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New application of axitinib

A technique for obesity, disease, applied in the field of medicinal chemistry

Active Publication Date: 2016-02-03
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

In recent years, it has also been found that axitinib has the effect of treating non-small cell lung cancer and leukemia, but it has not been reported that axitinib can promote the browning of white adipocytes

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Axitinib dose-dependently promotes browning of white adipocytes in vitro

[0025] Isolation of white adipose-derived mesenchymal cells in the groin

[0026] 1) Take an adult mouse about 10 weeks old, kill it by neck dislocation, soak it in 75% alcohol for 5 minutes, then transfer it to the operating table, and take out the white fat in the groin;

[0027] 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) for 1g adipose tissue, and place it at 37°C for 40 minutes;

[0028] 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;

[0029] 4) The supernatant layer after centrifugation is mature adipocytes, which is transferred to a centrifuge tube filled with PBS solution, mixed evenly and then centrifuged again. The upper mature adipocytes separated again can be...

Embodiment 210

[0055] Example 210-week-old mice were fed with a high-fat feed while feeding with axitinib at a dose of 10 mg / kg, and the blank group was fed with the same dose of PBS. After 8 weeks, the brown color of the white adipocytes in the groin was detected. Changes in weight and body weight of mice and internal organs.

[0056] Gene expression characterization of adipose tissue

[0057] RNA extraction: using the Trizol method to extract, the specific operation is as follows:

[0058] Weigh 100 mg of adipose tissue isolated from mice, then add 1 ml of Trizol, grind it with a mortar for 30 minutes, and then transfer it to an EP tube; the rest of the steps are the same as the identification of gene expression in adipocytes.

[0059] The result is as figure 2 , image 3 and Figure 4 As shown, compared with the control group, the expression of UCP1 in iBAT and iWAT in axitinib-administered mice was significantly increased, the body weight was significantly decreased, and the weight ...

Embodiment 310

[0060] Example 3 10-week-old mice were fed with a high-fat diet while being fed with axitinib at a dose of 10 mg / kg. After 8 weeks, the glucose tolerance and insulin sensitivity in the body were detected.

[0061] Glucose Tolerance and Insulin Tolerance Tests

[0062] Prepare 20% glucose solution with physiological saline, then inject mice according to the dose of 2g glucose / kg body weight, and intraperitoneally inject mice that have fasted for 12 hours (9 o'clock in the evening to 9 o'clock in the morning of the next day). The blood glucose concentration of mice at different time points (15 minutes, 30 minutes, 60 minutes, 120 minutes) before injection (0 minute) and after injection was monitored with a blood glucose meter, and the time error was controlled within 5 seconds.

[0063] The insulin dose used in the insulin resistance test was 0.5 unit / kg body weight. However, the fasting time is 6 hours (9 am to 3 pm), and the rest of the operation methods are consistent with t...

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Abstract

The invention discloses new application of axitinib. Axitinib can be used for preparing medicine for promoting white fat cell browning and used for preventing and treating obesity and diseases related to obesity. The medicine can promote primary white fat cell browning in vitro, thereby enhancing expression of brown fat cell marker gene uncoupling protein 1 (UCP1), and can promote the increase of beige fat cells in white fat tissue of groin and the increase of expression of UCP1; the medicine can resist obesity and insulin insensitivity caused by high-fat diet and has an effect on treating fatty livers.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a new application of axitinib. Background technique [0002] Obesity refers to the obvious thick fat layer and overweight to a certain extent, which are mostly caused by the energy imbalance of the body's metabolism. At present, with the economic development and the improvement of people's living standards, the pressure of life and work continues to increase, and the number of obese patients continues to rise around the world. Obesity is not only an independent disease, but also a risk factor for type 2 diabetes, vascular disease, hypertension, stroke and various cancers, and is listed by the World Health Organization as one of the risk factors leading to disease burden. [0003] While understanding the health hazards of obesity, people realize that it is urgent to develop safe and effective weight loss drugs. Unfortunately, the number of drugs currently used for weight contr...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61P3/04A61P3/00A61P3/10A61P1/16
Inventor 吴东海毛刘锋聂涛丁克
Owner GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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