CN107854461A - Apigenin is preparing the application in treating and preventing kidney fibrosis medicine - Google Patents
Apigenin is preparing the application in treating and preventing kidney fibrosis medicine Download PDFInfo
- Publication number
- CN107854461A CN107854461A CN201610839602.5A CN201610839602A CN107854461A CN 107854461 A CN107854461 A CN 107854461A CN 201610839602 A CN201610839602 A CN 201610839602A CN 107854461 A CN107854461 A CN 107854461A
- Authority
- CN
- China
- Prior art keywords
- apigenin
- kidney fibrosis
- kidney
- treating
- medicine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Abstract
The invention provides applications of the Apigenin in the medicine for treating or preventing kidney fibrosis is prepared, belong to technical field of new application of medicine, belong to first public, because framework types belong to brand-new framework types, and it is strong for kidney fibrosis inhibitory activity, possess prominent substantive distinguishing features, while obviously there is significant progress for the preventing and treating of kidney fibrosis.
Description
Technical field
The present invention relates to compound Apigenin new application, more particularly to Apigenin to prepare treatment and prevention kidney fibre
Tie up the application in chemical drug thing.
Background technology
Kidney fibrosis (including kidney region fibrosis and glomerulosclerosis) is the last rank of kidney damage caused by a variety of causes
The main pathological basis of section, kidney fibrosis mechanism is complex, relevant with many factors, wherein mainly and extracellular matrix
Cell produces celliferous propagation and activation, and vaso-active substance, cell factor and extracellular matrix conversion are unbalance relevant, between kidney
Matter fibrosis is almost so primary or secondary kidney trouble proceeds to the common pathway of end stage renal failure.
Compound Apigenin of the present invention is one and delivers within 2011 (Ebenezer de Mello Cruz, et
al.,Leishmanicidal activity of Cecropia pachystachya flavonoids:Arginase
inhibition and altered mitochondrial DNA arrangement.Phytochemistry,89(2013)
71-77.) noval chemical compound, the compound possess brand-new framework types (Ebenezer de Mello Cruz, et al.,
Leishmanicidal activity of Cecropia pachystachya flavonoids:Arginase
inhibition and altered mitochondrial DNA arrangement.Phytochemistry,89(2013)
71-77.), purposes of the Apigenin of the present invention in treatment and prevention kidney fibrosis medicine is prepared belongs to first public.
The content of the invention
It is an object of the invention to do not find that it has in studying according to existing Apigenin to treat and prevent kidney fibrosis
The present situation of the report of activity, there is provided Apigenin is preparing the application in treating and preventing kidney fibrosis medicine.
Shown in the compound Apigenin structures such as formula (I)：
Applications of the Apigenin in kidney fibrosis medicine is treated and prevented, reduce kidney region fibrosis hydroxyproline
Content.
One kind treats and prevents kidney fibrosis medicine, is that active component addition auxiliary material is prepared by Apigenin, prepares
Method adds 195 grams of dextrin, mixed, Conventional compression is made 1000 to take 5 g of compound Apigenin.
One kind treats and prevents kidney fibrosis medicine, is that active component addition auxiliary material is prepared by Apigenin, prepares
Method adds 195 grams of starch, mixing is encapsulated to be made 1000 to take 5 g of compound Apigenin.
Purposes of the Apigenin of the present invention in treatment or prevention kidney fibrosis medicine is prepared belongs to first public,
Because framework types belong to brand-new framework types, and it is strong for kidney fibrosis inhibitory activity, possesses prominent substance
Feature, while obviously there is significant progress for the preventing and treating of kidney fibrosis.
Embodiment
Compound Apigenin involved in the present invention preparation method referring to document (Ebenezer de Mello Cruz,
et al.,Leishmanicidal activity of Cecropia pachystachya flavonoids:Arginase
inhibition and altered mitochondrial DNA arrangement.Phytochemistry,89(2013)
71–77.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific reality
Any restrictions of example are applied, but are defined in the claims.
Embodiment 1：The preparation of compound Apigenin tablets involved in the present invention：
Take 5 g of compound Apigenin to add 195 grams of dextrin, mix, Conventional compression is made 1000.
Embodiment 2：The preparation of compound Apigenin capsules involved in the present invention：
Take 5 g of compound Apigenin to add 195 grams of starch, mix, it is encapsulated to be made 1000.
Its pharmaceutical activity is further illustrated below by pharmacodynamic experiment.
Test example 1：Influences of the Apigenin to Rats Undergoing Unilateral Urethral Ligation kidney region fibrosis
1.1 material
Benazepil, Novartis Pharma AG's production；Biological public affairs are built up in hydroxyproline (HYP) kit, Nanjing
Department；Fibronectin (FN) kit is purchased from Shanghai institute of Biological Products.
Experimental animal：Regular grade Wistar rats, male, body weight 150-200g, Nanjing Medical University's Experimental Animal Center.
1.2 test methods and result
Rat 90, random point 9 groups, i.e. sham-operation group, model group, benazepil gavage 10mg/kg groups, Apigenin is quiet
Arteries and veins injection 2.5mg/kg groups, Apigenin intravenous injection 5mg/kg groups, Apigenin intravenous injection 25mg/kg groups, Apigenin
Gavage 5mg/kg groups, Apigenin gavage 10mg/kg groups, Apigenin gavage 50mg/kg groups, animal feeding 1 week, each rat with
After 10% chloraldurate 3.0mL/kg intraperitoneal injection of anesthesia, will rat right lateral position fix with operating table on, after cropping with the tincture of iodine,
75% alcohol disinfecting field of operation, row left side abdomen otch successively cut skin, muscle and each layer of stomach wall, exposure and to separate left side defeated
Urinary catheter, sham-operation group only cuts abdominal cavity and free left side ureter, but does not ligature and cut, other each group rat 4-0 silk threads
Twice are ligatured, the upper point of ligation together is horizontal positioned at left inferior pole of kidney, and then ligaturing point in twice cuts ureter, layer-by-layer suture, art
Each group animal is put to death after 10 days 10% chloral hydrate anesthesias afterwards, takes blood, explanation measure explanation fiber is determined by Fibronectin
Connexin (FN).Physiological saline leaves and takes left kidney after lavation repeatedly, and nephridial tissue is fixed through 4% paraformaldehyde buffer solution.
Appropriate nephridial tissue is cut, illustrates measure hydroxyproline by hydroxyproline kit measurement.
Routine pathology is checked and 1. visually observed：Sham-operation group kidney color is scarlet, shows smooth, coating gloss, without viscous
Even.Other each group Kidney Volumes increase, and color is pale, shows to be in granular form, and similar human body branny kidney, a few regions kidney peplos glue
Even.2. light microscopy checking：Sham-operation group nephron result is clear, and Bowman's capsule is without expansion or cell infiltration.Model control group is big
Piece renal tubular necrosis, renal interstitial fibroblast proliferation, tubular ectasia, inside there are a large amount of brown color shading materials or necrosis to come off
Epithelial cell, glomerulus number are reduced, and part glomerulus fibrosis simultaneously disappears with bowman's capsule wall adhesion, blister cavities.Each group is administered
Lesion is similar with model control group, but has different degrees of morphology to improve, and is shown especially with Apigenin gavage heavy dose each groups
Write, relatively have notable difference with model control group.
Influences of the Apigenin of table 1 to Rats Undergoing Unilateral Urethral Ligation kidney region fibrosis
*p<0.05, * * p<0.01, compared with model group
T inspections are carried out to each group FN, HYP.It the results are shown in Table 1, Apigenin intravenous injection 5mg/kg groups, Apigenin veins
Injecting 25mg/kg groups, Apigenin gavage 10mg/kg groups, Apigenin gavage 50mg/kg groups reduces FN, HYPP level (with mould
Type control group compares, P<0.05 or 0.01).
Conclusion：Apigenin can significantly reduce the horizontal rise of kidney region fibrosis FN, HYPP, suppress renal interstitial fiber
Change, can be used for preparing anti-kidney fibrosis medicine.
Claims (4)
- Applications of the 1.Apigenin in kidney fibrosis medicine is treated and prevented, the compound Apigenin structures such as formula (I) It is shown：
- 2. applications of the Apigenin as claimed in claim 1 in kidney fibrosis medicine is treated and prevented, it is characterised in that reduce Kidney region fibrosis hydroxyproline content.
- 3. one kind treats and prevents kidney fibrosis medicine, it is characterised in that the Apigenin as described in claim 1 is active component Addition auxiliary material is prepared, and preparation method adds 195 grams of dextrin, mixed, Conventional compression system to take 5 g of compound Apigenin Into 1000.
- 4. one kind treats and prevents kidney fibrosis medicine, it is characterised in that the Apigenin as described in claim 1 is active component Addition auxiliary material is prepared, and preparation method adds 195 grams of starch, mixing is encapsulated to be made to take 5 g of compound Apigenin 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610839602.5A CN107854461A (en) | 2016-09-22 | 2016-09-22 | Apigenin is preparing the application in treating and preventing kidney fibrosis medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610839602.5A CN107854461A (en) | 2016-09-22 | 2016-09-22 | Apigenin is preparing the application in treating and preventing kidney fibrosis medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107854461A true CN107854461A (en) | 2018-03-30 |
Family
ID=61698310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610839602.5A Pending CN107854461A (en) | 2016-09-22 | 2016-09-22 | Apigenin is preparing the application in treating and preventing kidney fibrosis medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107854461A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107628936A (en) * | 2017-09-30 | 2018-01-26 | 南京正宽医药科技有限公司 | The extracting method of vanillic aldehyde and its application |
| CN110237067A (en) * | 2018-03-07 | 2019-09-17 | 上海市计划生育科学研究所 | The application of apiolin and its derivative in the drug that preparation treats or prevents nephrosis |
-
2016
- 2016-09-22 CN CN201610839602.5A patent/CN107854461A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107628936A (en) * | 2017-09-30 | 2018-01-26 | 南京正宽医药科技有限公司 | The extracting method of vanillic aldehyde and its application |
| CN110237067A (en) * | 2018-03-07 | 2019-09-17 | 上海市计划生育科学研究所 | The application of apiolin and its derivative in the drug that preparation treats or prevents nephrosis |
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Legal Events
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| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180330 |