CN104000877A - Blood glucose reducing composition and application thereof - Google Patents
Blood glucose reducing composition and application thereof Download PDFInfo
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- CN104000877A CN104000877A CN201410238109.9A CN201410238109A CN104000877A CN 104000877 A CN104000877 A CN 104000877A CN 201410238109 A CN201410238109 A CN 201410238109A CN 104000877 A CN104000877 A CN 104000877A
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Abstract
The invention belongs to the technical field of pharmacy, and particularly relates to a blood glucose reducing composition and application thereof. The composition is prepared from the following components in parts by weight: 10-30 parts of cordyceps sinensis, 50-80 parts of ginseng, 150-200 parts of fructus swietenia macrophylla, 30-60 parts of bitter gourd and 25-55 parts of cactus. The blood glucose reducing composition has the beneficial effects that regarding treatment on type 2 diabetes, the relationship among liver, bile, pancreas, stomach and kidney can be comprehensively balanced, the comprehensive metabolic capability can be gradually improved, the hemoglobin level can be smoothly restored and reduced, and the status of diabetic complications can be reduced. The blood glucose reducing composition does not have toxic or side effects, and is safe and reliable for long-term administration.
Description
Technical field
The invention belongs to pharmaceutical technology field, in particular to a kind of compound for reducing blood suger and application thereof.
Background technology
Xiang Tianguo (formal name used at school Fructus Swietenia Macrophylla), belong to Meliaceae plant, have another name called Fructus Fici Beecheyanae, Solomon Islands, the South Pacific Ocean is originated in source, to high approximately 30 meters to 40 meters of sky fruit tree, because its fruit is gained the name to sky growth, to sky, be really described as " after plant ", it can adjust body metabolism function, the insulin of self is able to " resurrection " and play one's part to the full, have direct hypoglycemic activity, the hepatoprotective effect simultaneously having, can alleviate or prevent some oral hypoglycemic thing infringements to liver.
The sickness rate of diabetes raises year by year, and at present, nearly 2.85 hundred million diabeticss, account for 6.4% of world population in the world, expect 2030, and this numeral will reach 4.38 hundred million.Diabetes are to take due to what insulin resistant in human body and hyposecretion caused the metabolic disease that blood sugar increasing is feature.Mainly be divided into 1 type (T1DM) and 2 types (T2DM).The former is because pancreaticβ-cell can not produce due to enough insulins (insulin definitely lacks), the multiple teenager of being born in; The latter is due to due to hypoinsulinism or insulin resistant (insulin lacks relatively), is more common in middle-aged and elderly people.In diabetics, approximately have 90%～95% to belong to T2DM, therefore become the main Types of medicament research and development.The limitation of T2DM treatment is that most medicine all exists obvious untoward reaction, and for example metformin can cause obvious gastrointestinal reaction, causes diarrhoea, feels sick, lactic acidosis etc.; Sulfonylurea drugs and insulin can cause that hypoglycemia and body weight increase; Thiazolidinediones also can cause that body weight increases and edema phenomenon; Newfound medicine can cause nausea, vomits, suffer from diarrhoea as incretin analog.In addition, even if several oral hypoglycemic use in conjunction is also difficult to reach the object of effective control blood glucose.
The glucose transporter (SGLTs) that sodium relies on is the transporter gene family that a class is found in small intestinal mucosa and kidney proximal tubule, and the process that kidney heavily absorbs glucose is mainly mediated by SGLTs.Wherein, SGLT1 and SGLT2 are the most important, and SGLT2 plays a leading role.Optionally suppress SGLT2 and can significantly reduce the heavily absorption of body to glucose, thereby reduce blood sugar level by increasing the discharge of glucose in urine.SGLT2 inhibitor is a kind of creationary therapeutic strategy, and its action target spot is all different from existing antidiabetic drug with mechanism, becomes the focus of hypoglycemic medicine research.Therefore, be badly in need of the medicine of a kind of anti-T2DM based on new mechanism of exploitation to overcome above-mentioned shortcoming, the discovery of SGLT2 inhibitor is expected to make up the shortcoming of current hypoglycemic medicine, becomes effective antihypelipidemic preparation of new class.
Summary of the invention
For solving the problems of the technologies described above, the invention provides a kind of compound for reducing blood suger and application thereof.
A kind of compound for reducing blood suger of the present invention, by Cordyceps, Radix Ginseng, Xiang Tianguo, Fructus Momordicae charantiae, Radix et Caulis Opuntiae Dillenii forms, and wherein, described Cordyceps is 10-30 part, and Radix Ginseng is 50-80 part, and Xiang Tianguo is 150-200 part, and Fructus Momordicae charantiae is 30-60 part, and Radix et Caulis Opuntiae Dillenii is 25-55 part.
Further, described Cordyceps is 15-25 part, and Radix Ginseng is 61-69 part, and Xiang Tianguo is 170-180 part, and Fructus Momordicae charantiae is 45-55 part, and Radix et Caulis Opuntiae Dillenii is 34-48 part.
Further, a kind of compound for reducing blood suger and pharmaceutically acceptable carrier form.
Described carrier comprises
Further, described medicine is granule, pill, decoction, tablet, capsule or powder.
Described dosage form is common process and makes.
Further, this preparation method comprises the steps: raw material powder to be broken into fine powder, to sieve, to mix in proportion, and obtains.
Wherein, hypoglycemic medicine is preferably the pharmaceutical composition containing oriented day fruit for blood sugar lowering.
The present invention also provides described pharmaceutical composition application in preparing hypoglycemic medicine as effective ingredient.
Process for preparing medicine of the present invention is: aforesaid raw material is mixed by corresponding weight proportion, first with clear water, clean remove impurity, the warm water soaking 1-3h of 30-50 ℃ of quality such as then used, then, add raw material weight 3-5 water doubly, at 75-90 ℃, extract 3-5 time, after cold filtration, at 65 ℃ of following concentrated flowing soaking pastes that become with the quality such as raw material, shake up sealing, as for shady and cool ventilation place, preserve.Above-mentioned extractum can directly be done medicinal, also can be used for as animal blood sugar lowering model test.
In prescription, Cordyceps is a kind of fungus, containing cordycepic acid, vitamin B12, fat, albumen etc., impotence due to deficiency of the kidney, waist knee joint ache etc. is had to good curative effect.Radix Ginseng, modern experiment shows that Radix Ginseng extract, ginseng polysaccharide, ginseng polypeptide, Stem and leaf of Radix Ginseng polysaccharide, the non-Saponin part of Radix Ginseng all have hypoglycemic activity, can be used for the treatment of diabetes.Xiang Tianguo,, convergence cool in nature, antipyretic to sky fruit, kernel bitter in the mouth, puckery, contains multiple antioxidant, flavone and polyphenol, has good reduction blood glucose, improves the effect of immunity.Fructus Momordicae charantiae is rich in vitamin and the trace element such as carotene, retinol, thiamine, riboflavin, nicotinic acid and selenium, is especially rich in and has the Charantin that reduces blood glucose effect.Radix et Caulis Opuntiae Dillenii nutritious, contains a large amount of vitamin and mineral, and its contained vitamin can suppress the absorption of metabolism of lipid and cholesterol, and can slow down the picked-up to glucose, thereby has the effect of blood sugar lowering, blood fat reducing, blood pressure lowering.
Beneficial effect of the present invention is: compound for reducing blood suger of the present invention, mainly in treatment type 2 diabetes mellitus, described compound for reducing blood suger is according to modern anatomy new concept, from outer digestive gland, start with, the relation of overall balance liver and gall pancreas stomach kidney, progressively improve comprehensive metabolic capacity, steadily recover and reduce (HbA1c) glycolated hemoglobin level, reduce diabetic complications state.Without any toxic and side effects, long-term taking is safe and reliable simultaneously.Compound for reducing blood suger oral administration enters after gastrointestinal, can grow and secrete polypeptide parahormone by stimulating gastrointestinal, promotes B cell excreting insulin, and then reduces blood glucose.
The specific embodiment
Below in conjunction with specific embodiment, the present invention is described in further detail, the embodiment providing is only in order to illustrate the present invention, rather than in order to limit the scope of the invention.
Experimental technique in following embodiment, if no special instructions, is conventional method.Test material used in following embodiment, if no special instructions, is and purchases available from routine biochemistry reagent shop.
embodiment 1:
Chinese medicine composition by following raw material is by weight ratio: Cordyceps is 10 grams, and Radix Ginseng is 50 grams, and Xiang Tianguo is 200 grams, and Fructus Momordicae charantiae is 60 grams, and Radix et Caulis Opuntiae Dillenii is 55 grams.
Preparation method is: aforesaid raw material is mixed by corresponding weight proportion, first with clear water, clean remove impurity, the warm water soaking 1h of 50 ℃ that the quality such as is then used, then, adds the water of 5 times of raw material weights, at 75 ℃, extract 3 times, after cold filtration, at 65 ℃ of following concentrated flowing soaking pastes that become with the quality such as raw material, obtain compound for reducing blood suger No. 1, shake up sealing, be placed in shady and cool ventilation place and preserve.
embodiment 2:
Chinese medicine composition by following raw material is by weight ratio: Cordyceps is 30 grams, and Radix Ginseng is 80 grams, and Xiang Tianguo is 150 grams, and Fructus Momordicae charantiae is 30 grams, and Radix et Caulis Opuntiae Dillenii is 25 grams.
Preparation method is: aforesaid raw material is mixed by corresponding weight proportion, first with clear water, clean remove impurity, the warm water soaking 3h of 30 ℃ that the quality such as is then used, then, adds the water of 3 times of raw material weights, at 80 ℃, extract 5 times, after cold filtration, at 65 ℃ of following concentrated flowing soaking pastes that become with the quality such as raw material, obtain compound for reducing blood suger No. 2, shake up sealing, be placed in shady and cool ventilation place and preserve.
embodiment 3:
Chinese medicine composition by following raw material is by weight ratio: Cordyceps is 10 grams, and Radix Ginseng is 50 grams, and Xiang Tianguo is 200 grams, and Fructus Momordicae charantiae is 60 grams, and Radix et Caulis Opuntiae Dillenii is 55 grams.
Preparation method is: aforesaid raw material is mixed by corresponding weight proportion, first with clear water, clean remove impurity, the warm water soaking 2.5h of 44 ℃ that the quality such as is then used, then, adds the water of 4 times of raw material weights, at 90 ℃, extract 4 times, after cold filtration, at 65 ℃ of following concentrated flowing soaking pastes that become with the quality such as raw material, shake up sealing, obtain compound for reducing blood suger No. 3, be placed in cool ventilation and preserve.
embodiment 4:
In the present embodiment, proved that by experiment compositions has good effect aspect blood sugar lowering.
materials and methods
1.1 test compounds
Title: No. 1, compound for reducing blood suger; No. 2, compound for reducing blood suger; No. 3, compound for reducing blood suger, preservation condition: 4
oc
the preparation of 1.2 testing compound solutions
1.2.1 the preparation of No. 1 solution of compound for reducing blood suger
First, No. 1 100.3mg of compound for reducing blood suger that weighs (BS 124 S, Sartorius) is dissolved in 5mL DPBS, vortex 1min, ultrasonic 10min, the centrifugal 5min of 10000rpm, obtains the mother solution that concentration is 20mg/mL.Then with DPBS, dilute mother solution, contain 2,6, No. 1 solution of compound for reducing blood suger of 20 mg/mL to ultimate density respectively.
the preparation of No. 2 solution of compound for reducing blood suger
First, No. 2 10.2mg of compound for reducing blood suger that weigh (BS 124 S, Sartorius) are dissolved in 5mL DPBS, vortex 1min, ultrasonic 10min, the centrifugal 5min of 10000rpm, obtains the mother solution that concentration is 2mg/mL.Then with DPBS, dilute mother solution, No. 2 solution of compound for reducing blood suger that contain 0.2,0.6,2mg/mL to ultimate density respectively.
the preparation of No. 3 solution of compound for reducing blood suger
First, No. 3 10.1mg of compound for reducing blood suger that weigh (BS 124 S, Sartorius) are dissolved in 5mL DPBS, vortex 1min, ultrasonic 10min, the centrifugal 5min of 10000rpm, obtains the mother solution that concentration is 2mg/mL.Then with DPBS, dilute mother solution, No. 3 solution of compound for reducing blood suger that contain 0.2,0.6,2mg/mL to ultimate density respectively.
detection system
1.3.1 material
A. people's transport of drug body SGLT2 stable gene is expressed HEK293 cell: to have inserted the mammal of people's transport of drug body SGLT2 gene, express this cell of pcDNA3.1 carrier transfection, and with geneticin screening patience cell, and then obtain the cell strain that surface of cell membrane SGLT2 stablizes high expressed.
B. culture medium
The DMEM in high glucose culture medium (Lot No. NYM1045, Hyclone) that contains 10% hyclone (Lot No. 1227693, Invitrogen ' s Gibco) is for the cell culture of this research.
C. pancreatin
0.25%?Trypsin-EDTA（1×）（Lot?No.1155732,?Invitrogen’s?Gibco）
D. radiolabeled probe's substrate
Uric?acid,?[8-
14C]-?(Lot?No.?742-107-0578-B-20121130-SBA,?Moravek)
Glucose?D,?[
14C（U）]-?(Lot?No.?120319,?ARC)
E. buffer solution
Dulbecco’s?Phosphate?Buffered?Saline,?DPBS?(Lot?No.?070M8306,?Sigma-Aldrich)
1.3.2 experimental procedure
A. HEK293 monolayer cell culture
After trypsinization, transport of drug body SGLT2 gene expression cell is inoculated in the coated 24 hole culture plates (Lot No. 20130801, CHI SCIENTIFIC) of lysine, and cell inoculum density is 10
5cells/well cultivates 2 days in 37 ℃, the incubator of 5% CO2, saturated humidity.
B. radiolabeled probe's concentration of substrate
Preparation concentration is the Uric acid of 60 μ M, [8-
14c]-, then mix with testing compound equal-volume, making its ultimate density is 30 μ M.
Preparation concentration is the Glucose D of 60 μ M, [
14c(U)], then mix with testing compound equal-volume, making its ultimate density is 30 μ M.
C. nonlabelled compound concentration
Various testing samples (2 * final concentration), and with 60 μ M radioactive label Uric acid, [8-
14c]-and the Glucose D of 60 μ M, [
14c(U)] equal-volume mixes.The ultimate density of A1 is 1,3,10 mg/mL, the ultimate density of B1 is 0.1,0.3,1mg/mL, the ultimate density of C1 is 0.1,0.3,1mg/mL, the ultimate density of FSM1 is 0.03,0.1,0.3,1,3,10mg/mL, and the ultimate density of FSM2 is 0.03,0.1,0.3,1,3,10mg/mL.
D. cellular uptake test
First remove culture fluid in culture plate, DPBS for cultured cell is cleaned to twice, and temperature is bathed 10min in 37 ° of C DPBS buffer, then with 500 μ L, containing radiolabeled probe substrate solution displacement DPBS, start to take in the cell of medicine; After 2min, by ice bath DPBS buffer cessation reaction, and clean 3 times; Then 500 μ l 0.1mol/L NaOH cell lysis are added in each hole; Extract lysate in scintillation vial, add the scintillation solution (Aquasol-2) of 3mL, and by the radioactive intensity in Tri-Carb 2910TR liquid scintillation instrument (PerkinElmer, Waltham, USA) working sample.In cellular uptake test, each concentration repeats 3 times (n=3).
interpretation of result
1.4.1 inhibitory action
The absorption activity containing nonradioactive labeling's probe substrate and the radiolabeled probe substrate of testing compound is not defined as to 100%(control), as the percent absorption under the various compound existence conditions of criterion calculation.
statistical method
Microsoft Excel 2010 computed in software for Mean ± standard error (SD).Each numerical value represents the meansigma methods of two measured values of an experiment.GraphPad Prism 5.0 softwares are used for drawing nonlinear regression curve chart, and the IC of computerized compound on the impact of transport of drug body transport activity
50.
result
Table 1: compound for reducing blood suger mediates glucose transporter (SGLT2) for No. 1, No. 2, No. 3
14the impact of C-Glucose transport activity, does not add under inhibitor condition SGLT2 couple
14the absorption ratio of C-Glucose is defined as 100%(control).The interpolation that variable concentrations compound for reducing blood suger is No. 1, No. 2, No. 3, mediates SGLT2
14c-Glucose absorption ratio obviously declines with the increase of No. 1, No. 2, No. 3 concentration of compound for reducing blood suger, and has significant significant difference.By each concentration point, calculated the IC of No. 1, compound for reducing blood suger
50for 2.14mg/mL, the IC that No. 2, compound for reducing blood suger
50for 0.27mg/mL, the IC that No. 3, compound for reducing blood suger
50for 0.97mg/mL.
conclusion
Result of the test demonstration, compound for reducing blood suger all has inhibitory action to the transport activity of SGLT2 No. 1, No. 2, No. 3, to the inhibitory action activity series of SGLT2, is wherein No. 2 (IC of compound for reducing blood suger
50=0.27mg/mL) No. 3 (IC of > compound for reducing blood suger
50=0.97mg/mL) No. 1 (IC of > compound for reducing blood suger
50=2.14mg/mL).
table 1. compound for reducing blood suger mediates glucose transporter for No. 1, No. 2, No. 3
14
the impact of C-Glucose transport activity (n=3)
Claims (6)
1. a compound for reducing blood suger, is characterized in that, by Cordyceps, and Radix Ginseng, Xiang Tianguo, Fructus Momordicae charantiae, Radix et Caulis Opuntiae Dillenii forms, and wherein, described Cordyceps is 10-30 part, and Radix Ginseng is 50-80 part, and Xiang Tianguo is 150-200 part, and Fructus Momordicae charantiae is 30-60 part, and Radix et Caulis Opuntiae Dillenii is 25-55 part.
2. a kind of compound for reducing blood suger according to claim 1, is characterized in that, described Cordyceps is 15-25 part, and Radix Ginseng is 61-69 part, and Xiang Tianguo is 170-180 part, and Fructus Momordicae charantiae is 45-55 part, and Radix et Caulis Opuntiae Dillenii is 34-48 part.
3. compound for reducing blood suger according to claim 1, is characterized in that forming with pharmaceutically acceptable carrier.
4. according to the compound for reducing blood suger described in claim 1-3 any one, it is characterized in that, described medicine is granule, pill, decoction, tablet, capsule or powder.
5. according to the preparation method of the compound for reducing blood suger described in claim 1-3 any one, this preparation method comprises the steps: raw material powder to be broken into fine powder, to sieve, to mix in proportion, and obtains.
6. pharmaceutical composition as claimed in claim 1 application in preparing hypoglycemic medicine as effective ingredient.
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|---|---|---|---|
| CN201410238109.9A CN104000877A (en) | 2014-05-30 | 2014-05-30 | Blood glucose reducing composition and application thereof |
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| CN201410238109.9A CN104000877A (en) | 2014-05-30 | 2014-05-30 | Blood glucose reducing composition and application thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105685863A (en) * | 2015-12-31 | 2016-06-22 | 苗娥 | Fructus swietenia macrophylla nutrition powder capable of lowering blood glucose and preparation method thereof |
| CN105943840A (en) * | 2016-05-10 | 2016-09-21 | 上海天慈国际药业有限公司 | Health care product for reducing blood glucose and reducing fat |
| CN108497392A (en) * | 2018-05-29 | 2018-09-07 | 闫峻峰 | A kind of food preventing hyperglycemia hypertension |
-
2014
- 2014-05-30 CN CN201410238109.9A patent/CN104000877A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| 张军: ""向天果——维持健康的神奇之果"", 《中国保健营养》 * |
| 汪东篱等: ""降血糖的天然食品"", 《现代预防医学》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105685863A (en) * | 2015-12-31 | 2016-06-22 | 苗娥 | Fructus swietenia macrophylla nutrition powder capable of lowering blood glucose and preparation method thereof |
| CN105943840A (en) * | 2016-05-10 | 2016-09-21 | 上海天慈国际药业有限公司 | Health care product for reducing blood glucose and reducing fat |
| CN108497392A (en) * | 2018-05-29 | 2018-09-07 | 闫峻峰 | A kind of food preventing hyperglycemia hypertension |
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