CN101530451B - Method for preparing pterocarpus indicus water extract used for endothelium-dependent vasodilation agent and applications of method - Google Patents
Method for preparing pterocarpus indicus water extract used for endothelium-dependent vasodilation agent and applications of method Download PDFInfo
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- CN101530451B CN101530451B CN200810084962.4A CN200810084962A CN101530451B CN 101530451 B CN101530451 B CN 101530451B CN 200810084962 A CN200810084962 A CN 200810084962A CN 101530451 B CN101530451 B CN 101530451B
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Abstract
The invention relates to a method for preparing pterocarpus santalinus water extract used for endothelium-dependent vasodilator and applications of the extract on the medicine or health products of endothelium-independent vasodilatior. The preparation method comprises the steps of extracting the pterocarpus santalinus powders thrice in a back-flow way by 70% of water of 6 times, 5 times and 3 times respectively for 2.5h, 2h and 1.5h, decompressing, concentrating, cooling and drying the extract, and finally obtaining the pterocarpus santalinus extract. Suitable auxiliary material is added into the pterocarpus santalinus extract so as to prepare the medicines or health products such as powder injection, drops, troche, capsule, oral liquid, grain agents and the like.
Description
Technical field
The present invention relates to a kind of red sandalwood water extract as direct vasodilation, and this extract is in the medicine of the cardiovascular disease such as treatment hypertension or the application in health product.
Background technology
Blood vessel endothelium, except because plaing between blood and vascular smooth muscle physiologic barrier effect, also has active metabolism endocrine function, to maintain the balance of environment in blood vessel.Endothelium-dependent vasodilatation (Endothelium-dependentVasodilation, EDD) be one of blood vessel endothelium critical function, its functional disorder, the early origin of atherosclerosis (Atherosclerosis, AS) especially cardiovascular disease, development and complication are played to mastery reaction.
Vasodilation has two kinds of mode: EDD: 1. refer to endotheliocyte in chemical substance as acetylcholine, under the effect of Kallidin I etc. or physiological stimulation (as reactive hyperemia), discharge EDRF and cause vasodilation, it depends on structural integrity and normally functioning endotheliocyte, normal EDD function can maintain antiotasis, anticoagulant, suppress mononuclear cell and neutrophil(e) cell and adhere to, suppress vascular SMC propagation; 2. dependent/non-dependent vasodilation (or claim smooth muscle dependency vasodilation): refer to that exogenous NO precursor does not rely on blood vessel endothelium as medicines such as nitroglycerin, sodium nitroprusside, directly the caused vasodilation of NO vasoactive SMC of release.Two kinds of modes are both independent, unified again, jointly complete the diastolic function of blood vessel.Now confirm, EDRF is exactly NO, and it comes from arginine metabolism, and the activity of nitricoxide synthase (NOSynthase, NOS) directly affects the synthetic of NO and discharges, and ET-1 is the strongest contracting Angiogenesis that endotheliocyte generates, and its physiological action is contrary with NO.As endothelial injury, to medicine and physiological stimulation are reactive, reduce, cause NO synthesis secretion and reduce, vasodilation is abnormal and weaken, and shows as vasospasm or shrink to strengthen.
Existing research shows that following medicine may improve vascular endothelial function or EDD function.
1, the improvement mechanism of HCG-COA reductase inhibitor lipid-lowering statins is except generating with reduction cholesterol, minimizing superoxide anion, outside the Pass minimizing NO inactivation has, also relevant to the expansion vascular reaction of NO with endothelium under its enhancing stimulation state and base state, also there is unique non-effect for reducing fat with it, as improve endothelial function, stablize atheromatous plaque, minimizing platelet aggregation or antithrombotic, antiinflammatory or antioxidation.
2, angiotensin converting enzyme suppresses the activation of machine agent (ACEI) renin-angiotensin system (RAS), by making to increase in blood with Kallidin I, decompose and accelerate two approach and make endothelial hypofunction, ACEI, itself also can be suppressed Kallidin I and decompose because RAS activates the damage to endothelium by antagonism.
3, thereby antioxidant antioxidant can be offset the Oxidation protection endothelial function of superoxide anion.Generally acknowledged antioxidant has vitamin C, E, tocopherol etc. at present.
Take large doses of vitamin C (2g) remarkable impaired EDD function after high-fat meal is had to protective effect.
4, endothelin-receptor antagonists endothelin receptor, antagonist are that the endogenous vasoconstriction mechanism that exists during based on endothelial injury is used and raw, at SMC, find that there is the pressurization that ET-A and two kinds of receptor subtypes of ET-B can mediate Endothelin, blood vessel endothelium also has ET-B receptor and can mediate EDD by discharging NO and PGI.
5, L-arginine can be converted into NO and bring into play physiological effect with NOS effect in vivo as the precursor of NO;
And present stage is used as red sandalwood water extract the vasodilation that endothelium relies on, have not been reported.
The botanical term of Lignum pterocarpi indici is red sandalwood, is pulse family Pterocarpus.Latin is called Pterocarpussantalinus L.F, and commodity are called red sanders, red sandal-wood.
Its timber can make body shrink, to augment and diaphoresis. the timber of pasty state is as cold therapy inflammation and headache. it is said that this is to help treat depression and dermatosis. the medicine of enduring out is as astringent cardiac tonic chronic dysentery bark powder gruel, to be used for the treatment of diarrhoea. drink Lignum pterocarpi indici water and be used for the treatment of diabetes twice every day. local also referred to as other timber with generic of rakthachandan. and bark, Pterocarpus marsupium Roxb. P.marsupium is on record hypoglycemic activity.
The Li Shizhen (1518-1593 A.D.) < < of Ming Dynasty Compendium of Materia Medica > > our department the 34 volume is said: " Lignum pterocarpi indici-salty, is slightly cold, nontoxic, energy and ying-qi detumescence poison.Available this sawdust is decocted water and is smeared affected part; And have relax through invigorating blood circulation, blood circulation promoting and antihypertensive effect.
But present stage is treated hypertensive medicine or health product by red sandalwood water extract as vasodilation, have not been reported.
Summary of the invention
1. the present invention has confirmed that Lignum pterocarpi indici extract, to there being the dilating effect of the animal thoracic aortic ring blood vessel of endothelium, has great clinical meaning to Cardiovarscular.
2. the present invention can obtain by following method: with the water reflux, extract, of 6 times, 5 times and 3 times three times, each time is respectively 2.5h, 2h and 1.5h respectively, concentrating under reduced pressure, and cool drying, obtains Lignum pterocarpi indici extract.
3. the invention provides effective dosage that Lignum pterocarpi indici extract can make interior cutaneous vessel expansion.
4. the Lignum pterocarpi indici extract in the present invention can be mixed and made into preparation mutually with pharmaceutically acceptable excipient, carrier, buffer agent and/or stabilizing agent.Comprise peroral dosage form, have tablet, capsule, oral liquid, granule etc., and injection type, injection and powder ampoule agent for injection etc. had.
5. the invention provides the route of administration that Lignum pterocarpi indici extract can make interior cutaneous vessel expansion, can be oral, injection or other approach.
6. the Lignum pterocarpi indici in the present invention is red sandalwood, India Lignum pterocarpi indici, Pterocarpus marsupium Roxb. or kiaat.
The invention provides medicine or the application of health product in treatment hypertension, coronary heart disease, apoplexy and myocardial infarction prepared by Lignum pterocarpi indici extract
The specific embodiment
Embodiment 1: concentration is the vasoconstrictor effects of the inhibition phyenlephrinium that relies on of the water extract endothelium of 0.0025g/ml Lignum pterocarpi indici
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing and be oxidized with normal saline solution, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11), keeps the temperature of 4 degrees Celsius.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, with a smooth waddy, rub gently inner surperficial, successfully remove interior micromicro and confirm by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine while meeting.The isometric stretching of recording large artery trunks ring by the myograph system that computer is processed.After the balance through at least 1.5 grams of preloading of 90 minutes (this is preloading best in our previous test), the challenge of twice that arterial ring faces the potassium chloride of 60 milliliters in the interval of 30 minutes is to set up a contractile reaction baseline.
With the lax percentage of lax reflection Forskohlin, recently calculate.The relaxation curve of the accumulation reaction density of pterocarpus santalinus water extract has just produced, and the lax of the water of Lignum pterocarpi indici extract and ethanol is that endothelium relies on and the non-dependence of endothelium.
Result of the test:
The water extract of 0.0025g/ml Lignum pterocarpi indici, to by the pretreated vasodilator effect that has large artery trunks ring endothelium, complete of phyenlephrinium, be equivalent to 1 μ M Forskohlin lax effect 15%.
Embodiment 2: concentration is the vasoconstrictor effects of the inhibition phyenlephrinium that relies on of the water extract endothelium of 0.0035g/ml Lignum pterocarpi indici
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing and be oxidized with normal saline solution, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11), keeps the temperature of 4 degrees Celsius.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, with a smooth waddy, rub gently inner surperficial, successfully remove interior micromicro and confirm by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine while meeting.The isometric stretching of recording large artery trunks ring by the myograph system that computer is processed.After the balance through at least 1.5 grams of preloading of 90 minutes (this is preloading best in our previous test), the challenge of twice that arterial ring faces the potassium chloride of 60 milliliters in the interval of 30 minutes is to set up a contractile reaction baseline.
With the lax percentage of lax reflection Forskohlin, recently calculate.The relaxation curve of the accumulation reaction density of pterocarpus santalinus water extract has just produced, and the lax of the water of Lignum pterocarpi indici extract and ethanol is that endothelium relies on and the non-dependence of endothelium.
Result of the test:
The water extract of 0.0035g/ml Lignum pterocarpi indici, to by the pretreated vasodilator effect that has large artery trunks ring endothelium, complete of phyenlephrinium, be equivalent to 1 μ M Forskohlin lax effect 30%.
Embodiment 3: concentration is the vasoconstrictor effects of the inhibition phyenlephrinium that relies on of the water extract endothelium of 0.005g/ml Lignum pterocarpi indici
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing and be oxidized with normal saline solution, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11), keeps the temperature of 4 degrees Celsius.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, with a smooth waddy, rub gently inner surperficial, successfully remove interior micromicro and confirm by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine while meeting.The isometric stretching of recording large artery trunks ring by the myograph system that computer is processed.After the balance through at least 1.5 grams of preloading of 90 minutes (this is preloading best in our previous test), the challenge of twice that arterial ring faces the potassium chloride of 60 milliliters in the interval of 30 minutes is to set up a contractile reaction baseline.
With the lax percentage of lax reflection Forskohlin, recently calculate.The relaxation curve of the accumulation reaction density of pterocarpus santalinus water extract has just produced, and the lax of the water of Lignum pterocarpi indici extract and ethanol is that endothelium relies on and the non-dependence of endothelium.
Result of the test:
The water extract of 0.005g/ml Lignum pterocarpi indici, to by the pretreated vasodilator effect that has large artery trunks ring endothelium, complete of phyenlephrinium, be equivalent to 1 μ M Forskohlin lax effect 35%.
Embodiment 4: concentration is the vasoconstrictor effects of the inhibition phyenlephrinium that relies on of the water extract endothelium of 0.01g/ml Lignum pterocarpi indici
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing and be oxidized with normal saline solution, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11), keeps the temperature of 4 degrees Celsius.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, with a smooth waddy, rub gently inner surperficial, successfully remove interior micromicro and confirm by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine while meeting.The isometric stretching of recording large artery trunks ring by the myograph system that computer is processed.After the balance through at least 1.5 grams of preloading of 90 minutes (this is preloading best in our previous test), the challenge of twice that arterial ring faces the potassium chloride of 60 milliliters in the interval of 30 minutes is to set up a contractile reaction baseline.
With the lax percentage of lax reflection Forskohlin, recently calculate.The relaxation curve of the accumulation reaction density of pterocarpus santalinus water extract has just produced, and the lax of the water of Lignum pterocarpi indici extract and ethanol is that endothelium relies on and the non-dependence of endothelium.
Result of the test:
The water extract of 0.01g/ml Lignum pterocarpi indici, to by the pretreated vasodilator effect that has large artery trunks ring endothelium, complete of phyenlephrinium, be equivalent to 1 μ M Forskohlin lax effect 43%.
Embodiment 5: concentration is the vasoconstrictor effects of the inhibition phyenlephrinium that relies on of the water extract endothelium of 0.015g/ml Lignum pterocarpi indici
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing and be oxidized with normal saline solution, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11), keeps the temperature of 4 degrees Celsius.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, with a smooth waddy, rub gently inner surperficial, successfully remove interior micromicro and confirm by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine while meeting.The isometric stretching of recording large artery trunks ring by the myograph system that computer is processed.After the balance through at least 1.5 grams of preloading of 90 minutes (this is preloading best in our previous test), the challenge of twice that arterial ring faces the potassium chloride of 60 milliliters in the interval of 30 minutes is to set up a contractile reaction baseline.
With the lax percentage of lax reflection Forskohlin, recently calculate.The relaxation curve of the accumulation reaction density of pterocarpus santalinus water extract has just produced, and the lax of the water of Lignum pterocarpi indici extract and ethanol is that endothelium relies on and the non-dependence of endothelium.
Result of the test:
The water extract of 0.015g/ml Lignum pterocarpi indici, to by the pretreated vasodilator effect that has large artery trunks ring endothelium, complete of phyenlephrinium, be equivalent to 1 μ M Forskohlin lax effect 52%.
Embodiment 6: concentration is the vasoconstrictor effects of the inhibition phyenlephrinium that relies on of the water extract endothelium of 0.02g/ml Lignum pterocarpi indici
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing and be oxidized with normal saline solution, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11), keeps the temperature of 4 degrees Celsius.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, with a smooth waddy, rub gently inner surperficial, successfully remove interior micromicro and confirm by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine while meeting.The isometric stretching of recording large artery trunks ring by the myograph system that computer is processed.After the balance through at least 1.5 grams of preloading of 90 minutes (this is preloading best in our previous test), the challenge of twice that arterial ring faces the potassium chloride of 60 milliliters in the interval of 30 minutes is to set up a contractile reaction baseline.
With the lax percentage of lax reflection Forskohlin, recently calculate.The relaxation curve of the accumulation reaction density of pterocarpus santalinus water extract has just produced, and the lax of the water of Lignum pterocarpi indici extract and ethanol is that endothelium relies on and the non-dependence of endothelium.
Result of the test:
The water extract of 0.02g/ml Lignum pterocarpi indici, to by the pretreated vasodilator effect that has large artery trunks ring endothelium, complete of phyenlephrinium, be equivalent to 1 μ M Forskohlin lax effect 60%.
Embodiment 7: concentration is the vasoconstrictor effects of the inhibition phyenlephrinium that relies on of the water extract endothelium of 0.028g/ml Lignum pterocarpi indici
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing and be oxidized with normal saline solution, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11), keeps the temperature of 4 degrees Celsius.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, with a smooth waddy, rub gently inner surperficial, successfully remove interior micromicro and confirm by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine while meeting.The isometric stretching of recording large artery trunks ring by the myograph system that computer is processed.After the balance through at least 1.5 grams of preloading of 90 minutes (this is preloading best in our previous test), the challenge of twice that arterial ring faces the potassium chloride of 60 milliliters in the interval of 30 minutes is to set up a contractile reaction baseline.
With the lax percentage of lax reflection Forskohlin, recently calculate.The relaxation curve of the accumulation reaction density of pterocarpus santalinus water extract has just produced, and the lax of the water of Lignum pterocarpi indici extract and ethanol is that endothelium relies on and the non-dependence of endothelium.
Result of the test:
The water extract of 0.028g/ml Lignum pterocarpi indici, to by the pretreated vasodilator effect that has large artery trunks ring endothelium, complete of phyenlephrinium, be equivalent to 1 μ M Forskohlin lax effect 66%.
Claims (6)
1. the application of the vasodilation that Lignum pterocarpi indici or its water extract that belongs to thing together rely on as endothelium in the medicine of preparation treatment cardiovascular and cerebrovascular disease, it is characterized in that: described medicine also comprises the acceptable excipient of pharmacy, carrier, buffer agent and/or stabilizing agent, wherein, to belong to thing together be red sandalwood, India Lignum pterocarpi indici, Pterocarpus marsupium Roxb., kiaat for described Lignum pterocarpi indici or its.
2. application as claimed in claim 1, is characterized in that: the dosage form of described medicine adopts any dosage form of approving on pharmaceutics.
3. the application as described in claim 1-2 any one, is characterized in that: described application is the application in treatment hypertension.
4. the application as described in claim 1-2 any one, is characterized in that: described application is the application in the medicine of preparation treatment coronary heart disease.
5. the application as described in claim 1-2 any one, is characterized in that: described application is the application in the medicine of preparation prevention and treatment apoplexy
6. the application as described in claim 1-2 any one, is characterized in that: described application is the application in the medicine of preparation prevention and treatment myocardial infarction.
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| CN200810084962.4A CN101530451B (en) | 2008-03-11 | 2008-03-11 | Method for preparing pterocarpus indicus water extract used for endothelium-dependent vasodilation agent and applications of method |
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| CN200810084962.4A CN101530451B (en) | 2008-03-11 | 2008-03-11 | Method for preparing pterocarpus indicus water extract used for endothelium-dependent vasodilation agent and applications of method |
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| CN101530451B true CN101530451B (en) | 2014-09-17 |
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Non-Patent Citations (2)
| Title |
|---|
| 杨菊贤等.糖尿病是一种心血管疾病和心身疾病的观点探讨.《健康教育与健康促进》.2006,第1卷(第3期),73-74. * |
| 王玉芹.紫檀茎皮提取物对实验动物血糖水平的影响.《国外医药.植物药分册》.2002,第17卷(第1期),25. * |
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Free format text: CORRECT: INVENTOR; FROM: CHEN LIHUA MOLARDER FLIDE BIAN KA CHEN ZHENXING ZHAO YONG TO: CHEN LIHUA MOLARDER FLIDE CHEN ZHENXING ZHAO YONG |
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