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Application of rhodanine to treatment of metabolic diseases

A technology of derivatives and drugs, applied in the field of application of rhodanine derivatives in the treatment of metabolic diseases, can solve problems such as side effects and ineffective effects

Active Publication Date: 2020-07-21
SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current anti-obesity drugs mainly limit energy intake by reducing fat absorption or suppressing appetite, but the clinical effect is not obvious, and there are side effects
Clinically, there is no drug to treat obesity by increasing energy utilization. By increasing the heat production function of brown adipose tissue BAT, the body's energy is consumed in the form of heat energy, which can be used as a target for the treatment of obesity and related metabolic diseases

Method used

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  • Application of rhodanine to treatment of metabolic diseases
  • Application of rhodanine to treatment of metabolic diseases
  • Application of rhodanine to treatment of metabolic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Embodiment 1, in vitro verification

[0075] 1) BML-260 can promote the expression of UCP1 in mature brown adipocytes

[0076]Experimental procedure: Ucp1-2A-GFP primary brown adipocytes that have been successfully constructed are used (the 2A-GFP sequence is inserted after the Ucp1 stop codon in situ in the cell, so that the expression of GFP can reflect the expression level of endogenous UCP1 protein to a certain extent , the inserted 2A-GFP sequence is:, SEQ ID NO: 1), adding BML-260 at different stages of differentiation for different time. Three compound treatment methods were designed: adding BML-260 (10 μM) on day 1 for 10 days (re-adding 10 μM BML-260 when changing the medium); on day 7 of differentiation (mature brown adipocyte stage ) were treated with BML-260 (10 μM) for 1 day, 2 days, and 3 days respectively; BML-260 (10 μM) was only treated on the 1st to 3rd day of differentiation (differentiation induction stage), and samples were collected on the 10th da...

Embodiment 2

[0096] Embodiment 2, verification in vivo

[0097] 1) BML-260 activates the expression of UCP1 in subcutaneous white fat of mice and increases thermogenesis

[0098] Experimental procedure: eight-week-old C57BL / 6J male mice (Slack) were orthotopically injected with BML-260 in the subcutaneous fat, the solvent was used as a negative control, and CL-316243 (CL) was used as a positive control. Three days after the injection, the mice were weighed, the subcutaneous fat of the mice was taken and weighed, and the protein was extracted for Western blot to detect the expression of UCP1. And the mouse subcutaneous fat was embedded in paraffin, and hematoxylin-eosin staining (HE-staining) or UCP1 protein immunohistochemistry was performed to observe the morphology of adipose tissue and the expression of UCP1 in situ. After the in situ injection, a cold stimulation experiment was performed to test the tolerance of the mice to continuous low temperature.

[0099] Experimental results su...

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Abstract

It is the first time for the invention to disclose that a rhodanine derivative can activate STAT3, CREB and PPARs signal paths, significantly increase expression of UCP1, enhance expression of mitochondrial oxidative phosphorylation genes, effectively increase thermogenesis, and can be used for treating the metabolic diseases. Accordingly, the invention relates to application of the rhodanine derivative to treatment of the metabolic diseases. The invention further relates to a pharmaceutical composition containing the rhodanine derivative as an active ingredient, and the pharmaceutical composition is used for treatment of the metabolic diseases.

Description

technical field [0001] The invention relates to the application of rhodanine derivatives in the treatment of metabolic diseases. Background technique [0002] Obesity is a chronic metabolic disease caused by a variety of factors, characterized by an increase in the volume and number of fat cells in the body, resulting in an abnormally high percentage of body fat as a percentage of body weight, and excessive fat deposition in some areas. The current anti-obesity drugs mainly restrict energy intake by reducing fat absorption or suppressing appetite, but the clinical effect is not very obvious, and there are side effects. Clinically, there is no medicine to treat obesity by increasing the utilization of energy. By increasing the heat production function of brown adipose tissue BAT, the energy of the body is consumed in the form of heat energy, which can be used as a target for the treatment of obesity and related metabolic diseases. Contents of the invention [0003] The inv...

Claims

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Application Information

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IPC IPC(8): A61K31/426A61P3/04A61P3/00
CPCA61K31/426A61P3/04A61P3/00
Inventor 丁秋蓉冯庄慧
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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