CN103751182B - The application of a kind of compound in treatment myocardial ischemia drug - Google Patents

The application of a kind of compound in treatment myocardial ischemia drug Download PDF

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Publication number
CN103751182B
CN103751182B CN201310635141.6A CN201310635141A CN103751182B CN 103751182 B CN103751182 B CN 103751182B CN 201310635141 A CN201310635141 A CN 201310635141A CN 103751182 B CN103751182 B CN 103751182B
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China
Prior art keywords
myocardial ischemia
compound
mollolide
application
treatment myocardial
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CN201310635141.6A
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CN103751182A (en
Inventor
涂瑞强
王闪闪
何武春
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Shanghai Xinhe Pharmaceutical Co., Ltd
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涂瑞强
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Abstract

The invention provides the application of a kind of compound Mollolide A in preparation treatment or prevention Ischemic/reperfusion medicine, belong to first public, because framework types belongs to brand-new framework types, and its inhibit activities for myocardial ischemia is strong, possessing outstanding substantive distinguishing features, for resisting myocardial ischemia, obviously there is significant progress simultaneously.

Description

The application of a kind of compound in treatment myocardial ischemia drug
Technical field
The present invention relates to the novelty teabag of a kind of compound Mollolide A, particularly relate to the application of Mollolide A in preparation treatment myocardial ischemia drug.
Background technology
The present inventor is found by a large amount of experiments, and Mollolide A 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 Mollolide A that the present invention relates to is one and delivers (Yong Li in 2013, et al., MollolideA, a Diterpenoid with a New1, 10:2, 3-Disecograyanane Skeleton from the Roots ofRhododendron molle Organic Letters, 2013, 15 (12): 3074 – 3077.) noval chemical compound, this compound has brand-new framework types, current purposes finds antibacterial (the Yong Li of its energy, et al., Mollolide A, a Diterpenoid with a New1, 10:2, 3-Disecograyanane Skeleton from the Roots ofRhododendron molle Organic Letters, 2013, 15 (12): 3074 – 3077.), the purposes of the Mollolide A that the present invention relates in preparation treatment myocardial ischemia drug belongs to first public.
Summary of the invention
The invention provides Mollolide A to prepare treatment or prevent the application in the medicine of Ischemic/reperfusion.
The present inventor demonstrates by the experiment in detailed description of the invention the effect that Mollolide A has treatment or prevention myocardial ischemia drug disease.
Described compound Mollolide A structure is as shown in formula I:
The Mollolide A 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 strong, possessing outstanding substantive distinguishing features, for resisting myocardial ischemia, obviously there is significant progress simultaneously.
Detailed description of the invention
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.
The preparation method of compound Mollolide A involved in the present invention is see document (Yong Li, et al., MollolideA, a Diterpenoid with a New1,10:2,3-Disecograyanane Skeleton from the Roots ofRhododendron molle Organic Letters, 2013,15 (12): 3074 – 3077.), prepare compound Mollolide A according to the method described above.
Embodiment 1: the preparation of compound Mollolide A tablet involved in the present invention:
Get 5 g of compound Mollolide A and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound Mollolide A capsule involved in the present invention:
Get 5 g of compound Mollolide A and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1:Mollolide 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, Nanjing Medical University's Experimental Animal Center.
(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, administration group 3 groups, often organizes 8.Administration group gastric infusion, two matched groups 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.Complete in experimental group, positive controls sublingual vein injection of pituitrin 5IU/kg(5s, positive controls is 10min lumbar injection nitroglycerin 5mg/kg before injection of pituitrin) the Electrocardiographic change of record 15min continuously after 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 controls, negative control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, two matched groups give the distilled water gavage of consubstantiality accumulated amount every day, each continuous gavage 7d.Record standard II lead electrocardiogram after rats by intraperitoneal injection pentobarbital sodium 30mg/kg anaesthetizes.Tracheal intubation, connect 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 controls is 3min sublingual vein injection Propranolol 1.0mg/kg before following coronary artery occlusion).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 controls, negative control group, administration group 3 groups, often organizes 8.Administration group gastric infusion, two matched groups 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.All data all represent with x ± s, and 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 controls, negative control group myocardial infarction and ligature, myocardial Mass Measured percentage ratio is respectively in table 1.
Table 1Mollolide A is on the impact of scheming weight ratio under myocardial infarction and ligature
Compare with negative control group, * * p<0.01, * p<0.05
Mollolide A on the impact of the acute myocardial ischemia that pituitrin causes in table 2.
Table 2Mollolide A is on the impact of the acute myocardial ischemia that pituitrin causes
Compare with negative control group, * * p<0.01, * p<0.05
Conclusion: Mollolide A can reduce the generation of myocardial infarction, Mollolide A obviously can change the change of electrocardio degree, does not change heart rate.More than experiment can illustrate, Mollolide A can treat myocardial ischemia/perfusion.

Claims (1)

1. the application of compound in preparation treatment myocardial ischemia drug, described compound Mollolide A structure is as shown in formula I:
CN201310635141.6A 2013-11-29 2013-11-29 The application of a kind of compound in treatment myocardial ischemia drug Expired - Fee Related CN103751182B (en)

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CN103751182B true CN103751182B (en) 2015-10-07

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