CN103356595B - The application of Chukrasone B in preparation treatment myocardial ischemia drug - Google Patents
The application of Chukrasone B in preparation treatment myocardial ischemia drug Download PDFInfo
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- CN103356595B CN103356595B CN201310278111.4A CN201310278111A CN103356595B CN 103356595 B CN103356595 B CN 103356595B CN 201310278111 A CN201310278111 A CN 201310278111A CN 103356595 B CN103356595 B CN 103356595B
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- myocardial ischemia
- chukrasone
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Abstract
The invention provides the application of Chukrasone B in preparation treatment or prevention myocardial ischemia drug.The Chukrasone B 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.
Description
Technical field
The present invention relates to the application of Chukrasone B in preparation treatment or prevention myocardial ischemia drug.
Background technology
The present inventor is found by a large amount of experiments, and Chukrasone B 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 C hukrasone B that the present invention relates to is one and delivers (Liu in 2012, H.B.et al., 2012.Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with NewSkeletons from Chukrasia tabularis.Organic Letters 14 (17), 4438 – 4441.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to potassium-channel inhibit activities (Liu, H.B.et al., 2012.Chukrasones A and B:Potential Kv1.2 Potassium ChannelBlockers with New Skeletons from Chukrasia tabularis.Organic Letters 14 (17), 4438 – 4441.), the Chukrasone B that the present invention relates to is belonged 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, possesses outstanding substantive distinguishing features, for resisting myocardial ischemia, obviously there is significant progress simultaneously.
Summary of the invention
The invention provides Chukrasone B to prepare treatment or prevent the application in the medicine of Ischemic/reperfusion.
The present inventor demonstrates by the experiment in detailed description of the invention the effect that Chukrasone B has treatment or prevention myocardial ischemia drug disease.
Described Compound C hukrasone B structure is as shown in formula I:
The Chukrasone B 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 C hukrasone B involved in the present invention is see document (Cai, J.Y.et al., 2012.Chukrasone B, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixispolystachya.Organic Letters 14 (10), 2524 – 2527.).
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 C hukrasone B tablet involved in the present invention:
Get 20 g of compound Chukrasone B, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasone B capsule involved in the present invention:
Get 20 g of compound Chukrasone B, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: Chukrasone B 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 drug control group, model control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, positive drug control group and model control group 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 positive drug control group, model control group and administration group sublingual vein injection of pituitrin 5IU/kg (complete in 5s, positive drug control group 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 drug control group, model control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, positive drug control group and model control group give the distilled water gavage of consubstantiality accumulated amount every day, the continuous gavage 7d of each group.Record standard II lead electrocardiogram after rats by intraperitoneal injection pentobarbital sodium 30mg/kg anaesthetizes.Tracheal intubation, meets 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 drug control group 3min sublingual vein before following coronary artery occlusion injects Propranolol 1.0mg/kg).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 drug control group, model control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, positive drug control group and model control group 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.
So data all represent with x ± s, 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 drug control group, model control group myocardial infarction and ligature, myocardial Mass Measured percentage ratio is respectively in table 1.
Table 1 Chukrasone B is on the impact of scheming weight ratio under myocardial infarction and ligature
Compare with model comparison, * * p<0.01, * p<0.05
Chukrasone B on the impact of the acute myocardial ischemia that pituitrin causes in table 2.
Table 2 Chukrasone B is on the impact of the acute myocardial ischemia that pituitrin causes
Compare with model comparison, * * p<0.01, * p<0.05
Conclusion: Chukrasone B can reduce the generation of myocardial infarction, Chukrasone B obviously can change the change of electrocardio degree, does not change heart rate.More than experiment can illustrate, Chukrasone B can prevention and therapy myocardial ischemia.
Claims (1)
1.Chukrasone B preparation treatment or prevention myocardial ischemia drug in application, described Compound C hukrasone B structure as
formula Ishown in:
formula I.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310278111.4A CN103356595B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone B in preparation treatment myocardial ischemia drug |
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| CN201310278111.4A CN103356595B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone B in preparation treatment myocardial ischemia drug |
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| CN103356595A CN103356595A (en) | 2013-10-23 |
| CN103356595B true CN103356595B (en) | 2015-08-19 |
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Non-Patent Citations (1)
| Title |
|---|
| "Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletones from Chukrasia tabularis";hongbing liu et al.;《Organic Letters》;20121008;第14卷(第17期);4438-4441 * |
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