CN107865859A - Orientin is preparing the application in reducing hypoglycemic medicament - Google Patents
Orientin is preparing the application in reducing hypoglycemic medicament Download PDFInfo
- Publication number
- CN107865859A CN107865859A CN201610849143.9A CN201610849143A CN107865859A CN 107865859 A CN107865859 A CN 107865859A CN 201610849143 A CN201610849143 A CN 201610849143A CN 107865859 A CN107865859 A CN 107865859A
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- CN
- China
- Prior art keywords
- orientin
- group
- compound
- blood glucose
- hypoglycemic medicament
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Classifications
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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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- 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)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention discloses a kind of applications of Orientin in antidiabetic medicine is prepared, Orientin of the invention application is proved to have significant anti-diabetic effect；Compound with clear and definite chemical constitution, belong to brand-new framework types, and its preventing and treating diabetic activity is strong, possesses prominent substantive distinguishing features, while obviously have significant progress for treating anti-diabetic.
Description
Technical field
The present invention relates to compound Orientin new application, more particularly to Orientin is in reduction hypoglycemic medicament is prepared
Application.
Background technology
Diabetes (diabetes mellitus) are asking for getting worse in developed country and developing country
Topic, it causes serious and costly consequence, including blindness, heart disease and nephrosis etc..It is estimated that from 2000 to 2050
Year, the number of whole world diabetic will increase by 165%.According to the statistics of IDF, current China has 4.3%
Population suffer from diabetes, the number of patient will break through 50,000,000 in following 20 years.Diabetes are second in modern diseases
Killer, its harm to human body are only second to cancer, and serious threat the health of the mankind.
Compound Orientin of the present invention is one and delivers 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, and current purposes merely relates to overcome S. aureus L-forms resistance
Property (Ebenezer de Mello Cruz, et al., Leishmanicidal activity of Cecropia
pachystachya flavonoids:Arginase inhibition and altered mitochondrial DNA
Arrangement.Phytochemistry, 89 (2013) 71-77.), Orientin of the present invention is preparing reduction blood glucose
Purposes in medicine belongs to first public.
The content of the invention
The present invention proposes that Orientin is preparing the application in reducing hypoglycemic medicament.Find out from pharmacological evaluation, Orientin
Play the role of preferably to reduce blood glucose.Due to pharmacologic actions of the first public Orientin of the present invention in terms of blood glucose is reduced.
Shown in the compound Orientin structures such as formula (I)：
The technical scheme is that：Orientin application, specifically it is applied to prepare antidiabetic medicine.
Applications of the Orientin in hypoglycemic medicament is reduced, Orientin has hypoglycemic to experimental type 2 diabetes mellitus
Effect.
One kind reduces hypoglycemic medicament, is prepared by described Orientin addition auxiliary materials, preparation method is to take 5 grams of chemical combination
Thing Orientin, 195 grams of dextrin is added, mixed, Conventional compression is made 1000.
One kind reduces hypoglycemic medicament, is prepared by described Orientin addition auxiliary materials, preparation method is to take 5 grams of chemical combination
Thing Orientin, 195 grams of starch is added, mixed, it is encapsulated to be made 1000.
The beneficial effects of the invention are as follows：The present invention carries out the hypoglycemic experiment of experimental animal, explanation to Orientin
Orientin has good hypoglycemic effect to experimental type 2 diabetes mellitus.Orientin of the present invention is anti-in preparation treatment
Purposes in diabetes medicament belongs to first public, and because framework types belong to brand-new framework types, and it prevents and treats glycosuria
Sick activity is unexpectedly strong, and in the absence of the possibility that any enlightenment is provided by other compounds, possesses prominent substantive distinguishing features,
Simultaneously for treating anti-diabetic obviously with significant progressive.
Embodiment
Compound Orientin involved in the present invention preparation method 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 Orientin tablets involved in the present invention：
5 g of compound Orientin are taken, add 195 grams of dextrin, are mixed, Conventional compression is made 1000.
Embodiment 2：The preparation of compound Orientin capsules involved in the present invention：
5 g of compound Orientin 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 Orientin 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 Orientin, according to the form below again afterwards
Successive administration 1 week.
Administration time and dosage are shown in Table 1：
Table 1Orientin effect experiment animal packets
| 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 | 0.25 |
| Middle dose group | 12 | 0.5 |
| High dose group | 12 | 1 |
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 Orientin 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, Orientin is high, neutralizes the blood glucose of low dose group
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, Orientin is high, low dose of neutralization
The front and rear blood glucose value of amount group administration compares, and has significant difference (P<0.01).Result above shows that Orientin can be reduced
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 | 6.70±0.31 | 6.69±1.43 |
| Model control group | 10 | 14.32±3.54 | 34.86±2.26 |
| Positive drug group | 10 | 31.21±2.75 | 17.46±3.89**△△ |
| Low dose group | 10 | 32.46±3.32 | 22.43±4.17**△△ |
| Middle dose group | 10 | 33.89±2.36 | 15.12±2.36**△△ |
| High dose group | 10 | 38.13±3.68 | 17.28±3.16**△△ |
*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：Orientin can significantly reduce the blood glucose of diabetes B animal model, can be used for preparing anti-diabetic
Medicine.
Claims (4)
- Applications of the 1.Orientin in hypoglycemic medicament is reduced, shown in the compound Orientin structures such as formula (I)：
- 2. applications of the Orientin as claimed in claim 1 in hypoglycemic medicament is reduced, it is characterised in that Orientin is to experiment Property diabetes B has hypoglycemic effect.
- 3. one kind reduces hypoglycemic medicament, it is characterised in that is prepared, made by the Orientin addition auxiliary materials described in claim 1 Preparation Method adds 195 grams of dextrin, mixed, Conventional compression is made 1000 to take 5 g of compound Orientin.
- 4. one kind reduces hypoglycemic medicament, it is characterised in that is prepared, made by the Orientin addition auxiliary materials described in claim 1 Preparation Method adds 195 grams of starch, mixing is encapsulated to be made 1000 to take 5 g of compound Orientin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610849143.9A CN107865859A (en) | 2016-09-25 | 2016-09-25 | Orientin is preparing the application in reducing hypoglycemic medicament |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610849143.9A CN107865859A (en) | 2016-09-25 | 2016-09-25 | Orientin is preparing the application in reducing hypoglycemic medicament |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107865859A true CN107865859A (en) | 2018-04-03 |
Family
ID=61750626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610849143.9A Pending CN107865859A (en) | 2016-09-25 | 2016-09-25 | Orientin is preparing the application in reducing hypoglycemic medicament |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107865859A (en) |
-
2016
- 2016-09-25 CN CN201610849143.9A patent/CN107865859A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180403 |