CN107865885A - Isovitexin is preparing the application in reducing hypoglycemic medicament - Google Patents
Isovitexin is preparing the application in reducing hypoglycemic medicament Download PDFInfo
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- CN107865885A CN107865885A CN201610850049.5A CN201610850049A CN107865885A CN 107865885 A CN107865885 A CN 107865885A CN 201610850049 A CN201610850049 A CN 201610850049A CN 107865885 A CN107865885 A CN 107865885A
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- isovitexin
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- compound
- antidiabetic medicine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention discloses a kind of applications of Isovitexin in antidiabetic medicine is prepared.The present invention provides a kind of brand-new selection and thinking for current antidiabetic medicine, has widened the selection field of antidiabetic medicine, has also been contributed for the development of the technical field；The Isovitexin of present invention application is proved to have significant anti-diabetic effect；What the present invention selected is the compound with clear and definite chemical constitution.Purposes of the Isovitexin of the present invention in treatment antidiabetic medicine is prepared belongs to first public, because framework types belong to brand-new framework types, and it is prevented and treated diabetic activity and is unexpectedly strong, in the absence of the possibility that any enlightenment is provided by other compounds, possess prominent substantive distinguishing features, while obviously there is significant progress for treating anti-diabetic.
Description
Technical field
The present invention relates to compound Isovitexin new application, more particularly to a kind of Isovitexin to prepare reduction blood
Application in sugared medicine.
Background technology
Diabetes (diabetes mellitus) are one of current most common chronic disease, wherein diabetes B
(the diabetes mellitus of Type II, are called Non-Insulin Dependent Diabetes Mellitus, non-insulin-
Depentdiabetes mellitus, NIDDM) account for more than the 90% of diabetic.Diabetes are in developed country and development
The problem of middle country is a getting worse, it causes serious and costly consequence, including blindness, heart disease and kidney
Disease etc..It is estimated that from 2000 to the year two thousand fifty, the number of whole world diabetic will increase by 165%.According to international diabetes
The statistics of alliance, the population that current China has 4.3% suffer from diabetes, and the number of patient will break through 5000 within 20 years futures
Ten thousand.Diabetes are the second killers in modern diseases, and its harm to human body is only second to cancer, and serious threat the strong of the mankind
Health, and present diabetes have the tendency of extension and rejuvenation, how to prevent diabetes from turning into current the world of medicine's emphasis
One big problem of concern.
Compound Isovitexin of the present invention be one deliver within 2013 (Ebenezer de Mello Cruz,
et al.,Leishmanicidal activity of Cecropia pachystachya flavonoids:Arginase
inhibition and altered mitochondrial DNA arrangement.Phytochemistry,89(2013)
71-77.) noval chemical compound, the compound possess brand-new framework types, current purposes only immunological regulation (Ebenezer
De Mello Cruz, et al., Leishmanicidal activity of Cecropia pachystachya
flavonoids:Arginase inhibition and altered mitochondrial DNA
Arrangement.Phytochemistry, 89 (2013) 71-77.), made for a kind of Isovitexin of the present invention
The purposes made preparation for dropping in hypoglycemic medicament belongs to first public.
The content of the invention
The present invention proposes that a kind of Isovitexin is preparing the application in reducing hypoglycemic medicament.Find out from pharmacological evaluation, this
Kind Isovitexin plays the role of preferably to reduce blood glucose.Because a kind of first public Isovitexin of the present invention is reducing blood glucose
The pharmacologic action of aspect.
Shown in the compound Isovitexin structures such as formula (I)：
The technical scheme is that：This Isovitexin application, specifically it is applied to prepare antidiabetic medicine.
Applications of the Isovitexin in hypoglycemic medicament is reduced, Isovitexin have drop to experimental type 2 diabetes mellitus
Blood glucose acts on.
One kind reduces hypoglycemic medicament, is that active component addition auxiliary material is prepared by Isovitexin, preparation method is to take 5
G of compound Isovitexin, 195 grams of dextrin is added, mixed, Conventional compression is made 1000.
One kind reduces hypoglycemic medicament, is that active component addition auxiliary material is prepared by Isovitexin, preparation method is to take 5
G of compound Isovitexin, 195 grams of starch is added, mixed, it is encapsulated to be made 1000.
The beneficial effects of the invention are as follows：
1) present invention provides a kind of brand-new selection and thinking for current antidiabetic medicine, has widened anti-diabetic
Selection field, also contributed for the development of the technical field；2) Isovitexin of the invention application is proved to have aobvious
The anti-diabetic effect of work.
Above all：The present invention carries out the hypoglycemic experiment of experimental animal to Isovitexin, in lasting gavage fat
On the basis of breast makes rat generation insulin resistance, using low dose of Streptozotocin impaired isle β cells, rat blood sugar is caused
Rise, it is similar with diabetes B to make animal model.After rat model of type 2 diabetes mellitus gives Isovitexin treatments,
Isovitexin is high, neutralizes the blood glucose value of low dose group compared with model group blood glucose value, it may have significant difference (P<0.01),
Isovitexin is high, neutralizes the front and rear blood glucose value of low dose group administration compares, it may have significant difference (P<0.01), explanation
Isovitexin has good hypoglycemic effect to experimental type 2 diabetes mellitus.
Purposes of the Isovitexin of the present invention in treatment antidiabetic medicine is prepared belongs to first public, due to
Framework types belong to brand-new framework types, and it is prevented and treated diabetic activity and is unexpectedly strong, in the absence of by other chemical combination
Thing provides the possibility of any enlightenment, possesses prominent substantive distinguishing features, while obviously have significantly for treating anti-diabetic
It is progressive.
Embodiment
Compound Isovitexin involved in the present invention preparation method is referring to document (Ebenezer de Mello
Cruz, et al., Leishmanicidal activity of Cecropia pachystachya flavonoids:
Arginase inhibition and altered mitochondrial DNA arrangement.Phytochemistry,
89(2013)71–77.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific reality
Any restrictions of example are applied, but are defined in the claims.
Embodiment 1：The preparation of compound Isovitexin tablets involved in the present invention：
5 g of compound Isovitexin are taken, add 195 grams of dextrin, are mixed, conventional tablet presses are made 1000.
Embodiment 2：The preparation of compound Isovitexin capsules involved in the present invention：
5 g of compound Isovitexin are taken, add 195 grams of starch, are mixed, it is encapsulated to be made 1000.
Its pharmaceutical activity is further illustrated below by pharmacodynamic experiment.
Experimental example 1：Influences of the Isovitexin to rat model of type 2 diabetes mellitus
1st, animal packet
Healthy Wistar rats (SPF levels), male, body weight 180-220g (are carried by Nanjing Medical University's Experimental Animal Center
For), free water feed is randomly divided into Normal group and modeling group, and modeling group establishes model, modeling success as follows
Model group animal is randomly divided into model control group, positive drug gliclazide group, high, normal, basic group of Isovitexin again afterwards, pressed
Table successive administration 1 week.
Administration time and dosage are shown in Table 1：
The Isovitexin effect experiment animal packets of table 1
| Group | Number of animals (only) | Dosage (mg/kgBW) |
| Normal group | 12 | |
| Model control group | 12 | |
| Positive drug group | 12 | 35.5 |
| Low dose group | 12 | 0.2 |
| Middle dose group | 12 | 0.4 |
| High dose group | 12 | 0.8 |
2nd, prepared by rat model
The daily gavage distilled water of normal rats, the high daily morning and evening gavage self-control Fat Emulsion (1ml/ of fat group rat
100gBW).After continuous gavage Fat Emulsion 2 weeks, water 24h, 10 tail vein injection physiology salts of blank control group are can't help in animal fasting
Water, equal tail vein injection 30mg/kgBW Streptozotocins (hereinafter abbreviated as STZ) solution (prepared before use) of remaining rat.Give
After medicine 48h, water 12h is can't help in fasting, and blood is taken every 3 hours eyeball rear vein beards, empty according to the time-and-motion study of blood sugar detection kit
Abdomen blood glucose value, METHOD FOR CONTINUOUS DETERMINATION 3 times, fasting blood sugar >=16.7mmol/L for modeling success rat.
3rd, the measure of blood glucose
After last dose, water 12h is can't help in animal fasting, and eyeball rear vein beard takes blood, is surveyed respectively according to the method for kit
Determine blood glucose value.Using SPSS13.0 statistical softwares, analyze and compare the situation of change of each group blood glucose value.
4th, influences of the Isovitexin to rat model of type 2 diabetes mellitus blood glucose
Experimental result is shown in Table 2, and as known from Table 2, after injecting STZ, rat blood sugar rises, and fasting blood sugar after 72h >=
16.7mmol/L, illustrate diabetes model success.After administration, positive drug group, Isovitexin is high, neutralizes the blood of low dose group
Sugared value has significant difference (P compared with model group blood glucose value<0.01).
The T of blood glucose and blood glucose after administration examines display before each group administration, and positive drug group, Isovitexin is high, neutralization is low
The front and rear blood glucose value of dosage group administration compares, and has significant difference (P<0.01).Result above shows that Isovitexin can
Reduce the blood glucose of rat model of type 2 diabetes mellitus.
The experimental result of table 2
| Group | Number of animals (only) | Blood glucose value before administration | Blood glucose value after administration |
| Normal group | 10 | 5.76±0.38 | 5.83±1.45 |
| Model control group | 9 | 16.68±2.23 | 36.54±2.39 |
| Positive drug group | 9 | 34.32±2.18 | 18.21±2.43**△△ |
| Low dose group | 8 | 32.79±2.57 | 23.16±3.26**△△ |
| Middle dose group | 10 | 35.35±1.75 | 18.42±2.17**△△ |
| High dose group | 9 | 38.86±2.14 | 17.48±3.21**△△ |
*p<0.05vs model group * * p<0.01vs model groups△p<Before 0.05vs is with group administration△△p<0.01vs is same to organize administration
Before
Conclusion：Isovitexin of the present invention can significantly reduce the blood glucose of diabetes B animal model, can be used for preparing
Antidiabetic medicine.
Claims (4)
- Applications of the 1.Isovitexin in hypoglycemic medicament is reduced, shown in the compound Isovitexin structures such as formula (I)：
- 2. applications of the Isovitexin as claimed in claim 1 in hypoglycemic medicament is reduced, it is characterised in that Isovitexin pairs Experimental type 2 diabetes mellitus has hypoglycemic effect.
- 3. one kind reduces hypoglycemic medicament, it is characterised in that the Isovitexin as described in claim 1 is that active component adds auxiliary material It is prepared, preparation method adds 195 grams of dextrin, mixed, Conventional compression is made 1000 to take 5 g of compound Isovitexin Piece.
- 4. one kind reduces hypoglycemic medicament, it is characterised in that the Isovitexin as described in claim 1 is that active component adds auxiliary material It is prepared, preparation method adds 195 grams of starch, mixing is encapsulated to be made 1000 to take 5 g of compound Isovitexin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610850049.5A CN107865885A (en) | 2016-09-25 | 2016-09-25 | Isovitexin is preparing the application in reducing hypoglycemic medicament |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610850049.5A CN107865885A (en) | 2016-09-25 | 2016-09-25 | Isovitexin is preparing the application in reducing hypoglycemic medicament |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107865885A true CN107865885A (en) | 2018-04-03 |
Family
ID=61751757
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610850049.5A Pending CN107865885A (en) | 2016-09-25 | 2016-09-25 | Isovitexin is preparing the application in reducing hypoglycemic medicament |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107865885A (en) |
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2016
- 2016-09-25 CN CN201610850049.5A patent/CN107865885A/en active Pending
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|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180403 |
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| WD01 | Invention patent application deemed withdrawn after publication |