CN106727470B - Application of the benserazide hydrochloride in the drug of preparation treatment acute inflammation - Google Patents
Application of the benserazide hydrochloride in the drug of preparation treatment acute inflammation Download PDFInfo
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- CN106727470B CN106727470B CN201611128161.4A CN201611128161A CN106727470B CN 106727470 B CN106727470 B CN 106727470B CN 201611128161 A CN201611128161 A CN 201611128161A CN 106727470 B CN106727470 B CN 106727470B
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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 drug of preparation treatment acute inflammation, belong to biomedicine technical field.For the present invention by animal experiment study therapeutic effect of the benserazide hydrochloride to acute inflammation, the inflammatory factor that test result shows that benserazide hydrochloride generates lipopolysaccharides induced mice acute inflammation has inhibiting effect.Acute inflammation model is constructed particular by lipopolysaccharide-induced C57BL/6 mouse, it is treated using the benserazide hydrochloride of various concentration, as a result, it has been found that benserazide hydrochloride can reduce the inflammatory factor level and liver tissue lesions' degree generated when C57BL/6 chmice acute inflammation, wherein, the benserazide hydrochloride effect of low dosage is best.The various preparations that benserazide hydrochloride is prepared into clinical needs by adding pharmaceutically acceptable carrier, the beneficial effect is that: new approach is provided to prepare acute inflammation drug.
Description
Technical field
The present invention relates to application of the benserazide hydrochloride in the drug of preparation treatment acute inflammation, belong to biological medicine technology
Field.
Background technique
Inflammation is that the group rich in blood vessel is woven in a kind of physiological reaction occurred after local damage.In the process, various can
Dissolubility medium and inflammatory cell are played a role together in the form of system, with eliminate cause body injury factor show as it is red,
Swollen, heat, pain and dysfunction.Studies have shown that inflammatory process participates in the pathogenic process of a variety of diseases, such as human infection, tumour, the heart
Cerebrovascular disease, senile dementia and neurodegenerative disease, allergic disease etc..Clinic display, anti-inflammatory drug is to be only second to resist
Second major class drug 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 object, the concentration of SAP can conspicuousness be increased to several times to several
Hundred times are differed.IL-1, IL-6 are the main inducible factors of SAP expression.When body tissue is by destroying, the secretion of TNF-α is lured
Sending out IL-1 and IL-6 intracorporal largely discharges, thus inducing hepatocyte rapid synthesis 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 decarboxylase inhibitors, often combines with levodopa and compound formulation is made
Benserazide is used for the treatment of Parkinson's disease.But there has been no the reports of benserazide hydrochloride treatment acute inflammation at present.
Summary of the invention
The object of the present invention is to provide benserazide hydrochlorides as the application in treatment acute inflammation drug.
The present invention shows salt by animal experiment study therapeutic effect of the benserazide hydrochloride to acute inflammation, test result
The inflammatory factor that sour benserazide generates lipopolysaccharides induced mice acute inflammation has inhibiting effect.Particular by lipopolysaccharide-induced
C57BL/6 mouse constructs acute inflammation model, is treated using the benserazide hydrochloride of various concentration to it, as a result, it has been found that hydrochloric acid
Benserazide can reduce the inflammatory factor level and liver tissue lesions' degree generated when C57BL/6 chmice acute inflammation, wherein
The benserazide hydrochloride effect of low dosage is best.Benserazide hydrochloride is prepared into clinical need by adding pharmaceutically acceptable carrier
The various preparations wanted, the beneficial effect is that: new approach is provided to prepare acute inflammation drug.
Detailed description of the invention
Fig. 1 is blank control group mouse liver organization HE dyeing microscopic examination figure.
Fig. 2 is model control group mouse liver tissue HE dyeing microscopic examination figure.
Fig. 3 is benserazide hydrochloride high dose group mouse liver tissue HE dyeing microscopic examination figure.
Fig. 4 is benserazide hydrochloride middle dose group mouse liver tissue HE dyeing microscopic examination figure.
Fig. 5 is benserazide hydrochloride low dose group mouse liver tissue HE dyeing microscopic examination figure.
Fig. 6 is the ELISA result of SAP expression in mice serum.
Fig. 7 is the ELISA result of TNF-α expression in mice serum.
Fig. 8 is the ELISA result of IL-6 expression in mice serum.
Specific embodiment
The present invention will be further described combined with specific embodiments below, but the present invention should not be limited by the examples.
Embodiment
Establish acute inflammation animal model and drug treatment
All mouse are raised in SPF grades of animal houses, and take the feeding manner of free choice feeding and drinking-water.By 50
C57BL/6 mouse (be purchased from Nanjing University model organism research institute) is randomly divided into five groups, and every group 10, respectively blank control
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).
To above-mentioned five groups of mouse using after basal feed adaptable fed 1 week, benserazide hydrochloride low dose group mouse is injected
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
Manage salt water.After successive administration is handled 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
0h, 2h, 4h after injecting lipopolysaccharides, 8h collect blood sample, and 8h puts to death mouse after taking blood, obtains liver organization sample.Then
Carry out ELISA experiment and HE dyeing.
HE Coloration experiment
It after experiment, takes liver and is fixed in 10% formalin solution, conventional to draw materials, dehydration, paraffin embedding is cut
Piece (4 microns of thickness).HE dyeing: (1) paraffin section routinely dewaxes: dimethylbenzene (I) 15min → dimethylbenzene (II) (answering fully transparent)
10min；(2) downlink graded ethanol impregnates aquation: 100% ethyl alcohol (I) ethyl alcohol of 2min → 100% (II) second of 2min → 95% step by step
The ethyl alcohol of alcohol 2min → 80% 2min → tap water rinses a moment；(3) it dyeing: distilled water develops a film quarter → haematoxylin liquid dye core 5min →
It is anti-blue that tap water rinses the differentiation of a moment → 1% acidic alcohol 30s (mention insert several under) → flowing water flushing a moment → weak ammonia liquor aqueous solution
Several seconds → flowing water rinses 10min → sets in 0.5% Yihong aqueous solution and redyes 10min；(4) ascending gradient ethanol dehydration step by step: from
Water flushing a moment (differentiation Yihong) → 95% ethyl alcohol (I) ethyl alcohol of 2min → 95% (II) ethyl alcohol of 2min → 100% (I) 2min →
100% ethyl alcohol (II) 2min；(5) transparent: dimethylbenzene (I) 5min → dimethylbenzene (II) 5min；(6) fixed, mounting: under coverslip
Resinene fixes, mounting.(6) it is checked under optical microscopy.
Optical microphotograph microscopic observation result: blank control group, hepatic tissue are made 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, is such as schemed
1.Model control group, the same blank group of hepatic tissue structure, structure are still clear.It is visible thin to show as liver cell endochylema for liver cell fatty degeneration
The fat drips vacuole of another typical material shape；Visible leukocytic margination in central vein；Kupffer's cells hyperplasia；The wherein visible stove of 1 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 is clear in structure, disease
Reason changes, lesion degree slightly mitigation consistent with model group, 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 mitigates, 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
It is slightly heavy, such as Fig. 5.
ELISA detects SAP in mice serum, TNF-α, IL-6 expression variation
After blood specimen collection, it is immediately placed on ice.After 2h, 3000r/min4 DEG C of centrifugation, time 15min.It mentions
After taking serum, ELISA detection is carried out.(1) it is loaded: the every empty 100 μ L of blood serum sample.(2) plus detect antibody: 50 μ L/well are added
Biotinylated antibody working solution.After mixing, sealing plate film is covered, 37 DEG C are incubated for 90 minutes.(3) board-washing: button removes liquid in hole, 300 μ
Cleaning solution is added in L/well；Liquid in hole is discarded after stopping 1 minute.It is repeated 4 times, is buckled on filter paper each time dry.(4) enzyme:
100 μ L/well Streptavidin-HRP working solutions.Sealing plate film is covered, 37 DEG C are incubated for 30 minutes.(5) board-washing: step 3 is repeated.
(6) develop the color: 100 μ L/well be added TMD, 37 DEG C Incubation in dark 5-30 minutes, sentenced according to the depth (navy blue) of color in hole
It is fixed to terminate reaction.Usually colour developing 10-20 minutes.(7) terminate reaction: 100 μ L/well are rapidly added terminate liquid and terminate 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 embodiments.It is all to be formed using equivalent substitution or equivalent transformation
Technical solution, fall within the scope of protection required by the present invention.
Claims (4)
1. purposes of the benserazide hydrochloride in the drug of preparation treatment acute inflammation.
2. purposes of the benserazide hydrochloride in the drug of preparation treatment acute inflammation according to claim 1, it is characterised in that:
The various preparations that the benserazide hydrochloride is prepared into clinical needs by adding pharmaceutically acceptable carrier.
3. purposes of the benserazide hydrochloride in the drug of preparation treatment acute inflammation according to claim 2, it is characterised in that:
The additive amount of the benserazide hydrochloride is 25-100mg/kg/d.
4. purposes of the benserazide hydrochloride in the drug of preparation treatment acute inflammation according to claim 3, it is characterised in that:
The additive amount of the benserazide hydrochloride is 25mg/kg/d.
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| CN106727470B true CN106727470B (en) | 2019-10-01 |
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Families Citing this family (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 |
| CN111743884A (en) * | 2019-03-26 | 2020-10-09 | 深圳先进技术研究院 | Use of benserazide or derivatives thereof |
| 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 |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1837169A (en) * | 2006-03-14 | 2006-09-27 | 房学迅 | Compound capable of inhibiting zinc ion metalloproteinases |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1837169A (en) * | 2006-03-14 | 2006-09-27 | 房学迅 | Compound capable of inhibiting zinc ion metalloproteinases |
Non-Patent Citations (2)
| Title |
|---|
| ACUTE-PHASE REACTANTS OF MICE II. Strain Dependence of Serum Amyloid P-Component (SAP) Levels and Response to Inflammation;RICHARD F等;《THE JOURNAL OF IMMUNOLOG》;19830228;第130卷(第2期);第885-889页，尤其是摘要 * |
| 基于SAP靶标的抗动脉粥样硬化研究;刁曙荣;《医药前沿》;20161031;第6卷(第29期);第102-103页，尤其是摘要 * |
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