CN106309437A - Application of Ternatusine A in preparation of medicaments for treating myocardial ischemia - Google Patents
Application of Ternatusine A in preparation of medicaments for treating myocardial ischemia Download PDFInfo
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- CN106309437A CN106309437A CN201610818547.1A CN201610818547A CN106309437A CN 106309437 A CN106309437 A CN 106309437A CN 201610818547 A CN201610818547 A CN 201610818547A CN 106309437 A CN106309437 A CN 106309437A
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- Prior art keywords
- ternatusine
- myocardial ischemia
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- medicaments
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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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 application of Ternatusine A in the preparation of medicaments for the treatment or prevention of myocardial ischemia/reperfusion. The application of Ternatusine A in the preparation of anti-myocardial ischemic drugs according to the present invention is first disclosed. The skeletal type is brand-new, the inhibitory activity against myocardial ischemia is surprising, and there is no enlightenment given by other compounds, so that the application has outstanding substantive characteristics, and has made great improvement for anti-myocardial ischemia.
Description
Technical field
The present invention relates to the new application of compound Ternatusine A, particularly relate to Ternatusine A in preparation treatment
Application in myocardial ischemia drug.
Background technology
The present inventor is found by substantial amounts of experiment, and Ternatusine 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.
The compound Ternatusine A that the present invention relates to be one within 2013, deliver (Zhi lai Zhan, et al.,
Ternatusine A,a New Pyrrole Derivative with an Epoxyoxepino Ring from
Ranunculus ternatus.ORGANIC LETTERS, 2013,15 (8): 1,970 1973.) noval chemical compound, this compound
Having brand-new framework types, current purposes merely relates to antibacterial (Zhi lai Zhan, et al., Ternatusine A, a
New Pyrrole Derivative with an Epoxyoxepino Ring from Ranunculus
Ternatus.ORGANIC LETTERS, 2013,15 (8): 1,970 1973.), for the Ternatusine A that the present invention relates to
Purposes in preparation treatment myocardial ischemia drug belongs to first public, owing to belonging to brand-new structure type, and its for
Treatment myocardial ischemia activity is unexpectedly strong, and there is not the possibility being provided any enlightenment by other compounds, possesses prominent
Substantive distinguishing features, the preventing and treating being simultaneously used for myocardial ischemia obviously has the most progressive.
Summary of the invention
The invention provides the application in the medicine of Ternatusine A preparation treatment or prevention Ischemic/reperfusion.
The present inventor demonstrates Ternatusine A by the experiment in detailed description of the invention and has treatment or prevention cardiac muscle
The effect of ischemia drugs disease.
Described compound Ternatusine A structure is as shown in formula I:
The Ternatusine A that the present invention relates to purposes in preparing medicaments for resisting myocardial ischemia belongs to first public, by
Belong to brand-new framework types in framework types, and it is unexpectedly strong for the inhibitory activity of myocardial ischemia, does not exists
Being provided the possibility of any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for resisting myocardial ischemia obviously tool
Have the most progressive.
Detailed description of the invention
The preparation method of compound Ternatusine A involved in the present invention see document (Zhilai Zhan, et al.,
Ternatusine A,a New Pyrrole Derivative with an Epoxyoxepino Ring from
Ranunculus ternatus.ORGANIC LETTERS,2013,15(8):1970–1973.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Execute any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound Ternatusine A tablet involved in the present invention:
Take 20 g of compound Ternatusine A additions and prepare the customary adjuvant 180 grams of tablet, mixing, conventional tablet presses
Make 1000.
Embodiment 2: the preparation of compound Ternatusine A capsule involved in the present invention:
Take 20 g of compound Ternatusine A additions and prepare the customary adjuvant such as starch 180 grams of capsule, mixing, dress
Capsule makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: the Ternatusine A impact on myocardial ischemia/reperfusion injury in rats
(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 controls, negative right
According to group, administration group 3 groups, often group 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount every day, respectively
Organize continuous gavage 7d.All 1.5～2.0h lumbar injection pentobarbital sodium 30mg/kg anesthesia after the 7th day gavage, uses MS2302
Multimedia biological signal collecting analyzes systems stay record standard II lead electrocardiogram.Experimental group, positive controls sublingual vein
(completing in 5s, positive controls 10min lumbar injection nitric acid before injection of pituitrin is sweet for injection of pituitrin 5IU/kg
Oil 5mg/kg) the record Electrocardiographic change of 15min continuously after 10min.If electrocardiogram occurring the change of one below: T ripple is low
Flat, two-way, it to be inverted, ST section level moves down >=0.05mV, remembers 1 point.Finally the total score of every rat is analyzed, as with
Reducing after medicine score, prompting myocardial ischemia has improvement.Medicine pair is represented with changes in heart rate percentage rate before and after injection of pituitrin
The impact of heart rate.
Cardiac muscle ischemia resisting reperfusion injury experiment: rat is randomly divided into 5 groups: positive controls, negative control group, it is administered
Organize 3 groups, often group 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount, each continuous gavage every day
7d.Record standard II lead electrocardiogram 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 at the 4th～5 intercostals, exposes heart, at pulmonary conus left border, left auricle
At lower edge 1mm, with 320 silk thread ligation ramus descendens anterior arteriae coronariae sinistraes, (positive controls is 3min sublingual vein before following coronary artery occlusion
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.Cardiac muscle sheet is placed in the TTC solution of 1%, hatches 5min in 37 DEG C.The heart is washed with water immediately after dyeing
Dyestuff unnecessary on flesh sheet.Cut off the non-infarcted region cardiac muscle that each cardiac muscle sheet is colored, undyed infarcted myocardium and the ischemia heart
Flesh is weighed.
Hemodynamics is tested: rat is randomly divided into 5 groups: positive controls, negative control group, administration group 3 groups,
Often group 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount every day, continuous gavage 5d of each group.The
Lumbar injection urethane 10mg/kg anesthesia in 6 days.Record standard II lead electrocardiogram.Longitudinally slit right skin of neck, separates right neck
Total tremulous pulse, inserts the left ventricular catheter having been filled with heparin 0.9% sodium chloride, conduit slowly inserts left ventricular cavity.Cut left lower extremity
Inside skin, separates femoral artery, inserts ductus arteriosus.Cut-in pressure transducer, transports to multimedia bio signal record signal
Instrument is observed.After balance 30min, record is administered front each hemodynamic index.All data all represent with x ± s, experimental group
Check with the matched group data analysis sided t of two sample averages.
2) result
Ischemia/reperfusion injury test result indicate that, administration group, positive controls, negative control group myocardial infarction and knot
Under binding, myocardial Mass Measured percentage ratio is shown in Table 1 respectively.
Table 1 Ternatusine A is on myocardial infarction and the impact of scheming weight ratio under ligature
Compare with negative control group, * * p < 0.01, * p < 0.05
The impact of the acute myocardial ischemia that pituitrin is caused by Ternatusine A is shown in Table 2.
The impact of the acute myocardial ischemia that pituitrin is caused by table 2 Ternatusine A
Compare with negative control group, * * p < 0.01, * p < 0.05
Conclusion: Ternatusine A can reduce the generation of myocardial infarction, Ternatusine A can substantially change the heart
The change of electric degree, does not change heart rate.More than experiment can illustrate, Ternatusine A can treat myocardial ischemia/perfusion.
Claims (1)
1.Ternatusine A application in treatment myocardial ischemia drug, described compound Ternatusine A structure such as formula
(I) shown in:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610818547.1A CN106309437A (en) | 2016-09-12 | 2016-09-12 | Application of Ternatusine A in preparation of medicaments for treating myocardial ischemia |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610818547.1A CN106309437A (en) | 2016-09-12 | 2016-09-12 | Application of Ternatusine A in preparation of medicaments for treating myocardial ischemia |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106309437A true CN106309437A (en) | 2017-01-11 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610818547.1A Pending CN106309437A (en) | 2016-09-12 | 2016-09-12 | Application of Ternatusine A in preparation of medicaments for treating myocardial ischemia |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106309437A (en) |
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2016
- 2016-09-12 CN CN201610818547.1A patent/CN106309437A/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: 20170111 |