CN102861035A - Application of Gypensapogenin B in medicine for treating myocardial ischemia - Google Patents
Application of Gypensapogenin B in medicine for treating myocardial ischemia Download PDFInfo
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- CN102861035A CN102861035A CN2012104181295A CN201210418129A CN102861035A CN 102861035 A CN102861035 A CN 102861035A CN 2012104181295 A CN2012104181295 A CN 2012104181295A CN 201210418129 A CN201210418129 A CN 201210418129A CN 102861035 A CN102861035 A CN 102861035A
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- gypensapogenin
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Abstract
The invention provides application of Gypensapogenin B in preparing a medicine for treating or preventing myocardial ischemia. The application of Gypensapogenin B in preparing the medicine for treating myocardial ischemia, which is provided by the invention, is disclosed for the first time. The skeleton type belongs to brand-new skeleton type, and the myocardial ischemia resisting activity of Gypensapogenin B is extremely strong, so that no possibility for providing any prompt by other compounds exists. Gypensapogenin B has outstanding actual characteristics. Meanwhile, Gypensapogenin B has outstanding progress when being used for resisting myocardial ischemia.
Description
Technical field
The present invention relates to the application in Gypensapogenin B preparation treatment or the prevention myocardial ischemia drug.
Background technology
The inventor finds by a large amount of experiment, and Gypensapogenin B has and resists myocardial ischemia/pharmacological action of reperfusion injury the medical usage with prevention or treatment myocardial ischemia disease.
The chemical compound Gypensapogenin B that the present invention relates to is one and delivered (Li in 2012, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to the cytotoxic activity (Li of human tumor cell line, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178.), belong to open first for the purposes of the Gypensapogenin B 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 Gypensapogenin B preparation treatment or prevention Ischemic/reperfusion.
The inventor has the effect for the treatment of or prevention myocardial ischemia drug disease by the Gypensapogenin B that experimental results show that in the specific embodiment.
Described chemical compound Gypensapogenin B structure is shown in formula I:
The purposes of the Gypensapogenin B 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 chemical compound Gypensapogenin B involved in the present invention is referring to document (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178. and Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45 (3): 167-171.).
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 chemical compound Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of chemical compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, 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: Gypensapogenin B 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 controls, negative control 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 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 experimental group, positive controls sublingual vein injection of pituitrin 5 IU/kg(5s, positive controls 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 controls, negative control 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 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 controls 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 controls, negative control 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 controls, negative control group myocardial infarction and the ligature.
Table 1 Gypensapogenin B is on the impact of scheming weight ratio under myocardial infarction and the ligature
**p<0.01，*p<0.05
Gypensapogenin B sees Table 2 to the impact of the acute myocardial ischemia that pituitrin causes.
The impact of the acute myocardial ischemia that table 2 Gypensapogenin B causes pituitrin
**p<0.01，*p<0.05
Conclusion: Gypensapogenin BA can reduce the generation of myocardial infarction, and Gypensapogenin B can obviously change the variation of electrocardio degree, does not change heart rate.More than experiment can illustrate that Gypensapogenin B can treat myocardial ischemia/perfusion.
Claims (1)
1.Gypensapogenin the application in B treatment or the prevention myocardial ischemia drug, described chemical compound Gypensapogenin B structure as
Formula IShown in:
Formula I.
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| CN201210418129.5A CN102861035B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicine for treating myocardial ischemia |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030060425A1 (en) * | 1998-11-24 | 2003-03-27 | Ahlem Clarence N. | Immune modulation method using steroid compounds |
| CN1602882A (en) * | 2004-08-10 | 2005-04-06 | 北京科信必成医药科技发展有限公司 | Orally disintegrating tablet of gypenosides and its preparation process |
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2012
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030060425A1 (en) * | 1998-11-24 | 2003-03-27 | Ahlem Clarence N. | Immune modulation method using steroid compounds |
| CN1602882A (en) * | 2004-08-10 | 2005-04-06 | 北京科信必成医药科技发展有限公司 | Orally disintegrating tablet of gypenosides and its preparation process |
Non-Patent Citations (1)
| Title |
|---|
| NING LI，等: "Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 * |
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