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Application of malonic-acid-modified fullerene C70 in preparation of medicine for treating non-alcoholic fatty liver disease

A technology for non-alcoholic and fatty liver disease, applied in the field of preparation of drugs for the treatment of non-alcoholic fatty liver disease, can solve problems such as difficult quality control, harsh preparation method conditions, and limited medicinal value, so as to reduce the damage of carbon cages , Retain the efficacy and activity of the medicine, which is beneficial to the effect of finished medicine

Pending Publication Date: 2020-04-07
武汉赛莱亚生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This kind of preparation method has harsh conditions, and the bulk structure of fullerene is severely damaged, which may easily lead to a decrease in the activity of fullerene or even toxicity.
In addition, such fullerene derivatives generally have no definite structure or molecular formula, resulting in differences in product batches, difficult quality control, and difficulty in making medicines, which limits their medicinal value in the medical field

Method used

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  • Application of malonic-acid-modified fullerene C70 in preparation of medicine for treating non-alcoholic fatty liver disease
  • Application of malonic-acid-modified fullerene C70 in preparation of medicine for treating non-alcoholic fatty liver disease
  • Application of malonic-acid-modified fullerene C70 in preparation of medicine for treating non-alcoholic fatty liver disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] [Example 1] C70-malonic acid derivative C 70 [C(CH 2 COONa) 2 ] 4 preparation of

[0024] 50mg of C70 was dissolved in 10ml of toluene, and 0.8ml of diethyl bromomalonate and 0.7ml of DBU were added under nitrogen protection. The reaction was stirred at room temperature for about 2 h. Separation and purification by silica gel column chromatography (ethyl acetate: toluene = 1:99), the fourth color band was taken and concentrated under reduced pressure. The resulting product was hydrolyzed by adding NaH under the protection of nitrogen, and stirred at 60°C for about 6 hours. After the reaction, methanol was added to quench the excess NaH, and centrifuged to obtain a precipitate. Wash the precipitate with ethanol three times and get brown C 70 [C(CH 2 COONa) 2 ] 4 product, its mass spectrometry results are as follows figure 1 shown.

Embodiment 2

[0025] [Example 2] C70-malonic acid derivative C 70 [C(CH 2 COONa) 2 ] 4 Preconditioning reduces fat accumulation in hepatocytes

[0026] Isolation and culture of primary mouse hepatocytes:

[0027] Primary mouse hepatocytes were isolated by type Ⅳ collagenase digestion. The mice were anesthetized by ether inhalation, the portal vein was punctured with an indwelling needle, and the liver was perfused in situ (SC-1 and SC-2 alternately perfused) until the liver was completely digested. The liver was removed, repeatedly pipetted and filtered, and the liver cell suspension was collected.

[0028] Petri dish coating: After diluting absolute ethanol to 30% ethanol with sterilized ultrapure water, filter through a 0.22 μM filter, and then dilute 100× rat tail glue to 1×. Add 200 μl of diluted rat tail glue to each well of the six-hole plate, and rotate the six-hole plate to make the glue cover the entire bottom of the plate. Open the lid and let it air dry overnight on a clean...

Embodiment 3

[0031] [Example 3] C70-malonic acid derivative C 70 [C(CH 2 COONa) 2 ] 4 Inhibits the progression of non-alcoholic fatty liver disease

[0032] 1 Experimental animals and feeding

[0033] Experimental animals: male C57BL / 6 mice aged 8-10 weeks and weighing 23.5-27.5 g were selected as the experimental subjects.

[0034] Breeding environment: SPF level experimental animal center, SPF level mouse feed was purchased from Beijing Huafukang Biotechnology Co., Ltd. Raising conditions: the room temperature is between 22-24° C., the humidity is between 40-70%, the lighting time is 12 hours alternately between light and dark, and free to drink and eat.

[0035] 2 Model construction and administration

[0036] C57 mice (20 in total) were fed with high-fat and high-cholesterol (HFHC) for 10 weeks to establish a NASH model. Afterwards, the mice were divided into two groups (10 in each group, the treatment group and the control group, respectively). 70 [C(CH 2 COONa) 2 ] 4 (10mg...

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Abstract

The invention discloses application of malonic-acid-modified fullerene C70 in preparation of a medicine for treating the non-alcoholic fatty liver disease. The medicine that uses the C70-malonic acidderivative as the active ingredient and is used for preventing, relieving and / or treating the non-alcoholic fatty liver disease and related diseases has the following advantages: firstly, the pharmacodynamic effect is obvious, the C70-malonic acid derivative can obviously inhibit lipid accumulation in primary hepatocytes of mice and obvious changes can be seen in 10 micrometers; in addition, the C70-malonic acid derivative also has an obvious improvement effect on liver lipid accumulation and fibrosis generated by HFHC diet induction; secondly, the malonic-acid-modified fullerene C70 can effectively reduce the damage of a carbon cage in a fullerene modification process, so that the pharmacodynamic activity of the fullerene body is better retained; and thirdly, the C70-malonic acid derivative has a determined molecular structure, problems that other water-soluble fullerene derivatives have no determined structure and are difficult in quality control are solved, and the patent medicine is realized conveniently.

Description

technical field [0001] The invention relates to the field of nano-biomedicine, in particular to the application of malonate-modified fullerene C70 in the preparation of drugs for treating non-alcoholic fatty liver disease. Background technique [0002] With the improvement of people's living standards and changes in lifestyle, the number of patients with nonalcoholic fatty liver disease (NAFLD) in China is increasing year by year, and it has become an important cause of chronic liver disease. According to statistics, there are currently more than 1 billion non-alcoholic fatty liver patients in the world, and the incidence of NAFLD among adults in my country is about 20% [1-3]. Patients with NAFLD usually have no history of excessive alcohol consumption, and are characterized by diffuse hepatic macrovesicular steatosis and fat accumulation. Moreover, if nonalcoholic fatty liver is not treated in time, it can also develop into nonalcoholic steatohepatitis (NASH), liver fibros...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/44A61P1/16A61P3/06A61P35/00
CPCA61K33/44A61P1/16A61P3/06A61P35/00
Inventor 李红良折志刚邹头君
Owner 武汉赛莱亚生物科技有限公司
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