Natural PPAR gamma receptor stimulant as well as preparation method and application thereof

A receptor agonist, natural technology, applied in steroids, metabolic diseases, organic chemistry, etc.

Active Publication Date: 2021-03-05
XIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These research results further indicate that it is more likely to find new lead compounds of PPARγ receptor agonists with less side effects

Method used

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  • Natural PPAR gamma receptor stimulant as well as preparation method and application thereof
  • Natural PPAR gamma receptor stimulant as well as preparation method and application thereof
  • Natural PPAR gamma receptor stimulant as well as preparation method and application thereof

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Experimental program
Comparison scheme
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Embodiment Construction

[0031]The present invention will be described in detail below with reference to the accompanying drawings and specific embodiments.

[0032]The method of preparation of a natural PPAR gamma agonist is implemented in accordance with the following steps:

[0033]Step 1: Plant extraction

[0034]Step 1.1: After pulverizing the hawthorn dry, the total extract is obtained with 75% industrial ethanol;

[0035]Step 1.2: Practice the dipper into the water, degreased by 3 times volume of petroleum ether degreasing, and the petroleum ether is obtained;

[0036]Step 1.3: The extracted phase of step 1.2 was added 3 times the volume of ethyl acetate, and the ethyl acetate is obtained.

[0037]Step 2: Separate purification

[0038]Step 2.1: Ethyl acetate extract obtained by step 1.3 is added to a solvent such as ethyl acetate, petroleum ether, methanol, etc., mixed with dry silica gel (200-300 mesh), and stir well, stir well. To enable the sample to be completely adsorbed by silica gel, after the solvent is evaporate...

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Abstract

The invention discloses a PPAR gamma receptor stimulant as well as a preparation method and application thereof. One receptor stimulant is ursolic acid extracted from asiatic cornelian cherry fruit. The preparation method specifically comprises the following steps: step 1, preparing an asiatic cornelian cherry fruit extract; and step 2, separating and purifying the asiatic cornelian cherry fruit extract obtained in the step 1 to obtain the receptor stimulant. The invention provides a novel natural PPAR gamma receptor stimulant, and the relative average intensity of the firefly luciferase activity and the internal control renilla luciferase activity of the compound is equivalent to that of the full stimulant rosiglitazone of the PPAR gamma receptor under the concentration of 3 microns; theresearch result provides a lead compound for research and development of novel natural antidiabetic drugs.

Description

Technical field[0001]The present invention belongs to a nuclear receptor hyperfront to activate the transcription factor preparation technique, and it is related to a natural PPAR gamma receptor agonist, and also relates to the preparation method and application of the above activation receptor agonist.Background technique[0002]Peroxide Media Proliferative Activation Receptor (PPARγ), PPARγ is highly expressed in fat cells, spleen, adrenal and colon, low expression of liver, kidney, brain, skeletal muscle. Among them, PPARγ research is most in-depth and is one of the most common targets of anti-diabetic drugs. It plays an important regulatory role in the proliferation and differentiation of various cells, activating PPARγ has the effect of promoting adipocyte differentiation, anti-atherosclerosis, and reduces inflammation, treatment of cancer. At present, new PPAR gamma agonists seeking non-side effects or side effects and their mechanisms have been developed to become one of the ho...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61P3/10
CPCC07J63/008A61P3/10
Inventor 何仰清李佳庆张丹杨谦
Owner XIAN UNIV OF TECH
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