CN105412073A - Application of Spirooliganone B in preparation of myocardial ischemia treatment drug - Google Patents
Application of Spirooliganone B in preparation of myocardial ischemia treatment drug Download PDFInfo
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- CN105412073A CN105412073A CN201510939327.XA CN201510939327A CN105412073A CN 105412073 A CN105412073 A CN 105412073A CN 201510939327 A CN201510939327 A CN 201510939327A CN 105412073 A CN105412073 A CN 105412073A
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- myocardial ischemia
- spirooliganoneb
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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
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- 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
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- 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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- General Health & Medical Sciences (AREA)
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Abstract
The invention provides an application of Spirooliganone B in preparation of a myocardial ischemia/reperfusion treatment or prevention drug. The application of the Spirooliganone B in preparation of the myocardial ischemia resistant drug is disclosed for the first time, due to the fact that a skeleton type is brand new, further, the activity of the Spirooliganone B for inhibiting myocardial ischemia is unexpectedly high, the probability of any revelation provided by other compounds does not exist, and the Spirooliganone B has the outstanding substantive features and has remarkable progress when applied to myocardial ischemia resistance.
Description
Technical field
The present invention relates to the novelty teabag of compound S pirooliganoneB, particularly relate to the application of SpirooliganoneB in preparation treatment myocardial ischemia drug.
Background technology
The present inventor is found by a large amount of experiments, and SpirooliganoneB has the/pharmacological action of reperfusion injury that resists myocardial ischemia, and has the medical usage of prevention or treatment myocardial ischemia disease.
The compound S pirooliganoneB that the present invention relates to is one and delivers (LinWei in 2014, etal., TotalSynthesesof (-)-SpirooliganonesAandB.Org.Lett.2014, 16, noval chemical compound 2784-2786.), this compound has brand-new framework types, current purposes only relates to treatment rheumatic arthritis (LinWei, etal., TotalSynthesesof (-)-SpirooliganonesAandB.Org.Lett.2014, 16, 2784-2786.), the purposes of the SpirooliganoneB that the present invention relates in preparation treatment myocardial ischemia drug is belonged to first public, owing to belonging to brand-new structure type, and it is active unexpectedly strong for treatment myocardial ischemia, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for myocardial ischemia obviously has significant progress.
Summary of the invention
The invention provides the application in the medicine of SpirooliganoneB preparation treatment or prevention Ischemic/reperfusion.
The present inventor demonstrates by the experiment in detailed description of the invention the effect that SpirooliganoneB has treatment or prevention myocardial ischemia drug disease.
Described compound S pirooliganoneB structure is as shown in formula I:
Formula I
The application of described SpirooliganoneB in preparation treatment myocardial ischemia drug, SpirooliganoneB can reduce the generation of myocardial infarction, and SpirooliganoneB changes the change of electrocardio degree, does not change heart rate.
One treats myocardial ischemia drug, and be that active component interpolation adjuvant is prepared from by SpirooliganoneB, preparation method, for getting 5 g of compound SpirooliganoneB, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
One treats myocardial ischemia drug, and be that active component adds adjuvant and is prepared from by SpirooliganoneB, preparation method, for getting 5 g of compound SpirooliganoneB, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
The SpirooliganoneB that the present invention relates to belongs to first public preparing the purposes in medicaments for resisting myocardial ischemia, because framework types belongs to brand-new framework types, and its inhibit activities for myocardial ischemia is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possessing outstanding substantive distinguishing features, for resisting myocardial ischemia, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of compound S pirooliganoneB involved in the present invention is see document (LinWei, etal., TotalSynthesesof (-)-SpirooliganonesAandB.Org.Lett.2014,16,2784-2786.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound S pirooliganoneB tablet involved in the present invention:
Get 5 g of compound SpirooliganoneB and add the customary adjuvant 95 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound S pirooliganoneB capsule involved in the present invention:
Get 5 g of compound SpirooliganoneB add prepare capsule customary adjuvant as starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: SpirooliganoneB is on the impact of 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 divided into 5 groups at random: positive controls, negative control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount every day, the continuous gavage 7d of each group.All after the 7th day gavage, 1.5 ~ 2.0h lumbar injection pentobarbital sodium 30mg/kg anaesthetizes, and adopts MS2302 multimedia biological signal collecting analytical system to continue record standard II lead electrocardiogram.The Electrocardiographic change of record 15min continuously after experimental group, positive controls sublingual vein injection of pituitrin 5IU/kg (complete in 5s, positive controls is 10min lumbar injection nitroglycerin 5mg/kg before injection of pituitrin) 10min.If there is one of following change in electrocardiogram: T ripple is low flat, two-way, and be inverted, ST section level moves down >=0.05mV, gives note 1 point.Finally analyze the total score of every rat, as reduced after medication score, prompting myocardial ischemia is improved.The impact of medicine on heart rate is represented with changes in heart rate percentage rate before and after injection of pituitrin.
Cardiac muscle ischemia resisting reperfusion injury experiment: rat is divided into 5 groups at random: positive controls, negative control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount every day, each continuous gavage 7d.Record standard II lead electrocardiogram after rats by intraperitoneal injection pentobarbital sodium 30mg/kg anaesthetizes.Tracheal intubation, connect artificial respirator (1.0mlg-1min-1), thoracic cavity is opened at 4th ~ 5 intercostals, expose heart, at pulmonary conus left border, left auricle lower edge 1mm place is with 320 silk thread ligation ramus descendens anterior arteriae coronariae sinistraes (positive controls is 3min sublingual vein injection Propranolol 1.0mg/kg before following coronary artery occlusion).After ligation 30min, cut off ligature, fill with 30min again.Quick taking-up heart, rinses well with 0.9% sodium chloride.Myocardium sheet is placed in the TTC solution of 1%, in 37 DEG C of hatching 5min.Rinse with water immediately after dyeing and remove dyestuff unnecessary on myocardium sheet.Cut off the non-infarcted region cardiac muscle that each myocardium sheet is colored, undyed infarcted myocardium and ischemic myocardium are weighed.
Hemodynamics is tested: rat is divided into 5 groups at random: positive controls, negative control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount every day, the continuous gavage 5d of each group.Within 6th day, lumbar injection urethane 10mg/kg anaesthetizes.Record standard II lead electrocardiogram.Longitudinally cut right skin of neck, be separated right common carotid artery, insert the left ventricular catheter being full of heparin 0.9% sodium chloride, conduit is slowly inserted left ventricular cavity.Cut left lower extremity inside skin, be separated femoral artery, insert ductus arteriosus.Cut-in pressure transducer, transports to multimedia bio signal monitor signal and observes.After balance 30min, each hemodynamic index before record administration.All data all represent with x ± s, and experimental group and the matched group data analysis sided t of two sample averages are checked.
2) result
Ischemia/reperfusion injury experimental result shows, under administration group, positive controls, negative control group myocardial infarction and ligature, myocardial Mass Measured percentage ratio is respectively in table 1.
Table 1SpirooliganoneB is on the impact of scheming weight ratio under myocardial infarction and ligature
Compare with negative control group, * * p<0.01, * p<0.05
SpirooliganoneB on the impact of the acute myocardial ischemia that pituitrin causes in table 2.
Table 2SpirooliganoneB is on the impact of the acute myocardial ischemia that pituitrin causes
Compare with negative control group, * * p<0.01, * p<0.05
Conclusion: SpirooliganoneB can reduce the generation of myocardial infarction, and SpirooliganoneB obviously can change the change of electrocardio degree, does not change heart rate.More than experiment can illustrate, SpirooliganoneB can treat myocardial ischemia/perfusion.
Claims (4)
- The application of 1.SpirooliganoneB in treatment myocardial ischemia drug, described compound S pirooliganoneB structure is as shown in formula I:Formula I.
- 2. the application of SpirooliganoneB in treatment myocardial ischemia drug as claimed in claim 1, it is characterized in that SpirooliganoneB can reduce the generation of myocardial infarction, SpirooliganoneB changes the change of electrocardio degree, does not change heart rate.
- 3. a treatment myocardial ischemia drug, it is characterized in that by SpirooliganoneB described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound SpirooliganoneB, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
- 4. a treatment myocardial ischemia drug, it is characterized in that by SpirooliganoneB described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound SpirooliganoneB, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510939327.XA CN105412073A (en) | 2015-12-16 | 2015-12-16 | Application of Spirooliganone B in preparation of myocardial ischemia treatment drug |
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| CN201510939327.XA CN105412073A (en) | 2015-12-16 | 2015-12-16 | Application of Spirooliganone B in preparation of myocardial ischemia treatment drug |
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| CN105412073A true CN105412073A (en) | 2016-03-23 |
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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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- 2015-12-16 CN CN201510939327.XA patent/CN105412073A/en active Pending
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: 20160323 |
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| WD01 | Invention patent application deemed withdrawn after publication |