CN103768051B - The application of Eryngiolide A in preparation treatment myocardial ischemia drug - Google Patents
The application of Eryngiolide A in preparation treatment myocardial ischemia drug Download PDFInfo
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- CN103768051B CN103768051B CN201210413328.7A CN201210413328A CN103768051B CN 103768051 B CN103768051 B CN 103768051B CN 201210413328 A CN201210413328 A CN 201210413328A CN 103768051 B CN103768051 B CN 103768051B
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Abstract
The invention provides the application of Eryngiolide A in preparation treatment or prevention Ischemic/reperfusion medicine.The Eryngiolide 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 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 Eryngiolide A to prepare treatment or prevent the application in myocardial ischemia drug.
Background technology
The present inventor is found by a large amount of experiments, and Eryngiolide 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 compd E ryngiolide A that the present invention relates to is one and delivers (Wang in 2012, S.J.et al., 2012.Eryngiolide A, a Cytotoxic Macrocyclic Diterpenoid with an Unusual CyclododecaneCore Skeleton Produced by the Edible Mushroom Pleurotus eryngii.Organic Letters14 (14), 3672 – 3675.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to the cytotoxic activity (Wang of cancerous cell, S.J.et al., 2012.Eryngiolide A, aCytotoxic Macrocyclic Diterpenoid with an Unusual Cyclododecane Core SkeletonProduced by the Edible Mushroom Pleurotus eryngii.Organic Letters 14 (14), 3672 – 3675.), the Eryngiolide A 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 Eryngiolide 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 Eryngiolide A has treatment or prevention myocardial ischemia drug disease.
Described compd E ryngiolide A structure is as shown in formula I:
The Eryngiolide 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 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 compd E ryngiolide A involved in the present invention is see document (Wang, S.J.et al., 2012.Eryngiolide A, a Cytotoxic Macrocyclic Diterpenoid with an UnusualCyclododecane Core Skeleton Produced by the Edible Mushroom Pleurotus eryngii.Organic Letters 14 (14), 3672 – 3675.).
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 compd E ryngiolide A tablet involved in the present invention:
Get 20 g of compound Eryngiolide A, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compd E ryngiolide A capsule involved in the present invention:
Get 20 g of compound Eryngiolide A, 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: Eryngiolide 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 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.The Electrocardiographic change of record 15min continuously after experimental group, positive controls sublingual vein injection of pituitrin 5IU/kg (complete in 5s, positive controls 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 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.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 controls 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 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.
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 controls, negative control group myocardial infarction and ligature, myocardial Mass Measured percentage ratio is respectively in table 1.
Table 1 Eryngiolide A is on the impact of scheming weight ratio under myocardial infarction and ligature
Compare with negative control, * * p<0.01, * p<0.05
Eryngiolide A on the impact of the acute myocardial ischemia that pituitrin causes in table 2.
Table 2 Eryngiolide A is on the impact of the acute myocardial ischemia that pituitrin causes
Compare with negative control, * * p<0.01, * p<0.05
Conclusion: Eryngiolide AA can reduce the generation of myocardial infarction, Eryngiolide A obviously can change the change of electrocardio degree, does not change heart rate.More than experiment can illustrate, Eryngiolide A can treat myocardial ischemia/perfusion.
Claims (1)
1.Eryngiolide A preparation treatment or prevention myocardial ischemia drug in application, described compd E ryngiolide A structure as
formula Ishown in:
formula I.
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| CN103768051B true CN103768051B (en) | 2015-10-07 |
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| CN105250269A (en) * | 2015-11-05 | 2016-01-20 | 淄博齐鼎立专利信息咨询有限公司 | Application of Nagelamides X in preparation of drug for treating myocardial ischemia |
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Non-Patent Citations (2)
| Title |
|---|
| Eryngiolide A, a Cytotoxic Macrocyclic Diterpenoid with an Unusual Cyclododecane Core Skeleton Produced by the Edible Mushroom Pleurotus eryngii;Shao-juan Wang et al;《Organic Letters》;20120706;第14卷(第14期);第3672-3675页 * |
| 赵蕾等.ST-1 抗豚鼠和兔心肌缺血再灌注损伤的血流动力学研究.《东南大学学报(医学版)》.2004,第23卷(第6期),第384-387页. * |
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Inventor after: Wu Junhua Inventor after: Wang Yufeng Inventor after: Huang Rong Inventor after: Zhang Guang Inventor after: Wang Zhongxia Inventor after: Gong Xia Inventor after: Feng Yi Inventor after: Gao Xiang Inventor after: Chen Qiuyan Inventor after: Zhou Lizhu Inventor before: Huang Rong Inventor before: Gong Xia Inventor before: Feng Yi Inventor before: Wu Junhua |
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Free format text: CORRECT: INVENTOR; FROM: HUANG RONG GONG XIA FENG YI WU JUNHUA TO: WU JUNHUA HUANG RONG ZHANG GUANGWANG ZHONGXIA GONG XIA FENG YI GAO XIANG CHEN QIUYAN ZHOU LIZHU WANG YUFENG |
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