CN103638012B - Application of Myrtucommuacetalone in medicine for treatment of myocardial ischemia - Google Patents
Application of Myrtucommuacetalone in medicine for treatment of myocardial ischemia Download PDFInfo
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- CN103638012B CN103638012B CN201310645723.2A CN201310645723A CN103638012B CN 103638012 B CN103638012 B CN 103638012B CN 201310645723 A CN201310645723 A CN 201310645723A CN 103638012 B CN103638012 B CN 103638012B
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- myrtucommuacetalone
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Abstract
The invention provides application of Myrtucommuacetalone in medicine for treatment or prevention of myocardial ischemia/reperfusion, which is disclosed for the first time; as the skeleton type belongs to a brand new skeleton type, and the myocardial ischemia treatment activity is high, the Myrtucommuacetalone has outstanding substantive features and has an obvious progress in the resisting of myocardial ischemia.
Description
Technical field
The present invention relates to the novelty teabag of compound Myrtucommuacetalone, particularly relate to the application of Myrtucommuacetalone in preparation treatment myocardial ischemia drug.
Background technology
The present inventor is found by a large amount of experiments, and Myrtucommuacetalone 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 Myrtucommuacetalone that the present invention relates to is one and delivers (M.Iqbal Choudhary in 2013, et al., New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis.Organic Letters, 2013, 15 (8): 862 – 1865.) noval chemical compound, this compound has brand-new framework types, current purposes finds that it can suppress NO to discharge (M.Iqbal Choudhary, et al., New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis.Organic Letters, 2013, 15 (8): 862 – 1865.), the purposes of the Myrtucommuacetalone that the present invention relates in preparation treatment myocardial ischemia drug belongs to first public.
Summary of the invention
The invention provides the application in the medicine of Myrtucommuacetalone preparation treatment or prevention Ischemic/reperfusion.
The present inventor demonstrates by the experiment in detailed description of the invention the effect that Myrtucommuacetalone has treatment or prevention myocardial ischemia drug disease.
Described compound Myrtucommuacetalone structure is as shown in formula I:
The Myrtucommuacetalone 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 strong, possessing outstanding substantive distinguishing features, for resisting myocardial ischemia, obviously there is significant progress simultaneously.
Detailed description of the invention
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.
The preparation method of compound Myrtucommuacetalone involved in the present invention is see document (M.Iqbal Choudhary, et al., New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis.Organic Letters, 2013,15 (8): 862 – 1865.), prepare compound Myrtucommuacetalone according to the method described above.
Embodiment 1: the preparation of compound Myrtucommuacetalone tablet involved in the present invention:
Get 5 g of compound Myrtucommuacetalone and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound Myrtucommuacetalone capsule involved in the present invention:
Get 5 g of compound Myrtucommuacetalone and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1:Myrtucommuacetalone 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, Nanjing Medical University's Experimental Animal Center.
(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.Complete in experimental group, positive controls sublingual vein injection of pituitrin 5IU/kg(5s, positive controls is 10min lumbar injection nitroglycerin 5mg/kg before injection of pituitrin) the Electrocardiographic change of record 15min continuously after 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 1Myrtucommuacetalone is on the impact of scheming weight ratio under myocardial infarction and ligature
Compare with negative control group, * * p<0.01, * p<0.05
Myrtucommuacetalone on the impact of the acute myocardial ischemia that pituitrin causes in table 2.
Table 2Myrtucommuacetalone is on the impact of the acute myocardial ischemia that pituitrin causes
Compare with negative control group, * * p<0.01, * p<0.05
Conclusion: Myrtucommuacetalone can reduce the generation of myocardial infarction, and Myrtucommuacetalone obviously can change the change of electrocardio degree, does not change heart rate.More than experiment can illustrate, Myrtucommuacetalone can treat myocardial ischemia/perfusion.
Claims (1)
- The application of 1.Myrtucommuacetalone in preparation treatment myocardial ischemia drug, described compound Myrtucommuacetalone structure is as shown in formula I:
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310645723.2A CN103638012B (en) | 2013-12-04 | 2013-12-04 | Application of Myrtucommuacetalone in medicine for treatment of myocardial ischemia |
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| CN201310645723.2A CN103638012B (en) | 2013-12-04 | 2013-12-04 | Application of Myrtucommuacetalone in medicine for treatment of myocardial ischemia |
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| CN103638012A CN103638012A (en) | 2014-03-19 |
| CN103638012B true CN103638012B (en) | 2015-05-20 |
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| CN107417697B (en) * | 2016-05-23 | 2019-07-19 | 暨南大学 | A kind of phloroglucin derivative and its application in preparation antibacterials |
| CN107501287B (en) * | 2017-08-22 | 2019-09-13 | 中国科学院华南植物园 | The preparation method of Myrtuco mmulone J and Myrtucommuacetalone and the like |
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Non-Patent Citations (2)
| Title |
|---|
| New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis;M. Iqbal Choudhary et al.;《Organic Letters》;20130403;第15卷(第8期);1862-1865 * |
| 氧化还原信号在心肌缺血再灌注损伤中保护作用机制的研究进展;陈德等;《中国循环杂志》;20131130;第28卷(第7期);545-548 * |
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