CN102397274A - Use of bergenin in preparation of drugs for treatment of diabetes - Google Patents
Use of bergenin in preparation of drugs for treatment of diabetes Download PDFInfo
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- CN102397274A CN102397274A CN2011100596181A CN201110059618A CN102397274A CN 102397274 A CN102397274 A CN 102397274A CN 2011100596181 A CN2011100596181 A CN 2011100596181A CN 201110059618 A CN201110059618 A CN 201110059618A CN 102397274 A CN102397274 A CN 102397274A
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Abstract
The present invention discloses a use of bergenin in preparation of drugs for treatment of diabetes, and belongs to the field of the pharmacological use of the bergenin. The results of animal experiments show that: with the bergenin, the model forming rate of type 2 diabetes rats can be significantly reduced, the occurrence and the development of insulin resistance can be prevented, the insulin resistance degree of the rats can be significantly reduced, and the insulin sensitivity of the type 2 diabetes rats can be effectively improved. In addition, the results provided by the present invention further show that: with the bergenin, the triglyceride content and the total cholesterol content in blood serum can be significantly reduced, and the lipid metabolism disorder of the type 2 diabetes rats can be effectively improved. Therefore, the results show that the bergenin can be used for preparing into the drugs for the treatment of the diabetes and the blood lipid reducing drugs.
Description
Technical field
The present invention relates to a kind of pharmacological use of Bergeninum, relate in particular to the purposes of Bergeninum in preparation treatment diabetes medicament, belong to the pharmacological use field of Bergeninum.
Background technology
Bergeninum (bergenin) is claimed arolisic acid B again, bergenin; Bergenin; Bergenin, bergenits etc. are saxifragaceae plant Rhizoma Seu Herba Bergeniae Bergenia purpurascens herb and Rhizoma Seu Herba Bergeniae (B.crassifoloa; Astilbe macroflora), the main component of the root of Myrsinacea plant Radix Ardisiae Crispae plants such as (Ardisia crispa), stem, leaf, molecular formula is C
14H
160
9, its structural formula is seen Fig. 1.
Bergeninum has pharmacologically active widely.Research show Bergeninum have immunological enhancement, antiinflammatory action, blood coagulation resisting function, anticoagulation and anti-arrhythmia effect, eliminate the phlegm, relieving asthma and antitussive action, liver protection effect, secretion inhibitor, antiulcer action, anti HIV-1 virus effect and antioxidation etc. (Xia Conglong etc., the progress of Bergeninum. the time precious the 17th the 3rd phase of volume of traditional Chinese medical science traditional Chinese medicines .2006).Up to now, there is not Bergeninum to have the relevant report that the pharmacologically active of insulin sensitivity takes place, improves the prevention insulin resistant as yet.
Metabolism syndrome is a kind of syndrome of following many syndromes such as central obesity, hypertension, pathoglycemia and blood fat disorder, has become global health problem at present.Insulin resistant is one of main pathogenesis of metabolism syndrome, and low chronic inflammatory reaction plays an important role in the generation of insulin resistant and evolution.
Along with the variation of dietary structure, at present the whole world is existing surpasses 100,000,000 obese patients, and the cardiovascular and cerebrovascular disease that is caused by obesity, diabetes etc. have become the public health problem that receives much attention.The obese patient; Particularly overweight people's body fat tissue of abdomen fat increase discharges a large amount of free fatties, the adipose cell factor comprises TNF-α, IL-6, leptin (Leptin), phylaxin (resistin) etc.; Cause the body inflammatory reaction, the state of this overnutrition of body can activating immune system.Research shows that the low grade inflammation reaction that obesity causes is to bring out one of most important reasons of metabolism syndrome such as insulin resistant, diabetes, cardiovascular disease.
Summary of the invention
Main purpose of the present invention provides a kind of new pharmacological use of Bergeninum;
Main purpose of the present invention realizes through following technical scheme:
The present invention has at first made up the type-II diabetes rat model, for understanding Bergeninum whether insulin resistant is had prevention and therapeutical effect, and the present invention has designed two kinds of experimental programs of prevention administration and treatment administration.Prevention administration experiment shows that Bergeninum can significantly reduce the one-tenth mould rate of type-II diabetes rat, the incidence and development of prevention insulin resistant.And in the animal that insulin resistant takes place, Bergeninum can significantly increase the GIR of insulin resistance rat, shows that Bergeninum can significantly reduce the insulin resistant degree of rat.
Through insulin tolerance experiment and body weight, blood fat Comprehensive Assessment; The present invention selects the type-II diabetes rat of insulin resistant; Give Bergeninum; Find the be significantly increased GIR of type-II diabetes rat of each dose groups of Bergeninum, show that Bergeninum can significantly improve type-II diabetes rat insulin sensitivity.
In addition, the present invention finds that also Bergeninum can obviously reduce triglyceride in the serum (TG) and triglyceride (TCHO) content, and it is disorderly to show that Bergeninum can significantly improve the type-II diabetes lipid metabolism in rats.
Another object of the present invention provides the pharmaceutical composition of a kind of prevention or treatment diabetes or blood fat reducing, and this pharmaceutical composition is cooperated with pharmaceutically acceptable carrier, excipient or diluent by the Bergeninum of effective dose and forms.According to different medications, pharmaceutical composition of the present invention can contain 0.1%-99% weight, the Bergeninum of preferred 10-60% weight.
Can be according to the conventional drug formulation process in this area; In Bergeninum, add acceptable accessories or preparing carriers commonly used in the preparations shaping and become any suitable clinical preparation; These all are that those skilled in the art understand thoroughly, and for example can be oral formulations (tablet, oral liquid, granule, capsule, soft capsule or drop pill etc.) etc.; Wherein, described adjuvant can be antioxygen chelating agent, filler, framework material etc.; Described pharmaceutically acceptable carrier is one or more in xylitol, mannitol, lactose, fructose, glucosan, glucose, polyvinylpyrrolidone, low molecular dextran, sodium chloride, calcium gluconate or the calcium phosphate.
Description of drawings
The chemical structural formula of Fig. 1 Bergeninum.
The insulin sensitivity experimental result takes place, improves in the opposing of Fig. 2 Bergeninum prevention type-II diabetes rat insulin.
Fig. 3 Bergeninum reduces type-II diabetes rat insulin opposing degree, improves the insulin sensitivity experimental result.
Fig. 4 Bergeninum improves the experimental result of lipid metabolic disorder.
The specific embodiment
Further describe the present invention below in conjunction with specific embodiment, advantage of the present invention and characteristics will be more clear along with description.But these embodiment only are exemplary, scope of the present invention are not constituted any restriction.It will be understood by those skilled in the art that and down can make amendment with form or replace without departing from the spirit and scope of the present invention, but these modifications and replacing all fall in protection scope of the present invention the details of technical scheme of the present invention.
Experimental example 1
1, main agents and laboratory animal
Bergeninum grinds living biochemical reagents company limited, purity >=98% available from Shanghai.Glucose, TG (triglyceride) and TCHO (T-CHOL) detection kit are available from giving birth to high-tech technology company in Beijing; The SABC test kit is available from China fir company in Beijing, and high lipid food (containing 7.5% Adeps Sus domestica, 7.5% safflower oil, 1% cholesterol, 1% casein, 10% sucrose etc.) is available from Chinese Academy of Medical Sciences's Experimental Animal Center.
In the experiment employed animal be SPF level SD rat (male, 120～140g), available from Beijing Vital River Experimental Animals Technology Co., Ltd., animal quality certification SCXK (capital) 2002-0003.Animal feeding is in the SPF of China Medical Sciences Academy Medical Plants Institute level experimental animal room, constant temperature and humidity, high fat diet.
2, experimental technique
2.1, type-II diabetes rat model preparation and experiment divide into groups
The preparation of type-II diabetes rat model: after high lipid food was fed 1 month, (fasting glucose was the modeling success greater than 120mg/dl to continuous three days lumbar injection streptozotocins for STZ, Sigma.) 35mg/kg.
Prevention administration group: 4 age in week male rat begin administration, 16 every group, be divided into model control group and Bergeninum group (i.g.150mg/kg, once/sky), administration time is 1 month.Give high lipid food and STZ after January.
Treatment administration group: select the successful type-II diabetes rat of modeling for use; According to type-II diabetes rat 40 minutes blood glucose decline percents, fasting serum glucose, blood triglyceride, blood T-CHOL and body weight in the insulin tolerance experiment; Evenly be divided into 5 groups; Be respectively matched group, positive control drug metformin group (Metformin, i.g 100mg/kg) and basic, normal, high three dose groups of Bergeninum, be respectively 100mg/kg, 200mg/kg, 400mg/kg.Other gets the SD rat as the normal control group.12 of every treated animals.Administration time is 60 days.
2.2, the experiment of the positive blood glucose of hyperinsulinism pincers
Row jugular vein intubate is with infusion high level insulin (8mU/kg.min) and 10% glucose solution behind the anesthetized rat; Femoral arteriography monitoring blood glucose; Every measure the input rate of glucose level, make animal blood glucose, when animal blood glucose during near 5.0mM near 5.0mM with suitable increase glucose at a distance from 10min; Every 5min measures blood glucose; And fine setting glucose input rate makes animal blood glucose maintain 5.0 ± 0.2mM, and continuous 5 points think that promptly animal blood glucose reaches steady-state level, and this moment, the input rate of glucose equaled peripheral tissues's elimination speed to glucose under exogenous insulin action.5--6 glucose infusion speed under the record stable state, its meansigma methods is as GIR (glucose infusion rate).The GIR value is high more, explains that animal is high more to the sensitivity of insulin.
3, experimental result
3.1 the insulin sensitivity result takes place, improves in the opposing of Bergeninum prevention type-II diabetes rat insulin
For understanding Bergeninum whether insulin resistant is had prevention and therapeutical effect, this experimental design two kinds of experimental programs of prevention administration and treatment administration.1.96 times difference with normal control group blood glucose decline percentage rate meansigma methods and its standard deviation in the insulin tolerance experiment is a boundary, then is insulin resistant less than this value person.Prevention administration experiment shows; The rat type-II diabetes becomes the mould rate to be respectively 81.25%; Bergeninum prevention administration after 1 month the rat type-II diabetes become the mould rate to be respectively 56.25%; Show that Bergeninum can significantly reduce the one-tenth mould rate of type-II diabetes rat, the incidence and development (Fig. 2 A) of prevention insulin resistant.And in the animal that insulin resistant takes place, Bergeninum can significantly increase the GIR of insulin resistance rat, shows that Bergeninum can significantly reduce the insulin resistant degree of rat (Fig. 2 B).
3.2 Bergeninum reduces type-II diabetes rat insulin opposing degree, improves insulin sensitivity
Through insulin tolerance experiment and body weight, blood fat Comprehensive Assessment; Select the type-II diabetes rat of insulin resistant, after the random packet, give 60 days Bergeninums; Find that the Bergeninum high dose group can significantly reduce insulin level in the animal blood; In dose groups significantly reduce fasting blood glucose level, other each group influence not obvious (Fig. 3 A, B).The be significantly increased GIR (Fig. 3 C) of type-II diabetes rat of each dose groups of Bergeninum shows that Bergeninum can significantly improve type-II diabetes rat insulin sensitivity.
3.3 Bergeninum improves lipid metabolic disorder
The Bergeninum high dose group can obviously reduce triglyceride in the serum (TG) and triglyceride (TCHO) content, and it is disorderly to show that Bergeninum can significantly improve the type-II diabetes lipid metabolism in rats.
The preparation of embodiment 1 oral liquid
It is an amount of to get Bergeninum, adds an amount of solubilizing agent, grinds, and adds the low amounts of water dilution again, and mixing adds correctives and antiseptic then, and mixing adds water to ormal weight.Mixing, packing, sterilization promptly gets.
The preparation of embodiment 2 tablets
It is an amount of to get Bergeninum, adds right amount of auxiliary materials, and mixing is processed granule, drying, and compacting promptly gets in flakes.
The preparation of embodiment 3 dispersible tablets
It is an amount of to get Bergeninum, and it is an amount of to add crosslinked carboxymethyl fecula sodium, crospolyvinylpyrrolidone, microcrystalline Cellulose, micropowder silica gel, protein sugar, and mixing is granulated, drying, and compacting promptly gets in flakes.
The preparation of embodiment 4 capsules
It is an amount of to get Bergeninum, adds right amount of auxiliary materials, and mixing is processed granule, and drying incapsulates, and promptly gets.
Embodiment 5 preparation of soft capsule
It is an amount of to get Bergenin, is ground into fine powder, subsequent use; It is an amount of to get compound stabilizer, in 60 ℃ of water-bath heat fused, adds in the soybean salad oil, stirs miscible; Said extracted thing fine powder is added in the fluid, and stirring and evenly mixing is regulated the colloid mill fineness between 5～15 μ m, adds the soup circulation and mills 0.5 hour, and fully mixing filters (crossing 100 mesh sieves), makes soft capsule content; It is an amount of to get gelatin, glycerine, distilled water, pigment, after changing glue, makes rubber, the embedding pelleting, and dry 12 hours, alcohol was washed ball, drying, is promptly got.
The preparation of embodiment 6 drop pills
It is an amount of to get Bergeninum, is ground into fine powder, subsequent use; Other get mix Polyethylene Glycol (PEG6000: PEG1500=1: 1) an amount of, be heated to 90～100 ℃, treat whole fusions after; Add the Bergeninum fine powder, fully mixing and insulation are at 70～80 ℃, from top to bottom; Splash in the liquid paraffin; With the drop pill drop of molding to the greatest extent and the erasing liquor paraffin body, dry below 40 ℃, promptly get.
The preparation of embodiment 7 granules
It is an amount of to get Bergeninum, adds appropriate amount of auxiliary materials and correctives, and mixing is processed granule, and drying promptly gets.
The preparation of embodiment 8 pills
It is an amount of to get Bergeninum, adds starch, maltose is an amount of, puts mixing in the coating pan, and pill adds after a small amount of Pulvis Talci rolls evenly, and microwave drying with an amount of polishing of Cera Chinensis, promptly gets.
Claims (9)
1. Bergeninum is treated the purposes in the diabetes medicament in preparation.
2. according to the described purposes of claim 1, it is characterized in that: described diabetes are type-II diabetes.
3. Bergeninum reduces human body to the purposes in the insulin resistant degree medicine in preparation.
4. Bergeninum improves human body to the purposes in the medicine of insulin sensitivity in preparation.
5. Bergeninum is in the purposes of preparation in the blood lipid-lowering medicine.
6. a pharmaceutical composition of treating diabetes is characterized in that: form by treating Bergeninum and the pharmaceutically acceptable carrier of going up effective dose.
7. a pharmaceutical composition that reduces human body to the insulin resistant degree is characterized in that: form by treating Bergeninum and the pharmaceutically acceptable carrier of going up effective dose.
8. a pharmaceutical composition that improves human body to insulin sensitivity is characterized in that: form by treating Bergeninum and the pharmaceutically acceptable carrier of going up effective dose.
9. the pharmaceutical composition of a blood fat reducing is characterized in that: form by treating Bergeninum and the pharmaceutically acceptable carrier of going up effective dose.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108653278A (en) * | 2018-07-05 | 2018-10-16 | 天津中医药大学 | A kind of fat protective agents and method of Bergenin preparation |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1634049A (en) * | 2004-11-05 | 2005-07-06 | 云南省药物研究所 | Bergeninum buccal tablets and its preparation process |
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- 2011-03-11 CN CN2011100596181A patent/CN102397274A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1634049A (en) * | 2004-11-05 | 2005-07-06 | 云南省药物研究所 | Bergeninum buccal tablets and its preparation process |
Non-Patent Citations (2)
| Title |
|---|
| S. RASTOGI, A.K.S. RAWAT: "A comprehensive review on bergenin, a potential hepatoprotective and anti-oxidative phytoconstituent", 《HERBA. POLONICA》 * |
| 王继良 等: "岩白菜素的研究进展", 《中国民族民间医药杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108653278A (en) * | 2018-07-05 | 2018-10-16 | 天津中医药大学 | A kind of fat protective agents and method of Bergenin preparation |
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Application publication date: 20120404 |