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Application of deferoxamine to preparation of medicine for treating nonalcoholic fatty liver

A technology for preparing drugs and deferoxamine, which can be used in drug combinations, active ingredients of amides, digestive system, etc., and can solve problems such as difficult adherence of patients

Active Publication Date: 2017-09-22
INST OF GENETICS & DEVELOPMENTAL BIOLOGY CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, calorie restriction and exercise are the only effective means to treat NAFLD, but it is often difficult for most patients to adhere to

Method used

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  • Application of deferoxamine to preparation of medicine for treating nonalcoholic fatty liver
  • Application of deferoxamine to preparation of medicine for treating nonalcoholic fatty liver
  • Application of deferoxamine to preparation of medicine for treating nonalcoholic fatty liver

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Desferoxamine mesylate used in Example 1 and Example 2 is Desfer (deferoxamine mesylate for injection), which is white to off-white loose block or powder, Novartis Pharma Stein AG (Swiss Novartis Pharmaceutical Co., Ltd.), import drug registration certificate number H20140678. The deferoxamine mesylate used in Example 3 was produced by Sigma-Aldrich (Shanghai) Trading Co., Ltd., product number D9533.

[0046] The structural formula of deferoxamine mesylate is shown in formula (I).

[0047]

[0048] Desferoxamine mesylate solution: dissolve deferoxamine mesylate in sterilized 0.9% physiological saline solution, so that the concentration of deferoxamine mesylate is 0.00625 g / ml.

[0049] HepG2 cells (human liver cancer cells): American Type Culture Collection.

[0050] Embodiment 1, animal test

[0051] 1. Group processing

[0052] Take 17.5~23.3g, 6-8 week old male C57BL / 6 mice, feed them adaptively for 2 weeks, then divide them randomly into four groups (8 mice i...

Embodiment 2

[0071] Embodiment 2, animal test

[0072] 1. Group processing

[0073] 16.7-21.3g, 6-week-old male C57BL / 6 mice were taken, fed for 2 weeks, and then tested. The test was divided into two consecutive stages.

[0074] The first stage is as follows:

[0075] The mice were randomly divided into two groups, a control group (25) and a model group (55);

[0076] Control group (CTR): fed with common feed for 18 weeks;

[0077] Model group (HCD): fed with high-cholesterol diet for 18 weeks.

[0078] After 18 weeks of the first stage (time point 1), 5 mice were randomly selected from each group to be killed, and the method in step 2 of Example 1 was used for relevant detection. The remaining mice proceeded to the second stage.

[0079] The second stage is as follows:

[0080] The remaining 20 control mice were randomly divided into two groups, a blank control group and a drug control group, with 10 mice in each group.

[0081] The remaining 50 mice in the model group were random...

Embodiment 3

[0092] Embodiment 3, cell experiment

[0093] HepG2 cells were starved for 24 hours, and then divided into three groups, which were treated as follows:

[0094] Blank control group: cultured in basal medium containing 10g / 100mL BSA for 24h;

[0095] Model group: cultured in basal medium containing 10g / 100mL BSA and 100μg / ml cholesterol for 24h;

[0096] Treatment group: cultured in basal medium containing 10 g / 100 mL BSA, 100 μg / ml cholesterol and 50 μM deferoxamine mesylate for 24 hours.

[0097] After completing the above grouping treatment, discard the culture supernatant, wash the cells with PBS buffer, then add 4% PFA solution and fix at 37°C for 10min, then soak with 60% isopropanol solution for 30s, and then use Oil Red O working solution After staining for 30 min, 60% isopropanol solution was added to wash, and then washed three times with PBS buffer, and then the staining was observed under a microscope (Nikon ECLIPSE Ti). see photos Figure 5 . Compared with the...

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Abstract

The invention discloses a novel usage of deferoxamine, namely application of the deferoxamine to preparation of a medicine for treating nonalcoholic fatty liver. The application of a substance A or a substance B or a substance C to the preparation of the medicine is protected for the first time; the substance A is the deferoxamine; the substance B is pharmaceutically acceptable salt of the deferoxamine; the substance C is a solvate of the deferoxamine; the medicine is used for treating and / or preventing fatty liver. The inventor proves that the deferoxamine can be used for remarkably relieving liver tissue pathological changes induced by high cholesterol through establishing a high-cholesterol animal model, alleviating injuries to liver cells and reducing intrahepatic lipid accumulation. The novel usage of the deferoxamine is developed, and a new way is provided for treating the nonalcoholic fatty liver.

Description

technical field [0001] The invention relates to a new application of deferoxamine, that is, the application of deferoxamine in the preparation of medicine for treating nonalcoholic fatty liver. Background technique [0002] Non-alcoholic fatty liver disease (NAFLD) refers to a clinicopathological syndrome characterized by excessive fat deposition in liver cells caused by alcohol and other definite liver-damaging factors. Clinical symptoms and signs can develop into cirrhosis and liver cancer. [0003] In recent years, with the improvement of living standards, the incidence of NAFLD has been increasing year by year. About 14% to 24% of the general population suffer from NAFLD, which has become one of the most common liver diseases. [0004] At present, calorie restriction and exercise are the only effective means to treat NAFLD, but it is often difficult for most patients to adhere to. Therefore, it is necessary to develop effective drugs for the treatment of NAFLD. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/16A61P1/16
CPCA61K31/16
Inventor 税光厚王饶旭
Owner INST OF GENETICS & DEVELOPMENTAL BIOLOGY CHINESE ACAD OF SCI
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