CN103479620A - Application of Neonectrolide A to in preparation of medicament for treating myocardial ischemia - Google Patents
Application of Neonectrolide A to in preparation of medicament for treating myocardial ischemia Download PDFInfo
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- CN103479620A CN103479620A CN201310478936.0A CN201310478936A CN103479620A CN 103479620 A CN103479620 A CN 103479620A CN 201310478936 A CN201310478936 A CN 201310478936A CN 103479620 A CN103479620 A CN 103479620A
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- neonectrolide
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Abstract
The invention provides an application of Neonectrolide A to in preparation of a medicament for treating or preventing myocardial ischemia/reperfusion. The application in the invention belongs to a first disclosure. The Neonectrolide A belongs to a brand new matrix type, and has high inhibitory activity on myocardial ischemia and the characteristic of outstanding substantiality; meanwhile, the Neonectrolide A is a significant progress in the resistance of myocardial ischemia.
Description
Technical field
The present invention relates to the new purposes of compound N eonectrolide A, relate in particular to the application of Neonectrolide A in preparation treatment myocardial ischemia drug.
Background technology
The inventor is by a large amount of experiment discoveries, and Neonectrolide A has the pharmacological action of resist myocardial ischemia/reperfusion injury, has the medical usage of prevention or treatment myocardial ischemia disease.
The compound N eonectrolide A the present invention relates to is one and within 2012, delivers (Jinwei Ren, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012, 14(24) 6226 – 6229.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to and suppresses part tumor cell proliferation (Jinwei Ren, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012, 14(24) 6226 – 6229.), the purposes of the Neonectrolide A the present invention relates in preparation treatment myocardial ischemia drug belongs to open first.
Summary of the invention
The invention provides the application in the medicine of Neonectrolide A preparation treatment or prevention Ischemic/reperfusion.
The inventor has the effect for the treatment of or prevention myocardial ischemia drug disease by the Neonectrolide A that experimental results show that in the specific embodiment.
Described compound N eonectrolide A structure is as shown in formula I:
It is open first that the purposes of Neonectrolide A in preparing medicaments for resisting myocardial ischemia the present invention relates to belongs to, because framework types belongs to brand-new framework types, and its inhibition for myocardial ischemia is active strong, possess outstanding substantive distinguishing features, obviously there is significant progress simultaneously for resisting myocardial ischemia.
The specific embodiment
The preparation method of compound N eonectrolide A involved in the present invention is referring to document (Jinwei Ren, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012,14(24) 6226 – 6229.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound N eonectrolide A tablet involved in the present invention:
Get 5 and digest compound Neonectrolide A and add dextrin 195 grams, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound N eonectrolide A capsule involved in the present invention:
Get 5 and digest compound Neonectrolide A and add starch 195 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The impact of experimental example 1:Neonectrolide A on 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 that pituitrin is induced: rat is divided into to 5 groups at random: positive controls, negative control group, 3 groups of administration groups, 8 every group.Administration group gastric infusion, two matched groups give the distilled water gavage of same volume every day, and each organizes continuous gavage 7d.All 1.5～2.0h lumbar injection pentobarbital sodium 30mg/kg anesthesia after the 7th day gavage, adopt MS2302 multimedia biological signal collecting analytical system to continue record standard II lead electrocardiogram.In experimental group, positive controls sublingual vein injection of pituitrin 5IU/kg(5s, complete, positive controls is 10min lumbar injection nitroglycerin 5mg/kg before injection of pituitrin) the Electrocardiographic variation of continuous record 15min after 10min.If occur one of following variation in electrocardiogram: the T ripple is low flat, two-way, is inverted, and move down >=0.05mV of ST section level, remember 1 minute.Finally the total points of every rat is analyzed, as reduced after the medication score, the prompting myocardial ischemia is improved.Mean the impact of medicine on heart rate with changes in heart rate percentage rate before and after injection of pituitrin.
Cardiac muscle ischemia resisting reperfusion injury experiment: rat is divided into to 5 groups at random: positive controls, negative control group, 3 groups of administration groups, 8 every group.Administration group gastric infusion, two matched groups give the distilled water gavage of same volume every day, each continuous gavage 7d.Record standard II lead electrocardiogram after rats by intraperitoneal injection pentobarbital sodium 30mg/kg anesthesia.Tracheal intubation, connect artificial respirator (1.0mlg-1min-1), open thoracic cavity at 4th～5 intercostals, expose heart, at the pulmonary conus left border, 320 silk thread ligation ramus descendens anterior arteriae coronariae sinistraes for left auricle lower edge 1mm place (positive controls is 3min sublingual vein injection Propranolol 1.0mg/kg before following coronary artery occlusion).After ligation 30min, cut off ligature, fill with again 30min.Take out fast heart, rinse well with 0.9% sodium chloride.Myocardium sheet is placed in 1% TTC solution, in 37 ℃ of hatching 5min.After dyeing, dyestuff unnecessary on myocardium sheet is removed in water flushing immediately.Cut off the non-infarcted region cardiac muscle that each myocardium sheet is colored, undyed infarcted myocardium and ischemic myocardium are weighed.
Hemodynamics experiment: rat is divided into to 5 groups at random: positive controls, negative control group, 3 groups of administration groups, 8 every group.Administration group gastric infusion, two matched groups give the distilled water gavage of same volume every day, and each organizes continuous gavage 5d.Lumbar injection urethane 10mg/kg anesthesia in the 6th day.Record standard II lead electrocardiogram.Vertically cut right skin of neck, separate right common carotid artery, insert the left ventricular catheter that has been full of heparin 0.9% sodium chloride, conduit is slowly inserted to left ventricular cavity.Cut the left lower extremity inside skin, separate femoral artery, insert ductus arteriosus.The cut-in pressure transducer, transport to multimedia bio signal monitor to signal and observed.After balance 30min, record front each hemodynamic index of administration.All data all mean with x ± s, the sided t check of two sample means for experimental group and matched group data analysis.
2) result
The 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.
The impact of table 1Neonectrolide A on scheming weight ratio under myocardial infarction and ligature
With negative control group, compare,
*p<0.01,
*p<0.05
The impact of the acute myocardial ischemia that Neonectrolide A causes pituitrin is in Table 2.
The impact of the acute myocardial ischemia that table 2Neonectrolide A causes pituitrin
With negative control group, compare,
*p<0.01,
*p<0.05
Conclusion: Neonectrolide A can reduce the generation of myocardial infarction, and Neonectrolide A can obviously change the variation of electrocardio degree, does not change heart rate.Above experiment can illustrate, Neonectrolide A can treat myocardial ischemia/perfusion.
Claims (1)
1.Neonectrolide the application of A in preparation treatment myocardial ischemia drug, described compound N eonectrolide A structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310478936.0A CN103479620A (en) | 2013-10-14 | 2013-10-14 | Application of Neonectrolide A to in preparation of medicament for treating myocardial ischemia |
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| CN201310478936.0A CN103479620A (en) | 2013-10-14 | 2013-10-14 | Application of Neonectrolide A to in preparation of medicament for treating myocardial ischemia |
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| CN103479620A true CN103479620A (en) | 2014-01-01 |
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| CN201310478936.0A Pending CN103479620A (en) | 2013-10-14 | 2013-10-14 | Application of Neonectrolide A to in preparation of medicament for treating myocardial ischemia |
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Application publication date: 20140101 |