CN109793748A - A kind of prevention and treatment cerebral ischemia causes the drug and its preparation of inflammatory reaction - Google Patents
A kind of prevention and treatment cerebral ischemia causes the drug and its preparation of inflammatory reaction Download PDFInfo
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- CN109793748A CN109793748A CN201910254341.4A CN201910254341A CN109793748A CN 109793748 A CN109793748 A CN 109793748A CN 201910254341 A CN201910254341 A CN 201910254341A CN 109793748 A CN109793748 A CN 109793748A
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- cerebral ischemia
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- inflammatory reaction
- rhoifolin
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Abstract
The present invention relates to a kind of drugs for preventing cerebral ischemia from causing inflammatory reaction, it includes aurantiin and Rhoifolin, the aurantiin and Rhoifolin are the ingredients that Huajuhong extracts, the present invention has effects that inflammatory reaction caused by preventing and treating cerebral ischemia it has been investigated that the drug that aurantiin and Rhoifolin are formed can significantly inhibit inflammation caused by cerebral arterial thrombosis (abbreviation cerebral ischemia).
Description
Technical field
The present invention relates to biomedicine technical fields, and the drug of inflammatory reaction is caused more particularly to a kind of prevention and treatment cerebral ischemia
And its preparation.
Background technique
Ischemic cerebrovascular disease is also known as cerebral ischemia diseases, is the most common cranial vascular disease, and seriously affect patient
The disease of health and quality of life, it includes transient ischemic attack, invertibity neurological dysfunction and cerebral infarction.And
When symptoms of cerebral ischemia occurs, inflammatory reaction is often brought, inflammation refers to body when by various destructive stimulus, and height is living in vivo
Property molecule such as active oxygen radical (reactive oxygen species, ROS) and active nitrogen free radical (reactive
Nitrogen species, RNS) generate excessive, removing of the degree of oxidation beyond oxide, oxidative system and antioxidant system mistake
Weighing apparatus will cause the not normal and immune function of a series of metabolism once this coordination generates disorder and imbalance with dynamic equilibrium
It can reduce, form oxygen radical chain reaction, damage biomembrane and its function, so that cell transparency lesion, fibrosis are formed,
Large area cellular damage is caused into nerve, tissue, organ equivalent damage, very big to human health damage.
Summary of the invention
A kind of Huajuhong is provided and is prevented and treated in preparation it is an object of the invention to avoid shortcoming in the prior art
Cerebral ischemia causes the drug and pharmaceutical preparation of inflammatory reaction.
The purpose of the present invention is achieved through the following technical solutions:
A kind of prevention and treatment cerebral ischemia causes the drug of inflammatory reaction, includes aurantiin and Rhoifolin, and the aurantiin and open country are painted
The ratio for setting glycosides is 7:5 ~ 20:1.
Preferably, the drug is the extractive of general flavone of Huajuhong, and the extractive of general flavone includes above-mentioned
Aurantiin and Rhoifolin.
It preferably, further include having naringenin, the ratio of naringenin and Rhoifolin is 1:2 ~ 2:1.
It preferably, further include before having protocatechuic acid, shaddock (glycosides) aglucon -7-O- glucoside, merazin hydrate, aqua oxidation
Hu Su, meranzin, different meranzin, apiolin, Isomperatorin, auraptene and bergapten.
Preferably, the aurantiin, Rhoifolin, naringenin, protocatechuic acid, shaddock (glycosides) aglucon -7-O- glucoside, hydration
Meranzin, aqua oxidation peucedanin, meranzin, different meranzin, apiolin, Isomperatorin, auraptene and fingered citron
Lactone is extracted from Huajuhong together, and each component content ratio is identical in the ratio and Huajuhong between each ingredient of extract.
Preferably, the Huajuhong is the Exocarpium Citri Rubrum fruit for being grown in Maoming City Huazhou City.
Prevention and treatment cerebral ischemia causes the preparation of inflammatory reaction, uses medicine preparation mouth described in 4 any one of Claims 1-4
Take liquid, pill, particle or capsule.
Beneficial effects of the present invention:
Aurantiin and Rhoifolin are the ingredients that Huajuhong extracts, and the present invention is it has been investigated that aurantiin and Rhoifolin are formed
Drug can significantly inhibit inflammation caused by cerebral arterial thrombosis (abbreviation cerebral ischemia), have prevention and treatment cerebral ischemia caused by inflammation
The effect of reaction.
Specific embodiment
The invention will be further described with the following Examples.
Embodiment 1
A kind of prevention and treatment cerebral ischemia of the present embodiment causes the drug of inflammatory reaction to extract for the general flavone of Huajuhong (Exocarpium Citri Grandis)
Object, wherein the Huajuhong that the present embodiment is taken is the Exocarpium Citri Rubrum fruit for being grown in Maoming City Huazhou City.The extractive of general flavone packet
Containing aurantiin and Rhoifolin, the ratio of the aurantiin and Rhoifolin is 20:1.It can be by existing using the drug
Some pharmaceutical technologies are prepared into oral solution, pill, particle or capsule.
It includes following steps that the prevention and treatment cerebral ischemia, which causes the water of the drug of inflammatory reaction to obtain through refining Preparation Method:
(1) Exocarpium Citri Rubrum fruit processes: harvesting when Exocarpium Citri Rubrum summer fruit prematurity, removes pericarp in fruit flesh and part, compression moulding is done again
It is dry；
(2) it pulverizes: by the Exocarpium Citri Rubrum fruit abrasive flour after processing；
(3) water extracts: encased with gauze, the bubble for being 95 DEG C or more with temperature leaching obtain effective component concentration be 1.03% ~
1.05% aqueous solution, the content of aurantiin is 0.104% in aqueous solution, and Rhoifolin contains 0.005%.
Embodiment 2
The present embodiment difference from example 1 is that, the prevention and treatment cerebral ischemia of the present embodiment causes in the drug of inflammatory reaction
The content of aurantiin is 12:2.4, and the aqueous solution that effective component concentration is 1.03% ~ 1.05%, the content of aurantiin is in aqueous solution
0.124%, Rhoifolin contains 0.025%.
Embodiment 3
The present embodiment difference from example 1 is that, the prevention and treatment cerebral ischemia of the present embodiment causes in the drug of inflammatory reaction
The content of aurantiin is 7:5, and the aqueous solution that effective component concentration is 1.03% ~ 1.05%, the content of aurantiin is in aqueous solution
0.058%, Rhoifolin contains 0.041%.
Embodiment 4
The present embodiment difference from example 1 is that, the prevention and treatment cerebral ischemia of the present embodiment causes the drug of inflammatory reaction also
It include naringenin, the ratio of naringenin and Rhoifolin is 1:2.
Embodiment 5
The present embodiment difference from example 1 is that, the prevention and treatment cerebral ischemia of the present embodiment causes the drug of inflammatory reaction also
It include naringenin, the ratio of naringenin and Rhoifolin is 2:1.
Embodiment 6
The present embodiment difference from example 1 is that, the prevention and treatment cerebral ischemia of the present embodiment causes the drug of inflammatory reaction also
It include naringenin, the ratio of naringenin and Rhoifolin is 1:1.
Embodiment 7
The prevention and treatment cerebral ischemia of the present embodiment causes the drug of inflammatory reaction to include aurantiin, Rhoifolin, naringenin, former catechu
Acid, shaddock (glycosides) aglucon -7-O- glucoside, merazin hydrate, aqua oxidation peucedanin, meranzin, different meranzin, celery
Element, Isomperatorin, auraptene and bergapten, aforesaid components are extracted from Huajuhong together, each ingredient of extract
Between ratio and Huajuhong in each component content ratio it is identical, content between each ingredient of extract is that Huajuhong extract is more
Within the scope of the maximum value and minimum value of secondary measurement content.
Experiment: drug causes the effect in inflammation in prevention and treatment cerebral ischemia
1. test material
1.1 trial drugs and dose design
The prevention and treatment cerebral ischemia of embodiment 1 to 6 causes the drug of inflammatory reaction respectively to set 1 dosage group, is 0.9g/kg.
Experimental animal
Healthy male SD rat (weight 280-300g), Animal adaptability can be tested after raising 1 week.
2. test method
2.1 animal packets and drug-treated
2.1.1 animal packet
108 male SD rats are randomly divided into 9 groups, every group 12, are respectively as follows:
1. sham-operation group
Arteria cerebri media embolism Reperfu- sion 2. (MCAO/R) model group
3. example 1 group
4. 2 groups of embodiment
5. 3 groups of embodiment
6. 4 groups of embodiment
7. 5 groups of embodiment
8. 6 groups of embodiment
9. 7 groups of embodiment
4.1.2 drug-treated
Example 1 group, 2 groups of embodiment, 3 groups of embodiment, 4 groups of embodiment, 5 groups of embodiment, 6 groups of embodiment in MCAO operation consent
One week gastric infusion, sham-operation group and MCAO/R the model group rats then isometric physiological saline of stomach-filling.
Cerebral ischemia re-pouring injured (MCAO/R) model
Cerebral ischemia re-pouring injured (MCAO/R) model is made using line brush.Surgical procedure strict aseptic technique, chief surgical
Process is as follows: 4% chloraldurate (10mL/kg) intraperitoneal injection of anesthesia rat isolates arteria carotis communis (CCA), external carotid artery
(ECA) and internal carotid (ICA) arteria carotis communis, is closed with arteriole folder folder, with the branch of bipolar coagulation coagulation external carotid artery.Trip
From external carotid artery trunk, away from ligation at 3~4 mm of arteria carotis communis bifurcated.Temporarily folder closes internal carotid, eye scissors to arteriole folder
External carotid artery is cut into an osculum, the 4-0 filament nylon line of first polysiloxane coated is inserted into, makes a call to a turpentine in external carotid artery clip
To block the blood reflux of internal carotid, the arteriole folder of internal carotid is removed, nylon wire is touched and enters internal carotid, reach cranium
Interior arteria cerebri anterior blocks the opening of arteria cerebri media (MCA), insertion depth about 18-22mm.Remove the fine motion of arteria carotis communis
Arteries and veins folder, layer-by-layer suture subcutaneous tissue and skin after disinfection, Yu Shuhou 2h slowly extract nylon wire out and carry out Reperfu- sion for 24 hours.Sham-operation
For group in addition to being not inserted into nylon wire, remaining operation is identical as model group.The rectal temperature dimension of all rats in the entire experiment process
It holds at 37 DEG C.
Inflammation index detection
All rats are taken, serum is taken after abdominal aortic blood 5mL, 3000rpm centrifugation 10min, separates cerebral cortex and hippocampus group
It knits, takes supernatant after 3000rpm centrifugation 10min after 10% homogenate.Using ELISA kit detection inflammation index nadph oxidase,
It is 4- Hydroxynonenal (4-HNE), 8- hydroxylation deoxyguanosine (8-OHdG), protein carbonyl (Protein carbonyl), blood red
Plain oxygenase 1(HO-1) and quinone oxidoreductase 1(NQO-1) horizontal.
Data processing
All data are handled by SPSS22.0 for Windows statistical software, and data are with mean ± standard deviation (mean ± SD)
It indicates.It is examined using t and One-way ANOVA is for statistical analysis to continuous data, made two-by-two with least significant difference (LSD)
Compare, withP< 0.05 indicates that difference is statistically significant.
5. experimental result
Table 1 can significantly inhibit the inflammation of MCAO/R rat model
Continuous upper table
Note: ##,P< 0.01 vs sham-operation group；*,P< 0.05 vs MCAO/R model group；*,P< 0.01 vs MCAO/R mould
Type group.
MCAO/R model group.
KYN: urinary ammonia acid；
HsCRP: High-sensitivity C reactive protein；
MCP-1: monocyte chemoattractant protein-1；
TNF-α: tumor necrosis factor；
IL-1 β: interleukin 1；
IL-6: interleukin-6；
CD11a: leukocyte differentiation antigen molecule；
ICAM-1: intercellular adhesion molecule-1；
IL-4: interleukin 4
IL-10: interleukin 10
Experiments verify that knowing: compared with MCAO/R model group, rat blood serum KYN, MCP- of 1 to 6 group of the embodiment of the present invention
1, IL-6 level substantially reduces (P < 0.01), and drug of the invention is preventing and inhibiting inflammatory reaction caused by cerebral ischemia with bright
Aobvious effect.
Finally it should be noted that the above examples are only used to illustrate the technical scheme of the present invention explanation rather than right is wanted
Ask the limitation of protection scope.Those skilled in the art should be appreciated that referring to preferred embodiment and can be to of the invention
Technical solution is modified or replaced equivalently, but belongs to the substantially identical and protection scope of technical solution of the present invention.
Claims (7)
1. a kind of prevention and treatment cerebral ischemia causes the drug of inflammatory reaction, it is characterised in that: it include aurantiin and Rhoifolin, it is described
The ratio of aurantiin and Rhoifolin is 7:5 ~ 20:1.
2. the drug that a kind of prevention and treatment cerebral ischemia according to claim 1 causes inflammatory reaction, which is characterized in that the drug
For the extractive of general flavone of Huajuhong, the extractive of general flavone includes above-mentioned aurantiin and Rhoifolin.
3. the drug that a kind of prevention and treatment cerebral ischemia according to claim 1 causes inflammatory reaction, which is characterized in that further include having
The ratio of naringenin, naringenin and Rhoifolin is 1:2 ~ 2:1.
4. the drug that a kind of prevention and treatment cerebral ischemia according to claim 3 causes inflammatory reaction, which is characterized in that further include having
Protocatechuic acid, shaddock (glycosides) aglucon -7-O- glucoside, merazin hydrate, aqua oxidation peucedanin, meranzin, in different orange peel
Ester, apiolin, Isomperatorin, auraptene and bergapten.
5. the drug that a kind of prevention and treatment cerebral ischemia according to claim 4 causes inflammatory reaction, which is characterized in that the shaddock ped
Glycosides, Rhoifolin, naringenin, protocatechuic acid, shaddock (glycosides) aglucon -7-O- glucoside, merazin hydrate, the aqua oxidation root of purple-flowered peucedanum
Element, meranzin, different meranzin, apiolin, Isomperatorin, auraptene and bergapten are mentioned from Huajuhong together
It takes, each component content ratio is identical in the ratio and Huajuhong between each ingredient of extract.
6. the drug that a kind of prevention and treatment cerebral ischemia according to claim 4 or 5 causes inflammatory reaction, which is characterized in that described
Huajuhong is the Exocarpium Citri Rubrum fruit for being grown in Maoming City Huazhou City.
7. the preparation that prevention and treatment cerebral ischemia causes inflammatory reaction, which is characterized in that using described in 4 any one of Claims 1-4
Medicine preparation oral solution, pill, particle or capsule.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110420262A (en) * | 2019-03-31 | 2019-11-08 | 李锋 | Huajuhong causes the application of inflammatory reaction drug in preparation prevention and treatment cerebral ischemia |
| CN114796201A (en) * | 2022-05-10 | 2022-07-29 | 南京鼓楼医院 | Application of bergapten in preparation of medicine for treating cerebral arterial thrombosis |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110420262A (en) * | 2019-03-31 | 2019-11-08 | 李锋 | Huajuhong causes the application of inflammatory reaction drug in preparation prevention and treatment cerebral ischemia |
| CN114796201A (en) * | 2022-05-10 | 2022-07-29 | 南京鼓楼医院 | Application of bergapten in preparation of medicine for treating cerebral arterial thrombosis |
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