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Application of dibutyacyladenosine cyclophosphate salts in preparation of fat-reducing diet drugs for external use

A technology of dibutyryl cyclic adenosine phosphate and dibutyryl cyclic adenosine phosphate sodium, which is applied in the field of medicine and can solve the problems that dibutyryl cyclic adenosine phosphate has no reported effect on fat loss and weight loss.

Inactive Publication Date: 2017-07-14
GUANGZHOU YIXIN BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the fat-reducing and weight-reducing effects of dibutyryl cyclic adenosine monophosphate

Method used

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  • Application of dibutyacyladenosine cyclophosphate salts in preparation of fat-reducing diet drugs for external use
  • Application of dibutyacyladenosine cyclophosphate salts in preparation of fat-reducing diet drugs for external use
  • Application of dibutyacyladenosine cyclophosphate salts in preparation of fat-reducing diet drugs for external use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0021] Example: Preparation of Dibutyryl Cyclic Adenosine Phosphate

[0022] In a dry reaction flask, add 3.2g (0.01mol) of cyclic adenosine monophosphate triethylamine salt, 100ml of chloroform, 4g (0.05ml) of pyridine and 15.82g (0.10mol) of n-butyric anhydride and stir at 60°C for 48h. After the reaction is complete, after the solvent is recovered, 100 ml of water is added, extracted several times with isohexanone and discarded. Concentrate the water layer to 15ml under reduced pressure, extract with 30ml×3 chloroform, combine the organic layers, recover the solvent, add 30ml of water to the residue, stir and dissolve, then purify with Amberlite IR-120 resin, concentrate and cool, and precipitate a solid , and dried to obtain 4.32 g (88%) of dibutyryl cyclic adenosine monophosphate, mp240°C (dec).

[0023] Experimental preparation: 3T3-L1 preadipocytes were induced to differentiate into adipocytes. Rat fibroblast cell line 3T3-L1 was used at 5×10 4 The cells were inocula...

experiment example 1

[0026] Experimental Example 1: The effect of dibutyryl cyclic adenosine monophosphate on promoting lipolysis. To determine the effect of dibutyryl cyclic adenosine monophosphate on promoting lipolysis in adipocytes, 3T3-L1 adipocytes differentiated in experimental preparations were used. Replace the cell culture medium with new DMEM medium (containing 10% FBS) containing 10 mg / mL dibutyryl cyclic adenosine monophosphate, and then, detect the accumulation of fat in the adipocytes according to the experimental method 1. The result is as figure 1 shown.

[0027] figure 1 The results showed that compared with the control group, the fat mass of adipocytes treated with dibutyryl cyclic adenosine monophosphate significantly decreased, and the effect of decomposing fat was better than caffeine, a positive comparison control known to have a fat decomposing effect.

experiment example 2

[0028] Experimental Example 2: The effect of forskolin on promoting lipolysis. To determine the effect of forskolin on promoting lipolysis in adipocytes, 3T3-L1 adipocytes differentiated in experimental preparations were used. Replace the cell culture medium with a new DMEM medium (containing 10% FBS) containing 8.2 μg / L forskolin, and then detect the accumulation of fat in the adipocytes according to the experimental method 1. The result is as figure 2 shown.

[0029] figure 2 The results showed that, compared with the control group, the amount of neutral fat in the adipocytes treated with forskolin decreased to a certain extent.

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PUM

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Abstract

The invention discloses an application of dibutyacyladenosine cyclophosphate salts in the preparation of fat-reducing diet drugs for external use. Dibutyacyladenosine cyclophosphate salts can directly enter fat cells and activate PKA proteins, and thus hormone sensitive lipase (HSL) is activated to catalyze fat decomposition to generate free fatty acid and glycerin. At the same time, the destructive effect of phosphodiesterase is prevented, and compared with those of cAMP, the action time is longer, and the effect is quicker.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the use of dibutyryl cyclic adenosine monophosphate in the preparation of external fat-reducing and weight-reducing medicines. Background technique [0002] Obesity can be divided into systemic obesity and partial obesity (upper body obesity, lower body obesity, and abdominal obesity) according to the distribution of adipose tissue in the whole body. Systemic obesity has become a global and serious social public health problem. According to statistics released by the World Health Organization, there are at least 1 billion overweight adults and 300 million obese people in the world. Population obesity has seriously threatened global development. Although partial obesity generally does not cause serious health problems, it is a more common social problem. It refers to obesity caused by excessive accumulation of fat in a certain part of the body, such as the abdomen (general belly / beer belly...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7076A61K31/522A61K31/197A61K36/53A61P3/04
CPCA61K31/197A61K31/522A61K31/7076A61K36/53A61K2300/00
Inventor 王伟章谭杰峰涂传明
Owner GUANGZHOU YIXIN BIOTECH CO LTD
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