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Application of betulinic acid in promotion of fatty-acid oxidation

A technology of fatty acid oxidation and betulinic acid, applied in medical preparations containing active ingredients, digestive system, metabolic diseases, etc., can solve the problems of identification and judgment of long-term toxicity, increased energy consumption, etc., to reduce lipids Effects of deposition, improvement of fat metabolism, and weight loss of fat metabolism

Inactive Publication Date: 2018-11-09
SHANGHAI INST FOR ENDOCRINE & METABOLIC DISEASES
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug selectively inhibits the reuptake of 5-HT and NE, and its side effects are significantly less than those of previous drugs. Definite evaluation, and differential judgment of long-term toxicity will take time
2. Metabolic enhancers: adrenoceptor agonists that promote thermogenesis and thus increase energy expenditure, but their effects are still being studied
However, it has not been reported that betulinic acid can treat related diseases by promoting fatty acid oxidation.

Method used

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  • Application of betulinic acid in promotion of fatty-acid oxidation
  • Application of betulinic acid in promotion of fatty-acid oxidation
  • Application of betulinic acid in promotion of fatty-acid oxidation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Effects of betulinic acid on the body weight of obese mice induced by high-fat diet:

[0040] 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 ).

[0041] Experimental results show that betulinic acid can significantly inhibit the weight gain of mice fed a high-fat diet and treat obesity.

Embodiment 2

[0043] Effects of betulinic acid on the levels of key genes related to fatty acid oxidation in liver tissue, subcutaneous white adipose tissue and visceral white adipose tissue of hyperlipidemia mice:

[0044] The day before the end of the experiment, the mice were starved for 16 hours. At 9 a.m. the next day, the eyeballs were picked and blood was collected for subsequent measurement of relevant serum indicators. Mice were sacrificed by cervical dislocation. The corresponding tissue pieces were taken out from the mice and put into 1.5ml cryopreservation tubes and paraformaldehyde to fix the tissues. The tissue tubes were stored in liquid nitrogen for a short time, and then sorted and stored in a -80°C refrigerator until used in subsequent experiments. First, the inventors used real-time quantitative PCR to detect the expression of the key gene pyruvate dehydrogenase kinase 4 (PDK4) in fatty acid oxidation.

[0045] Pyruvate dehydrogenase kinase 4 (PDK4) is a key enzyme for ...

Embodiment 3

[0049] Effects of betulinic acid on serum β-hydroxybutyrate in hyperlipidemia mice:

[0050] The inventors used ELISA to detect the serum β-hydroxybutyric acid content of mice in the high-fat control group and the high-fat plus betulinic acid intervention group. As a result, it was found that the content of β-hydroxybutyric acid in the betulinic acid group of high-fat mice was significantly higher than that of normal high-fat mice (P Figure 4 ).

[0051] The experimental results showed that the fatty acid oxidation of the mice in the betulinic acid intervention group increased, that is, betulinic acid can promote the oxidation of fatty acids, which is also consistent with the results of Example 2.

[0052] In summary, the body weight of the high-fat mouse group treated with betulinic acid was significantly reduced, the key gene PDK4 in fatty acid oxidation was significantly up-regulated in different tissues, and the level of β-hydroxybutyric acid in serum was also significantl...

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Abstract

The invention discloses application of betulinic acid in promotion of fatty-acid oxidation and particularly relates to the application of betulinic acid in preparation of medicines for preventing or treating related diseases of fatty-acid oxidation. The application disclosed by the invention has the beneficial effects that a fat C57 mouse with high-fat feeding for modeling is adopted as a researchobject, and the experimental result shows that the gene levels of the high-fat mouse treated by betulinic acid and the fatty-acid oxidation are respectively and obviously increased in different tissues, and the content of beta-hydroxybutyric acid (beta-OHB) in serum is also increased, i.e., betulinic acid can promote fatty-acid oxidation. Meanwhile, the body weight of the high-fat mouse treated by betulinic acid is obviously reduced; the application provides actual evidence of betulinic acid for treating obesity, non-alcoholic fatty liver disease (NAFLD) and other diseases related to the fatty-acid oxidation, has important scientific value and medical significance, and meanwhile can provide precious experiences for developing more natural-medicine active components for treating related diseases by promoting the fatty-acid oxidation.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and in particular relates to the use of betulinic acid to prepare related medicines by promoting fatty acid oxidation. Background technique [0002] The Global Obesity Report released by the World Health Organization in 2014 pointed out that obesity is now a global epidemic, and at least 2.8 million deaths each year can be attributed to overweight or obesity. The most commonly used measure of overweight and obesity in adults is body mass index (BMI), which is weight in kilograms divided by height in meters squared (kg / m^2). "Overweight" was defined as a body mass index ≥ 25, and "obese" was defined as a body mass index ≥ 30. The 2016 study published in The Lancet collected data from 1975 to 2014 and provided a full picture of BMI trends in adults. In the past 40 years, the number of obese people in the world has exploded: in 1975, it was only 105 million, and it rose to 641 million in 2014. ...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P3/04A61P1/16A61P3/06
CPCA61K31/56A61P1/16A61P3/04A61P3/06
Inventor 宁光童蕾张志国韩璐宇袁依妮
Owner SHANGHAI INST FOR ENDOCRINE & METABOLIC DISEASES
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