CN105832718A - Application of sophoraflavanone G in preparation of medicine for preventing and treating diabetic mellitus - Google Patents
Application of sophoraflavanone G in preparation of medicine for preventing and treating diabetic mellitus Download PDFInfo
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- CN105832718A CN105832718A CN201610263505.6A CN201610263505A CN105832718A CN 105832718 A CN105832718 A CN 105832718A CN 201610263505 A CN201610263505 A CN 201610263505A CN 105832718 A CN105832718 A CN 105832718A
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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 application of sophoraflavanone G in preparation of a medicine for preventing and treating diabetic mellitus. Experimental researches indicate that the sophoraflavanone G has a good effect of treating diabetic mellitus, and has a very good treatment effect on diabetic mellitus, diabetic hepatopathy and other diseases. In the experiment process, no toxic or side effect is shown, so that the sophoraflavanone G is expected to be developed into a safe and effective medicine for preventing and treating diabetic mellitus and complications thereof.
Description
Technical field
The present invention relates to a kind of flavones Sophoraflavanone G new application, be specifically related to flavones Sophoraflavanone G in system
Application in standby preventing and treating diabetes medicament.
Background technology
Diabetes are one of worldwide modal epidemic diseases, and its death rate is only second to vascular diseases, pernicious in developed country
Tumour, becomes the lethal cause of disease disease of the 3rd.It is a kind of relevant with inherent cause, the most relevant to multiple environmental factor again
Chronic systemic disease, be because of insulin secretion or under-utilized and cause body carbohydrate, the syndrome of fat metabolic disturbance,
And diabetes hepatopathy has become in chronic complicating diseases of diabetes, and in addition to kidney, heart, retina, DPN, another draws day by day
Play the chronic complicating diseases that people pay attention to.China diabetic quantity in recent years is fairly obvious ascendant trend, and main
Type is diabetes B patient, it has also become one of problem of chief threat our people's life and health.
Despite substantial amounts of hypoglycemic drug in clinical practice, but owing to its side effect is big, use inconvenience, curative effect unstable,
Do not find a kind of effective medicine the most yet.Natural antidiabetic medicine is so that its toxic and side effect is little and to be not likely to produce drug resistance general
All over being paid close attention to by medical circle.Containing polytype flavone compounds such as flavones, flavonols, chalcone in Sophora alopecuroide.Closely
Nian Lai, the calmness of Sophora alopecuroide, analgesia, anticonvulsion, cooling, anti-arrhythmia, anti-inflammatory, antitumor, myocardial preservation, fall blood
The research of the pharmacological actions such as fat is gradually understood by people, and the report for metabolism class disease is less.
Sophora alopecuroide monomer flavones Sophoraflavanone G, can extract isolated from Sophora alopecuroide cauline leaf or Sophora alopecuroide root, existing
Report that it has antibacterial activity, there are no the report of preventing and treating treatment diabetes medicament.
Summary of the invention
Goal of the invention: it is an object of the invention to, on the basis of flavones original effect of Sophoraflavanone G, develop it new
Clinical application, it is provided that flavones Sophoraflavanone G application in preparation preventing and treating diabetes medicament.Test result indicate that,
It has well prevents and treats diabetes and the effect of diabetes merging hepatopathy thereof, and has no adverse reaction.
Technical scheme: in order to realize object above, the technical scheme that the present invention takes is:
Flavones its molecular formula of Sophoraflavanone G is C25H28O6, entitled 5,7,2', 4'-tetrahydroxy-8-lavender base two
Hydrogen flavones.Structural formula is as follows:
The present invention is shown by lot of experiments, and flavones Sophoraflavanone G has the effect well treating diabetes,
Can be used for the application in preparation treatment diabetes medicament.
Preferably, flavones Sophoraflavanone G application in preparation prevents and treats diabetes merging liver medicine.
Flavones Sophoraflavanone G of the present invention merges in liver disease drug at preparation preventing and treating diabetes medicament or diabetes
Application, makes capsule, granule, spray, note by flavones Sophoraflavanone G and pharmaceutically acceptable carrier
Penetrate agent, micro-capsule, tablet, lozenge, suppository, ointment or the medicine of skin-permeable and control-released plaster formulation.
Flavones Sophoraflavanone G and carrier breast when the flavones Sophoraflavanone G that the present invention provides makes capsule
Sugar or cornstarch mix, and whole grain the most encapsulated makes capsule.
When the flavones Sophoraflavanone G that the present invention provides is made tablet, flavones Sophoraflavanone G and lactose
Or cornstarch, add magnesium stearate lubricant when needing, mix, then tablet made by compressing tablet.
When the flavones Sophoraflavanone G that the present invention provides makes granule, flavones Sophoraflavanone G and dilution
Agent lactose or cornstarch mix, whole grain, are dried, make granule.
When the flavones Sophoraflavanone G that the present invention provides makes parenteral solution, take flavones Sophoraflavanone G and add raw
Reason salt solution dissolves and is subsequently adding activated carbon, stirs, and 80 DEG C are heated 30 minutes, filter, and regulate pH value, use incipient fusion glass
Funnel or other filter filter to clear and bright, filling, within 30 minutes, make parenteral solution 100 to 115 DEG C of sterilizings.
After the flavones Sophoraflavanone G depyrogenation that the present invention provides, through aseptic filtration, freeze-drying, injected
Use powder-injection.
Beneficial effect: the present invention carries out new purposes exploitation on the basis of flavones original effect of Sophoraflavanone G, real
Test research and show that flavones Sophoraflavanone G has the effect well treating diabetes, diabetes and diabetes thereof are closed
And hepatopathy etc. is diseases related is respectively provided with in extraordinary result for the treatment of, and experimentation, do not show the bad reactions such as side effect,
It is expected to be developed into a new generation safely and effectively, for preventing and treating the medicine of diabetes.
Accompanying drawing explanation
Fig. 1 is each experimental group liver tissues of rats pathological section figure.
Detailed description of the invention
According to following embodiment, the present invention be may be better understood.But, as it will be easily appreciated by one skilled in the art that embodiment
Described concrete material proportion, process conditions and result thereof are merely to illustrate the present invention, and should be also without limitation on right
The present invention described in detail in claim.
Embodiment 1
Sophora alopecuroide monomer flavones Sophoraflavanone G compound is to diabetes B and the therapeutic action of diabetes B hepatopathy
1, animal: pure lines cleaning grade Wistar rat 40,180-220g.
2, packet: after all rats raise 1w in advance, be randomly divided into two groups: normal group (K group) 8 is only given normal diet；
Remaining 32 is only given high fat high-carbonhydrate diet and adds tail vein injection Streptozotocin (STZ) and carry out modeling, and in 8 weeks laggard line spaces
Abdomen blood sugar (FBG) measures, and FBG >=16.8mmol/L person is modeling success.Successful for modeling 24 rats are randomly divided into four
Group: model group (M group), melbine group (Y group, 150mg/kg compare as positive drug), Sophoraflavanone G
Low concentration monomer group (D2 group, 20mg/kg), Sophoraflavanone G high concentration monomer group (G2 group, 40mg/kg), all
Continue to give high fat high-carbonhydrate diet；Normal group still gives normal diet.
3, dosage regimen: melbine group gives melbine aqueous solution 150mg/kg gavage from the 10th week；Treatment group every day
Give 20mg/kg Sophoraflavanone G, 40mg/kg Sophoraflavanone G gavage respectively；Normal group and model group are then
Give equal-volume distilled water gavage, pharmaceutical intervention totally 1 week.
4, experiment reagent: Sophoraflavanone G, metformin hydrochloride tablet, Streptozotocin, ALT, AST measure examination
Agent box, insulin radioimmunoassay immunoassay kits.
Testing index: the 1. change of blood sugar, insulin and liver function；2. use Hematoxylin-eosin (HE) decoration method detection rats'liver
Histopathologic change situation.
5, statistical analysis: application SPSS13.0 statistical software is analyzed, withRepresent；Employing single factor test is compared between group
Variance analysis, compares employing q inspection two-by-two between group；Relation correlation analysis between index.
6, experimental result
The change of 6.1 blood sugar, insulin and liver function
Model group is compared with normal group, and fasting blood sugar substantially increases, and after positive drug is treated, numerical value reduces, through low dosage list
Body flavones Sophoraflavanone G, high dose monomer flavones Sophoraflavanone G drug treatment, after 5 days, FBG value is relatively
Model group the most substantially reduces, and statistically significant；After monomer flavones Sophoraflavanone G treatment, insulin content is relatively
Model group substantially reduces, and has statistical significance；ALT, AST content relatively model group more also decreases, and has system
Meaning learned by meter.Illustrate that this monomer flavones Sophoraflavanone G can quickly reduce the blood glucose value of diabetes rat, weaken pancreas islet
Element opposing, the hepatic pathology damage to diabetes rat improves significantly.Detailed results is shown in Table 1.
Table 1 respectively organizes rat blood sugar, insulin and liver function change (x ± s, n=6)
Measurement data represents with X ± S.Comparing with model group, statistical significant difference is: * * P ＜ 0.001, * P ＜ 0.05.
6.2 pathological changes respectively organizing liver tissues of rats
Compared with model group, monomer flavones group Sophoraflavanone G liver cell intracytoplasmic lipid drips quantity to be reduced, steatosis,
Lobuli hepatis obscure boundary, liver rope arrangement disorder, sinus hepaticus and central vein expansion phenomenon are the most substantially alleviated.Detailed results is shown in
Fig. 1.
By test result indicate that above, the flavones group Sophoraflavanone G that the present invention provides not only has obvious hypoglycemic work
With, it is possible to effectively correct the carbohydrate metabolism disturbance of diabetes, improve the effect of sugar tolerance, and can significantly alleviate diabetes hepatopathy
Rat fat sex change, lobuli hepatis obscure boundary, liver rope arrangement disorder, sinus hepaticus and central vein expansion phenomenon, and there are no bad
Reaction, security is good.
The above is only the preferred embodiment of the present invention, it is noted that for those skilled in the art,
Under the premise without departing from the principles of the invention, it is also possible to make some improvements and modifications, these improvements and modifications also should be regarded as this
Bright protection domain.
Claims (4)
1. flavones Sophoraflavanone G application in preparation preventing and treating diabetes medicament.
2. flavones Sophoraflavanone G application in preparation prevents and treats diabetes merging liver disease drug.
The flavones Sophoraflavanone G the most according to claim 1 application in preparation preventing and treating diabetes medicament, its
Be characterised by, flavones Sophoraflavanone G and pharmaceutically acceptable carrier are made capsule, granule, spray,
Injection, micro-capsule, tablet, ointment or the medicine of skin-permeable and control-released plaster formulation.
Flavones Sophoraflavanone G the most according to claim 1 prevents and treats diabetes in preparation and merges in liver disease drug
Application, it is characterised in that flavones Sophoraflavanone G and pharmaceutically acceptable carrier are made capsule, granule,
Spray, injection, micro-capsule, lozenge, suppository, tablet, ointment or the medicine of skin-permeable and control-released plaster formulation.
Priority Applications (1)
| 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 |
Applications Claiming Priority (1)
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105832718A true CN105832718A (en) | 2016-08-10 |
| CN105832718B CN105832718B (en) | 2018-08-21 |
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| CN201610263505.6A Expired - Fee Related CN105832718B (en) | 2016-04-26 | 2016-04-26 | Flavones Sophoraflavanone G are preparing the application in preventing diabetes medicament |
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Citations (5)
| 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 |
| 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 |
| 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 |
-
2016
- 2016-04-26 CN CN201610263505.6A patent/CN105832718B/en not_active Expired - Fee Related
Patent Citations (5)
| 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 |
| 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 |
| 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 |
|---|
| HANQING WANG ET AL.: "Protective effect of Sophoraflavanone G on streptozotocin (STZ)-induced inflammation in diabetic rats", 《BIOMEDICINE & PHARMACOTHERAPY》 * |
| HYUN AH JUNG ET AL.: "Inhibitory activities of prenylated flavonoids from Sophora flavescens against aldose reductase and generation of advanced glycation endproducts", 《JOURNAL OF PHARMACY AND PHARMACOLOGY》 * |
| JIN HYO KIM ET AL.: "Glycosidase Inhibitory Flavonoids from Sophora flavescens", 《BIOL. PHARM. BULL.》 * |
| V.N.SYROV ET AL.: "Isolation, Chemical Analysis, And Study of The Hepatoprotector and Biligenic Activity of Total Flavonoid Preparations From Thermopsis dolichocarpa And Vexibia alopecuroides", 《PHARMACEUTICAL CHEMISTRY JOURNAL》 * |
| XINZHOU YANG ET AL.: "Antidiabetic effects of flavonoids from Sophora flavescens EtOAc extract in type2 diabetic KK-aymice", 《JOURNAL OF ETHNOPHARMACOLOGY》 * |
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| CN105832718B (en) | 2018-08-21 |
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Granted publication date: 20180821 Termination date: 20190426 |