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Application of sea cucumber long-chain alkali and derivatives thereof in preparation of products for regulating PPAR-gamma

A derivative and long-chain technology, which is applied in the application field of sea cucumber long-chain base and its derivatives in the preparation and regulation of PPAR-γ products, and achieves the effect of broad market prospects

Pending Publication Date: 2022-03-22
OCEAN UNIV OF CHINA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still no research on sea cucumber long-chain alkaloids and their derivatives as PPAR-γ regulators

Method used

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  • Application of sea cucumber long-chain alkali and derivatives thereof in preparation of products for regulating PPAR-gamma
  • Application of sea cucumber long-chain alkali and derivatives thereof in preparation of products for regulating PPAR-gamma
  • Application of sea cucumber long-chain alkali and derivatives thereof in preparation of products for regulating PPAR-gamma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1: PPAR-γ transactive test

[0050] The use of the long chain base (LCB) and / or their pharmaceutically acceptable salts of the present invention as the PPAR-gamma modifier in PPAR-γ-related diseases will be described by the conventional experiments described below.

[0051] The activation of the PPAR-γ receptor causes gene expression by an agonist (activator) in the human cervical cancer cell line (HELA cell line), and the luciferase will be emitted in the presence of a substrate. In the presence of a reference agonist, the regulation of the PPAR-γ receptor is measured by quantifying fluorescence generated after the cell culture. The ligand replaces the agonist from its site. The measurement of the activity is carried out by measuring the amount of light produced. This method of determining the compound of the invention is possible to determine the regulatory activity of the compound of the invention by measuring the molecules to be tested. Since this value can fl...

Embodiment 2

[0052] Example 2: Evaluation of the compound of the invention in a 3T3-L1 pre-fat cell model

[0053] The PPAR-γ regulation activity of the compound of the present invention is determined by measuring the mechanism of the long chain alkali 1 (LCB1, D17: 1) on the energic differentiation of the forekin cells.

[0054] 3T3-L1 cells were cultured in 5% CO2, 37 ° C incubator with a DMEM containing 10% FBS. Cells were converged to 90% or so. The concentration of the cells was adjusted and added to a 24-well plate, so that the number of cells per well was 2 × 104. After the cells were full and contacted inhibition of 48h, they were exchanged to contain FBS (10%), 3-isobutyl-1-methyl xanthine (0.5m mol / L), dexamethasone (1 μmol / L), insulin ( Continue in a fully medium medium in 10 μg / mL. After 48 h, a high sugar DMEM medium containing insulin (10 μg / mL) and FBS (10%). After each 2D, the serum volume fraction is 10% high sugar DMEM complete culture solution. A culture solution con...

Embodiment 3

[0055] Example 3: Evaluation of the compounds of the invention in a dietary induction obesity mouse model

[0056] The PPAR-γ regulation activity of the compound of the present invention is determined by measuring the regulation of fatty mice, blood fat, blood glucose, etc. of obese mice by measuring lepid base 1 (LCB1, D17: 1).

[0057] C57BL / 6 mice were divided into 4 groups: a low fat control group (LOW FAT, LF), high-fat obese group (HIGHFAT, HF), and high fat addition of 0.01% long chain base group (LCB). In addition to the low fat group, feed high-fat feed (22.5% (w / w) fat, 40% (w / w) sucrose), oral glucose tolerance experiment (OGTT) was carried out after 4 weeks. After another week, the mice were sacrificed and serum Tg and insulin were determined. The results show that LCB significantly inhibits high-fat mice oral glucose concentration and reduces blood insulin content, and has significant improved effect on insulin sensitivity and insulin resistance. Figure 4 A and ...

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Abstract

The invention relates to a new application of a sea cucumber-derived long-chain alkali compound and a derivative thereof, in particular to an application of sea cucumber long-chain alkali and a derivative thereof in preparation of a product for regulating PPAR-gamma. The sea cucumber long-chain alkali comprises d17: 1, d18: 1, d18: 2 and t17: 0; the derivative comprises precursor ceramide of sea cucumber long-chain alkali and glucocerebroside. Experiments prove that the sea cucumber long-chain alkali and the derivatives thereof significantly regulate the activity of PPAR-gamma, the effect of the sea cucumber long-chain alkali and the derivatives thereof as PPAR-gamma regulators is verified for the first time, and a new way is provided for treatment of related diseases targeting PPAR-gamma.

Description

Technical field: [0001] The present invention relates to a new use of sea-cucumber-oriented long-chain base compounds and their derivatives, and particularly to sea-cucumber long chain bases and their derivatives in preparing to regulate PPAR-γ articles. Background technique: [0002] Peroxisome Proliferator-Activated Receptor, PPAR is a class of ligand activated nuclear transcription factors super family members. Peroxisome is a subcateic structure in vivo, which includes removing molecular oxygen and hydrogen peroxide, and related to sugar, lipid, cholesterol, cholic acid synthesis and fatty acid oxidation. A series of natural or artificially synthetic fatty acid chemicals can stimulate the proliferation of peroxidase, referred to as Peroxisome ProLiferation. Peroxidase proliferation can activate its receptor, thereby triggeting a series of biological effects, so that this type of receptor is referred to as a peroxidase proliferative agent (PPAR). PPAR includes three phenotypes...

Claims

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Application Information

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IPC IPC(8): A61K31/133A23L33/10A61P5/50A61P3/06A61P29/00A61P9/10A61P35/00A61P25/16A61P43/00
CPCA61K31/133A61P5/50A61P3/06A61P29/00A61P9/10A61P35/00A61P25/16A61P43/00A23L33/10A23V2002/00A23V2200/328A23V2200/326A23V2200/30A23V2250/2042
Inventor 王玉明王成成张恬恬薛长湖徐杰薛勇李兆杰毛相朝王静凤姜晓明常耀光唐庆娟丛培旭
Owner OCEAN UNIV OF CHINA
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