CN102988351A - Application of Aphanamixoid A for preparing medicine for treating myocardial ischemia - Google Patents
Application of Aphanamixoid A for preparing medicine for treating myocardial ischemia Download PDFInfo
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- CN102988351A CN102988351A CN201210468890XA CN201210468890A CN102988351A CN 102988351 A CN102988351 A CN 102988351A CN 201210468890X A CN201210468890X A CN 201210468890XA CN 201210468890 A CN201210468890 A CN 201210468890A CN 102988351 A CN102988351 A CN 102988351A
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- aphanamixoid
- myocardial ischemia
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- medicine
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Abstract
The invention provides application of Aphanamixoid A for preparing a medicine for treating or preventing myocardial ischemia/reperfusion. The application of Aphanamixoid A for preparing the medicine for treating myocardial ischemia is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the myocardial ischemia inhibitory activity of Aphanamixoid A on ischemic brain injury is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Aphanamixoid A has outstanding substantive characteristics; and simultaneously, Aphanamixoid A has obvious progress for resisting myocardial ischemia.
Description
Technical field
The present invention relates to the application of Aphanamixoid A in preparation treatment or prevention myocardial ischemia drug.
Background technology
The inventor finds by a large amount of experiment, and Aphanamixoid A has and resists myocardial ischemia/pharmacological action of reperfusion injury the medical usage with prevention or treatment myocardial ischemia disease.
The compd A phanamixoid A that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to insect antifeedant activity (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Aphanamixoid A 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 chemical compounds, possess 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 Aphanamixoid A preparation treatment or prevention Ischemic/reperfusion.
The inventor has the effect for the treatment of or prevention myocardial ischemia drug disease by the Aphanamixoid A that experimental results show that in the specific embodiment.
Described compd A phanamixoid A structure is shown in formula I:
The purposes of the Aphanamixoid A 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 chemical compounds, possess outstanding substantive distinguishing features, be used for resisting myocardial ischemia simultaneously obviously have significant progress.
The specific embodiment
The preparation method of compd A phanamixoid A involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. 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 subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compd A phanamixoid A tablet involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A phanamixoid A capsule involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: Aphanamixoid A 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 that pituitrin is induced: rat is divided into 5 groups at random: positive drug matched group, model group, 3 administration groups, 8 every group.Administration group gastric infusion, positive drug matched group and model 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 adopts MS2302 multimedia biological signal collecting analytical system to continue record standard II lead electrocardiogram.Finish in positive drug matched group, model group and 3 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 Electrocardiographic variation of continuous record 15 min behind 10 min.If occur one of following variation in the 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 the 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 group, 3 administration groups, 8 every group.3 administration group gastric infusions, positive drug matched group and model group give the distilled water gavage with volume every day, and each organizes continuous gavage 7d.Record standard II lead electrocardiogram after the rats by intraperitoneal injection pentobarbital sodium 30 mg/kg anesthesia.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).Behind 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% the TTC solution, in 37 ℃ of hatching 5 min.Dyestuff unnecessary on the myocardium sheet is removed in immediately water flushing after the dyeing.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 group, 3 groups of administration groups, 8 every group.Administration group gastric infusion, two matched groups 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.Behind balance 30 min, each hemodynamic index before the record administration.
So data represent with x ± s that all experimental group and matched group data analysis are checked with the sided t of two sample means.
2) result
The ischemia/reperfusion injury experimental result shows that myocardial Mass Measured percentage ratio sees Table respectively 1 under administration group, positive drug matched group, model group myocardial infarction and the ligature.
Table 1 Aphanamixoid A is on the impact of scheming weight ratio under myocardial infarction and the ligature
Compare * * p＜0.01, * p＜0.05 with model group
Aphanamixoid A sees Table 2 to the impact of the acute myocardial ischemia that pituitrin causes.
The impact of the acute myocardial ischemia that table 2 Aphanamixoid A causes pituitrin
Compare * * p＜0.01, * p＜0.05 with model group
Conclusion: Aphanamixoid A can reduce the generation of myocardial infarction, and Aphanamixoid A can obviously change the variation of electrocardio degree, does not change heart rate.More than experiment can illustrate that Aphanamixoid A can treat myocardial ischemia.
Claims (1)
1.Aphanamixoid the application of A in preparation treatment or prevention myocardial ischemia drug, described compd A phanamixoid A structure is shown in formula I:
Formula I.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210468890XA CN102988351A (en) | 2012-11-19 | 2012-11-19 | Application of Aphanamixoid A for preparing medicine for treating myocardial ischemia |
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| CN201210468890XA CN102988351A (en) | 2012-11-19 | 2012-11-19 | Application of Aphanamixoid A for preparing medicine for treating myocardial ischemia |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103340886A (en) * | 2013-07-26 | 2013-10-09 | 杨仙君 | Application of Polyflavanostilbene A in preparation of medicine for treating myocardial ischemia |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1935800A (en) * | 2006-10-16 | 2007-03-28 | 闫福林 | Compound with anti cerebralischemia, myo cardialischemia and memory-improving functions, and its preparing method and use |
| US20100016387A1 (en) * | 2006-12-11 | 2010-01-21 | Avirup Bose | Method of treatment |
-
2012
- 2012-11-19 CN CN201210468890XA patent/CN102988351A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1935800A (en) * | 2006-10-16 | 2007-03-28 | 闫福林 | Compound with anti cerebralischemia, myo cardialischemia and memory-improving functions, and its preparing method and use |
| US20100016387A1 (en) * | 2006-12-11 | 2010-01-21 | Avirup Bose | Method of treatment |
Non-Patent Citations (2)
| Title |
|---|
| JIE-YUN CAI, ET AL.: "Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya", 《ORGANIC LETTERS》, vol. 14, no. 10, 27 April 2012 (2012-04-27), pages 2524 - 2527 * |
| 张虹，等: "柠檬苦素类似物的研究进展", 《食品与发酵工业》, vol. 28, no. 2, 20 March 2002 (2002-03-20), pages 80 - 83 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103340886A (en) * | 2013-07-26 | 2013-10-09 | 杨仙君 | Application of Polyflavanostilbene A in preparation of medicine for treating myocardial ischemia |
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Application publication date: 20130327 |