CN105832718B - Flavones Sophoraflavanone G are preparing the application in preventing diabetes medicament - Google Patents
Flavones Sophoraflavanone G are preparing the application in preventing diabetes medicament Download PDFInfo
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- CN105832718B CN105832718B CN201610263505.6A CN201610263505A CN105832718B CN 105832718 B CN105832718 B CN 105832718B CN 201610263505 A CN201610263505 A CN 201610263505A CN 105832718 B CN105832718 B CN 105832718B
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- sophoraflavanone
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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
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Abstract
The invention discloses flavones Sophoraflavanone G to prepare the application in preventing diabetes medicament.Experimental researches prove that, flavones Sophoraflavanone G have the function for the treatment of diabetes well, extraordinary therapeutic effect is all had to the diseases such as diabetes and its diabetes hepatopathy, and in experimentation, toxic side effect is not shown, it is expected to be developed into safely and effectively, the drug for preventing diabetes and its complication.
Description
Technical field
The present invention relates to a kind of flavones Sophoraflavanone G new applications, and in particular to flavones
Sophoraflavanone G are preparing the application in preventing diabetes medicament.
Background technology
Diabetes are one of worldwide most common epidemic diseases, and the death rate is only second to blood vessel in developed country
Disease, malignant tumour become the lethal cause of disease disease of third position.It is a kind of related with inherent cause, at the same again with a variety of rings
Factor relevant chronic systemic disease in border is body carbohydrate, fat metabolism because of caused by insulin secretion or underutilization
Disorderly syndrome, and diabetes hepatopathy has become in chronic complicating diseases of diabetes except kidney, heart, retina, neuropathy
The outer chronic complicating diseases that another is increasingly attracted people's attention.Quantity is in fairly obvious rising to China diabetic in recent years
Trend, and wherein main Types are diabetes B patients, it has also become one of the problem of chief threat our people's life and health.
In spite of a large amount of hypoglycemic drug in clinical application, but since its side effect is big, inconvenient for use, curative effect is unstable
It is fixed, do not find a kind of effective medicine yet at present.Natural antidiabetic medicine is small and be not likely to produce resistance to its toxic side effect
Pharmacological property is generally paid close attention to by medical field.Contain a plurality of types of flavonoids such as flavones, flavonols, chalcone in Sophora alopecuroide
Object.In recent years, the calmness, analgesia of Sophora alopecuroide, anticonvulsion, cooling, anti-arrhythmia, anti-inflammatory, antitumor, myocardial preservation, drop blood
The research of the pharmacological actions such as fat is gradually understood by people, and less for the report of metabolism class disease.
Sophora alopecuroide monomer flavones Sophoraflavanone G can be detached from Sophora alopecuroide cauline leaf or the extraction of Sophora alopecuroide root
It arrives, it is existing to report that it, with antibacterial activity, there are no the report of prevention treatment diabetes medicament.
Invention content
Goal of the invention：The purpose of the present invention is on the basis of flavones Sophoraflavanone G original effects, develop
Its new clinical application provides flavones Sophoraflavanone G and is preparing the application in preventing diabetes medicament.Experiment knot
Fruit shows that it has the function of that preventing diabetes and its diabetes well merges hepatopathy, and has no adverse reaction.
Technical solution：In order to achieve the goal above, the technical solution that the present invention takes is：
Its molecular formula of flavones Sophoraflavanone G is C25H28O6, entitled 5,7,2', 4'- tetrahydroxys -8- smokes clothing
Careless base flavanone.Structural formula is as follows：
The present invention shows that flavones Sophoraflavanone G have treatment diabetes well by lot of experiments
Effect, can be used for prepare treatment diabetes medicament in application.
Preferably, flavones Sophoraflavanone G answering in preparing prevention diabetes and merging liver drug
With.
Flavones Sophoraflavanone G of the present invention are preparing prevention diabetes medicament or diabetes merging liver
Application in medicine, by flavones Sophoraflavanone G and pharmaceutically acceptable carrier be made capsule, granule,
The drug of spray, injection, micro-capsule, tablet, pastille, suppository, ointment or skin-permeable and control-released plaster dosage form.
Flavones Sophoraflavanone when capsule is made in flavones Sophoraflavanone G provided by the invention
G and carrier lactose or cornstarch are uniformly mixed, and whole grain is then encapsulated that capsule is made.
When tablet is made in flavones Sophoraflavanone G provided by the invention, flavones Sophoraflavanone
G and lactose or cornstarch, are added magnesium stearate lubricant when needing, be uniformly mixed, tablet is made in then tabletting.
When granule is made in flavones Sophoraflavanone G provided by the invention, flavones Sophoraflavanone
G and diluent lactose or cornstarch are uniformly mixed, and whole grain is dry, and granule is made.
When injection is made in flavones Sophoraflavanone G provided by the invention, flavones Sophoraflavanone is taken
G is added physiological saline solution and activated carbon then is added, and stirs evenly, and 80 DEG C are heated 30 minutes, and filtering adjusts pH value, uses incipient fusion
Glass funnel or other filters are filtered to clear and bright, filling, sterilize 30 minutes at 100 to 115 DEG C and injection is made.
After flavones Sophoraflavanone G depyrogenations provided by the invention, through being sterile filtered, freeze-drying obtains
Powder ampoule agent for injection.
Advantageous effect：The present invention carries out new purposes on the basis of flavones Sophoraflavanone G original effects and opens
Hair, experimental study shows that flavones Sophoraflavanone G have the function for the treatment of diabetes well, to diabetes and its
Diabetes merging hepatopathy etc. is diseases related to all have extraordinary therapeutic effect, and in experimentation, does not show side effect
Equal adverse reactions are expected to be developed into of new generation safe and effective, the drug for preventing diabetes.
Description of the drawings
Fig. 1 is each experimental group liver tissues of rats pathological section figure.
Specific implementation mode
According to following embodiments, the present invention may be better understood.However, as it will be easily appreciated by one skilled in the art that real
It applies specific material proportion, process conditions and its result described in example and is merely to illustrate the present invention, without that should will not limit
The present invention described in detail in claims processed.
Embodiment 1
Sophora alopecuroide monomer flavones Sophoraflavanone G compounds control diabetes B and diabetes B hepatopathy
Treatment acts on
1, animal：It is sheerly cleaning grade Wistar rats 40,180-220g.
2, it is grouped：After all rats raise 1w in advance, it is randomly divided into two groups：Normal group (K groups) 8 is only given normal diet；Its
Remaining and 32 be only given high-carbonhydrate diet tailing high in fat intravenous injection streptozotocin (STZ) and carry out modeling, and carries out fasting blood after 8 weeks
Sugared (FBG) is measured, and FBG >=16.8mmol/L person is modeling success.Successful 24 rats of modeling are randomly divided into four groups：Model
Group (M groups), melbine group (Y groups, 150mg/kg are compareed as positive drug), Sophoraflavanone G low concentration monomers
Group (D2 groups, 20mg/kg), Sophoraflavanone G high concentration monomers groups (G2 groups, 40mg/kg), continues to give high in fat
High-carbonhydrate diet；Normal group still gives normal diet.
3, dosage regimen：Melbine group gives melbine aqueous solution 150mg/kg gavages from the 10th week；Treatment group
20mg/kg Sophoraflavanone G, 40mg/kg Sophoraflavanone G gavages are given respectively daily；Normal group
Isometric distilled water gavage, pharmaceutical intervention totally 1 week are then given with model group.
4, experiment reagent：Sophoraflavanone G, metformin hydrochloride tablet, streptozotocin, ALT, AST measure examination
Agent box, insulin radioimmunoassay immunoassay kits.
Testing index：1. the variation of blood glucose, insulin and liver function；2. big using the detection of Hematoxylin-eosin (HE) decoration method
Rat liver pathological change situation.
5, statistical analysis：It is analyzed using SPSS13.0 statistical softwares, withIt indicates；Comparison among groups use Dan Yin
Plain variance analysis is compared between group and is examined using q two-by-two；Relationship correlation analysis between index.
6, experimental result
The variation of 6.1 blood glucose, insulin and liver function
Compared with normal group, fasting blood sugar obviously increases model group, and numerical value reduces after positive drug is treated, through low dose
Monomer flavones Sophoraflavanone G, high dose monomer flavones Sophoraflavanone G drug treatments are measured, after 5 days
FBG values are just substantially reduced compared with model group, and statistically significant；After monomer flavones Sophoraflavanone G treatments, pancreas islet
Cellulose content is substantially reduced compared with model group, and has statistical significance；ALT, AST content are more also decreased compared with model group, and
With statistical significance.Illustrate that monomer flavones Sophoraflavanone G can quickly reduce the blood glucose value of diabetes rat,
Weaken insulin resistance, improves significantly to the hepatic pathology damage of diabetes rat.Detailed results are shown in Table 1.
1 each group rat blood sugar of table, insulin and liver function variation (x ± s, n=6)
Measurement data is indicated with X ± S.Compared with model group, statistical significant difference is：* P ＜ 0.001, * P ＜
0.05。
The pathological change of 6.2 each group liver tissues of rats
Compared with model group, monomer flavones group Sophoraflavanone G liver cell intracytoplasmic lipids, which drip quantity, to be reduced, fat
Fat denaturation, lobuli hepatis obscure boundary, liver rope be disorganized, sinus hepaticus and central vein expansion phenomenon obtain it is substantially reduced.In detail
The result is shown in Figure 1
The experimental results showed that, flavones group Sophoraflavanone G provided by the invention not only have apparent drop by above
Blood glucose acts on, and can effectively correct the carbohydrate metabolism disturbance of diabetes, improve the effect of sugar tolerance, and can significantly mitigate glycosuria
Sick hepatopathy rat fat denaturation, lobuli hepatis obscure boundary, liver rope be disorganized, sinus hepaticus and central vein are expanded phenomenon, and had no
There are adverse reaction, safety good.
The above is only a preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art
For member, various improvements and modifications may be made without departing from the principle of the present invention, these improvements and modifications are also answered
It is considered as protection scope of the present invention.
Claims (2)
1. applications of the flavones Sophoraflavanone G in preparing prevention diabetes and merging liver disease drug.
2. flavones Sophoraflavanone G according to claim 1 are in preparing prevention diabetes and merging liver disease drug
Application, which is characterized in that capsule, particle is made in flavones Sophoraflavanone G and pharmaceutically acceptable carrier
Agent, spray, injection, micro-capsule, pastille, suppository, tablet, ointment or skin-permeable and control-released plaster dosage form drug.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201610263505.6A CN105832718B (en) | 2016-04-26 | 2016-04-26 | Flavones Sophoraflavanone G are preparing the application in preventing diabetes medicament |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610263505.6A CN105832718B (en) | 2016-04-26 | 2016-04-26 | Flavones Sophoraflavanone G are preparing the application in preventing diabetes medicament |
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| Publication Number | Publication Date |
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| CN105832718A CN105832718A (en) | 2016-08-10 |
| CN105832718B true CN105832718B (en) | 2018-08-21 |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1676520A (en) * | 2004-04-01 | 2005-10-05 | 和记黄埔医药企业有限公司 | Kuh-seng flavone extract and preparation and use thereof |
| KR20090084439A (en) * | 2008-02-01 | 2009-08-05 | 부경대학교 산학협력단 | A composition comprising extract of sophora flavescens or prenylated flavonoids compounds isolated therefrom preventing or treating diabetic complication |
| CN103860638A (en) * | 2014-03-28 | 2014-06-18 | 吉林省中医药科学院 | Preparation method of sophora alopecuroide flavonoid composition and new medical application |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050226943A1 (en) * | 2004-04-01 | 2005-10-13 | Xiaoqiang Yan | Extract of sophora flavescens flavonoids and uses thereof |
| JP2008222622A (en) * | 2007-03-11 | 2008-09-25 | Nippon Suisan Kaisha Ltd | Na+/GLUCOSE TRANSPORTER INHIBITOR |
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2016
- 2016-04-26 CN CN201610263505.6A patent/CN105832718B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1676520A (en) * | 2004-04-01 | 2005-10-05 | 和记黄埔医药企业有限公司 | Kuh-seng flavone extract and preparation and use thereof |
| KR20090084439A (en) * | 2008-02-01 | 2009-08-05 | 부경대학교 산학협력단 | A composition comprising extract of sophora flavescens or prenylated flavonoids compounds isolated therefrom preventing or treating diabetic complication |
| CN103860638A (en) * | 2014-03-28 | 2014-06-18 | 吉林省中医药科学院 | Preparation method of sophora alopecuroide flavonoid composition and new medical application |
Non-Patent Citations (5)
| Title |
|---|
| Antidiabetic effects of flavonoids from Sophora flavescens EtOAc extract in type2 diabetic KK-aymice;Xinzhou Yang et al.;《Journal of Ethnopharmacology》;20150605;第171卷;161-170 * |
| Glycosidase Inhibitory Flavonoids from Sophora flavescens;Jin Hyo KIM et al.;《Biol. Pharm. Bull.》;20061231;第29卷(第2期);302-305 * |
| Inhibitory activities of prenylated flavonoids from Sophora flavescens against aldose reductase and generation of advanced glycation endproducts;Hyun Ah Jung et al.;《Journal of Pharmacy and Pharmacology》;20081231;第60卷;1227-1236 * |
| Isolation, Chemical Analysis, And Study of The Hepatoprotector and Biligenic Activity of Total Flavonoid Preparations From Thermopsis dolichocarpa And Vexibia alopecuroides;V.N.Syrov et al.;《Pharmaceutical Chemistry Journal》;20010131;第35卷(第1期);30-34 * |
| Protective effect of Sophoraflavanone G on streptozotocin (STZ)-induced inflammation in diabetic rats;Hanqing Wang et al.;《Biomedicine & Pharmacotherapy》;20161231;第84卷;1617-1622 * |
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Granted publication date: 20180821 Termination date: 20190426 |