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New applications for linifanib

A technology of cell and fat metabolism, applied in the field of medicine, to achieve the effect of inhibiting the formation of fat cells and promoting browning

Active Publication Date: 2021-08-17
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 obvious inhibitory effect on KDR, Flt-1, PDGFRβ and FLT3, but its application in the field related to fat metabolism , not reported

Method used

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  • New applications for linifanib
  • New applications for linifanib
  • New applications for 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) A 12-week-old mouse with a C57BL / 6J background was killed by neck dislocation, soaked in 75% alcohol for 5 minutes, then transferred to the operating table, and the white fat in the groin was removed;

[0034] (2) Wash 3 times with PBS, cut up the adipose tissue with scissors, add 10ml of collagenase Ⅰ solution (prepared with D-Hanks solution, add 0.1g collagenase Ⅰ to 100ml) of 1g of 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 mesench...

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 a new application of Linifanib. Linifanib can promote the browning of white adipocytes, promote the expression of uncoupling protein 1 (Ucp1), and promote the mRNA expression levels of browning marker genes PrDm16, Pgclα, Cidea, Dio2, Cox8b, and at the same time, it can inhibit the differentiation of preadipocytes For mature adipocytes, it significantly inhibits the mRNA expression of adipogenic marker genes Pparγ, Cebpα and Ap2. It can be seen that Linifanib can not only promote the browning of adipocytes, but also inhibit the formation of adipocytes. It plays an important role in the prevention and treatment of fat metabolism related diseases, including the prevention and treatment of obesity, diabetes, fatty liver, hyperlipidemia and There are huge application prospects in drug development.

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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Patent Type & Authority Patents(China)
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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