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Application of betulinic acid as fatty acid synthase (FAS) inhibitor

A technology of betulinic acid and inhibitors, which is applied in the field of pharmaceutical preparation, can solve the problems of rough activity and poor extract activity, and achieve the effects of reducing fat synthesis, weight loss, and improving liver lipid deposition

Inactive Publication Date: 2018-09-04
SHANGHAI INST FOR ENDOCRINE & METABOLIC DISEASES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 2002, the National Natural Products Research Center of the United States began to extract FAS inhibitors from plants, and extracted more than a dozen active ingredients from 5 plants, which may be due to the non-selective inhibition of tannins or other factors, resulting in monomer The activity of the crude extract is poorer than that of the crude extract

Method used

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  • Application of betulinic acid as fatty acid synthase (FAS) inhibitor
  • Application of betulinic acid as fatty acid synthase (FAS) inhibitor
  • Application of betulinic acid as fatty acid synthase (FAS) inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Effects of betulinic acid on the body weight of obese mice induced by high-fat diet:

[0038] After one week of adaptive feeding with common feed, the mice were randomly divided into two groups, ten in each group, and the average initial body weight of the two groups of mice was guaranteed to be the same. The mice were fed with high-fat diet and high-fat diet plus betulinic acid for two months, and the mice were weighed every three days. There was no difference in the initial body weight of the two groups of mice, but the difference in body weight between the high-fat mice and the high-fat plus betulinic acid mice began to appear on the 7th day of administration, and the body weight of the high-fat plus betulinic acid group was lower than that of the high-fat group (P figure 2 ).

[0039] Experimental results show that betulinic acid can significantly inhibit the weight gain of mice fed a high-fat diet and treat obesity.

Embodiment 2

[0041] Effects of betulinic acid on liver tissue of high-fat mice:

[0042] Non-alcoholic fatty liver disease (NAFLD) is generally caused by lipid deposition in the liver, and triglyceride is the most important indicator. Therefore, at the end of the experiment, the mouse liver tissue was taken for liver TG determination.

[0043] The specific measurement method is as follows: Firstly, homogenate the tissue, add 500ul of 5% NP40 into a 1.5ml EP tube, take out about 30mg of liver specimen and put it in (record the specific weight). Grind twice at 45s*60HZ in an ice bath to make a homogenate. Then transfer all the sample supernatant to a 1.5mL centrifuge tube. Then put the 1.5ml EP tube in a 95-degree water bath for 5 minutes (a white precipitate formed), and let it stand at room temperature for 10 minutes; then put it in a 95-degree water bath for 5 minutes, and then let it stand at room temperature for 10 minutes. The maximum speed is 13300g, centrifuge for 2 minutes, room ...

Embodiment 3

[0047] Effects of betulinic acid on the expression and activity of fatty acid synthase (FAS) in hyperlipidemia mice:

[0048] Fatty acid synthase (FAS) is the most critical enzyme in fat synthesis. Inhibiting FAS can significantly reduce fat anabolism. Therefore, inhibiting FAS is one of the effective strategies for the treatment of obesity, NAFLD, cancer and other related diseases. Therefore, the inventors first detected the FAS activity in mouse liver.

[0049] The method for measuring FAS activity in liver tissue is as follows: using ultraviolet spectrophotometry. First, fresh liver tissue was weighed (according to the ratio of tissue mass (g):buffer volume (mL) of 1:5-10) and placed in a solution containing 8% sucrose, 1mmol / L EDTA (pH8.0), and 20mmol / L 2-Mercaptoethanol was homogenized in 0.1 mol / L potassium phosphate buffer (pH 7.0), centrifuged at 3000g, 4°C for 10 minutes; at 17000g, 4°C, for 90 minutes. Immediately take 10ul supernatant and add to 80ul buffer (0.14m...

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Abstract

The invention discloses application of betulinic acid as a fatty acid synthase (FAS) inhibitor and application of betulinic acid in preparation of a medicament for preventing or treating a disease taking FAS as target. Obese C57 mice modeled by high-fat feeding is adopted as a research object, experiment results show that the FAS of the high-fat mice treated with betulinic acid is significantly down-regulated in the aspects of gene level and protein level, and the FAS activity is also significantly down-regulated, that is, betulinic acid can inhibit FAS simultaneously from both expression andactivity. At the same time, the body weight of the high-fat mice treated with betulinic acid is significantly reduced, and the liver tissue indexes of the mice are also improved to a considerable extent. The application disclosed by the invention provides tangible evidence for the treatment of obesity, nonalcoholic fatty liver disease (NAFLD) and cancer related diseases by betulinic acid, has important scientific and medical significance, and can also provide valuable experience for development of more natural pharmaceutical active ingredients for treating diseases related to FAS.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and in particular relates to the application of betulinic acid as an inhibitor of fatty acid synthase, in particular to the use of betulinic acid as an inhibitor of fatty acid synthase (FAS) and the preparation of drugs related to FAS. Background technique [0002] Fatty Acid Synthase (FAS) is a key enzyme that catalyzes the synthesis of endogenous long-chain fatty acids from acetyl CoA and malonyl CoA, and is mainly expressed in brain, lung, liver, fat, lactating mammary gland and other tissues under normal conditions middle. At present, it is generally believed that FAS plays an important role in energy metabolism. Studies have shown that mice treated with FAS inhibitor cerulenin and C75 can reduce their food intake, increase energy consumption, and have a significant weight loss effect. At the same time, FAS is abnormally highly expressed in cancer cells, which is necessary for tumor grow...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P3/04A61P1/16A61P35/00
CPCA61K31/56A61P1/16A61P3/04A61P35/00
Inventor 宁光张志国童蕾穆倩傅雪
Owner SHANGHAI INST FOR ENDOCRINE & METABOLIC DISEASES
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