CN106344579A - Application of Fistulains A in drugs for myocardial ischemia treatment - Google Patents
Application of Fistulains A in drugs for myocardial ischemia treatment Download PDFInfo
- Publication number
- CN106344579A CN106344579A CN201610864843.5A CN201610864843A CN106344579A CN 106344579 A CN106344579 A CN 106344579A CN 201610864843 A CN201610864843 A CN 201610864843A CN 106344579 A CN106344579 A CN 106344579A
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- China
- Prior art keywords
- fistulains
- myocardial ischemia
- application
- compound
- drugs
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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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
Abstract
The invention provides application of Fistulains A in preparing drugs for myocardial ischemia treatment or prevention or re-infusion drugs, which belongs to first publication. Since a skeleton type belongs to a brand new skeleton type, and the Fistulains A has high efficiency on inhibiting the activity of myocardial ischemia, the probability of any inspiration given by other compounds does not exist, and the Fistulains A has a prominent substantial characteristic, and makes remarkable progress on anti-myocardial ischemia at the same time.
Description
Technical field
The present invention relates to the new application of compound fistulains a, more particularly, to fistulains a are in the preparation treatment heart
Application in myocardial ischemia medicine.
Background technology
The present inventor passes through substantial amounts of experiment and finds, fistulains a has the/pharmacology of reperfusion injury that resists myocardial ischemia
Effect, has prevention or the medical usage for the treatment of myocardial ischemia disease.
Compound fistulains a according to the present invention be one deliver within 2014 (min zhou, et al.,
fistulains a and b,new bischromones from the bark of cassia fistula,and their
Activities.org.lett.2015,17,2638-2641.) noval chemical compound, this compound has brand-new framework types,
Current purposes merely relates to treat rheumatic arthritis (min zhou, et al., fistulains a and b, new
bischromones from the bark of cassia fistula,and their
Activities.org.lett.2015,17,2638-2641.), fistulains a according to the present invention is controlled in preparation
The purposes treated in myocardial ischemia drug belongs to first public, and due to belonging to brand-new structure type, and it is for treatment cardiac muscle
Ischemia activity is unexpectedly strong, and there is not the possibility being provided any enlightenment by other compounds, possesses prominent substantive spy
Point, the preventing and treating being simultaneously used for myocardial ischemia obviously has and significantly improves.
Content of the invention
The invention provides the application in the medicine of fistulains a preparation treatment or prevention Ischemic/reperfusion.
The present inventor demonstrates fistulains a by the experiment in specific embodiment and has treatment or prevention cardiac muscle
The effect of ischemia drugs disease.
Shown in described compound fistulains a structure such as formula ():
Application in preparation treatment myocardial ischemia drug for the described fistulains a, fistulains a can reduce the heart
The generation of flesh infarction, fistulains a changes the change of electrocardio degree, does not change heart rate.
One kind treats myocardial ischemia drug, adds adjuvant by fistulains a for active component and is prepared from, preparation side
Method is to take 5 g of compound fistulains a, adds 195 grams of dextrin, mixes, and Conventional compression makes 1000.
One kind treats myocardial ischemia drug, adds adjuvant by fistulains a for active component and is prepared from, preparation side
Method is to take 5 g of compound fistulains a, adds 195 grams of starch, mixes, and encapsulated makes 1000.
Purposes in preparing medicaments for resisting myocardial ischemia for the fistulains a according to the present invention belongs to first public, due to
Framework types belong to brand-new framework types, and it is unexpectedly strong for the inhibitory activity of myocardial ischemia, do not exist by
Other compounds provide the possibility of any enlightenment, possess prominent substantive distinguishing features, and being simultaneously used for resisting myocardial ischemia obviously has
Significantly improve.
Specific embodiment
The preparation method of compound fistulains a involved in the present invention referring to document (min zhou, et al.,
fistulains a and b,new bischromones from the bark of cassia fistula,and their
activities.org.lett.2015,17,2638-2641.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to concrete reality
Apply any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound fistulains a tablet involved in the present invention:
Take 5 g of compound fistulains a additions to prepare 95 grams of the customary adjuvant of tablet, mix, conventional tablet presses are made
1000.
Embodiment 2: the preparation of compound fistulains a capsule involved in the present invention:
Take 5 g of compound fistulains a additions to prepare customary adjuvant such as 195 grams of the starch of capsule, mix, fill glue
Capsule makes 1000.
To further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The impact to myocardial ischemia/reperfusion injury in rats for the experimental example 1:fistulains a
(1) experiment material: sd rat, male and female dual-purpose, body weight 190～210g.
(2) method and result
1) experimental technique: the acute myocardial ischemia experiment of pituitrin induction: rat is randomly divided into 5 groups: positive right
According to group, negative control group, 3 groups of administration group, every group 8.Administration group gastric infusion, two matched groups give the steaming of consubstantiality accumulated amount daily
Distilled water gavage, each group continuous gavage 7d.1.5～2.0h lumbar injection pentobarbital sodium 30mg/kg fiber crops all after the 7th day gavage
Liquor-saturated, record standard lead electrocardiogram is continued using ms2302 multimedia biological signal collecting analysis system.Experimental group, the positive are right
(complete in 5s, positive controls 10min abdomen before injection of pituitrin according to group sublingual vein injection of pituitrin 5iu/kg
Nitroglycerin 5mg/kg is injected in chamber) the continuous record Electrocardiographic change of 15min after 10min.If one below occurs in electrocardiogram
Change: t ripple is low flat, two-way, is inverted, and st section level moves down >=0.05mv, gives to remember 1 point.The finally total score to every rat
It is analyzed, such as reduces after medication score, point out myocardial ischemia to have improvement.With changes in heart rate percentage before and after injection of pituitrin
Rate represents the impact to heart rate for the medicine.
Myocardium ischemia resisting reperfusion injury experiment: rat is randomly divided into 5 groups: positive controls, negative control group, administration
Organize 3 groups, every group 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount, each continuous gavage daily
7d.Standard ecg leads are recorded after rats by intraperitoneal injection pentobarbital sodium 30mg/kg anesthesia.Tracheal intubation, connects and manually exhales
Suction machine (1.0ml g-1 min-1), opens thoracic cavity in the 4th～5 intercostal, exposes heart, in pulmonary conus left border, left auricle
Ramus descendens anterior arteriae coronariae sinistrae (positive controls 3min sublingual vein before following coronary artery occlusion is ligatured with 320 silk threads at lower edge 1mm
Injection Propranolol 1.0mg/kg).After ligation 30min, cut off ligature, fill 30min again.Quickly remove heart, use 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 with water immediately after dyeing
Unnecessary dyestuff on flesh piece.Cut off the non-infarcted region cardiac muscle that each cardiac muscle piece is colored, undyed infarcted myocardium and the ischemia 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 matched groups give the distilled water gavage of consubstantiality accumulated amount, each group continuous gavage 5d daily.The
Lumbar injection urethane 10mg/kg anesthesia in 6 days.Record standard lead electrocardiogram.Longitudinally slit right skin of neck, separates right neck
Total tremulous pulse, insertion has been filled with the left ventricular catheter of heparin 0.9% sodium chloride, conduit is slowly inserted left ventricular cavity.Cut left lower extremity
Inside skin, separates femoral artery, inserts ductus arteriosuss.Cut-in pressure transducer, transports to multimedia bio signal record signal
Instrument is observed.After balance 30min, each hemodynamic index before record administration.All data are all represented with x ± s, experimental group
Checked with the sided t of two sample averages with matched group data analysiss.
2) result: ischemia/reperfusion injury test result indicate that, administration group, positive controls, negative control group cardiac muscle stalk
Under dead and ligature, myocardial Mass Measured percentage ratio is shown in Table 1 respectively.
The impact to myocardial infarction and scheming weight ratio under ligature for the table 1 fistulains a
Compare with negative control group, * * p < 0.01, * p < 0.05
The impact of the acute myocardial ischemia that fistulains a causes to pituitrin is shown in Table 2.
The impact of the acute myocardial ischemia that table 2 fistulains a causes to pituitrin
Compare with negative control group, * * p < 0.01, * p < 0.05
Conclusion: fistulains a can reduce the generation of myocardial infarction, fistulains a can substantially change electrocardio
The change of degree, does not change heart rate.Above experiment can illustrate, fistulains a can treat myocardial ischemia/perfusion.
Claims (4)
- Application in treatment myocardial ischemia drug for the 1.fistulains a, described compound fistulains a structure such as formula Shown in ():
- 2. fistulains a as claimed in claim 1 treatment myocardial ischemia drug in application it is characterised in that Fistulains a can reduce the generation of myocardial infarction, and fistulains a changes the change of electrocardio degree, does not change heart rate.
- 3. one kind treats myocardial ischemia drug it is characterised in that being added for active component by fistulains a described in claim 1 Plus adjuvant is prepared from, preparation method is to take 5 g of compound fistulains a, adds 195 grams of dextrin, mixes, Conventional compression Make 1000.
- 4. one kind treats myocardial ischemia drug it is characterised in that being added for active component by fistulains a described in claim 1 Plus adjuvant is prepared from, preparation method is to take 5 g of compound fistulains a, adds 195 grams of starch, mixes, encapsulated system Become 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610864843.5A CN106344579A (en) | 2016-09-29 | 2016-09-29 | Application of Fistulains A in drugs for myocardial ischemia treatment |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610864843.5A CN106344579A (en) | 2016-09-29 | 2016-09-29 | Application of Fistulains A in drugs for myocardial ischemia treatment |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106344579A true CN106344579A (en) | 2017-01-25 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610864843.5A Pending CN106344579A (en) | 2016-09-29 | 2016-09-29 | Application of Fistulains A in drugs for myocardial ischemia treatment |
Country Status (1)
| Country | Link |
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| CN (1) | CN106344579A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107722081A (en) * | 2017-11-07 | 2018-02-23 | 全椒先奇医药科技有限公司 | One kind treats myocardial ischemia drug composition and its application |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105294720A (en) * | 2015-05-08 | 2016-02-03 | 云南民族大学 | Dimerization chromone alkaloid compound as well as preparation method and application thereof |
-
2016
- 2016-09-29 CN CN201610864843.5A patent/CN106344579A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105294720A (en) * | 2015-05-08 | 2016-02-03 | 云南民族大学 | Dimerization chromone alkaloid compound as well as preparation method and application thereof |
Non-Patent Citations (2)
| Title |
|---|
| MIN ZHOU, ET AL.: "Fistulains A and B, New Bischromones from the Bark of Cassia fistula, and Their Activities", 《ORG. LETT.》 * |
| 明磊等,: "抗心肌缺血中药有效成分研究进展", 《人参研究》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107722081A (en) * | 2017-11-07 | 2018-02-23 | 全椒先奇医药科技有限公司 | One kind treats myocardial ischemia drug composition and its application |
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Application publication date: 20170125 |