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Application of 9-demethylberberine in preparation of hypolipidemic drug

A technology for desmethylberberine and medicine is applied in the application field of 9-desmethylberberine in the preparation of blood lipid-lowering medicines, and can solve the problems of rhabdomyolysis, pharmacokinetic influence, reduction of medicine effect and the like

Inactive Publication Date: 2014-07-16
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Clinically, although statins and other drugs have good lipid-lowering effects, long-term use may cause toxic side effects such as liver toxicity and rhabdomyolysis, and have a greater impact on drug-metabolizing enzymes in the liver
However, changes in the expression and activity of drug-metabolizing enzymes in the liver may affect the pharmacokinetics of co-administered drugs in vivo, resulting in drug interactions and resulting in reduced drug efficacy or toxic side effects.

Method used

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  • Application of 9-demethylberberine in preparation of hypolipidemic drug
  • Application of 9-demethylberberine in preparation of hypolipidemic drug
  • Application of 9-demethylberberine in preparation of hypolipidemic drug

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example 9

[0009] Example 9-Demethylberberine lipid-lowering effect

[0010] C57BL / 6 mice (30, purchased from the Academy of Military Medical Sciences, weighing 18±2g) were used for the experiment. With AIN93 standard feed (according to calorific value, containing 10% fat, 75.9% carbohydrate, 14.1% protein, 3601 kcal / kg) and standard feeding environment (free eating and drinking, alternate day and night, each 12 hours), adapt Sex feeding for a week. Subsequently, they were randomly divided into 5 groups by body weight, one group continued to be given normal feed, and the other four groups were all given high-fat feed (calculated by calorie value, containing 60% fat, 25.9% carbohydrate, 14.1% protein, and 5018 kcal of heat). / kg) (Nantong Trofe Feed Technology Co., Ltd.), and all rats had free access to drinking water. The above-mentioned 5 groups of animals were fed under the same conditions. Blood was collected at 3 weeks, serum plasma was separated, and total triglyceride (TG), total...

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Abstract

The invention provides a hypolipidemic compound 9-demethylberberine. The 9-demethylberberine is derived from a main in-vivo metabolite of natural medicine berberine, and is also named as berberrubine. The researches on model animals with hyperlipidemia find that the 9-demethylberberine has good drug effects of reducing cholesterol, triglyceride, low density lipoprotein (LDL) and the like, and has no obvious side effects for 6 weeks of continuous medication. The discovery can lead to discovery of a new hypolipidemic drug, and provides another alternative medicine for clinic treatment of hyperlipidemia, lipid metabolism disorder and high fat and obese patients and related people wanting to lose weight.

Description

technical field [0001] The present invention relates to 9-desmethyl berberine with lipid-lowering pharmacological effects and its potential clinical application, in particular to 9-desmethyl berberine showing good lipid-lowering effect on hyperlipidemia model animals, which is expected to pass Further research and development will become a class of innovative drugs, which are used for clinically lowering blood lipids, regulating abnormal lipid metabolism and used for weight loss of obese people. Background technique [0002] Hyperlipidemia is a major risk factor for cardiovascular and cerebrovascular diseases and an important factor that endangers human health. Clinically, although statins and other drugs have good lipid-lowering effects, long-term use may cause toxic side effects such as liver toxicity and rhabdomyolysis, and have a greater impact on drug-metabolizing enzymes in the liver. The changes in the expression and activity of drug-metabolizing enzymes in the liver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61P3/06A61P3/04A61P3/10A61P3/00
Inventor 阿基业王广基孙润彬葛纯杨娜俞晓忆肖文璟
Owner CHINA PHARM UNIV
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