CN102579603A - Application of polygonum cuspidatum (PC) in prevention and treatment of insulin resistance and relative metabolic diseases - Google Patents

Abstract

The invention discloses the use of Polygonum Cuspidatum (PC) and its extract for preparing anti-insulin resistance and related metabolic diseases prevention and treatment medicine; and also discloses the preparation method of the extract In addition, it also discloses the use of a pharmaceutical composition containing Polygonum plants or (and) extracts of plants of the genus as medicines and health products, especially for the preparation of medicines and medicines for the treatment and prevention of insulin resistance and its related metabolic diseases Health products and other uses.

Description

Use of Polygonum cuspidatum to prevent and treat insulin resistance and related metabolic diseases

The patent application for the present invention is a divisional application. The application number of the original application is 200710177331.2, the application date is November 14, 2007, and the title of the invention is: Polygonum cuspidatum for preventing and treating insulin resistance and related metabolic diseases.

technical field

The present invention relates to extracting an extract capable of increasing insulin sensitivity from the plant Polygonum cuspidatum, a preparation method of the extract, a pharmaceutical composition containing Polygonum cuspidatum or the plant extract, and Polygonum cuspidatum or the plant extract and its pharmaceutical composition as The use of medicines, especially medicines and health products for treating and preventing insulin resistance and related metabolic diseases.

Background technique

Insulin resistance refers to the reduced sensitivity and/or responsiveness of the body to insulin, which is the main pathophysiological basis of metabolic syndrome, and it is related to impaired glucose tolerance/type 2 diabetes and its complications, obesity, dyslipidemia, Clinical abnormalities such as non-alcoholic fatty liver disease and coronary heart disease are closely related. Metabolic syndrome is a series of chronic diseases and has developed into the third largest disease in the world. The number of patients is increasing year by year. It not only seriously affects the quality of life of patients, even threatens their lives, but also brings heavy economic burden to the society.

The mechanism of insulin resistance is very complex, and accordingly there are many targets of insulin sensitizers. However, the current clinical applications are all thiazolidinedione drugs with PPARγ as the target. In addition, it has also been reported that traditional antidiabetic drugs such as biguanides, lipid metabolism regulators such as fibrates, and some traditional Chinese medicine ingredients all show certain effects of increasing the body's insulin sensitivity.

Representative drugs that have been marketed as insulin sensitizers include thiazolidinediones such as rosiglitazone. The main target of thiazolidinediones is peroxisome proliferator-activated receptor gamma (PPARγ), which can directly enhance the insulin sensitivity of liver, muscle and adipose tissue in patients with type 2 diabetes, making fasting and meal After the blood sugar is lowered, and does not cause hypoglycemia. In recent years, it has developed rapidly, and troglitazone, rosiglitazone, and pioglitazone have been listed successively. Troglitazone was withdrawn from the market due to severe hepatotoxicity (liver failure). The main side effects of these drugs are edema and weight gain.

Biguanides mainly include metformin and phenformin. Although such drugs have been used to treat diabetes in the late 1950s, their main function is to increase the utilization of glucose by peripheral tissues. Modern studies have found that it has a certain insulin-sensitizing effect. Its main side effects are gastrointestinal irritation and lactic acid poisoning. In particular, phenformin has been banned in many countries because of its serious adverse reactions.

Polygonum cuspidatum has a long history of medicinal use, which was first recorded in "Bielu of Famous Doctors". It is a product with yang in yin. Its yin, masters the liver and gallbladder in the lower energizer, clears the damp-heat in the lower energizer, promotes the gallbladder and relieves jaundice; enters the lower energizer and large intestine, functions to purify the bowels, clears the intestines and stops bleeding; enters the blood system, cools the blood to stop bleeding; it can also clear heat and detoxify, dampness and sores. For its yang, go through the meridians, unblock the blood vessels, promote blood circulation, remove turbidity, dispel wind and dredge collaterals; in clearing diarrhea, it also has the property of penetrating and dispersing, which can clear away summer heat; Therefore, the complete description of the performance of Polygonum cuspidatum should be: bitter, pungent, astringent, cold in nature, and returns to the liver, gallbladder, large intestine and lung meridian. To dredge collaterals, clear away heat and detoxify, clear away damp-heat, clear away summer-heat, eliminate phlegm and turbidity, relieve diarrhea and relieve constipation, diuresis and relieve stranguria. External use can also detoxify, dampness and sores.

In modern TCM prescriptions, Polygonum cuspidatum is often used for bronchitis, pneumonia, rheumatic arthralgia, painful urination, unknown swelling, poisonous snake bites, amenorrhea, postpartum blood stasis and abdominal pain, blood stasis and swelling pain caused by traumatic injuries, snake bites and burns. wait. The main pharmacological effects include strengthening the heart and dilating blood vessels, inhibiting platelet aggregation, anti-thrombosis, improving microcirculation, anti-shock and lowering blood lipids, etc. on the cardiovascular system; antitussive, asthma, etc. on the respiratory system; protecting the liver and promoting choleresis effects on the digestive system; and antibacterial, antiviral, anticancer, antioxidative, hemostatic, anti-inflammatory and sedative effects.

Contents of the invention

The object of the present invention is to provide an extract extracted from the plant Polygonum cuspidatum.

Another object of the present invention is to provide a method for preparing such an extract.

Another object of the present invention is to provide a pharmaceutical composition, including Polygonum cuspidatum, Polygonum cuspidatum extract and carriers commonly used in the pharmaceutical field.

Another object of the present invention is to provide the application of Polygonum cuspidatum and/or Polygonum cuspidatum extract, or a composition containing Polygonum cuspidatum and/or Polygonum cuspidatum extract in the preparation of drugs with insulin-sensitizing effect.

Another object of the present invention is to provide the application of Polygonum cuspidatum and/or Polygonum cuspidatum extract, or a composition containing Polygonum cuspidatum and/or Polygonum cuspidatum extract in preparing health products with insulin-sensitizing effect.

Another object of the present invention is to provide the application of Polygonum cuspidatum and/or Polygonum cuspidatum extract, or a composition containing Polygonum cuspidatum and/or Polygonum cuspidatum extract in the preparation of medicines for treating and preventing insulin resistance and related metabolic diseases.

Another object of the present invention is to provide the application of Polygonum cuspidatum and/or Polygonum cuspidatum extract, or a composition containing Polygonum cuspidatum and/or Polygonum cuspidatum extract in the preparation of health care products for treating and preventing insulin resistance and related metabolic diseases.

In order to accomplish the purpose of the present invention, can adopt following technical scheme:

The raw medicinal material of Polygonum cuspidatum is dried and properly crushed to increase the contact area between the medicinal material and the solvent and improve the efficiency. Water, alcohols, or a mixture of water and alcohols are used as solvents for extracting raw medicinal materials. Preferred alcohols include ethanol. A mixture of water and alcohols, such as water containing 40%-98% (volume ratio) of alcohol compounds. The amount of solvent during extraction is 4-14 times of the original drug weight. Extraction can be static or dynamic, preferably under dynamic conditions. The temperature of the extraction is in the range from room temperature (eg 20° C.) to the reflux temperature of the solvent, preferably at the reflux temperature. Extraction can be carried out continuously or intermittently, and can be repeated 1-4 times during intermittent extraction.

After the above steps are completed, the filtrates are combined, and the filtrates are heated and concentrated under normal pressure or reduced pressure in a dynamic state.

The filtrates were combined and further concentrated,

The extract can be freeze-dried to a dry powder.

The plant Polygonum cuspidatum is selected from the roots, rhizomes and whole plants of the perennial herb Polygonum cuspidatum of the genus Polygonaceae.

Products described in the present invention include medicines and health care products.

The present invention also relates to a pharmaceutical composition containing the extract of the present invention as an active ingredient and conventional pharmaceutical excipients or adjuvants. Usually the pharmaceutical composition of the present invention contains 0.1-95% by weight of the extract of the present invention.

The present invention also provides a pharmaceutical composition, which comprises an effective dose of the active ingredient of Polygonum cuspidatum and/or Polygonum cuspidatum extract according to the method of the present invention and a pharmaceutically acceptable carrier.

The pharmaceutical composition of the extract of the present invention can be prepared according to methods known in the art. When used for this purpose, if necessary, the extract of the present invention can be combined with one or more solid or liquid pharmaceutical excipients and/or adjuvants to make a suitable administration form that can be used as human medicine or veterinary medicine or dosage form.

The extract of the present invention or the pharmaceutical composition containing it can be administered in the form of a unit dose, and the route of administration can be enteral or parenteral, such as oral, nasal cavity, oral mucosa, skin, peritoneal or rectal administration, etc., preferably oral administration medicine.

The route of administration of the extract of the present invention or the pharmaceutical composition containing it also includes injection administration. Injection includes intravenous injection, intramuscular injection, subcutaneous injection, intradermal injection and the like.

The dosage forms for administration may be liquid dosage forms or solid dosage forms. For example, the liquid dosage forms can be true solutions, colloids, particulate dosage forms, emulsion dosage forms, and suspension dosage forms. Other dosage forms such as tablets, capsules, drop pills, aerosols, pills, powders, solutions, suspensions, emulsions, granules, suppositories, freeze-dried powder injections, etc.

The extract of the present invention can be made into common preparations, sustained-release preparations, controlled-release preparations, targeted preparations and various microparticle drug delivery systems.

Various carriers known in the art can be widely used for tableting unit dosage forms. Examples of carriers are, for example, diluents and absorbents such as starch, dextrin, calcium sulfate, lactose, mannitol, sucrose, sodium chloride, glucose, urea, calcium carbonate, kaolin, microcrystalline cellulose, silicic acid Aluminum, etc.; wetting agents and binders, such as water, glycerin, polyethylene glycol, ethanol, propanol, starch paste, dextrin, syrup, honey, glucose solution, acacia mucilage, gelatin paste, sodium carboxymethylcellulose , shellac, methylcellulose, potassium phosphate, polyvinylpyrrolidone, etc.; disintegrants, such as dry starch, alginate, agar powder, brown algae starch, sodium bicarbonate and citric acid, calcium carbonate, polyoxyethylene sorbate Sugar alcohol fatty acid esters, sodium lauryl sulfonate, etc.; lubricants, such as talc, silicon dioxide, corn starch, stearate, boric acid, liquid paraffin, polyethylene glycol, etc. Tablets can also be further made into coated tablets, such as sugar-coated tablets, film-coated tablets, enteric-coated tablets, or double-layer tablets and multi-layer tablets.

For example, in order to form a dosage unit into a pellet, various carriers known in the art can be widely used. Examples of carriers are, for example, diluents and absorbents, such as glucose, lactose, starch, cocoa butter, hydrogenated vegetable oil, polyvinylpyrrolidone, Gelucire, kaolin, talc, etc.; binders, such as acacia, tragacanth, Gelatin, ethanol, honey, glucose solution, mucilage arabic, gelatin paste, sodium carboxymethylcellulose, shellac, methylcellulose, potassium phosphate, polyvinylpyrrolidone, etc.; disintegrants such as dry starch, alginate , agar powder, algae starch, sodium bicarbonate and citric acid, calcium carbonate, polyoxyethylene sorbitol fatty acid ester, sodium dodecyl sulfonate, methyl cellulose, ethyl cellulose, etc.; disintegration inhibition Agents, such as sucrose, glyceryl tristearate, cocoa butter, hydrogenated oil, etc.; absorption enhancers, such as quaternary ammonium salts, stearates, boric acid, liquid paraffin, polyethylene glycol, etc. Tablets can also be further made into coated tablets, such as sugar-coated tablets, film-coated tablets, enteric-coated tablets, or double-layer tablets and multi-layer tablets.

For example, in order to form a dosage unit into a pellet, various carriers known in the art can be widely used. Examples of carriers are, for example, diluents and absorbents such as glucose, lactose, starch, cocoa butter, hydrogenated vegetable oil, polyvinylpyrrolidone, Gelucire, kaolin, talc, etc.; binders such as acacia, tragacanth, Gelatin, ethanol, honey, liquid sugar, rice paste, etc. Disintegrants, such as agar powder, dry starch, alginate, sodium dodecylsulfonate, methylcellulose, etc. For example, in order to form a dosage unit into a capsule, the active ingredient extract of the present invention is mixed with the above-mentioned various carriers, and the mixture thus obtained is placed in a hard gelatin capsule or a soft capsule. The active ingredient extract of the present invention can also be made into microcapsules, suspended in an aqueous medium to form a suspension, and can also be packed into hard capsules or made into injections for application.

For example, the extract of the present invention is made into injection preparations, such as solutions, suspension solutions, emulsions, and freeze-dried powder injections. This preparation can be aqueous or non-aqueous, and can contain one and/or more A pharmaceutically acceptable carrier, diluent, binder, lubricant, preservative, surfactant or dispersant. For example, the diluent may be selected from water, ethanol, polyethylene glycol, 1,3-propylene glycol, ethoxylated isostearyl alcohol, polyoxylated isostearyl alcohol, polyoxyethylene sorbitan fatty acid ester, and the like. In addition, in order to prepare an isotonic injection injection, an appropriate amount of sodium chloride, glucose or glycerin can be added to the injection preparation, and in addition, conventional co-solvents, buffers, pH regulators, etc. can also be added. These excipients are commonly used in the art. In addition, colorants, preservatives, fragrances, correctives, sweeteners or other materials can also be added to the pharmaceutical preparations, if necessary.

In order to achieve the purpose of medication and enhance the therapeutic effect, the medicine or pharmaceutical composition of the present invention can be administered by any known administration method.

The dosage of the extract pharmaceutical composition of the present invention depends on many factors, such as the nature and severity of the disease to be prevented or treated, the sex, age, body weight, personality and individual reaction of the patient or animal, the route of administration, and the number of administrations , therapeutic purposes, so the therapeutic dosage of the present invention can vary widely. Generally speaking, the dosages of the pharmaceutical ingredients in the present invention are well known to those skilled in the art. According to the actual amount of drug contained in the final preparation of the extract composition of the present invention, it can be adjusted appropriately to meet the requirement of its therapeutically effective dose, so as to complete the preventive or therapeutic purpose of the present invention. The suitable daily dosage range of the extract of the present invention is 0.001-100g crude drug/kg body weight, preferably 0.01-50g crude drug/kg body weight, most preferably 0.05-25g crude drug/kg body weight. The above-mentioned dosage may be administered in a single dosage form or divided into several, such as two, three or four dosages, subject to the clinical experience of the administering physician and the dosage regimen including the use of other therapeutic means. The total dosage required for each treatment may be divided into multiple doses or administered in a single dose. The extract or composition of the present invention can be taken alone, or used in combination with other therapeutic drugs or symptomatic drugs and adjusted in dosage.

For diet-induced IRF mice with insulin resistance and other metabolic syndrome characteristics, Polygonum cuspidatum extract can significantly improve insulin resistance, and has obvious regulatory effects on animal blood sugar, weight gain and other metabolic diseases.

Description of drawings

Figure 1. The effect of Polygonum cuspidatum extract on blood sugar after exogenous insulin load (n=10.#, ##, ###, p<0.05, 0.01, 0.001vsCon; ^* , ^** , ^*** , p<0.05 , 0.01, 0.001 vs IRF.)

Figure 2. The effect of Polygonum cuspidatum extract on the area under the blood glucose-time curve after insulin load (n=10.###, p<0.001vsCon; ^** , ^*** , p<0.01, 0.001vs IRF.)

Figure 3. Effect of Polygonum cuspidatum extract on changes in blood sugar after glucose load (n=10.#, ##, p<0.05, 0.01vsCon; ^* , ^** , p<0.05, 0.01vsIRF.)

Figure 4. The effect of Polygonum cuspidatum extract on the area under the blood glucose-time curve after glucose load (n=10.##, p<0.01vsCon; ^* , ^** , p<0.05, 0.01vs IRF.)

Figure 5. The effect of Polygonum cuspidatum extract on the steady-state glucose infusion rate GIR in the normal glucose clamp test of IRF mice (n=10.###, p<0.001vs Con; ^*** , p<0.001vs IRF. )

Figure 6. The effect of Polygonum cuspidatum extract on the blood sugar level of IRF mice (n=10.###, p<0.001vsCon; ^*** , p<0.001vs IRF.)

Figure 7. The effect of Polygonum cuspidatum extract on weight gain of IRF mice (n=10.###, p<0.001vs Con; ^* , p<0.05vs IRF.)

Detailed ways

Preparation of Polygonum cuspidatum extract

Example 1.

The roots and rhizomes of Polygonum cuspidatum are sliced and dried, crushed into coarse powder, the coarse powder is extracted with 40% ethanol under reflux, the extract is filtered, concentrated and dried to obtain the Polygonum cuspidatum extract. Concrete method: 1) get 200 g of dried rhizomes of Polygonum cuspidatum, add 1500 ml of 95% ethanol, extract under reflux for 45 minutes, cool, and pour out the ethanol extract; under the same conditions, extract twice again. The combined extracts were concentrated by a rotary evaporator to 200 ml under reduced pressure, and the concentrated solution was freeze-dried to obtain 36.4 g of a yellow-brown blocky extract.

Example 2.

Take the roots and rhizomes of Polygonum cuspidatum as raw materials, slice them, dry them, crush them into coarse powder, take 200g, add 1500ml of 75% ethanol, extract under reflux for 45 minutes, cool, pour out the ethanol extract; and extract twice under the same conditions. The combined extracts were concentrated by a rotary evaporator to 200 ml under reduced pressure, and the concentrated solution was freeze-dried to obtain 30 g of a yellow-brown blocky extract.

Example 3.

The roots and rhizomes of Polygonum cuspidatum are sliced and dried, crushed into coarse powder, the coarse powder is extracted with 95% ethanol under reflux, the extract is filtered, concentrated and dried to obtain the Polygonum cuspidatum extract. Concrete method: 1) get 200 g of dried rhizomes of Polygonum cuspidatum, add 1500 ml of 95% ethanol, extract under reflux for 45 minutes, cool, and pour out the ethanol extract; under the same conditions, extract twice again. The extracts were combined, concentrated to 200 ml by a rotary evaporator under reduced pressure, and the concentrate was freeze-dried to obtain 36.0 g of a yellow-brown blocky extract.

Example 4.

The roots and rhizomes of Polygonum cuspidatum are sliced and dried, then crushed into coarse powder, the coarse powder is extracted with water as solvent, refluxed, the extract is filtered, concentrated and dried to obtain Polygonum cuspidatum extract. Specific methods: 1) Take 100 g of dried rhizomes of Polygonum cuspidatum, add 1500 ml of water, extract under reflux for 45 minutes, cool, pour out the water extract; and extract twice under the same conditions. The combined extracts were concentrated by a rotary evaporator to 200 ml under reduced pressure, and the concentrated solution was freeze-dried to obtain 34 g of a yellow-brown blocky extract.

Pharmacological experiment

Example 1 Effect of Polygonum cuspidatum Extract on Insulin Tolerance in Insulin-resistant IRF Mice

method:

C57BL mice were fed with high-fat and high-sugar diet to form insulin resistance mouse model (IRF). The model animals were randomly divided into 3 groups, which were model animal control group (IRF), rosiglitazone group, and Polygonum cuspidatum extract group, and water, positive control drug rosiglitazone 15mg/kg, and Polygonum cuspidatum extract 200mg were orally administered respectively. /kg. At the same time, the same batch of normal animals fed with normal feed were set as the normal control group (Con). Inject 0.4U/kg insulin subcutaneously to the animals, observe the change of blood glucose after insulin loading, and calculate the area under the blood glucose-time curve (AUC), that is, the insulin tolerance test (ITT).

result:

Insulin-resistant animals were administered continuously for 14 days, and ITT experiments were carried out. The results showed (Fig. 1) that compared with the normal control group Con, the decline in blood glucose at each time point of the animals in the IRF group after insulin load was significantly higher, showing obvious insulin resistance. Compared with the IRF model animals, the percentages of blood glucose decline at each time point after the insulin load in the insulin sensitizer rosiglitazone group were significantly lower, indicating that the sensitivity of the animal to insulin was significantly increased; The blood sugar decreased, and the trough value of blood sugar at 30 minutes and the recovery value of blood sugar at 120 minutes were both significantly reduced, and the area under the blood glucose-time curve (AUC) was significantly reduced (Figure 2). This effect is similar to that of the insulin sensitizer rosiglitazone, indicating that the extract of Polygonum cuspidatum has a certain insulin-sensitizing effect on IRF mice.

Example 2. Effect of Polygonum cuspidatum extract on oral glucose tolerance in insulin resistant IRF mice

method:

C57BL mice were fed with high-fat and high-sugar diet to form insulin resistance mouse model (IRF). The model animals were randomly divided into 3 groups, which were model animal control group (IRF), rosiglitazone group, and Polygonum cuspidatum extract group, and water, positive control drug rosiglitazone 15mg/kg, and Polygonum cuspidatum extract 200mg were orally administered respectively. /kg. At the same time, the same batch of C57BL mice were fed with normal feed as the normal control group (Con). Continuous administration for 6 days, oral glucose 2g/kg was given to animals, the changes in blood glucose after glucose loading were observed, and the area under the blood glucose-time curve (AUC) was calculated, namely the Oral Glucose Tolerance Test (OGTT).

result:

The results showed ( FIG. 3 ), compared with Con, the blood glucose of animals in the IRF group was significantly higher at each time point, showing obvious impaired glucose tolerance. Compared with the animals in the IRF group, the blood glucose of the animals in the rosiglitazone group decreased significantly at each time point after the glucose load, showing the effect of significantly improving the glucose tolerance of the animals; the blood glucose of the animals in the Polygonum cuspidatum extract group decreased significantly at each time point after the glucose load, Moreover, both the 30-min peak blood glucose and 120-min blood glucose recovery values were significantly reduced, and the area under the blood glucose-time curve AUC was significantly reduced (Figure 4). This effect is similar to that of the insulin sensitizer rosiglitazone, indicating that the extract of Polygonum cuspidatum can improve the body's glucose tolerance to a certain extent in insulin-resistant mice.

Example 3. Effect of Polygonum cuspidatum Extract on Glucose Infusion Rate GIR at Steady State in Ecglucose Clamp Experiment of Insulin Resistance IRF Mice

method:

C57BL mice were fed with high-fat and high-sugar diet to form insulin resistance mouse model (IRF). The model animals were randomly divided into 3 groups, which were model animal control group (IRF), rosiglitazone group, and Polygonum cuspidatum extract group, and water, positive control drug rosiglitazone 15mg/kg, and Polygonum cuspidatum extract 200mg were orally administered respectively. /kg. At the same time, the same batch of C57BL mice were fed with normal feed as the normal control group (Con). Continuously administered for 20-25 days, a hyperinsulinemic clamp (orthoglycemic clamp) experiment with normal glucose levels was performed. That is, the animals were fasted for 4 hours, weighed, anesthetized by intraperitoneal injection of pentobarbital sodium, fixed on a 37°C constant temperature plate, surgically separated from the jugular vein, intubated, injected with 1000U/ml heparin for anticoagulation, and connected to a microinjector (COLE PARMER, 789100C, U.S.) infused insulin 60pmol/kg/min at a constant rate, and a microperistaltic pump (ISMATEC, 78001-00, U.S.) infused 10% glucose solution at a variable rate; the carotid artery was surgically separated for blood collection. Blood was collected every 10 minutes, and blood glucose levels were monitored with a blood glucose meter (BIOSEN 5030, Germany). Adjust the glucose infusion rate according to the blood sugar level, so that the blood sugar is stable within the range of 95±5 mg/dl. After the blood sugar is stable for at least 30 minutes, measure the glucose infusion rate 3 times continuously, and take the average value as the steady state in the normal glucose clamp test of the animal. glucose infusion rate (GIR).

result:

The GIRF value of glucose infusion rate at steady state in hyperinsulinemic clamp (euglycemic clamp) experiment with normal glucose level is currently recognized as the gold standard for evaluating insulin resistance. The experimental results showed ( FIG. 5 ) that in the glucose clamp experiment, compared with Con, the GIRF level of animals in the IRF group was significantly lower, indicating that the model animals already had obvious insulin resistance. Compared with IRF model animals, insulin sensitizer rosiglitazone and Polygonum cuspidatum extract increased GIRF levels by 277.9% and 106.9% respectively. It shows that Polygonum cuspidatum extract is similar to rosiglitazone, and both have the effect of significantly increasing the sensitivity of insulin-resistant IRF mice to exogenous insulin.

Example 4. Effect of Polygonum cuspidatum extract on blood glucose level in insulin resistant IRF mice

method:

C57BL mice were fed with high-fat and high-sugar diet to form insulin resistance mouse model (IRF). The model animals were randomly divided into 3 groups, which were model animal control group (IRF), rosiglitazone group, and Polygonum cuspidatum extract group, and water, positive control drug rosiglitazone 15mg/kg, and Polygonum cuspidatum extract 200mg were orally administered respectively. /kg. At the same time, the same batch of normal animals fed with normal feed were set as the normal control group (Con).

result:

Insulin-resistant animals were given continuous administration for 14 days, and changes in blood glucose levels were observed. The results showed that compared with the normal control Con group, the blood glucose level of the IRF mouse model was significantly increased. Both the extract of Polygonum cuspidatum and rosiglitazone showed obvious hypoglycemic effects, so that the blood glucose levels of animals in the Polygonum cuspidatum extract group and rosiglitazone group were significantly lower than those in the model control IRF group ( FIG. 6 ).

Example 5. Effect of Polygonum cuspidatum extract on weight gain of insulin resistant IRF mice

method:

C57BL mice were fed with high-fat and high-sugar diet to form insulin resistance mouse model (IRF). The model animals were randomly divided into 3 groups, which were model animal control group (IRF), rosiglitazone group, and Polygonum cuspidatum extract group, and water, positive control drug rosiglitazone 15mg/kg, and Polygonum cuspidatum extract 200mg were orally administered respectively. /kg. At the same time, the same batch of normal animals fed with normal feed were set as the normal control group (Con).

result:

Insulin-resistant animals were administered continuously for 14 days, and the changes in body weight were observed compared with those before administration. The results showed that, compared with the normal control Con group, the weight gain of the IRF mouse model was significantly accelerated. Compared with the model control IRF group, Polygonum cuspidatum extract can significantly slow down the weight growth rate of animals, and significantly reduce the average weight gain (Figure 7); while rosiglitazone has a tendency to accelerate the weight gain of animals.

Claims (9)

1. Application of plant Polygonum cuspidatum in the preparation of insulin sensitizer products. 2. The application of the plant Polygonum cuspidatum in the preparation of products for the treatment and prevention of insulin resistance and related metabolic diseases. 3. The application according to claim 1-2, characterized in that, the plant Polygonum cuspidatum is the whole grass, aerial parts, roots, and rhizomes of the perennial herb Polygonum cuspidatum of the Polygonaceae genus Polygonum cuspidatum. 4. The preparation method of Polygonum cuspidatum extract, which is characterized by drying and crushing Polygonum cuspidatum into coarse powder; extracting coarse powder with water or 40-95% ethanol, concentrating and drying the extract to obtain Polygonum cuspidatum extract. 5. The preparation method according to claim 4, characterized in that the Polygonum cuspidatum is selected from the whole herb of Polygonum cuspidatum, aerial parts, roots and rhizomes. 6. The Polygonum cuspidatum extract prepared according to claims 4-5. 7. the application of the Polygonum cuspidatum extract of claim 6 in the preparation of insulin sensitizer products. 8. The application of the Polygonum cuspidatum extract according to claim 6 in the preparation of products for the treatment and prevention of insulin resistance and related metabolic diseases. 9. A pharmaceutical composition, characterized in that it comprises the extract of Polygonum cuspidatum according to claim 6 and a pharmaceutically acceptable carrier in an effective dosage.

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