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Novel targeted medicament targeted to brown adipose tissues for treating obesity

A brown adipose tissue, targeted technology, applied in the field of biomedicine, can solve the problems of hyperlipidemia, obesity, reduced tissue oxygen consumption, etc., and achieve the effect of reducing obesity, reducing the promotion of inflammation, and small changes in spatial position

Inactive Publication Date: 2015-02-11
JIANGSU PROVINCE HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the mouse Jhdm2a (a specific demethylase) gene knockout resulted in the loss of brown fat, although its food intake did not increase, it still caused obesity and high blood pressure due to reduced tissue oxygen consumption and glycerol release. The occurrence of lipemia

Method used

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  • Novel targeted medicament targeted to brown adipose tissues for treating obesity
  • Novel targeted medicament targeted to brown adipose tissues for treating obesity
  • Novel targeted medicament targeted to brown adipose tissues for treating obesity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Take a four-week-old C57BL / 6J male mouse, inject 10ul of green fluorescent FITC-labeled polypeptide (concentration: 1mM) into the mouse body through the tail vein of the mouse, cut off the neck after 10min to kill the mouse, and take fresh tissue (white fat tissue, brown adipose tissue, muscle tissue, liver tissue), and immediately protected from light by embedding in paraffin, sectioning, and directly observing the fluorescence under a laser confocal microscope, the results showed that only in the capillary network of brown adipose Obviously, suggesting that the polypeptide can indeed be targeted to brown adipose tissue (such as figure 1 shown).

Embodiment 2

[0030] BVT.2733 200mg / kg.day was used to gavage C57BL / 6J obese mice induced by high-fat diet for 2w, and the brown adipose tissue of the mice was extracted, and the brown fat marker genes UCP-1, Elovl3, Pgc-1a, Expression of Cox7a1 mRNA. Such as figure 2 As shown, it is shown that the 11β-HSD1 inhibitor (BVT.2733) can significantly promote the expression of brown fat marker genes UCP-1 and Elovl3 in brown adipose tissue of mice.

[0031] Extract primary pre-brown adipocytes from C57BL / 6J mice, induce their differentiation, and add 11β-HSD1 inhibitor (BVT.2733 2.0mM) at the same time to collect the cells after brown adipocyte differentiation and maturity, and detect the brown adipose marker gene UCP by real-time quantitative PCR -1, Elovl3, Pgc-1a, Cox7a1 mRNA expression. Such as image 3 as shown, image 3 It was shown that 11β-HSD1 inhibitor (BVT.2733) can significantly promote the expression of brown fat marker genes UCP-1, Elovl3, Pgc-1a, and Cox7a1 in primary brown adi...

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Abstract

The invention relates to the technical field of biomedicine, in particular to a novel targeted medicament targeted to brown adipose tissues for treating obesity. According to the novel targeted medicament targeted to the brown adipose tissues for treating obesity, the medicament is formed by connecting brown adipose tissue-targeted polypeptide CKGGRAKDC-NH2 and an 11beta hydroxysteroid dehydrogenase 1 inhibitor, acts on the brown adipose tissues in a targeted way, amplifies the function of brown adipose, and has no affinity or actions on other visceral organs, so that the purpose of treating the obesity more efficiently is achieved.

Description

technical field [0001] The invention relates to the field of biomedical technology, in particular to a novel targeted drug targeting brown adipose tissue for treating obesity. Background technique [0002] With the development of society and economy, obesity has become a hot issue in the world. As the incidence of obesity increases, obesity-related diseases also increase accordingly, including type 2 diabetes, hypertension, lipid metabolism disorders, etc., resulting in a significant increase in cardiovascular and cerebrovascular diseases. [0003] Current studies have found that the body contains two forms of fat: white adipose tissue (WAT) and brown adipose tissue (BAT). White fat is the form of energy storage in the body. The more energy ingested, the greater the volume and quantity of white fat; on the contrary, brown fat cells are rich in a large number of mitochondria, and the free lipid particles in lipid particles are released by oxidative phosphorylation of mitocho...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/496A61P3/04A61K47/42A61K47/64
Inventor 丁国宪钟毅刘娟
Owner JIANGSU PROVINCE HOSPITAL
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