CN107837263A - Apigenin is preparing the application in treating myocardial ischemia drug - Google Patents
Apigenin is preparing the application in treating myocardial ischemia drug Download PDFInfo
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- CN107837263A CN107837263A CN201610835074.6A CN201610835074A CN107837263A CN 107837263 A CN107837263 A CN 107837263A CN 201610835074 A CN201610835074 A CN 201610835074A CN 107837263 A CN107837263 A CN 107837263A
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- Prior art keywords
- apigenin
- myocardial ischemia
- compound
- prepared
- ischemia drug
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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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides applications of the Apigenin in treatment or prevention Ischemic/reperfusion medicine is prepared.Purposes of the Apigenin of the present invention in medicaments for resisting myocardial ischemia is prepared belongs to first public, because framework types belong to brand-new framework types, and it is unexpectedly strong for the inhibitory activity of myocardial ischemia, in the absence of the possibility that any enlightenment is provided by other compounds, possess prominent substantive distinguishing features, while there is significant progress for resisting myocardial ischemia obviously.
Description
Technical field
The present invention relates to compound Apigenin new application, more particularly to Apigenin to prepare treatment myocardial ischemia medicine
Application in thing.
Background technology
For the present inventor by largely testing discovery, Apigenin has the/pharmacological action of reperfusion injury that resists myocardial ischemia,
With the medical usage for preventing or treating myocardial ischemia disease.
Compound Apigenin of the present invention is one and delivers within 2014 (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, and current purposes merely relates to treat rheumatism joint
Inflammation (Ebenezer de Mello Cruz, et al., Leishmanicidal activity of Cecropia
pachystachya flavonoids:Arginase inhibition and altered mitochondrial DNA
Arrangement.Phytochemistry, 89 (2013) 71-77.), preparing treatment for Apigenin of the present invention
Purposes in myocardial ischemia drug belongs to first public, and due to belonging to brand-new structure type, and it is lacked for treatment cardiac muscle
Blood activity is unexpectedly strong, and in the absence of the possibility that any enlightenment is provided by other compounds, possesses prominent substantive distinguishing features,
The preventing and treating for myocardial ischemia obviously has significant progressive simultaneously.
The content of the invention
The application in the medicine for treating or preventing Ischemic/reperfusion is prepared the invention provides Apigenin.
The present inventor demonstrates Apigenin by the experiment in embodiment has treatment or prevention myocardial ischemia
The effect of medicine disease.
Shown in the compound Apigenin structures such as formula (I)：
Applications of the Apigenin in treatment myocardial ischemia drug is prepared, Apigenin can reduce myocardial infarction
Occur, Apigenin changes the change of electrocardio degree, does not change heart rate.
One kind treats myocardial ischemia drug, is that active component addition auxiliary material is prepared by Apigenin, preparation method is
5 g of compound Apigenin are taken, add 195 grams of dextrin, are mixed, Conventional compression is made 1000.
One kind treats myocardial ischemia drug, is that active component addition auxiliary material is prepared by Apigenin, preparation method is
5 g of compound Apigenin are taken, add 195 grams of starch, are mixed, it is encapsulated to be made 1000.
Purposes of the Apigenin of the present invention in medicaments for resisting myocardial ischemia is prepared belongs to first public, due to skeleton
Type belongs to brand-new framework types, and it is unexpectedly strong for the inhibitory activity of myocardial ischemia, in the absence of by other
Compound provides the possibility of any enlightenment, possesses prominent substantive distinguishing features, while have significantly for resisting myocardial ischemia obviously
Progress.
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 additions to prepare 95 grams of the customary adjuvant of tablet, mix, conventional tablet presses are made 1000
Piece.
Embodiment 2：The preparation of compound Apigenin capsules involved in the present invention：
Take 5 g of compound Apigenin additions to prepare customary adjuvant such as 195 grams of the starch of capsule, mix, encapsulated system
Into 1000.
Its pharmaceutical activity is further illustrated below by pharmacodynamic experiment.
Experimental example：Influences of the Apigenin to myocardial ischemia/reperfusion injury in rats
(1) experiment material：SD rats, male and female dual-purpose, 190~210g of body weight.
(2) method and result
1) experimental method
The acute myocardial ischemia experiment of pituitrin induction：Rat is randomly divided into 5 groups：Positive controls are negative right
According to group, 3 groups of administration group, every group 8.Administration group gastric infusion, two control groups give the distilled water gavage of androgynous accumulated amount daily, respectively
Group continuous gavage 7d.Yellow Jackets 30mg/kg anesthesia is injected intraperitoneally in 1.5~2.0h after the 7th day gavage, using MS2302
Multimedia biological signal collecting analysis system continues the lead electrocardiogram of record standard II.Experimental group, positive controls sublingual vein
Injection of pituitrin 5IU/kg (is completed, it is sweet that nitric acid is injected intraperitoneally in positive controls 10min before injection of pituitrin in 5s
Oily 5mg/kg) change of continuous record 15min electrocardiograms after 10min.If occurs the change of one below in electrocardiogram：T ripples are low
It is flat, it is two-way, it is inverted, ST section levels move down >=0.05mV, give 1 point of note.Finally the total score of every rat is analyzed, such as used
Reduced after medicine score, prompt myocardial ischemia to have improvement.Medicine pair is represented with changes in heart rate percentage before and after injection of pituitrin
The influence of heart rate.
The anti-ischemical reperfusion injury experiment of cardiac muscle：Rat is randomly divided into 5 groups：Positive controls, negative control group, administration
3 groups, every group 8 of group.Administration group gastric infusion, two control groups give the distilled water gavage of androgynous accumulated amount, each continuous gavage daily
7d.The lead electrocardiogram of record standard II after rats by intraperitoneal injection yellow Jackets 30mg/kg anesthesia.Trachea cannula, connect and manually exhale
Suction machine (1.0mlg-1min-1), thoracic cavity, exposure heart, in pulmonary conus left border, left auricle of heart are opened in the 4th~5 intercostal
At lower edge 1mm ramus descendens anterior arteriae coronariae sinistrae (positive controls 3min sublingual veins before following coronary artery occlusion are ligatured with 320 silk threads
Inject Propranolol 1.0mg/kg).After ligaturing 30min, ligature is cut, fills 30min again.Heart is quickly removed, with 0.9% chlorine
Change sodium to rinse well.Myocardium piece is placed in 1% TTC solution, hatches 5min in 37 DEG C.The heart is washed after dyeing with water immediately
Unnecessary dyestuff on flesh piece.The non-infarcted region cardiac muscle that each myocardium piece is colored is cut off, undyed infarcted myocardium and the ischemic heart
Flesh is weighed.
Hemodynamics are tested：Rat is randomly divided into 5 groups：Positive controls, negative control group, 3 groups of administration group,
Every group 8.Administration group gastric infusion, two control groups give the distilled water gavage of androgynous accumulated amount, each group continuous gavage 5d daily.The
Intraperitoneal injection urethane 10mg/kg anesthesia in 6 days.The lead electrocardiogram of record standard II.Longitudinally slit right skin of neck, separates right neck
Total artery, insertion have been filled with the left ventricular catheter of the sodium chloride of heparin 0.9%, conduit are slowly inserted into left ventricular cavity.Cut left lower extremity
Inside skin, femoral artery is separated, insert arterial duct.Cut-in pressure transducer, signal is transported to multimedia bio signal record
Instrument is observed.After balancing 30min, each hemodynamic index before record administration.All data represent with x ± s, experimental group
Examined with control group data analysis with the sided t of two sample averages.
2) result
Ischemia/reperfusion injury test result indicates that, administration group, positive controls, negative control group myocardial infarction with knot
Myocardial Mass Measured percentage is shown in Table 1 respectively under binding.
Table 1Apigenin to scheming weight under myocardial infarction and ligature than influence
Compared with negative control group, * * p<0.01, * p<0.05
Influences of the Apigenin to acute myocardial ischemia caused by pituitrin is shown in Table 2.
Influences of the table 2Apigenin to acute myocardial ischemia caused by pituitrin
Compared with negative control group, * * p<0.01, * p<0.05
Conclusion：Apigenin can reduce the generation of myocardial infarction, and Apigenin can substantially change the change of electrocardio degree,
Do not change heart rate.Experiment can illustrate that Apigenin can treat myocardial ischemia/perfusion above.
Claims (4)
- Applications of the 1.Apigenin in myocardial ischemia drug is treated, shown in the compound Apigenin structures such as formula (I)：
- 2. applications of the Apigenin as claimed in claim 1 in myocardial ischemia drug is treated, it is characterised in that Apigenin energy The generation of myocardial infarction is enough reduced, Apigenin changes the change of electrocardio degree, do not change heart rate.
- 3. one kind treats myocardial ischemia drug, it is characterised in that the Apigenin as described in claim 1 is that active component addition is auxiliary Material is prepared, and preparation method adds 195 grams of dextrin, mixed, Conventional compression is made 1000 to take 5 g of compound Apigenin Piece.
- 4. one kind treats myocardial ischemia drug, it is characterised in that the Apigenin as described in claim 1 is that active component addition is auxiliary Material is prepared, and preparation method adds 195 grams of starch, mixing is encapsulated to be made 1000 to take 5 g of compound Apigenin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610835074.6A CN107837263A (en) | 2016-09-19 | 2016-09-19 | Apigenin is preparing the application in treating myocardial ischemia drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610835074.6A CN107837263A (en) | 2016-09-19 | 2016-09-19 | Apigenin is preparing the application in treating myocardial ischemia drug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107837263A true CN107837263A (en) | 2018-03-27 |
Family
ID=61657362
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610835074.6A Pending CN107837263A (en) | 2016-09-19 | 2016-09-19 | Apigenin is preparing the application in treating myocardial ischemia drug |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107837263A (en) |
-
2016
- 2016-09-19 CN CN201610835074.6A patent/CN107837263A/en active Pending
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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: 20180327 |