A kind of natural ppar gamma receptor agonist and its preparation method and application

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

Active Publication Date: 2021-12-17
XIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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 from natural medicines. However, there are still few studies on seeking PPARγ receptor agonists from traditional Chinese medicinal materials.

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  • A kind of natural ppar gamma receptor agonist and its preparation method and application
  • A kind of natural ppar gamma receptor agonist and its preparation method and application
  • A kind of natural ppar gamma receptor agonist and its preparation method and application

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Embodiment Construction

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

[0032] A kind of preparation method of natural PPAR gamma agonist of the present invention, specifically implement according to the following steps:

[0033] Step 1: Plant Extraction

[0034] Step 1.1: After drying and crushing Cornus officinalis in the shade, extract the total extract with 75% industrial ethanol;

[0035] Step 1.2: Fully disperse the extract into water, degrease with 3 times the volume of petroleum ether, and obtain the petroleum ether part;

[0036] Step 1.3: The raffinate phase of step 1.2 was added to 3 times the volume of ethyl acetate for extraction, and spin-dried to obtain the ethyl acetate fraction.

[0037] Step 2: Separation and purification

[0038] Step 2.1: Add ethyl acetate, petroleum ether, methanol and other solvents to dissolve the ethyl acetate extract obtained in step 1.3, mix it with dry silica gel (20...

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Abstract

The invention discloses a PPARγ receptor agonist and its preparation method and application. The first receptor agonist is ursolic acid extracted from Cornus officinalis. Specifically, it is implemented according to the following steps: preparing the cornus officinalis extract; step 2: separating and purifying the cornus officinalis extract obtained in step 1 to obtain a receptor agonist. The present invention discloses a novel natural PPARγ receptor agonist. At a concentration of 3 μM, the relative average intensity of firefly luciferase activity and Renilla luciferase activity of the compound is the same as that of the full agonist of PPARγ receptor Rosiglitazone, the results of this study provide a lead compound for the development of new natural antidiabetic drugs.

Description

technical field [0001] The invention belongs to the technical field of preparation of ligand-activated transcription factors of the nuclear receptor superfamily, relates to a natural PPARγ receptor agonist, and also relates to a preparation method and application of the above-mentioned activated receptor agonist. Background technique [0002] Peroxide medium proliferator-activated receptor (PPARγ), PPARγ is highly expressed in adipocytes, spleen, adrenal gland and colon, and lowly expressed in liver, kidney, brain, skeletal muscle and other tissues. Among them, PPARγ is the most in-depth study and is one of the most commonly used targets for antidiabetic drug screening. It plays an important regulatory role in the proliferation and differentiation of various cells. Activating PPARγ can promote the differentiation of adipocytes, resist atherosclerosis, reduce the occurrence of inflammation, and treat cancer. At present, the search for new PPARγ agonists with no side effects ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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