CN103381178A - Application of Houttuynoid D in drug for treatment of myocardial ischemia - Google Patents
Application of Houttuynoid D in drug for treatment of myocardial ischemia Download PDFInfo
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- CN103381178A CN103381178A CN 201310253870 CN201310253870A CN103381178A CN 103381178 A CN103381178 A CN 103381178A CN 201310253870 CN201310253870 CN 201310253870 CN 201310253870 A CN201310253870 A CN 201310253870A CN 103381178 A CN103381178 A CN 103381178A
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- houttuynoid
- myocardial ischemia
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Abstract
The invention provides an application of Houttuynoid D in preparing a drug for treatment or prevention of myocardial ischemia. The application of Houttuynoid D in preparing the anti-myocardial ischemia drug is disclosed for the first time. Because a skeleton type of Houttuynoid D belongs to a brand new skeleton type, Houttuynoid D has an unexpectedly high inhibition activity on myocardial ischemia, and the possibility that other compounds give any enlightenment does not exist, Houttuynoid D has prominent substantial characteristics and simultaneously obviously has significant progress in resisting myocardial ischemia.
Description
Technical field
The present invention relates to the application of Houttuynoid D in preparation treatment or prevention myocardial ischemia drug.
Background technology
The inventor finds by a large amount of experiment, and Houttuynoid D has and resists myocardial ischemia/pharmacological action of reperfusion injury, the medical usage with prevention or treatment myocardial ischemia disease.
the compound H outtuynoid D that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S. D. et al., 2012. Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), belong to open first for the purposes of the Houttuynoid D that the present invention relates in the preparation medicaments for resisting myocardial ischemia, because framework types belongs to brand-new framework types, and its inhibition for myocardial ischemia is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, be used for resisting myocardial ischemia simultaneously obviously have significant progress.
Summary of the invention
The invention provides the application in the medicine of Houttuynoid D preparation treatment or prevention Ischemic/reperfusion.
The inventor has the effect for the treatment of or prevention myocardial ischemia drug disease by the Houttuynoid D that experimental results show that in the specific embodiment.
Described compound H outtuynoid D structure is as shown in formula I:
Formula I
The purposes of the Houttuynoid D that the present invention relates in the preparation medicaments for resisting myocardial ischemia belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for myocardial ischemia is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for resisting myocardial ischemia simultaneously obviously have significant progress.
The specific embodiment
The preparation method of compound H outtuynoid D involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compound H outtuynoid D tablet involved in the present invention:
Get 20 and digest compound Houttuynoid D, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid D capsule involved in the present invention:
Get 20 and digest compound Houttuynoid D, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: the impact of Houttuynoid D 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 that pituitrin is induced: rat is divided into 5 groups at random: positive drug matched group, model control group, 3 groups of administration groups, 8 every group.Administration group gastric infusion, positive drug matched group and model control group give the distilled water gavage with volume every day, and each organizes continuous gavage 7d.All 1.5 ~ 2.0h lumbar injection pentobarbital sodium, 30 mg/kg anesthesia after the 7th day gavage adopt MS2302 multimedia biological signal collecting analytical system to continue record standard II lead electrocardiogram.Complete in positive drug matched group, model control group and administration group sublingual vein injection of pituitrin 5 IU/kg(5s, the positive drug matched group is 10 min lumbar injection nitroglycerin 5 mg/kg before injection of pituitrin) the continuous record 15 Electrocardiographic variations of min after 10 min.If occur one of following variation in electrocardiogram: the T ripple is low flat, two-way, is inverted, and ST section level moves down 〉=0.05 mV, remembers 1 minute.At last the total points of every rat is analyzed, as reducing after the medication score, the prompting myocardial ischemia is improved.Represent that with changes in heart rate percentage rate before and after injection of pituitrin medicine is on the impact of heart rate.
Cardiac muscle ischemia resisting reperfusion injury experiment: rat is divided into 5 groups at random: positive drug matched group, model control group, 3 groups of administration groups, 8 every group.Administration group gastric infusion, positive drug matched group and model control group give the distilled water gavage with volume every day, and each organizes continuous gavage 7d.Record standard II lead electrocardiogram after the 30 mg/kg anesthesia of rats by intraperitoneal injection pentobarbital sodium.Tracheal intubation meets artificial respirator (1.0 mlg
-1Min
-1), open the thoracic cavity at the 4th ~ 5 intercostal, expose heart, at the pulmonary conus left border, left auricle lower edge 1mm place is with 320 silk thread ligation ramus descendens anterior arteriae coronariae sinistraes (positive drug matched group 3 min sublingual veines before following coronary artery occlusion are injected Propranolol 1.0 mg/kg).After ligation 30 min, cut off ligature, fill with again 30 min.Take out fast heart, rinse well with 0.9% sodium chloride.Myocardium sheet is placed in 1% TTC solution, in 37 ℃ of hatching 5 min.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 5 groups at random: positive drug matched group, model control group, 3 groups of administration groups, 8 every group.Administration group gastric infusion, positive drug matched group and model control group give the distilled water gavage with volume every day, and each organizes continuous gavage 5d.Lumbar injection urethane 10 mg/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 left ventricular cavity.Cut the left lower extremity inside skin, separate femoral artery, insert ductus arteriosus.The cut-in pressure transducer is transported to multimedia bio signal monitor to signal and is observed.After balance 30 min, record front each hemodynamic index of administration.
So data all represent with x ± s, experimental group and matched group data analysis are with the sided t check of two sample means.
2) result
The ischemia/reperfusion injury experimental result shows, under administration group, positive drug matched group, model control group myocardial infarction and ligature, myocardial Mass Measured percentage ratio sees Table respectively 1.
The impact of table 1 Houttuynoid D on scheming weight ratio under myocardial infarction and ligature
Compare * * p<0.01, * p<0.05 with model
Houttuynoid D sees Table 2 to the impact of the acute myocardial ischemia that pituitrin causes.
The impact of the acute myocardial ischemia that table 2 Houttuynoid D causes pituitrin
Compare * * p<0.01, * p<0.05 with model
Conclusion: Houttuynoid D can reduce the generation of myocardial infarction, and Houttuynoid D can obviously change the variation of electrocardio degree, does not change heart rate.Above experiment can illustrate, Houttuynoid D can prevent and treat myocardial ischemia.
Claims (1)
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CN 201310253870 CN103381178A (en) | 2013-06-24 | 2013-06-24 | Application of Houttuynoid D in drug for treatment of myocardial ischemia |
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CN 201310253870 CN103381178A (en) | 2013-06-24 | 2013-06-24 | Application of Houttuynoid D in drug for treatment of myocardial ischemia |
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Application publication date: 20131106 |