...

Embodiment 2

[0026] Example 2: Effects of Araloside on Glucose Uptake and Fatty Acid Oxidation in C2C12 Muscle Cells

[0027] Treat C2C12 muscle cells with 1ug / ml araloside for 15min, and use radioactive isotope-labeled glucose 2-deoxy-[1- 3 H]-glucose was used to detect the uptake of glucose by cells, and the release rate of CoA-SH was used to evaluate the activity of CPT-1. The results showed that araloside significantly increased the uptake of glucose by C2C12 myoblasts (see figure 2 left) and CPT-1 activity (see figure 2 right).

Embodiment 3

[0028] Example 3: Effect of araloside on insulin-resistant C2C12 muscle cells AMPK and its target protein ACC

[0029] The insulin-resistant C2C12 muscle cells were randomly divided into 5 groups: (1) control group (0min group), insulin-resistant C2C12 muscle cells; (2) 15min group, insulin-resistant C2C12 muscle cells were given 1 μg / ml The wood saponins were collected for 15 minutes; (3) 30 minutes group, insulin-resistant C2C12 muscle cells were given 1 μg / ml araloside for 30 minutes to collect; (4) 60 minutes group, insulin-resistant C2C12 muscle cells were given 1 μg / ml araloside for 60 minutes to collect (5) In the 120min group, insulin-resistant C2C12 muscle cells were collected with 1 μg / ml araloside for 120 minutes.

[0030] The detection method of AMPK and ACC is the same as in Example 1, and the experimental results show that araloside significantly increases the expression of phosphorylated AMPK and ACC in insulin-resistant C2C12 muscle cells (see image 3 ), sugg...

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Abstract

The present invention discloses an aralia chinensis saponin extract. According to the present invention, aralia chinensis root bark is subjected to reflux extraction with ethanol with a volume concentration percentage of 65-85%; the resulting extract liquid is filtered, and is subjected to merge concentration to obtain a material with a relative density of 1.01; the resulting material is extracted with water-saturated n-butyl alcohol; the resulting n-butyl alcohol layer is filtered, and is subjected to merge concentration to obtain an aralia chinensis saponin extract concrete with an aralia chinensis total saponin mass percentage of 60-80%; and the concrete is dried and crushed to obtain the aralia chinensis saponin extract, wherein the aralia chinensis saponin extract can be used for preparation of adenosine monophosphate-activated protein kinase (AMPK) agonists, the AMPK agonists can be used for a plurality of metabolic diseases such as diabetes, hypertension, dyslipidemia, obesity, and the like, and insulin resistance exists in the metabolic diseases. Compared with AMPK agonists in the prior art, the aralia chinensis saponin of the present invention has characteristics of strong AMPK agonism activity, less adverse reaction, low price, and easy availability.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a protein kinase agonist activated by adenosine monophosphate for anti-insulin resistance. Background technique [0002] Insulin resistance is common in people with diabetes and runs through the whole process of diabetes development. The incidence of insulin resistance in patients with type 2 diabetes exceeds 80%. Early prevention and treatment of insulin resistance is the key to avoiding the disease in susceptible people with type 2 diabetes. In addition, insulin resistance also exists in many metabolic diseases such as obesity, hypertension, and dyslipidemia. Currently, drugs that improve insulin resistance (insulin sensitizers) mainly include metformin and thiazolidinediones. Unfortunately, metformin's side effects on the digestive system, blood system, etc. make the decision of physicians to prescribe more difficult. Side effects such as edema, weight gain,...

Claims

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Application Information

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IPC IPC(8): A61K36/25A61P5/50A61P3/04A61P3/06A61P3/10A61P9/12
Inventor 奚苗苗李玉文文爱东关月翁琰崔佳
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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