CN102670583A - Application of flavonoids in moldavica dragonhead in the preparation of myocardial ischemic antagonist - Google Patents
Application of flavonoids in moldavica dragonhead in the preparation of myocardial ischemic antagonist Download PDFInfo
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- CN102670583A CN102670583A CN2012101913200A CN201210191320A CN102670583A CN 102670583 A CN102670583 A CN 102670583A CN 2012101913200 A CN2012101913200 A CN 2012101913200A CN 201210191320 A CN201210191320 A CN 201210191320A CN 102670583 A CN102670583 A CN 102670583A
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- flavonoids
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- luteolin
- kaempferol
- moldavica dragonhead
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Abstract
The invention relates to the technical field of natural medicine and especially to anti-myocardial ischemic function of flavonoids in moldavica dragonhead. As shown in a pharmacology experiment, the flavonoids in moldavica dragonhead, especially luteolin, kaempferol and galuteolin, have excellent anti-myocardial ischemic function, and the drug effect of luteolin, kaempferol and galuteolin is stronger than that of other flavonoids in the moldavica dragonhead and stronger than that of general flavone in the moldavica dragonhead.
Description
Technical field
The present invention relates to natural medicine technical field, be specifically related in the Herba Dracocephali the particularly function of resisting myocardial ischemia of luteolin, kaempferol, luteoloside of chromocor compound.
Background technology
Cardiovascular disease is the common disease of one type of serious harm human health, occupies first of the ten the most fatal big diseases of the world.According to WHO statistics, global annual cardiovascular disease death toll is about 1,670 ten thousand (account for total death toll 30%), and wherein about 700 die ten thousand deaths in ischemic heart desease (account for cardiovascular disease death toll 42%).According to the epidemiologic data prediction, global ischemic heart desease death toll 2020 will increase by 74.6% than the nineteen ninety.And, have every year 1500000 people to die from ischemic heart desease (account for the world 21%) approximately in China, and just in rising trend, so the preventing and controlling task is arduous.
Ischemic heart desease (mainly being coronary heart disease) is because of coronary blood supplies sharply to reduce or to interrupt, and makes serious, the persistent acute ischemia of cardiac muscle and causes myocardial infarction or heart failure, causes mortality rate very high.Therefore, the damage of resisting myocardial ischemia property is the key of control ischemic heart desease.
Luteolin, kaempferol, luteoloside are isolated flavone compounds from Herba Dracocephali.Existing bibliographical information, luteolin tool antiinflammatory, antitumor, antiallergic, fibrosis, antifertility, antibacterium and virus, inhibition angiogenic growth and protection H
2O
2Cause effects such as myocardial cell and vascular endothelial cell damage, blood fat reducing, the liver protecting ischemical reperfusion injury; Luteoloside has protection H
2O
2And the effect of simulation hypoxic-ischemic myocardial cell injury.But these three chemical combination systems are carried out treating myocardial ischemia damage protective effect research not to appear in the newspapers.
Summary of the invention
The present invention has studied the activity of the flavone compound that derives from the Herba Dracocephali and its total flavones; The result is through relatively finding; Luteolin, kaempferol, luteoloside have strong function of resisting myocardial ischemia; Its activity is better than other flavone compound that derives from Herba Dracocephali, like diosmetin, acacetin, apiin, agastachoside etc., and also is better than the activity of Herba Dracocephali total flavones.
The above-mentioned flavone compound structure that is derived from Herba Dracocephali is following:
Luteolin, kaempferol, luteoloside derive from any natural drug or composite.Can add pharmaceutically acceptable carrier and process various preparations.Monomer component effective dose every day of adult's medication is 10～5000mg/70kg.The also visual concrete state of an illness departs from this scope.
Do further elaboration below in conjunction with embodiment.
The specific embodiment
Embodiment 1
The protection isoproterenol causes the mouse cardiac muscle ischemia
1. experiment grouping and mouse cardiac muscle ischemia model prepare 110 of mices, are divided into 11 groups at random, and 10 every group, male and female half and half.Every day, subcutaneous injection ISP or normal saline were 1 time, gastric infusion 1 time, continuous 5 days.Normal group: distilled water is irritated stomach, subcutaneous injection normal saline; Model group: distilled water is irritated stomach, subcutaneous injection ISP (10mg/kg, down together); Drug group: gastric infusion, subcutaneous injection ISP; Positive drug Radix Salviae Miltiorrhizae Tabellae group: gastric infusion, subcutaneous injection ISP.This collection of the laggard rower of 5d gastric infusion in morning 2h.
2. Protein, superoxide dismutase (SOD), malonaldehyde (MDA), glutathion peroxidase (GSH-Px) mensuration mice are plucked eyeball and get blood in SCK (CK) and lactic acid dehydrogenase (LDH) and the cardiac muscular tissue; Room temperature is placed 1h; Put 4 ℃ of refrigerator overnight then, serum is separated out.The centrifugal 30min of 1500rpm draws supernatant, presses the test kit rule of operation and measures CK and LDH; The mice sacrificed by exsanguination is taken out heart immediately, removes the roguing tissue, rinsing in ice-cold normal saline; Remove blood, filter paper blots, and weighs; Shred and put into the homogenate pipe, add 9 times of amount 0.86% cold salines, manual homogenate; The centrifugal 10min of 2000rpm separates supernatant and gets the homogenate of 10% cardiac muscular tissue, presses the test kit rule of operation and measures SOD, MDA, GSH-PX.
3. result
(1) luteolin, kaempferol, luteoloside extremely significantly suppress myocardial ischemia mice LDH secretion and CK vigor (P＜0.01 or P＜0.001), and its activity is better than other several flavone compounds and Herba Dracocephali total flavones.See table 1.
The influence of CK and LDH in the table 1 pair myocardial ischemia mice serum (n=10,
Annotate: compare ##P＜0.01, ###P＜0.001 with normal group; Compare * P＜0.05, * * P＜0.01, * * *＜0.001 with model group
(2) luteolin, kaempferol, luteoloside significantly reduce myocardial ischemia mice MDA content, increased SOD and GSH-Px vigor (P＜0.01), and its activity is better than other several flavone compounds and Herba Dracocephali total flavones.See table 2.
The influence of MDA, SOD and GSH-Px (n=10,
in the table 2 pair myocardial ischemia mouse cardiac muscle tissue
Annotate: < 0.01, ###P < 0.001 to compare ##P with normal group; With model group relatively * P 0.05, * * P < 0.01
4. conclusion
Luteolin, kaempferol, luteoloside have stronger protection isoproterenol and cause the effect of mouse cardiac muscle ischemia.
Embodiment 2
Protection rat heart muscle ischemia
1. the ischemical reperfusion injury model prepares 280～320g male SD rat, 20% urethane abdominal cavity light anaesthesia, trans-oral tracheal intubation, respirator positive airway pressure (80 times/min of respiratory frequency, tidal volume 20ml, respiratory quotient 1: 2, air pressure 0).It is subcutaneous that needle electrode is inserted three limbs, connects BL-420s biological function experimental system passage 1 or 2, opens systems soft ware and respective channel, measures electrocardio.Shave off left side portion's hair in the heart, sterilization, the longitudinal incision skin 1cm at the heartbeat place separates the flesh layer in the 4th, 5 intercostal passivity, struts Intercostal muscle and pleura and gets into the thoracic cavity.Draw back the thoracic cavity, tear pericardium, extrude heart.Coronary artery place between aortic root arterial cone and left auricle carries out ligation (lining Bao Yigen silica gel tube) with 6/0 band pin finedraw zygonema around branch of coronary artery.Heart is sent back in the thoracic cavity, and extruding thoracic cavity air-out is sewed up thoracic wall rapidly, recovers autonomous respiration, stops the artificial respiration, measures electrocardiogram (before recovering autonomous respiration), ligation 30min.
2. the medication rat is divided into sham operated rats, ischemia group (model group), drug group, metoprolol group, 12 every group at random.Preceding 3 days gastric infusions of administration group art, every day 1 time, sham operated rats and model group are given the equivalent normal saline.
3. observation index
(1) behind the serum myocardial enzyme ischemia 30min, eye socket is got blood, and separation of serum detects lactic acid dehydrogenase (LDH), glutamic oxaloacetic transaminase, GOT (AST), creatine kinase (CK) with test kit respectively.
(2) after myocardial infarct size is measured ischemia 30min, open the thoracic cavity, it is frozen to win heart, vertical with the heart longitudinal axis then 5 of the even thin slices of 2mm that are cut into, and 1%TTC discards dyeing liquor in 37 ℃ of constant temperature dyeing 15min, and normal saline flushing takes out to dry slightly and takes pictures.According to different each zone (redness is the hazardous area, and pale asphyxia is an infarcted region) of distinguishing of color, separate infarcted region after the title gross weight and weigh, calculate the ratio that infarcted region accounts for total heart.
4. result
(1) luteolin, kaempferol, luteoloside significantly suppress rats with myocardial ischemia LDH secretion, AST and CK vigor (P＜0.05 or P＜0.01), and its activity is better than other several flavone compounds and Herba Dracocephali total flavones.See table 3.
The influence of LDH secretion in the table 3 pair rats with myocardial ischemia serum, AST and CK vigor (n=12,
Annotate: compare with sham operated rats
##P ﹤ 0.01; Compare with model group
*P ﹤ 0.05,
*P ﹤ 0.01
(2) luteolin, kaempferol, luteoloside significantly suppress rats with myocardial ischemia myocardial infarction district proportion (P＜0.01), and its activity is better than other several flavone compounds and Herba Dracocephali total flavones.See table 4.
Influence (n=12,
of table 4 pair rats with myocardial ischemia myocardial infarction district proportion
Annotate: compare with model group
*P ﹤ 0.05,
*P ﹤ 0.01
5. conclusion
Luteolin, kaempferol, luteoloside have the effect of stronger protection rats with myocardial ischemia myocardial infarction.
Embodiment 3
The protecting myocardial cell anoxia-induced apoptosis
1. neonatal rat is got in former generation myocardial cell cultivation, isolating cardiac under the aseptic condition, and cold PBS cleans, and shreds into 1mm
3About fritter, with the gradation digestion under 37 ℃ of constant temperature stirring at low speed conditions of 0.0625g/L pancreatin, each 8min, totally 4 times.Promptly contain the DMEM culture medium termination digestion of 15%FBS behind each collection supernatant, centrifugal then (1000rpm * 10min), with culture medium washing 1 time, carry out the adherent normal cultured 90min of differential again behind the collection myocardial cell with equal-volume.Then with cell suspension with density 5 * 10
5Cells/mL is inoculated in 96 well culture plates, in 37 ℃, 5%CO
2Cultivate under the condition, every 2d changes a culture fluid.
2. the neonatal rat myocardial cell that former generation myocardial cell grouping carrying out medicine pretreatment and the preparation of anoxia-induced apoptosis model will be cultured to 5d divides into groups and the dosing pretreatment.Normal group: with the no phenol red DMEM culture fluid normal cultured that contains 12%FBS; Model group:, add 4mmol/L Na with the no phenol red DMEM culture fluid normal cultured that contains 12%FBS
2S
2O
4Anoxia 2h; VitE organizes (100 μ g/mL), supplies the examination drug group.After in containing the no phenol red DMEM culture fluid of 12%FBS, adding confession reagent normal cultured 24h, add 4mmol/L Na
2S
2O
4Anoxia, observation of cell form behind the 2h is collected and is respectively organized the culture fluid supernatant, presses test kit and detects LDH and T-SOD vigor and MDA content.
3. result
Luteolin, kaempferol, luteoloside significantly suppress LDH and discharge, and reduce MDA content, rising T-SOD vigor, and its activity is better than other several flavone compounds and Herba Dracocephali total flavones.See table 5.
Influence (n=6,
of LDH, T-SOD, MDA after the table 5 pair former generation myocardial cell anoxia-induced apoptosis
Annotate: < 0.05, ##P < 0.01 to compare #P with normal group; With model group relatively * P 0.05, * * P < 0.01
4. conclusion
Luteolin, kaempferol, luteoloside have the effect of protecting myocardial cell anoxia-induced apoptosis.
Claims (1)
1. luteolin, kaempferol or luteoloside are used to prepare the purposes of medicaments for resisting myocardial ischemia.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103356681A (en) * | 2013-06-24 | 2013-10-23 | 丁圣雨 | Application of Houttuynoid A in preparation of medicines for treating myocardial ischemia |
| CN104490910A (en) * | 2014-12-03 | 2015-04-08 | 南京睿鹰润泽生物医药科技有限公司 | Composition containing active components of dracocephalum moldavica l. and used for resisting myocardial ischemia-reperfusion injury |
| CN106822165A (en) * | 2015-11-24 | 2017-06-13 | 石河子大学医学院第附属医院 | The purposes of the O glucuronides of robinin 7 |
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| CN1403080A (en) * | 2002-10-21 | 2003-03-19 | 中国人民解放军第二军医大学 | Application of kaempferol and its derivative in preparing medicine for cardiac and cerebral vascular diseases |
| CN101219161A (en) * | 2007-12-25 | 2008-07-16 | 新疆维吾尔自治区药物研究所 | Dracocephalum moldavica extract and dracocephalum moldavica dropping pills, and method of preparing the same |
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| CN1403080A (en) * | 2002-10-21 | 2003-03-19 | 中国人民解放军第二军医大学 | Application of kaempferol and its derivative in preparing medicine for cardiac and cerebral vascular diseases |
| CN101219161A (en) * | 2007-12-25 | 2008-07-16 | 新疆维吾尔自治区药物研究所 | Dracocephalum moldavica extract and dracocephalum moldavica dropping pills, and method of preparing the same |
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| 《中药新药与临床药理》 20080731 周玲等 木犀草素-7-O-beta-D-葡萄糖苷对缺血缺氧培养乳鼠心肌细胞的保护作用 第259-261页 1 第19卷, 第4期 * |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103356681A (en) * | 2013-06-24 | 2013-10-23 | 丁圣雨 | Application of Houttuynoid A in preparation of medicines for treating myocardial ischemia |
| CN104490910A (en) * | 2014-12-03 | 2015-04-08 | 南京睿鹰润泽生物医药科技有限公司 | Composition containing active components of dracocephalum moldavica l. and used for resisting myocardial ischemia-reperfusion injury |
| CN104490910B (en) * | 2014-12-03 | 2017-05-31 | 南京睿鹰润泽生物医药科技有限公司 | A kind of Dracocephalum moldavica active ingredient compositions of the reperfusion injury that resists myocardial ischemia |
| EP3228316A4 (en) * | 2014-12-03 | 2018-04-25 | Nanjing Ruiying Runze Biopharmaceutical Technology Co., Inc. | Composition containing active components of dracocephalum moldavica l. against myocardial ischemia-reperfusion injury |
| CN106822165A (en) * | 2015-11-24 | 2017-06-13 | 石河子大学医学院第附属医院 | The purposes of the O glucuronides of robinin 7 |
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