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Fatty acid synthase inhibitor and application thereof

A fatty acid synthase and inhibitor technology, applied in the field of fatty acid synthase inhibitors, can solve the problems of low FAS activity and expression, and achieve the effects of fat content control, growth inhibition, and clear targets

Inactive Publication Date: 2013-01-02
CHINA ACAD OF SCI NORTHWEST HIGHLAND BIOLOGY INST +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In addition, many studies have found that in almost all non-pathological adult tissues, the activity and expression of FAS show extremely low levels

Method used

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  • Fatty acid synthase inhibitor and application thereof
  • Fatty acid synthase inhibitor and application thereof
  • Fatty acid synthase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 A fatty acid synthase inhibitor which contains 65% compound A and 30% compound B.

[0029] Wherein: Compound A is a compound with the 3'-substituent R in the structure shown below being -OH; compound B is a compound with the 3'-substituent R being -H in the structure shown below.

[0030]

[0031] The above-mentioned fatty acid synthase inhibitor was dissolved in DMSO as the test sample solution, and the test was carried out with the above-mentioned standard determination method of fatty acid synthase activity. The results showed that the inhibitor had a strong inhibitory effect on fatty acid synthase, and it was half inhibitory. The concentration IC50 value is 19 μg / mL.

[0032] The IC50 value of EGCG, a known and common fatty acid synthase inhibitor, is 24 μg / mL. The lower the IC50 value of the half-inhibitory concentration, the stronger the inhibitory activity, which shows that the inhibitor of the present invention has stronger activity than EGCG (see experimen...

Embodiment 2

[0033] Example 2 A fatty acid synthase inhibitor containing more than 95% of compound A. Among them, compound A is a compound in which the substituent R at the 3'position in the structure shown below is -OH.

[0034]

[0035] Take the above fatty acid synthase inhibitor and dissolve it in DMSO as the test sample solution. Use the above standard determination method for fatty acid synthase activity to test. The results show that the inhibitor has a strong inhibitory effect on fatty acid synthase, half The IC50 value of the inhibitory concentration is 26 μg / mL.

[0036] The IC50 value of EGCG, a known and common fatty acid synthase inhibitor, is 24 μg / mL. The lower the IC50 value of the semi-inhibitory concentration, the stronger the inhibitory activity, which shows that the inhibitor of the present invention has an activity equivalent to EGCG (see experimental results) figure 2 ).

Embodiment 3

[0037] Example 3 A fatty acid synthase inhibitor containing more than 95% compound B. Among them, compound B is a compound in which the 3'-position substituent R is -H in the structure shown below.

[0038]

[0039] Take the above-mentioned fatty acid synthase inhibitor and dissolve it in DMSO as the test sample solution. Use the above-mentioned standard determination method for fatty acid synthase activity to test. The results show that the inhibitor has a good inhibitory effect on fatty acid synthase, and half The IC50 value of the inhibitory concentration is 40 μg / mL.

[0040] The IC50 value of EGCG, a known and common fatty acid synthase inhibitor, is 24 μg / mL. The lower the IC50 value of the semi-inhibitory concentration, the stronger the inhibitory activity, which shows that the inhibitor of the present invention has an activity equivalent to EGCG (see experimental results) image 3 ).

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Abstract

The invention relates to a fatty acid synthase inhibitor which is prepared by being extracted from natural plant or being chemically synthesized. The fatty acid synthase inhibitor comprises at least one compound shown in the specification, wherein substituent group R of bit 3' can be independently -H or -OH. The fatty acid synthase inhibitor can be applied to preparing a weight-reducing medicine, a medicine for treating cancer, health-care food and functional cosmetics.

Description

Technical field [0001] The invention involves a fatty acid enzyme inhibitor and its application. Background technique [0002] About 1.2 billion human body in the world is overweight and at least 300 million people are obesity. Reducing fatty acid synthesis of obese people may be an effective treatment for obesity.Fatty acid enzymes (FAS) are the most important enzymes in the process of synthesis of biological cells.Tian Weixi and others proposed to control fatty acid enzyme activity as the theory of controlling the effective method of animal body fat level (Tian Weixi, 1994. The regulation of the body fat level and fatty acid composite activity of animals. Chemistry of life, 14, (1): 184) EssenceIn 2000, the results of the study of mouse fatty acid enzymes such as LOFTUS such as Hopkins University proved that inhibiting fatty acid enzymes can cause the accumulation of propyate monocytic enzyme A.Express that the appetite decreases without affecting the ability of mice and decrea...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/7034A61K8/60A23L1/29A61P3/04A61P35/00A23L33/00
Inventor 王小艳马晓丰袁木荣王洪伦田维熙李平索有瑞尤进茂
Owner CHINA ACAD OF SCI NORTHWEST HIGHLAND BIOLOGY INST
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