CN103393703B - The application of Houttuynoid B in preparation treatment myocardial ischemia drug - Google Patents
The application of Houttuynoid B in preparation treatment myocardial ischemia drug Download PDFInfo
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- CN103393703B CN103393703B CN201310255883.6A CN201310255883A CN103393703B CN 103393703 B CN103393703 B CN 103393703B CN 201310255883 A CN201310255883 A CN 201310255883A CN 103393703 B CN103393703 B CN 103393703B
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Abstract
Do you the invention provides Houttuynoid? the application of B in preparation treatment or prevention myocardial ischemia drug.The Houttuynoid that the present invention relates to? B 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 HouttuynoidB in preparation treatment or prevention myocardial ischemia drug.
Background technology
The present inventor is found by a large amount of experiments, and HouttuynoidB 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 H outtuynoidB that the present invention relates to is one and delivers (Chen in 2012, S.D.etal., 2012.HouttuynoidA-E, Anti-HerpesSimplexVirusActiveFlavonoidswithNovelSkeleton sfromHouttuyniacordata.OrganicLetters14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to the active Chen of anti-herpes simplex virus, S.D.etal., 2012.HouttuynoidA-E, Anti-HerpesSimplexVirusActiveFlavonoidswithNovelSkeleton sfromHouttuyniacordata.OrganicLetters14 (7), 1772 – 1775.), the HouttuynoidB 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 the application in the medicine of HouttuynoidB preparation treatment or prevention Ischemic/reperfusion.
The present inventor demonstrates by the experiment in detailed description of the invention the effect that HouttuynoidB has treatment or prevention myocardial ischemia drug disease.
Described compound H outtuynoidB structure is as shown in formula I:
The HouttuynoidB 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 H outtuynoidB involved in the present invention is see document (Chen, S.D.etal., 2012.HouttuynoidA-E, Anti-HerpesSimplexVirusActiveFlavonoidswithNovelSkeleton sfromHouttuyniacordata.OrganicLetters14 (7), 1772 – 1775.).
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 H outtuynoidB tablet involved in the present invention:
Get 20 g of compound HouttuynoidB, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound H outtuynoidB capsule involved in the present invention:
Get 20 g of compound HouttuynoidB, 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: HouttuynoidB 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 1HouttuynoidB is on the impact of scheming weight ratio under myocardial infarction and ligature
Compare with model comparison, * * p<0.01, * p<0.05
HouttuynoidB on the impact of the acute myocardial ischemia that pituitrin causes in table 2.
Table 2HouttuynoidB is on the impact of the acute myocardial ischemia that pituitrin causes
Compare with model comparison, * * p<0.01, * p<0.05
Conclusion: HouttuynoidBA can reduce the generation of myocardial infarction, and HouttuynoidB obviously can change the change of electrocardio degree, does not change heart rate.More than experiment can illustrate, HouttuynoidB can prevention and therapy myocardial ischemia.
Claims (1)
1.HouttuynoidB preparation treatment or prevention myocardial ischemia drug in application, described compound H outtuynoidB structure as
formula Ishown in:
formula I.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310255883.6A CN103393703B (en) | 2013-06-24 | 2013-06-24 | The application of Houttuynoid B in preparation treatment myocardial ischemia drug |
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| CN201310255883.6A CN103393703B (en) | 2013-06-24 | 2013-06-24 | The application of Houttuynoid B in preparation treatment myocardial ischemia drug |
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| CN103393703A CN103393703A (en) | 2013-11-20 |
| CN103393703B true CN103393703B (en) | 2016-02-24 |
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Non-Patent Citations (1)
| Title |
|---|
| Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata;Chen, S. D. et al.;《Organic Letters》;20121231;第14卷(第7期);第1772–1775页 * |
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Inventor after: Zhu Ping Inventor after: Li Xue Inventor after: Ding Hao Inventor after: Tian Weimao Inventor after: Shu Gang Inventor after: Zhao Mingyi Inventor after: Li Jiaxin Inventor after: Zhu Shuoji Inventor after: Huang Chengfeng Inventor after: Li Jiani Inventor after: Zhu Xiaolan Inventor after: Mohammed Aszyford Inventor after: Li Xiaokang Inventor before: Ding Shengyu |
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Effective date of registration: 20151125 Address after: 510080, room 27, No. 103, compound 91, Dongchuan Road, Yuexiu District, Guangdong, Guangzhou Applicant after: Zhu Ping Address before: 210009 Gulou District, Jiangsu, Nanjing Gu Ping Kong, No. 4 Applicant before: Ding Shengyu |
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Effective date of registration: 20151201 Address after: 510080 No. 96, Dongchuan Road, Guangzhou, Guangdong, Yuexiu District Applicant after: Guangdong Prov. Cardiovascular disease Inst. Applicant after: Guangdong General Hospital Address before: 510080, room 27, No. 103, compound 91, Dongchuan Road, Yuexiu District, Guangdong, Guangzhou Applicant before: Zhu Ping |
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