CN102861035B - 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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- CN102861035B CN102861035B CN201210418129.5A CN201210418129A CN102861035B CN 102861035 B CN102861035 B CN 102861035B CN 201210418129 A CN201210418129 A CN 201210418129A CN 102861035 B CN102861035 B CN 102861035B
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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 prevention myocardial ischemia drug.
Background technology
The inventor is by a large amount of experiment discoveries, and Gypensapogenin B has the pharmacological action of resist myocardial ischemia/reperfusion injury, has the medical usage of prevention or treatment myocardial ischemia disease.
The compound Gypensapogenin B the present invention relates to is one and within 2012, delivers (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.) New skeleton compound, this compound has brand-new framework types, current 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.), for the Gypensapogenin B the present invention relates to, in the purposes of preparing in medicaments for resisting myocardial ischemia, belong 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, 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 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 compound Gypensapogenin B structure is as shown in formula I:
The Gypensapogenin B the present invention relates to belongs to open first in the purposes of preparing in 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, possess outstanding substantive distinguishing features, for resisting myocardial ischemia, obviously there is significant progress simultaneously.
The specific embodiment
The preparation method of 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 subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add the conventional adjuvant of preparing capsule as 180 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example: the impact of Gypensapogenin B 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 of pituitrin induction: 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 of consubstantiality accumulated amount every day, respectively organize 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.In experimental group, positive controls sublingual vein injection of pituitrin 5 IU/kg(5s, complete, positive controls is 10 min lumbar injection nitroglycerin 5 mg/kg before injection of pituitrin) the Electrocardiographic variation of continuous record 15 min after 10 min.If there is one of following variation in electrocardiogram: T ripple is low flat, two-way, is inverted, and move down >=0.05 mV of ST section level, remembers 1 point.Finally the total score of every rat is analyzed, as reduced after medication score, prompting myocardial ischemia is improved.With changes in heart rate percentage rate before and after injection of pituitrin, represent the impact of medicine on 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 of consubstantiality accumulated amount every day, respectively organize 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), at 4th ~ 5 intercostals, open thoracic cavity, expose heart, at pulmonary conus left border, 320 silk thread ligation ramus descendens anterior arteriae coronariae sinistraes for left auricle lower edge 1mm place (positive controls is 3 min sublingual vein injection Propranolol 1.0 mg/kg before following coronary artery occlusion).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, water rinses and removes dyestuff unnecessary on myocardium sheet 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 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 consubstantiality accumulated amount every day, respectively organize continuous gavage 5d.Lumbar injection urethane 10 mg/kg anesthesia in the 6th day.Record standard II lead electrocardiogram.Longitudinally 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 left lower extremity inside skin, separate femoral artery, insert ductus arteriosus.Cut-in pressure transducer, transports to multimedia bio signal monitor signal and observes.After balance 30 min, record the front each hemodynamic index of administration.
So data all represent with x ± s, the sided t check of two sample averages for experimental group and matched group data analysis.
2) result
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 1 Gypensapogenin B on scheming weight ratio under myocardial infarction and ligature
**p<0.01，*p<0.05
The impact of the acute myocardial ischemia that Gypensapogenin B causes pituitrin is in Table 2.
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, Gypensapogenin B can obviously change the variation of electrocardio degree, does not change heart rate.More than experiment can illustrate, Gypensapogenin B can treat myocardial ischemia/perfusion.
Claims (1)
- The application of 1.Gypensapogenin B in preparation treatment or prevention myocardial ischemia drug, described compound Gypensapogenin B structure as formula Ishown in:
Formula I.
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