CN109620857B - Peanut coat active component and application thereof in preparation of anti-obesity and anti-diabetic drugs - Google Patents
Peanut coat active component and application thereof in preparation of anti-obesity and anti-diabetic drugs Download PDFInfo
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- CN109620857B CN109620857B CN201910040231.8A CN201910040231A CN109620857B CN 109620857 B CN109620857 B CN 109620857B CN 201910040231 A CN201910040231 A CN 201910040231A CN 109620857 B CN109620857 B CN 109620857B
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Abstract
The invention provides an active component of peanut coat, which is obtained by extracting peanut coat with ethanol, filtering, concentrating, separating with macroporous adsorption resin and collecting fractions. In anti-obesity and diabetes in vivo experiments, the peanut coat active components are proved by a diabetes animal model to be capable of adjusting adiponectin and leptin signal pathways to generate the effect of reducing weight and blood sugar, the food intake, the weight and the blood sugar of experimental obesity mice and type 2 diabetes model mice can be remarkably reduced, and the peanut coat active components have obvious improvement effect on the clinical symptoms of obesity and diabetes. Can be used in preparing food, health food and medicine for preventing and treating obesity and diabetes.
Description
Technical Field
The invention belongs to the field of medical food of compounds, and relates to an active component of peanut coat and application thereof in preparing anti-obesity and anti-diabetic medicines.
Background
Obesity and diabetes have become one of the biggest public health problems of the twenty-first century as a global epidemic, and more than 19 billion adults are overweight and more than 6 billion people are obese as reported by the world health organization in 2014. Obesity is a risk factor that causes a sharp increase in non-alcoholic fatty liver disease, type 2 diabetes, cardiovascular disease and cancer, all of which not only seriously affect the quality of life of humans, but also shorten the life span of humans. Especially type 2 diabetes, if not timely and effective treatment, complications such as coronary heart disease, cerebrovascular disease, nephropathy, retinopathy and the like are very easy to occur, and the complications become main reasons threatening the lives of patients with diabetes. Therefore, maintaining blood glucose levels close to the normal range is important for preventing diabetic complications.
Obesity and diabetes mellitus are endocrine-metabolic diseases with very complex etiology, and are endocrine-metabolic diseases caused by absolute or relative insufficiency of insulin in the body, and are marked by weight gain and chronically elevated blood glucose levels. At present, most of oral hypoglycemic drugs for treating obesity and diabetes have certain effects, but have the defects of easy rebound, multiple side effects and the like after drug withdrawal.
Active components derived from traditional Chinese medicine peanut coats are oligosaccharides and flavonoids, and the active components of the peanut coats are found to have obvious effects of losing weight and reducing blood sugar on experimental obese mice and type 2 diabetic mice by regulating adiponectin and leptin signal pathways.
Disclosure of Invention
The invention aims to provide an active component of peanut coat, which is obtained by the following preparation method: leaching peanut coat with 60% ethanol water solution (volume ratio) for 2 times, the first time for 1 hr, the second time for 0.5 hr, vacuum filtering, concentrating to 1/50, separating with macroporous adsorption resin HP-20, eluting with 40% ethanol water solution (volume ratio), and collecting fraction as peanut coat active component. The peanut coat active component mainly comprises a polysaccharide part and a non-saccharide part. The polysaccharide part consists of arabinose, xylose, D- (+) -inositol, myo-inositol, mannose, glucose and galactose, and the molar ratio is 3:6.9:1:1.5:3.2:21.5: 3.8. The non-sugar portion consists of polyphenols, mainly including dimers, trimers and tetramers of type a or type B procyanidins (table 1).
The invention also aims to provide application of the peanut coat active component in preparing anti-obesity and anti-diabetic medicines.
The invention further aims to provide application of the peanut coat active component in preparing health care products or foods for reducing obesity and blood sugar.
In vivo experiments on obesity and diabetes, the peanut coat active component can regulate adiponectin and leptin signal pathways to generate the effect of reducing weight and blood sugar, and the peanut coat active component is found to be capable of obviously reducing the food intake, the weight and the blood sugar of experimental obese mice and type 2 diabetes model mice (see figure 7).
The peanut coat active ingredient can be prepared into a pharmaceutically acceptable carrier or diluent according to any conventional process. The pharmaceutically acceptable carrier as used herein refers to a pharmaceutical carrier which is conventional in the pharmaceutical field, such as diluents, excipients and the like, fillers such as starch, sucrose, microcrystalline cellulose and the like; adhesives such as starch slurry, hydroxypropylcellulose, gelatin, polyethylene glycol, etc.; wetting agents such as magnesium stearate, colloidal silica, polyethylene glycols, etc.; absorption enhancer such as polysorbate and lecithin, surfactant poloxamer, sorbitan fatty acid, polysorbate, etc., and other adjuvants such as flavoring agent, sweetener, etc. can be added into the composition.
The administration dosage form can be tablet, pill, powder, dispersible tablet, sachet, elixir, suspension, emulsion, solution, syrup, aerosol, soft capsule, hard capsule, sterile injection, liniment or suppository. Can be prepared into conventional preparation with quick release, sustained release or delayed release.
The peanut coat active ingredient of the present invention can be administered by various routes including oral, intramuscular, subcutaneous, intraperitoneal, intravenous injection, etc.
The raw materials adopted by the invention are peanut coats with easily available sources and rich resources, and the peanut coats are mainly used for treating hemophilia, primary and secondary thrombocytopenic purpura, hepatic hemorrhage and the like in the traditional Chinese medicine. The peanut coat is treated by adopting a chemical separation and purification technology of a natural product, and the active component of the peanut coat is obtained by simple and effective extraction and macroporous resin separation. The active component mainly comprises oligosaccharide and procyanidins of different types. The active component has remarkable weight-losing effect on fat mice induced by high-fat, and also has good anti-diabetic effect on high-fat-induced type 2 diabetes mice, and the drug effect of the active component is equivalent to that of the marketed drug metformin for treating diabetes at a dose of 140 mg/kg. And has no obvious toxic or side effect.
Drawings
FIG. 1 shows the hydrogen spectrum of the saccharide part of the active component of peanut coat (deuterated methanol as solvent).
Fig. 2 is a carbon spectrum of the carbohydrate portion of the peanut coat active ingredient (deuterated methanol as solvent).
FIG. 3 is a hydrogen spectrum of the non-carbohydrate portion of the peanut coat active ingredient (deuterated methanol as solvent).
FIG. 4 is the carbon spectrum of the non-carbohydrate portion of the peanut coat active ingredient (deuterated methanol as solvent).
FIG. 5 is a GC/MS spectrum of the analysis of the monosaccharide composition of the carbohydrate portion of the peanut coat active ingredient. A standard monosaccharide sample mixture (A) spectrogram and a peanut coat active component spectrogram (B). Peak identification: 1. rhamnose; 2. trehalose; 3. arabinose; 4. xylose; 5. d- (+) -inositol; 6. inositol; 7. mannose; 8. glucose; 9. galactose.
FIG. 6 is a high resolution mass spectrum of the non-saccharide fraction of the peanut coat active ingredient.
FIG. 7 is a graph of the effect of peanut coat active ingredient on body weight in experimental obese mice. In the figure:**P<0.01 peanut coat active ingredient treatment group vs model control group,***P<0.001 peanut coat active ingredient treatment group vs model control group,#P<a 0.05 high fat diet vs normal control group,##P<a 0.01 high fat diet vs normal control group,###P<0.01 high fat diet vs normal control group. Number of animals per group: n is 10. ND is normal diet group, HFD is high fat diet group, HFD + PSE is high fat diet group plus peanut coat active group.
FIG. 8 is a graph of the effect of peanut coat active ingredient on food intake in experimental obese mice. In the figure:**P<0.01 peanut coat active ingredient treatment group vs model control group,***P<0.001 peanut coat active ingredient treatment group vs model control group,#P<a 0.05 high fat diet vs normal control group,##P<a 0.01 high fat diet vs normal control group,###P<0.01 high fat diet vs normal control group. Number of animals per group: n is 10. ND is normal diet group, HFD is high fat diet group, HFD + PSE is high fat diet group plus peanut coat active group.
FIG. 9 is the effect of peanut coat active ingredient on water intake in experimental obese mice. In the figure:**P<0.01 peanut coat active ingredient treatment group vs model control group,***P<0.001 peanut coat active ingredient treatment group vs model control group,#P<a 0.05 high fat diet vs normal control group,##P<a 0.01 high fat diet vs normal control group,###P<0.01 high fat diet vs normal control group. Number of animals per group: n is 10. ND is normal diet group, HFD is high fat diet group, HFD + PSE is high fat diet group plus peanut coat active group.
FIG. 10 is a graph of the effect of peanut coat active ingredient on adipose tissue in experimental obese mice. In the figure: c represents a normal control group, DM-C represents a diabetic control group, and Met represents a metformin-treated group; PSE stands for peanut coat active ingredient treatment group.###P<0.001 diabetes control VS normal control;*P<0.05 drug-treated vs diabetic control group,**P<0.01 drug-treated vs diabetic control group, n ═ 10.
FIG. 11 is a graph of the effect of peanut coat active on fasting plasma glucose in experimental type 2 diabetic mice. Wherein: c represents a normal control group, DM-C represents a diabetic control group, and Met represents a metformin-treated group; PSE stands for peanut coat active ingredient treatment group.###P<0.001 diabetes control VS normal control;*P<0.05 drug-treated vs diabetic control group,**P<0.01 drug-treated vs diabetic control group, n ═ 10.
Figure 12 is the effect of peanut coat active ingredient on food intake in experimental type 2 diabetic mice. Wherein: c represents positiveA normal control group, DM-C represents a diabetes control group, and Met represents a metformin treatment group; PSE stands for peanut coat active ingredient treatment group.*P<The control group of the 0.05vs model,**P<0.01vs model control, n 10.
FIG. 13 is the effect of peanut coat active ingredient on water intake in experimental type 2 diabetic mice. Wherein: c represents a normal control group, DM-C represents a diabetic control group, and Met represents a metformin-treated group; PSE stands for peanut coat active ingredient treatment group.*P<0.05，**P<0.01 drug-treated vs diabetic control group, n ═ 10.
FIG. 14 is a graph of the effect of peanut coat active ingredient on body weight change in experimental type 2 diabetic mice. Wherein: c represents a normal control group, DM-C represents a diabetic control group, and Met represents a metformin-treated group; PSE stands for peanut coat active ingredient treatment group.###P<0.001 diabetes control VS normal control;*P<0.05 drug-treated vs diabetic control group,**P<0.01 drug-treated vs diabetic control group, n ═ 10.
Figure 15 is the effect of peanut coat active on glucose tolerance in experimental type 2 diabetic mice. Wherein: (A) the change of the blood sugar value of the diabetic mouse is the change of the active components of the peanut coat after drenching and the glucose; (B) is the corresponding area under the curve when taking the drug. C represents a normal control group, DM-C represents a diabetic control group, and Met represents a metformin-treated group; PSE stands for peanut coat active ingredient treatment group.###P<0.001 diabetes control vs. normal control;***P<0.001 drug-treated vs diabetic control group, n-7.
FIG. 16 is a graph of the effect of peanut coat active ingredients on insulin resistance and experimental type 2 diabetic mice. Wherein: (A) the change of the blood sugar value of the diabetic mouse is the change of the active components of the peanut coat after drenching and the glucose; (B) is the corresponding area under the curve when taking the drug. C represents a normal control group, DM-C represents a diabetic control group, and Met represents a metformin-treated group; PSE stands for peanut coat active ingredient treatment group.###P<0.001 diabetes control vs. normal control; p<0.05,***P<0.001 drug treatment group vs diabetic pairsAccording to the group, n is 7.
FIG. 17 is a graph of the effect of peanut coat active ingredients on the intestinal microbial flora of experimental type 2 diabetic mice. Wherein: (A) is the analysis result of the diabetes mouse intestinal microbial flora clustering after the peanut coat active components and glucose are drenched; (B) is a species profiling histogram in the Phylum taxonomic level of the sample. C represents a normal control group, DM represents a diabetic control group, and Met represents a metformin-treated group; PSE stands for peanut coat active ingredient treatment group, n is 7.
Detailed Description
The invention is further explained by the accompanying drawings and examples.
Example 1 peanut coat active ingredient extraction
Extracting peanut coat with 60% ethanol for 2 times, the first time for 1 hr, the second time for 0.5 hr, vacuum filtering, concentrating to 1/50, separating with macroporous adsorbent resin HP-20, eluting with 40% ethanol, and collecting fraction, which is the active component of peanut coat.
Example 2 peanut coat active ingredient analysis
The experimental method comprises the following steps:
the active component of peanut coat is divided into two parts by High Performance Liquid Chromatography (HPLC), and the conditions are as follows: develosil ODS-UG-5(φ 20X 250mm), Nomura Chemical column, flow rate of 6ml/min, 0-15min, 18% methanol isocratic elution, collected as a saccharide fraction; gradient eluting with 18-100% methanol for 15-25min, isocratic eluting with 100% methanol for 25-40min, and collecting non-saccharide components. And then analyzing the components of the carbohydrate part and the non-carbohydrate part by spectral analysis, high-resolution mass spectrum and a chemical derivatization method.
The experimental results are as follows:
analysis of the hydrogen and carbon nuclear magnetic spectra of these two fractions (FIGS. 1 to 4) confirmed that these fractions were a carbohydrate fraction and a non-carbohydrate fraction, respectively. The carbohydrate fraction was then hydrolyzed, acetylated for GC/MS analysis and compared to the sample after acetylation of the standard sample to determine that the carbohydrate fraction consisted primarily of arabinose, xylose, D- (+) -inositol, myo-inositol, mannose, glucose and galactose in a molar ratio of 3:6.9:1:1.5:3.2:21.5:3.8 (fig. 5). The non-sugar fraction was analyzed by high resolution mass spectrometry (FIG. 6) and compared to the literature (Yu, JM et al, Peamut skin polypeptides: Composition and antioxidant activities as infected by processing, Journal of Food Composition and Analysis 19(2006)364 and 371), and was found to consist of polyphenols, mainly including dimers, trimers and tetramers of type A or B procyanidins (Table 1).
Table 1 peanut coat active ingredient non-saccharide fraction compound composition.
Example 2 Effect of peanut coat active ingredients on high fat diet-induced obese mice
The experimental method comprises the following steps:
this example divides six-week-old male mice into five groups of ten. The normal control group was taken water and normal diet. High Fat Diet (HFD) control group was drenched with the same amount of vehicle as treatment group and fed with high fat diet freely. The high-fat feed and the peanut coat active ingredient group are respectively irrigated with the peanut coat active ingredient according to the dosage of 4,80 and 160mg/kg body weight/day, and are freely fed with the high-fat feed and drinking water. The experimental period was 6 weeks, and body weight, food intake, and water intake were recorded weekly. After the last administration, the animals are fasted for 12h without water supply, blood is taken for detecting indexes such as blood sugar, triglyceride, cholesterol, creatinine, AST, ALT and the like in blood serum, and tissues such as heart, liver, pancreas, spleen, kidney, fat, muscle, brain and the like are taken.
The experimental results are as follows: the body weight and food intake of the mice in the high-fat diet group were significantly increased compared to those in the normal control group (fig. 7, fig. 8), but the water intake of the mice in the high-fat diet group was significantly decreased (fig. 9). The weight gain of mice is obviously reduced in a dose relationship (figure 7) and the food intake and water intake are also obviously reduced (figure 8 and figure 9) compared with the high fat group, and the weight of each tissue of each group is compared, so that the fat and liver weight of the peanut coat treated group and the weight of the model control group are obviously different (figure 10), and the peanut coat active component has obvious weight-reducing effect.
Example 3 research on preparation method of Experimental type 2 diabetic mice
High-fat feed is a main mode for inducing an obese type 2 diabetes model, and in order to correctly prepare experimental type 2 diabetes mice, the embodiment adopts a mode of feeding high-fat feed for a long time to construct a type 2 diabetes pathological model.
The experimental method comprises the following steps:
in this example, experimental animals were divided into a control group and a model group. The control group was given normal diet and the model group was given high fat diet (all provided by shanghai slyke laboratory animals ltd). The feeding period was 5 months, and the food intake, water intake, and body weight of the animals were measured weekly. And (3) fasting the mice in the last week of molding, measuring the blood sugar value of the mice, and judging the mice with the weight obviously increased and the blood sugar value more than 9 as type 2 diabetic mice.
The experimental results are as follows:
after the mice are fed with the high-fat feed for 5 months, the weight and the blood sugar of the mice are obviously increased. And the blood sugar value is more than 9. Therefore, the peanut coat can be used as an animal model of type 2 diabetes for researching the efficacy of the active components of the peanut coat.
Example 4 effect of peanut coat active ingredients on experimental type 2 diabetic mice a mouse model was prepared:
animal grouping:
10 healthy male mice and 50 type 2 diabetes models were randomly divided into a normal control group, a diabetes control group, a positive control group (metformin) and a peanut coat treatment group (high, medium and low dose groups). The normal control group was given normal diet, and the rest of the groups were all high-fat diet (provided by shanghai slyke laboratory animals ltd). The test period is 4 weeks, and the normal control group and the model control group are perfused with gastric water. The positive control group is infused with metformin, the peanut coat active ingredient treatment group is infused with 10,80 and 160mg/kg doses of peanut coat active ingredient respectively, fasting is carried out for 12 hours every other week, blood is taken from the tail part, and the blood sugar change value is determined. And daily food intake and daily water intake were measured. After the last administration, the animals are fasted for 12h without water supply, blood is taken for detecting indexes such as blood sugar, triglyceride, cholesterol, creatinine, AST, ALT and the like in blood serum, and tissues such as heart, liver, pancreas, spleen, kidney, fat, muscle, brain and the like are taken.
The experimental results are as follows:
after administration, the peanut coat active ingredient dose groups of 80mg/kg and 160mg/kg had significant differences compared with the blood glucose values of the model control group (fig. 11). In addition, the indexes in the serum are compared (table 2), and the significant difference is found between the blood glucose value in the serum of the peanut coat active component dose group of 80mg/kg and the blood glucose value in the serum of the model control group. The peanut coat active ingredient dosage groups of 80mg/kg and 160mg/kg were also significantly different from the model group in terms of food intake and water intake (fig. 12, 13). And the weights of tissues of all groups are compared, and the fat weights of the raw coating active component dose groups of 80mg/kg and 160mg/kg are obviously different from those of the modeling group (table 3, figure 14).
TABLE 2 Effect of peanut coat active ingredients on serum indices of Experimental type 2 obese mice
In this test, ALT represents glutamic-oxaloacetic transaminase, AST represents glutamic-pyruvic transaminase, TG represents triacylglycerol, TC represents total cholesterol, GLU represents blood glucose; MET for metformin#，##，###Indicates that the diabetic group is compared with the normal group P<0.05,P<0.01,P<0.001；*，**，***Shows the comparison of the diabetes group with the peanut coat active ingredient treatment group P<0.05,P<0.01,P<0.001; the number of animal samples was 10.
TABLE 3 Effect of peanut coat active ingredients on visceral organs of Experimental type 2 obese mice
MET for metformin, PSE for peanut coat active ingredient,##，###indicates that the diabetic group is compared with the normal group P<0.05,P<0.01,P<0.001；*，**，***Indicates the diabetic group andpeanut coat active ingredient treatment group comparison P<0.05,P<0.01,P<0.001; the number of animal samples was 10.
The results show that the peanut coat active component can reduce the blood sugar of experimental type 2 diabetes mice and remarkably relieve the symptoms of polydipsia and polyphagia in clinical manifestations of the type 2 diabetes mice.
Example 5 Effect of peanut coat active ingredients on sugar tolerance and insulin sensitivity in Experimental type 2 diabetic mice
The experimental method comprises the following steps:
the change in blood glucose value was measured using the Oral Glucose Tolerance Test (OGTT) and the intraperitoneal Insulin Tolerance Test (ITT) 4 weeks after the peanut coat active ingredient was drenched. The specific test method is as follows: after the test animals had fasted for 12 hours, the test animals were drenched with metformin or peanut coat active ingredient at different doses for 15 minutes and 2 g/glucose per test animal, and the change in blood glucose values at 0,15,30, 60,90, 120 minutes was measured using blood glucose test paper.
In addition, 0.4 unit of insulin per mouse was intraperitoneally injected into 4-hour fasted test animals, and blood glucose values were measured by a blood glucose test strip for 0,15,30, 60, and 90 minutes, which were changed.
The experimental results are as follows:
after the mice were infused with glucose, the blood glucose values of the peanut coat active ingredient 10mg/kg, 80mg/kg and 160mg/kg were significantly reduced, and the area under the AUC curve was significantly reduced, as compared with the diabetes model group (fig. 15). Further, the blood glucose level was significantly reduced and the area under the AUC curve was significantly reduced after the mice were injected with insulin (fig. 16). The results of these studies indicate that the glucose tolerance and insulin sensitivity of the 2-diabetic mice are significantly improved.
Example 6 effect of peanut coat active ingredients on intestinal microflora in experimental type 2 diabetic mice.
Influence of peanut coat active components on intestinal microbial flora of experimental type 2 diabetic mice
The experimental method comprises the following steps:
after 6 weeks of peanut coat active ingredient and metformin drenching, squirrel cage is cleaned, sterilized with alcohol and about 100mg (2-3 grains) of mouse feces samples of each group are collected. DNA was extracted and the 16S rDNA V4 region of the sample was amplified as indicated by the sequencing region. And PE250 sequencing analysis was performed using Hiseq 2500 instruments. Experimental results intra-group species complexity analysis as well as inter-group species difference analysis was performed.
The experimental results are as follows:
the results of the intestinal microflora cluster analysis of the mice show that the peanut coat active ingredient dose group of 10mg/kg is similar to the intestinal microflora of the model control group, while the intestinal microflora of the mice is similar to that of the blank control group after administration of 80mg/kg of peanut coat active ingredient and metformin for 6 weeks (17. A). In addition, the ratio of Firmicutes to Bacteroidetes in the gut microflora of the model control group was significantly increased compared to the blank control group, and significantly decreased after 6 weeks of drenching with 80mg/kg peanut coat active and metformin (fig. 17. B). And the ratio of 80mg/kg of the peanut coat active ingredient dose group to Proteobacteria (Proteobacteria) in the metformin intestinal microflora was significantly reduced compared with the model control group (fig. 17. B). In addition, actinomycetes (actinomycetes) appeared in the intestinal microflora of mice in the model control group compared with the blank control group (fig. 17.B), but after administration of 80mg/kg of peanut coat active ingredient and metformin for 6 weeks, the level of actinomycetes (actinomycetes) in the intestinal microflora of mice was consistent with that of the blank control group, and 10mg/kg of peanut coat active ingredient did not improve this phenomenon (fig. 17. B).
The results show that the peanut coat active component can regulate and control the intestinal microbial environment homeostasis of experimental type 2 diabetic mice.
Claims (4)
1. The application of the peanut coat active component in preparing the anti-obesity and anti-diabetes medicine is characterized in that the peanut coat active component is obtained by the following preparation method: leaching peanut coat with 60% ethanol for 2 times, the first time for 1 hr, the second time for 0.5 hr, vacuum filtering, concentrating to 1/50, separating with macroporous adsorption resin HP-20, eluting with 40% ethanol, and collecting fraction as active component of peanut coat.
2. The application of the peanut coat active component in preparing the health-care product for losing weight and assisting in reducing blood sugar is characterized in that the peanut coat active component is obtained by the following preparation method: leaching peanut coat with 60% ethanol for 2 times, the first time for 1 hr, the second time for 0.5 hr, vacuum filtering, concentrating to 1/50, separating with macroporous adsorption resin HP-20, eluting with 40% ethanol, and collecting fraction as active component of peanut coat.
3. The use according to claim 1, wherein the medicament is in the form of a solid or liquid formulation and is administered enterally.
4. The use according to claim 2, wherein the nutraceutical is in the form of a solid or a liquid.
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