CN106727470A - Application of the benserazide hydrochloride in the medicine for preparing treatment acute inflammation - Google Patents
Application of the benserazide hydrochloride in the medicine for preparing treatment acute inflammation Download PDFInfo
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- CN106727470A CN106727470A CN201611128161.4A CN201611128161A CN106727470A CN 106727470 A CN106727470 A CN 106727470A CN 201611128161 A CN201611128161 A CN 201611128161A CN 106727470 A CN106727470 A CN 106727470A
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- benserazide hydrochloride
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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Abstract
The present invention relates to application of the benserazide hydrochloride in the medicine for preparing treatment acute inflammation, belong to biomedicine technical field.The present invention passes through animal experiment study therapeutic effect of the benserazide hydrochloride to acute inflammation, and result of the test display benserazide hydrochloride has inhibitory action to the inflammatory factor that lipopolysaccharides induced mice acute inflammation is produced.Acute inflammation model is constructed particular by lipopolysaccharide-induced C57BL/6 mouse, it is treated using the benserazide hydrochloride of various concentrations, result finds that benserazide hydrochloride can reduce the inflammatory factor level and liver tissue lesions' degree produced during C57BL/6 chmice acute inflammation, wherein, the benserazide hydrochloride best results of low dosage.Benserazide hydrochloride is prepared into the various preparations of clinical needs by adding pharmaceutically acceptable carrier, its advantage is：New approach is provided to prepare acute inflammation medicine.
Description
Technical field
The present invention relates to application of the benserazide hydrochloride in the medicine for preparing treatment acute inflammation, belong to biological medicine technology
Field.
Background technology
Inflammation is a kind of physiological reaction of generation after the local damage of being organized in rich in blood vessel.In the process, it is various can
Dissolubility medium and inflammatory cell are together played a role in the form of system, with eliminate cause body injury factor show as it is red,
Swollen, heat, pain and dysfunction.Research shows that inflammatory process participates in the pathogenic process of various diseases, such as human infection, tumour, the heart
Cerebrovascular disease, senile dementia and nerve degenerative diseases, allergic disease etc..Clinic display, anti-inflammatory drug is to be only second to resist
Second major class medicine of infection medicine.Serum amyloid P component (SAP) belongs to pentamer plasma protein family, is a kind of
Highly conserved Acute response stage albumen, under the induction of inflammatory stimulus thing, the concentration meeting conspicuousness of SAP is increased to several times and arrives several
Hundred times.IL-1, IL-6 are the main inducible factors of SAP expression.When body tissue is destroyed, the secretion of TNF-α is lured
The IL-1 and IL-6 for sending out internal largely discharge, so that inducing hepatocyte Fast back-projection algorithm SAP.
Benserazide hydrochloride is recorded in Chinese Pharmacopoeia version (ChP 2010) in 2010, European Pharmacopoeia 7.0 editions (EP7.0) and Japan
Pharmacopeia 16 editions (JP16).Benserazide hydrochloride is a kind of periphery DCI, is often made compound formulation with combined with levodopa
Benserazide is used for the treatment of Parkinson's.But not yet there is benserazide hydrochloride to treat the report of acute inflammation at present.
The content of the invention
It is an object of the invention to provide benserazide hydrochloride as the application in treatment acute inflammation medicine.
The present invention passes through animal experiment study therapeutic effect of the benserazide hydrochloride to acute inflammation, result of the test display salt
Sour benserazide has inhibitory action to the inflammatory factor that lipopolysaccharides induced mice acute inflammation is produced.Particular by lipopolysaccharide-induced
C57BL/6 mouse construct acute inflammation model, and it is treated using the benserazide hydrochloride of various concentrations, as a result find hydrochloric acid
Benserazide can reduce the inflammatory factor level and liver tissue lesions' degree produced during C57BL/6 chmice acute inflammation, wherein,
The benserazide hydrochloride best results of low dosage.Benserazide hydrochloride is prepared into clinical need by adding pharmaceutically acceptable carrier
The various preparations wanted, its advantage is：New approach is provided to prepare acute inflammation medicine.
Brief description of the drawings
Fig. 1 is blank control group mouse liver tissue HE dyeing microscopic examination figures.
Fig. 2 is model control group mouse liver tissue HE dyeing microscopic examination figures.
Fig. 3 is benserazide hydrochloride high dose group mouse liver tissue HE dyeing microscopic examination figures.
Fig. 4 is benserazide hydrochloride middle dose group mouse liver tissue HE dyeing microscopic examination figures.
Fig. 5 is benserazide hydrochloride low dose group mouse liver tissue HE dyeing microscopic examination figures.
Fig. 6 is the ELISA results of SAP expression in mice serum.
Fig. 7 is the ELISA results of TNF-α expression in mice serum.
Fig. 8 is the ELISA results of IL-6 expression in mice serum.
Specific embodiment
With reference to specific embodiment, the present invention will be further described, but the present invention should not be limited by the examples.
Embodiment
Set up acute inflammation animal model and administration treatment
All mouse are raised in SPF grades of Animal House, and take the feeding manner of free choice feeding and drinking-water.By 50
C57BL/6 mouse (being purchased from model organism research institute of Nanjing University) are randomly divided into five groups, respectively every group 10, blank
Group, model control group, benserazide hydrochloride low dose group (25mg/kg/d), benserazide hydrochloride middle dose group (50mg/kg/d), salt
Sour benserazide high dose group (100mg/kg/d).
After being fed 1 week using basal feed adaptability to above-mentioned five groups of mouse, the injection of benserazide hydrochloride low dose group mouse
Benserazide hydrochloride 25mg/kg/d, benserazide hydrochloride middle dose group mouse injection benserazide hydrochloride 50mg/kg/d and benserazide hydrochloride
High dose group mouse injects benserazide hydrochloride 100mg/kg/d, and blank control group and model control group then inject the life of respective volume
Reason salt solution.After successive administration is processed 7 days, model control group, benserazide hydrochloride low dose group, benserazide hydrochloride middle dose group, salt
Sour benserazide high dose group injects 3mg/kg lipopolysaccharides, and blank control group mouse injects the physiological saline of respective volume.Respectively
The 0h after lipopolysaccharides is injected, 2h, 4h, 8h collect blood sample, and 8h puts to death mouse, obtains liver organization sample after taking blood.Then
Carry out ELISA experiments and HE dyeing.
HE Coloration experiments
After experiment terminates, take liver and be fixed in 10% formalin solution, conventional materials, dehydration, FFPE is cut
Piece (4 microns of thickness).HE is dyeed：(1) paraffin section routinely dewaxes：Dimethylbenzene (I) 15min → dimethylbenzene (II) (should be fully transparent)
10min；(2) descending graded ethanol soaks aquation step by step：100% ethanol (I) 2min → 100% ethanol (II) 2min → 95% second
Alcohol 2min → 80% ethanol 2min → running water rinses a moment；(3) dye：Distilled water develops a film quarter → and haematoxylin liquid dye core 5min →
It is anti-blue that running water rinses a moment → 1% acidic alcohol differentiation 30s (carry slotting several under) → flowing water flushing a moment → weak ammonia liquor aqueous solution
Several seconds → flowing water rinses in 10min → set to 0 .5% Yihong aqueous solution and redyes 10min；(4) ascending gradient ethanol dehydration step by step：From
Water flushing a moment (differentiation Yihong) → 95% ethanol (I) 2min → 95% ethanol (II) 2min → 100% ethanol (I) 2min →
100% ethanol (II) 2min；(5) it is transparent：Dimethylbenzene (I) 5min → dimethylbenzene (II) 5min；(6) fixed, mounting：Under cover glass
Resinene is fixed, mounting.(6) checked under light microscope.
Optical microphotograph Microscopic observation result：Blank control group, hepatic tissue is made up of lobuli hepatis and interlobular portal area, liver
Cell is arranged radially around central vein, the visible interlobular bile duct in portal area, interlobular veins and interlobular artery, such as schemes
1.Model control group, the same blank group of hepatic tissue structure, structure is still clear.Liver cell fatty degeneration, shows as liver cell endochylema visible thin
The fat drips vacuole of another typical material shape；Visible leukocytic margination in central vein；Kupffer's cells hyperplasia；The wherein 1 visible stove of mouse
Property necrosis of liver cells, focal inflammation.Such as Fig. 2.Benserazide hydrochloride high dose group, the same blank group of hepatic tissue structure, clear in structure, disease
Reason changes consistent with model group, and lesion degree slightly has mitigation, such as Fig. 3.Benserazide hydrochloride middle dose group, the same blank of hepatic tissue structure
Group, clear in structure, pathological change is consistent with model group, and lesion degree higher dosage group slightly has mitigation, such as Fig. 4.Benserazide hydrochloride
Low dose group, the same blank group of hepatic tissue structure, clear in structure, pathological change is consistent with model group, lesion degree higher dosage group
Slightly weigh, such as Fig. 5.
SAP, TNF-α, IL-6 expression changes in ELISA detection mice serums
After blood specimen collection is finished, it is immediately placed on ice.After 2h, 3000r/min4 DEG C of centrifugation, the time is 15min.Carry
After taking serum, ELISA detections are carried out.(1) it is loaded：Blood serum sample is per empty 100 μ L.(2) detection antibody is added：50 μ L/well are added
Biotinylated antibody working solution.After mixing, shrouding film is covered, 37 DEG C are incubated 90 minutes.(3) board-washing：Button removes liquid in hole, 300 μ
L/well adds cleaning solution；Liquid in hole is discarded after stopping 1 minute.It is repeated 4 times, buckles dry on filter paper each time.(4) it is enzyme-added：
100 μ L/well Streptavidin-HRP working solutions.Shrouding film is covered, 37 DEG C are incubated 30 minutes.(5) board-washing：Repeat step 3.
(6) develop the color：100 μ L/well add TMD, 37 DEG C Incubation in dark 5-30 minutes, the depth (navy blue) according to color in hole is sentenced
Determine terminating reaction.Generally colour developing 10-20 minutes.(7) terminating reaction：100 μ L/well are rapidly added terminate liquid terminating reaction.It is small
SAP, TNF-α, IL-6 expression result of variations are respectively such as Fig. 6, Fig. 7, Fig. 8 in mouse serum.
In addition to above-mentioned implementation, the present invention can also have other embodiment.All use equivalents or equivalent transformation are formed
Technical scheme, all fall within the protection domain of application claims.
Claims (4)
1. benserazide hydrochloride prepare treatment acute inflammation medicine in purposes.
2. according to claim 1 benserazide hydrochloride prepare treatment acute inflammation medicine in purposes, it is characterised in that：
The benserazide hydrochloride is prepared into the various preparations of clinical needs by adding pharmaceutically acceptable carrier.
3. according to claim 2 benserazide hydrochloride prepare treatment acute inflammation medicine in purposes, it is characterised in that：
The addition of the benserazide hydrochloride is 25-100mg/kg/d.
4. according to claim 3 benserazide hydrochloride prepare treatment acute inflammation medicine in purposes, it is characterised in that：
The addition of the benserazide hydrochloride is 25mg/kg/d.
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| Application Number | Priority Date | Filing Date | Title |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109091473A (en) * | 2018-10-26 | 2018-12-28 | 中国药科大学 | Application of the benserazide hydrochloride in preparation treatment acute lung injury drug |
| CN111700885A (en) * | 2020-08-06 | 2020-09-25 | 山东省千佛山医院 | Application of benserazide and composition of benserazide and fluconazole in preparation of antifungal product |
| CN111743884A (en) * | 2019-03-26 | 2020-10-09 | 深圳先进技术研究院 | Use of benserazide or derivatives thereof |
| CN115919823A (en) * | 2022-08-15 | 2023-04-07 | 浙江艾特为生物科技有限公司 | Application of benserazide hydrochloride in preparation of medicine for treating diseases caused by respiratory syncytial virus |
Citations (1)
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|---|---|---|---|---|
| CN1837169A (en) * | 2006-03-14 | 2006-09-27 | 房学迅 | Compound capable of inhibiting zinc ion metalloproteinases |
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2016
- 2016-12-09 CN CN201611128161.4A patent/CN106727470B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1837169A (en) * | 2006-03-14 | 2006-09-27 | 房学迅 | Compound capable of inhibiting zinc ion metalloproteinases |
Non-Patent Citations (2)
| Title |
|---|
| RICHARD F等: "ACUTE-PHASE REACTANTS OF MICE II. Strain Dependence of Serum Amyloid P-Component (SAP) Levels and Response to Inflammation", 《THE JOURNAL OF IMMUNOLOG》 * |
| 刁曙荣: "基于SAP靶标的抗动脉粥样硬化研究", 《医药前沿》 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109091473A (en) * | 2018-10-26 | 2018-12-28 | 中国药科大学 | Application of the benserazide hydrochloride in preparation treatment acute lung injury drug |
| CN111743884A (en) * | 2019-03-26 | 2020-10-09 | 深圳先进技术研究院 | Use of benserazide or derivatives thereof |
| CN111700885A (en) * | 2020-08-06 | 2020-09-25 | 山东省千佛山医院 | Application of benserazide and composition of benserazide and fluconazole in preparation of antifungal product |
| CN111700885B (en) * | 2020-08-06 | 2021-06-04 | 山东省千佛山医院 | Application of benserazide and composition of benserazide and fluconazole in preparation of antifungal product |
| CN115919823A (en) * | 2022-08-15 | 2023-04-07 | 浙江艾特为生物科技有限公司 | Application of benserazide hydrochloride in preparation of medicine for treating diseases caused by respiratory syncytial virus |
| CN115919823B (en) * | 2022-08-15 | 2024-04-05 | 浙江艾特为生物科技有限公司 | Application of benserazide hydrochloride in preparing medicament for treating diseases caused by respiratory syncytial virus |
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