CN105412068A - Application of Rearranged abietane diterpenoid in preparation of drugs for treating myocardial ischemia - Google Patents
Application of Rearranged abietane diterpenoid in preparation of drugs for treating myocardial ischemia Download PDFInfo
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- CN105412068A CN105412068A CN201510800777.0A CN201510800777A CN105412068A CN 105412068 A CN105412068 A CN 105412068A CN 201510800777 A CN201510800777 A CN 201510800777A CN 105412068 A CN105412068 A CN 105412068A
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- myocardial ischemia
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- abietane diterpenoid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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- Medicinal Chemistry (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention provides application of Rearranged abietane diterpenoid in preparation of drugs for treating or preventing myocardial ischemia/reperfusion, which is disclosed for the first time. As a skeleton type belongs to a brand new skeleton type, and the Rearranged abietane diterpenoid is high in myocardial ischemia inhibition activity and has outstanding substantive characteristics, it is obvious that a significant progress is made to use the Rearranged abietane diterpenoid for resisting myocardial ischemia.
Description
Technical field
The present invention relates to the novelty teabag of compound R earrangedabietanediterpenoid, particularly relate to the application of Rearrangedabietanediterpenoid in preparation treatment myocardial ischemia drug.
Background technology
The present inventor is found by a large amount of experiments, and Rearrangedabietanediterpenoid 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 R earrangedabietanediterpenoid that the present invention relates to is one and delivers (Wen-XuanWang in 2013, etal., RearrangedabietanediterpenoidsfromtherootsofClerodendrum trichotomumandtheircytotoxicitiesagainsthumantumorcells. Phytochemistry, 89 (2013) 89 – 95.) noval chemical compound, this compound has brand-new framework types, current purposes only suppresses part tumor cell proliferation (Wen-XuanWang, etal., RearrangedabietanediterpenoidsfromtherootsofClerodendrum trichotomumandtheircytotoxicitiesagainsthumantumorcells. Phytochemistry, 89 (2013) 89 – 95.), the purposes of the Rearrangedabietanediterpenoid that the present invention relates in preparation treatment myocardial ischemia drug belongs to first public.
Summary of the invention
The invention provides the application in the medicine of Rearrangedabietanediterpenoid preparation treatment or prevention Ischemic/reperfusion.
The present inventor demonstrates by the experiment in detailed description of the invention the effect that Rearrangedabietanediterpenoid has treatment or prevention myocardial ischemia drug disease.
Described compound R earrangedabietanediterpenoid structure is as shown in formula I:
The Rearrangedabietanediterpenoid 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 preparation method of compound R earrangedabietanediterpenoid involved in the present invention is see document (Wen-XuanWang, etal., RearrangedabietanediterpenoidsfromtherootsofClerodendrum trichotomumandtheircytotoxicitiesagainsthumantumorcells. Phytochemistry, 89 (2013) 89 – 95.)
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 compound R earrangedabietanediterpenoid tablet involved in the present invention:
Get 5 g of compound Rearrangedabietanediterpenoid and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound R earrangedabietanediterpenoid capsule involved in the present invention:
Get 5 g of compound Rearrangedabietanediterpenoid and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1:Rearrangedabietanediterpenoid 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.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, 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 1Rearrangedabietanediterpenoid is on the impact of scheming weight ratio under myocardial infarction and ligature
Compare with negative control group, * * p<0.01, * p<0.05
Rearrangedabietanediterpenoid on the impact of the acute myocardial ischemia that pituitrin causes in table 2.
Table 2Rearrangedabietanediterpenoid is on the impact of the acute myocardial ischemia that pituitrin causes
Compare with negative control group, * * p<0.01, * p<0.05
Conclusion: Rearrangedabietanediterpenoid can reduce the generation of myocardial infarction, and Rearrangedabietanediterpenoid obviously can change the change of electrocardio degree, does not change heart rate.More than experiment can illustrate, Rearrangedabietanediterpenoid can treat myocardial ischemia/perfusion.
Claims (1)
- The application of 1.Rearrangedabietanediterpenoid in preparation treatment myocardial ischemia drug, described compound R earrangedabietanediterpenoid structure is as shown in formula I:Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510800777.0A CN105412068A (en) | 2015-11-19 | 2015-11-19 | Application of Rearranged abietane diterpenoid in preparation of drugs for treating myocardial ischemia |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510800777.0A CN105412068A (en) | 2015-11-19 | 2015-11-19 | Application of Rearranged abietane diterpenoid in preparation of drugs for treating myocardial ischemia |
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| CN105412068A true CN105412068A (en) | 2016-03-23 |
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Application publication date: 20160323 |