CN-120305234-B - Ginger active ingredient composition and application thereof

Abstract

The invention provides a ginger active ingredient composition and application thereof. The ginger active ingredient composition comprises acetylated 12-gingerol, 8-gingerol and 10-gingerol in the mass ratio of (1-3) to (2-3). The ginger active ingredient composition can improve glucose tolerance abnormality, improve insulin sensitivity, reduce the content of triglyceride, total cholesterol and low-density lipoprotein cholesterol in serum, increase the content of high-density lipoprotein, reduce the activity of glutamic-pyruvic transaminase and glutamic-oxaloacetic transaminase of liver, improve the pathological changes of liver fat cavitation and reduce the content of lipid metabolism related metabolites of obese organisms, and simultaneously can improve the fat solubility, enhance the cell membrane penetrating capacity, reduce the oxidative degradation of phenolic hydroxyl groups, improve stability and release free 12-gingerol after enzymolysis so as to achieve a slow release effect.

Inventors

• WANG JING
• WANG YIFAN
• FENG FENGQIN
• ZHAO MINJIE

Assignees

• 浙江大学

Dates

Publication Date

20260505

Application Date

20250616

Claims (2)

1. 1. The ginger active ingredient composition is characterized by comprising acetylated 12-gingerol, 8-gingerol and 10-gingerol, wherein the mass ratio of the acetylated 12-gingerol to the 8-gingerol to the 10-gingerol is 1-3:2:2-3; the preparation method of the acetylated 12-gingerol comprises the following steps: S1, under the protection of nitrogen, mixing 1 mmol of 12-gingerol with 10 mL anhydrous dichloromethane, dropwise adding 1.2 mmol pyridine, and stirring for dissolution; S2, slowly dripping 1.5 mmol acetic anhydride, and stirring at 25 ℃ for reaction for 5 hours; s3, adding 10mL of ice water to quench the reaction, and separating liquid to collect an organic phase; S4, washing the organic phase with saturated NaHCO 3 solution and then drying the organic phase with anhydrous Na 2 SO 4 ; S5, removing the solvent by rotary evaporation, purifying the crude product by silica gel column chromatography, and performing gradient elution by using petroleum ether/ethyl acetate to obtain the acetylated 12-gingerol.
2. 2. Use of a ginger active ingredient composition according to claim 1 for the preparation of a medicament for the prevention and/or treatment of obesity.

Description

Ginger active ingredient composition and application thereof Technical Field The invention belongs to the technical field of health-care products and medicines, and particularly relates to a ginger active ingredient composition and application thereof. Background Obesity is a ubiquitous metabolic disorder that has a profound effect on public health throughout the world. Obesity is not simply a cause of weight gain, but its severity is the induction of diseases such as heart disease, diabetes, hypertension, renal failure, etc., as a "source of everything" for many conditions. Hyperlipidemia is one of the complications of obesity, and is represented by high levels of Triglyceride (TG), total Cholesterol (TC) and low density lipoprotein cholesterol (LDL-C), and the elevation of these lipid indicators may further lead to abnormal lipid metabolism, inducing fatty liver. Fatty liver can adversely affect fat metabolism, exacerbate hyperlipidemia and obesity, and thus form a vicious circle. Therefore, how to effectively prevent and treat obesity is a hot spot problem of research in metabolic disorder diseases. At present, the existing anti-obesity drugs have poor effects due to tolerance and obvious chronic toxic and side effects, and a plurality of traditional herbal extracts are expected to develop into safe and effective obesity replacement therapies. Ginger is one of the most common fragrances, containing a number of phenolic compounds that exhibit beneficial properties to human health, including enhancing digestive function, reducing inflammation, vomiting, cancer and metabolic syndrome. The anti-obesity effect of ginger is mainly attributed to gingerol, which is the most abundant bioactive compound, and the current research is mostly focused on 6-gingerol, 6-shogaol and other components, but the effects of the long-chain gingerols on improving diabetes, hypertension, non-alcoholic fatty liver and other aspects as compared with common 6-gingerols, such as 8-shogaol and 10-shogaol, are not reported yet. Disclosure of Invention Aiming at the problems, the invention aims to provide a ginger active ingredient composition and application thereof, explores the prevention and treatment effects of acetylated 12-gingerol, 8-shogaol and 10-shogaol on weight gain, fat accumulation, hyperlipidemia and lipid related metabolites of high-fat diet-induced obese mice, and provides a new view angle for treating obesity, hyperlipidemia, nonalcoholic fatty liver and chronic metabolic disorders in the fields of biological medicine, health care products and the like. The technical scheme is that the ginger active ingredient composition comprises acetylated 12-gingerol, 8-shogaol and 10-shogaol. Further, the mass ratio of the acetylated 12-gingerol, 8-shogaol and 10-gingerol is (1-3) 2 (2-3). Further, the preparation method of the acetylated 12-gingerol comprises the following steps: S1, under the protection of nitrogen, mixing 1-1.2 mmol of 12-gingerol with 10-15 mL of anhydrous dichloromethane, dropwise adding 1.0-1.2 of mmol pyridine, and stirring for dissolution; s2, slowly dripping 1.5-2.0 mmol acetic anhydride, and stirring at 25 ℃ for reaction for 4-6h; S3, adding 10-20 mL of ice water for quenching reaction, and collecting an organic phase in a liquid separation way; S4, washing the organic phase with saturated NaHCO 3 solution and then drying the organic phase with anhydrous Na 2SO4; S5, removing the solvent by rotary evaporation, and purifying the crude product by silica gel column chromatography to obtain the acetylated 12-gingerol. Further, the silica gel column chromatography adopts petroleum ether/ethyl acetate gradient elution. The application of the ginger active ingredient composition in preparing the medicine for preventing and/or treating obesity. Further, the medicament is a medicament for increasing glucose tolerance level of an obese organism, increasing insulin sensitivity, reducing triglyceride, total cholesterol and low density lipoprotein cholesterol level, and increasing high density lipoprotein level. Further, the medicine is a medicine for improving liver cell morphology, slowing down lipid accumulation in the liver, down regulating liver glutamate pyruvate transaminase activity, glutamate oxaloacetic transaminase activity and improving liver fat vacuolation pathological degree. Further, the medicine is a medicine for regulating the content of fat metabolism related metabolites of an obese organism. Further, the metabolites related to the regulation of fat metabolism in obese organisms include (20R, 22R) -20, 22-dihydroxycholesterol, galactose-1-phosphate, glycerophosphorylcholine, lysophosphatidylcholine (18:3), docosahexaenoic acid, lysophosphatidylcholine (20:3 (8Z, 11Z, 14Z)), phosphatidylcholine (17:0), phosphatidylcholine (20:0), phosphatidylcholine (18:1 (11Z)), phosphatidylcholine (16:1 (9Z)/0:0), (20R, 22-dihydroxycholesterol, galactose-1-phosphate, sphingosine-phosphate, and cholic acid. Advant