CN109602758A - Linarin is preparing the application in anti-hepatic fibrosis medicines - Google Patents
Linarin is preparing the application in anti-hepatic fibrosis medicines Download PDFInfo
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- CN109602758A CN109602758A CN201910132610.XA CN201910132610A CN109602758A CN 109602758 A CN109602758 A CN 109602758A CN 201910132610 A CN201910132610 A CN 201910132610A CN 109602758 A CN109602758 A CN 109602758A
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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Abstract
The invention discloses a kind of linarins to prepare the application in anti-hepatic fibrosis medicines, belongs to pharmaceutical technology field.Experimental result of the present invention: linarin administration can intervene the raising of liver coefficient caused by liver fibrosis；Linarin administration can reduce the glutamic-oxalacetic transaminease (AST) of Liver Fibrosis Model mice serum and the content of glutamic-pyruvic transaminase (ALT), and it has conspicuousness to the reduction of content；Linarin can be substantially reduced the content of hydroxyproline in liver organization, i.e. linarin can obviously inhibit the generation of collagenous fibres in mouse；Linarin administration group hepatic tissue structure pathological change is alleviated, and bile duct proliferation situation is inhibited, and tissue necrosis degree significantly reduces；Linarin can obviously inhibit the hepatic fibrosis in mice of tetrachloro-methane induction.
Description
Technical field
The invention belongs to pharmaceutical technology field, in particular to a kind of linarin is preparing answering in anti-hepatic fibrosis medicines
With.
Background technique
Liver fibrosis (liver fibrosis) is anti-secondary to the reparation organized after various types of chronic liver injuries
Process is answered, is that pathology holds sign, the cause of disease with the over-deposit of extracellular matrix components (extracellular matrix, ECM)
It is closely related with chronic viral hepatitis, alcohol, non-alcohol fatty liver, toxin and drug, autoimmune liver disease etc.,
To lead to cirrhosis, be further development of liver cancer prelude and necessary intermediate link, be the main reason for hepatopathy is dead.It has become
The all very high world medicine problem of one morbidity and mortality.
The morbidity of liver fibrosis is substantially excessive with the extracellular matrix as main component such as type i collagen, laminin
It generates and is deposited in hepatic tissue, the structure and function of liver is caused to be destroyed.Chinese herbal medicine and its effective component prevention and treatment liver are fine
Dimensionization is the characteristic and advantage in China, and Chinese medicine and its effective component have anti-liver injury, protects liver cell, promotes chronic injury liver
The recovery function of cell.
Linarin (linarin) also known as robinin, structural formulaIt is a kind of natural flavone methods of glycosides, is
The component target of reference substance and the quality control of Buddlejaceae butterflybush flower medicinal material chemical analysis, it is liquor-saturated to be also widely present in Buddlejaceae
Water shield, in the plants such as composite family wild chrysanthemum, field thistle.The medicinal materials such as butterflybush flower, wild chrysanthemum belong to it is traditional it is clearing heat and detoxicating, anti-inflammatory in
Medicine, herb resource is extremely abundant, and flavones ingredient is its important composition and effectiveness for playing the drug effects such as anti-inflammatory, liver protection.In recent years messenger
The pharmacological activity of linarin monomer therein is conducted extensive research.Xu Hanting et al. is research shows that linarin can reduce
The raising of interleukin-6 caused by lipopolysaccharide-induced vascular endothelial cell damage, in- γ inhibits TLR4 and leucocyte to be situated between
The expression of plain -1 receptor-associated kinase inhibits TNF-α mediated apoptosis signal path to play anti-inflammatory effect [Xu Hanting, Su Jie, Wu Ya
Army, Chen Suhong, influence [J] of the Lv Guiyuan linarin to lipopolysaccharide-induced vascular endothelial cell inflammation damage, herbal pharmacology with
Clinic 2016；32(1):29-32].However, up to the present, having no and being studied in terms for the treatment of liver fibrosis disease linarin
Report.The present invention proposes and demonstrates linarin have therapeutic effect to chronic hepatic fibrosis.Linarin low dose uses safe
Reliably, it has no toxic side effect, is a kind of very promising and Development volue treating liver fibrosis agent.
Summary of the invention
The purpose of the present invention is to provide linarins to prepare the application in anti-hepatic fibrosis medicines.
The present invention using linarin as raw material, be applied alone or with other pharmaceutical compositions with effect of anti hepatic fibrosis, press
The preparation method of conventional formulation is prepared into the anti-hepatic fibrosis medicines for being suitble to oral any dosage form, such as oral solution, tablet, glue
Capsule, granule or other injection dosage forms.
Liver Fibrosis Model is established in the quick liver fibrosis of present invention inducing mouse in a manner of tetrachloro-methane induction, and to small
Mouse liver function, hepatic tissue pathology structure, extent of liver fibrosis are detected, the results show that linarin is able to suppress liver fibre
The generation of dimensionization.
Specific embodiment
Test example: linarin anti-hepatic fibrosis experiment
1, experiment product:
Linarin (is purchased from Chengdu Puffy moral Science and Technology Development Co., Ltd., purity 98%).
Male mouse of kunming, 20 ± 2g of weight are purchased from Chongqing En Siweier Biotechnology Co., Ltd Experimental Animal Center
(production licence number: SCXK 2018-0003)；
Glutamic-pyruvic transaminase (alanine aminotransferase, ALT) kit, glutamic-oxalacetic transaminease (aspartate
Aminotransferase, AST) kit be purchased from Beijing Leaderman Biochemistry Co., Ltd；
Hydroxyproline testing cassete builds up Bioengineering Research Institute purchased from Nanjing；
Other reagents are domestic (analysis is pure)
2, experimental method:
Male mouse of kunming 45, it is divided into 5 groups, respectively low dose of solvent control group, model control group, linarin at random
Amount group (10mg/kg), linarin high dose group (30mg/kg), colchicin group
(0.1mg/kg).Rat drunk at modeling the 1st week phenobarbital (phenobarbital, 30mg are dissolved in 100ml water) with
It induces mixed-function oxidase activity to increase the generation of metabolite, improve modeling success rate and shortens the modeling period.Except solvent
Control group is subcutaneously injected outside equivalent peanut oil by kg body weight, and the mixing of 40% carbon tetrachloride peanut oil is subcutaneously injected in other groups for the first time
Liquid, 5ml/kg weight, later per injection 2ml/kg weight, 2 times 1 week, continuous injection induced Liver Fibrosis Model in 8 weeks.From
From modeling the 5th week, by volume, drug 10mg/kg, 30mg/kg linarin and the 0.1mg/kg autumn of various dose are given in stomach-filling respectively
Tazettine group.1 time a day, continuous 4 weeks, isometric drug solvent was given in solvent control group and model control group stomach-filling.
(1) influence of the linarin to liver fibrosis Mouse Liver coefficient
Influence (n=8) of 1 linarin of table to liver fibrosis Mouse Liver coefficient
Note: compared with model group,*P<0.05,*P<0.01
The results are shown in Table 1: Liver Fibrosis Model group Mouse Liver coefficient is apparently higher than normal group (p < 0.01), and linarin is given
Medicine can intervene the raising of liver coefficient caused by liver fibrosis, and compared to Liver Fibrosis Model group, administration group linarin high dose group can
To significantly inhibit the raising (p < 0.01) of Mouse Liver coefficient.Experimental result illustrates linarin for liver during hepatic fibrosis in mice
Increasing has significant intervention effect and is in dosage correlation.
(2) linarin influences the content of liver fibrosis Mouse Liver AST and ALT
Mouse fasting before experiment samples, with chloral hydrate anesthesia mouse, eyeball takes blood.Centrifugation, take serum detection serum and
The content of glutamic-oxalacetic transaminease (AST) and glutamic-pyruvic transaminase (ALT) in hepatic tissue.
2 linarin of table influences (n=8) to the content of liver fibrosis Mouse Liver AST and ALT
Note: compared with model group,*P<0.05,*P<0.01
The results are shown in Table 2: the glutamic-oxalacetic transaminease (AST) and glutamic-pyruvic transaminase of Liver Fibrosis Model group mice serum
(ALT) content is apparently higher than normal group, and the glutamic-oxalacetic transaminease that can reduce Liver Fibrosis Model mice serum is administered in linarin
(AST) and the content of glutamic-pyruvic transaminase (ALT), and its to the reduction of content have conspicuousness (administration group low dose group be p <
0.05, administration group high dose group is p < 0.01).Experimental result illustrates linarin to millet straw in serum during hepatic fibrosis in mice
Transaminase (AST) and the content of glutamic-pyruvic transaminase (ALT) have certain intervention effect, and are in dosage correlation.
(3) influence of the linarin to mouse liver hydroxyproline in tissue
Fasting before mouse samples puts to death rat, takes liver organization, accurately weigh 100mg, build up bioengineering according to Nanjing
Research institute's hydroxyproline testing cassete specification is operated, and hydroxyproline content in hepatic tissue is measured.
3 linarin of table influences (n=8) to hydroxyproline content in liver fibrosis murine liver tissue
Note: compared with model group,*P<0.05,*P<0.01
The results are shown in Table 3, and compared with normal mouse, model group mouse liver hydroxyproline in tissue is obviously risen
Height, after linarin is administered, mouse liver hydroxyproline in tissue is significantly reduced, and shows that linarin can be substantially reduced liver
The content of hydroxyproline in tissue, i.e. linarin can obviously inhibit the generation of collagenous fibres in mouse.
(4) linarin is on the morphologic influence of Liver Fibrosis Model murine liver tissue
Mouse liver tissue is taken, hepatomegaly leaf texture block is cut and is put into fixation in formalin.By dehydration, paraffin embedding,
The production paraffin sections such as slice, roasting piece.It is dyed using one eosin stains liquid of haematoxylin, microscopically observation mouse liver group
Knit pathologic structure situation of change.Blank control group mouse liver specimens lobuli hepatis structure is normal as the result is shown, hepatic cell cords arrangement
Rule, liver cell have no hyperplasia fibr tissue without denaturation, necrosis.Rule is owed in the arrangement of Liver Fibrosis Model group mouse liver cell, is had
Part of hepatocytes necrosis, steatosis and the variation of balloon sample, bile duct proliferation is fairly obvious, and tissue necrosis increased significantly.Linarin
Administration group hepatic tissue structure pathological change is alleviated, and bile duct proliferation situation is inhibited, and tissue necrosis degree significantly reduces, wherein high
Dosage administration group has more the influence of conspicuousness.Show that linarin can be obviously improved the pathologic structure of mouse liver tissue.
(5) inhibiting effect of the linarin to the hepatic fibrosis in mice of induction
Mouse paraffin section is taken to be dyed with Mass, observation mouse liver tissue fibrosis changes situation.The result shows that blank
Control group mice liver specimens have no hyperplasia fibr tissue.Liver Fibrosis Model group mouse portal area fibrosis expands, Dou Zhouke
See a few fibres hyperblastosis, the visible linear staple fiber interval in portal area is formed, and mouse liver tissue fibrosis degree obviously increases
Add.Linarin administration group portal area fiber deposition is significantly reduced compared with model group.Show that linarin can obviously inhibit carbon tetrachloride
The hepatic fibrosis in mice of induction.
The above described is only a preferred embodiment of the present invention, being not intended to limit the present invention in any form, appoint
What is to the above embodiments according to the technical essence of the invention any simply to repair without departing from technical solution of the present invention content
Change, equivalent variations and modification, all of which are still within the scope of the technical scheme of the invention.
Claims (3)
1. a kind of linarin is preparing the application in anti-hepatic fibrosis medicines.
2. application as described in claim 1, it is characterised in that: using linarin as raw material, be applied alone or have with other anti-
The pharmaceutical composition of fibrosis effect, routinely the preparation method of preparation, is prepared into the anti-hepatic fibrosis medicine of suitable peroral dosage form
Object.
3. application as claimed in claim 1 or 2, it is characterised in that: dosage form is oral solution, tablet, capsule, granule or needle
Agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910132610.XA CN109602758A (en) | 2019-02-22 | 2019-02-22 | Linarin is preparing the application in anti-hepatic fibrosis medicines |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910132610.XA CN109602758A (en) | 2019-02-22 | 2019-02-22 | Linarin is preparing the application in anti-hepatic fibrosis medicines |
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| Publication Number | Publication Date |
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| CN109602758A true CN109602758A (en) | 2019-04-12 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201910132610.XA Pending CN109602758A (en) | 2019-02-22 | 2019-02-22 | Linarin is preparing the application in anti-hepatic fibrosis medicines |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115068492A (en) * | 2022-07-26 | 2022-09-20 | 中山市中医院 | Application of linarin in preparation of drugs for preventing or treating pulmonary fibrosis |
-
2019
- 2019-02-22 CN CN201910132610.XA patent/CN109602758A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115068492A (en) * | 2022-07-26 | 2022-09-20 | 中山市中医院 | Application of linarin in preparation of drugs for preventing or treating pulmonary fibrosis |
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