Novel application of Linifanib

A technology of fat metabolism and cells, applied in the field of medicine

Active Publication Date: 2019-03-15
GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Linifanib, with the structure as formula (I), is a multi-target inhibitor of VEGF and PDGFR receptor family, which has obv

Method used

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  • Novel application of Linifanib
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  • Novel application of Linifanib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Isolation of primary adipose-derived mesenchymal cells of inguinal white fat

[0033] (1) Take a 12-week-old mouse with a C57BL / 6J background, kill it by neck dislocation, soak it in 75% alcohol for 5 minutes, then transfer it to the operating table, and remove the white fat in the groin;

[0034] (2) Wash 3 times with PBS, cut up the adipose tissue with scissors, add 10ml collagenase Ⅰ solution (prepared with D-Hanks solution, add 0.1g collagenase Ⅰ to 100ml) of 1g adipose tissue, and place it at 37°C for 40 minutes;

[0035] (3) Filter with a 250 μm filter membrane, add cell culture medium, then transfer to a centrifuge tube, and centrifuge at 1000 rpm for 3 minutes;

[0036] (4) The cells at the bottom after centrifugation are adipose-derived mesenchymal cells. After discarding the supernatant, suspend them with fresh culture medium, spread them on a culture plate, and change the medium the next day.

[0037] (5) The obtained adipose-derived mesenchymal ce...

Embodiment 2

[0041] Example 2 Real-time quantitative PCR analysis of the mRNA expression level of adipocyte browning marker genes

[0042] Get the adipocytes obtained from the complete differentiation of the primary adipose mesenchymal cells of the white fat of the groin described in Example 1, and replace the culture medium with a normal culture medium (the culture fluid of DMEM with 10% fetal bovine serum high glucose added) , while adding 0 μM (Control group) and 0.3 μM, 1 μM and 3 μM small molecule drug Linifanib to stimulate the adipocytes. After 24 hours, extract RNA and perform real-time quantitative PCR analysis, the steps are as follows:

[0043] RNA extraction: the specific operation is as follows:

[0044] 1) Add 300 μl RNA Lysis Solution and 300 μl RNA Diluent to the sample respectively, and let stand at room temperature for 5 minutes;

[0045] 2) Centrifuge at maximum speed for 5 minutes to absorb the supernatant;

[0046] 3) Add 0.5 times the volume of supernatant absolute...

Embodiment 3

[0062] Example 3 Western blot analysis Linifanib promotes the expression of Ucp1 protein in adipocytes

[0063] Get the adipocytes obtained by the primary adipose mesenchymal cell differentiation of the white fat of the groin described in Example 1, replace the culture medium with a normal culture medium (the culture medium of DMEM with 10% fetal calf serum high glucose added), At the same time, 0 μM (Control group), 0.3 μM, 1 μM and 3 μM drug Linifanib were added to stimulate the adipocytes. After 24 hours, extract the intracellular protein, and use the Western blot method to detect the change in the expression level of Ucp1 protein. The specific steps of Western blot are as follows:

[0064] (1) Glue dispensing: clean the glass plate and clean it with ddH 2 O rinse. Prepare a 12% separating gel, and load the sample after the gel is solidified.

[0065] (2) Sample treatment: rinse with PBS 2 to 3 times after removing the culture medium (cold PBS may cause the cells to fall...

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Abstract

The invention provides novel application of Linifanib. The Linifanib has the functions of promoting browning of white adipocytes, promoting the expression of an uncoupling protein 1 (Ucp1), promotingmRNA expression levels of browning marker genes PrDm16, Pgcl alpha, Cidea, Dio2 and Cox8b, inhibiting preadipocytes to be differentiated into adipocytes and remarkably inhibiting the adipocytes to generate mRNA expressions of marker genes Ppar gamma, Cebp alpha and Ap2. Therefore, the Linifanib has the functions of promoting the browning of the adipocytes and inhibiting generation of the adipocytes, so that the Linifanib plays an important role in preventing and treating diseases related to fat metabolism and has a great application prospect in prevention and development of drugs of adiposis,diabetes mellitus, fatty liver and hyperlipidaemia.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an application of Linifanib in preparing compositions, medicines or health care products for regulating fat metabolism. Background technique [0002] Obesity is increasing worldwide. Obesity and related diseases caused by it, such as insulin resistance, cardiovascular disease, tumor, hyperlipidemia, hypertension, type II diabetes, etc. seriously threaten human health. The imbalance between energy consumption and energy intake in the body is the main cause of obesity. Increasing energy consumption or reducing energy intake is an effective way to treat obesity. The main types of adipose tissue are white adipose tissue and brown adipose tissue. White adipose tissue is mainly composed of white adipocytes. White adipocytes contain huge lipid droplets, accounting for almost the vast majority of the entire cell. The nucleus is flat and located on the edge of the cell. The main func...

Claims

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Application Information

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IPC IPC(8): A61K31/416A61P3/04A61P3/10A61P3/06A61P1/16
CPCA61K31/416A61P1/16A61P3/04A61P3/06A61P3/10
Inventor 吴东海聂涛赵世亭张羽薇
Owner GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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