CN102727616B - Ethyl acetate extract product of Chinese fevervine herb and root and application thereof - Google Patents
Ethyl acetate extract product of Chinese fevervine herb and root and application thereof Download PDFInfo
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- CN102727616B CN102727616B CN201210209139.8A CN201210209139A CN102727616B CN 102727616 B CN102727616 B CN 102727616B CN 201210209139 A CN201210209139 A CN 201210209139A CN 102727616 B CN102727616 B CN 102727616B
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Abstract
The invention relates to an ethyl acetate extract product of Chinese fevervine herb and root and an application thereof. The ethyl acetate extract product of Chinese fevervine herb and root can substantially inhibit activity of butyrylcholine esterase in AD model. Therefore, the ethyl acetate extract product of Chinese fevervine herb and root can be used to prepare drugs for preventing and treating senile dementia.
Description
Technical field
The present invention relates to Chinese medicine extract, be specifically related to a kind of ethyl acetate extract and application thereof of Herba Paederiae.
Background technology
Herba Paederiae, another name: Strepopelia orientalis meal, female green grass or young crops, main dung rattan, but joint, all control that rattan, smelly rattan root, Corii Bovis seu Bubali are frozen, fevervine, smelly rattan, hair calabash, sweet rattan, Herba Schisandrae intermediae, smelly Canis familiaris L. rattan, Fissistigma bracteolatum Chatt., bitch rattan, Herba Solani Lyrati, horseshit rattan, Caulis Sinomenii, smelly dung rattan, chicken foot rattan, expelling summer-heat rattan, beautiful bright sand, chicken discharge rattan, passeris montani saturati rattan.Be Maguireothamnus speciosus Herba Paederiae .Paederia scandens (lour.) merr dry herb, there is effect of expelling wind and removing dampness, analgesic antidotal, promoting digestion and removing stagnation, promoting blood circulation and detumescence.The chemical composition of Herba Paederiae mainly contains volatile oil, iridoid glycoside and flavonoid and other compositions.Volatile oil component is mainly ester, hydrocarbon, ketone, aldehyde, carboxylic acid and organic compounds containing sulfur; Iridoid glycosides has Scandoside, Scandoside methyl ester etc.; Flavone compound is mainly kaempferol and Quercetin and glycoside thereof; Other compositions are that the separation of Petroleum ether extraction position obtains oils and fats and the phytosterin compounds such as hentriacontane, hentriacontanol, Palmic acid and oleanolic acid.
Modern pharmacological research confirmation, Herba Paederiae has following effect:
1, calm, analgesia and anticonvulsant action: Herba Paederiae total alkaloids lumbar injection can suppress mice voluntary activity, extends pentobarbital sodium length of one's sleep, has certain sedation.
2, antibacterial action: 0.5g/ml Herba Paederiae decoct has inhibitory action to external staphylococcus aureus and Fu Shigella flexneri, extractum also has bacteriostasis to staphylococcus aureus and streptococcus pneumoniae.
3, to smooth muscle effect: Herba Paederiae total alkaloids can suppress myenteron and shrink, and can antagonism myenteron contracture due to acetylcholine.
4, other effect: Herba Paederiae injection and ether extract, to Toad Sciatic Nerve specimen-gastrocnemius muscle, all have the local anesthetic action of conduction block.
CN200710152163.1 provides the alcohol extract of Maguireothamnus speciosus Herba Paederiae, and this extract has antiinflammatory, analgesic effect, and its contained active component is iridoid.
CN200810041111.1 Paederosidie Acid is disclosed or containing its plant extract in the application of preparing in anti-influenza A virus medicament.
CN200710022254.3 relates to the purposes of Chinese medicine preparation and the fevervine extract for the treatment of gout.
Senile dementia is the neurodegenerative diseases of serious threat human health.Alzheimer disease (being called for short AD) is a kind of main senile dementia, shows as the ability obstacles such as memory, understanding, calculating, judgement, orientation, language, abstract thinking, oneself's control, causes patient to live on one's own life and loses with ability to work.Along with the acceleration of social senilization, AD has become the 4th disease that causes greatly mankind's death, and China is about to enter aging society, and the rejuvenation trend that presents gradually of this disease, and sickness rate is increasing year by year.Not yet having up to now the effective means of curing senile dementia, is to treat at present the most effective therapeutic modality of senile dementia but take acetylcholinesteraseinhibitors inhibitors (ACHEI).The donepezil (donepezil) using clinically, the medicine ubiquity periphery side effect such as metrifonate (metrifonate) and huperzine A (huperzine A) are larger, the phenomenon that long-term treatment effect is undesirable.Recent studies on shows, gives perfusion selectivity BuCh enzyme inhibitor (BuCHEI) in rat cerebral cortex and can make acetylcholine concentration increase by 15 times, and do not find choline-like side effect.Clinical trial also shows, in cerebrospinal fluid, BuCHE suppresses to have dependency with AD patient's cognitive function.Therefore this is for finding curative effect AD disease, has with low cost, effectively, and the reactive compound that toxic and side effects is little provides new method.
Do not see the ethyl acetate extract of Herba Paederiae and the report of application aspect anti-senile dementia.
Summary of the invention
The object of this invention is to provide a kind of Herba Paederiae extract.
Herba Paederiae extract provided by the invention is the ethyl acetate extract of Herba Paederiae.
The ethyl acetate extract of Herba Paederiae, prepared by following methods: the 70%-90% ethanol extraction that Herba Paederiae is doubly measured with 3-6 2-3 time, each 1-3 hour, merge extractive liquid,, being concentrated into relative density is 1.15-1.20, obtains ethanol concentrated solution, is then extracted with ethyl acetate, collect the first volume, obtain ethyl acetate extract.
Preferably, the ethyl acetate extract of Herba Paederiae, prepared by following methods: 80% ethanol extraction of 3 times of amounts of Herba Paederiae 2 times, each 2 hours, merge extractive liquid,, was concentrated into relative density 1.15-1.20, obtain ethanol concentrated solution, then be extracted with ethyl acetate, collect upper strata, obtain ethyl acetate extract.
The ethyl acetate extract of Herba Paederiae, prepared by following methods: Herba Paederiae petroleum ether diafiltration, first soak 18-36h with petroleum ether, diafiltration is extracted into 3-8 times of medical material amount, reclaim residue, volatilize the petroleum ether in residue, use 70%-90% ethanol extraction, extracting solution concentrates to obtain ethanol concentrated solution, relative density is 1.15-1.20, then be extracted with ethyl acetate, pour out upper strata, obtain ethyl acetate extract.
Preferably, the ethyl acetate extract of Herba Paederiae is prepared by following methods: Herba Paederiae soaks 24h with petroleum ether, and diafiltration is extracted into 5 times of medical material amounts, obtain residue and percolate, volatilize the petroleum ether in residue, the ethanol extraction that is 80% by 3 times of amount volumetric concentrations 2 times, each 2 hours, merge extracted twice liquid, be evaporated to 1.15-1.20, obtain ethanol concentrated solution, use the ethyl acetate extraction with ethanol concentrated solution equivalent, pour out upper strata, obtain ethyl acetate extract.
Preferably, the particle diameter of described Herba Paederiae is 250-850 μ m.The present invention also provides the preparation method of ethyl acetate extract, comprise the following steps: the 70%-90% ethanol extraction that Herba Paederiae is doubly measured with 3-6 2-3 time, each 1-3 hour, merge extractive liquid,, being concentrated into relative density is 1.15-1.20, obtains ethanol concentrated solution, is then extracted with ethyl acetate, collect the first volume, obtain ethyl acetate extract.
The present invention also provides the preparation method of ethyl acetate extract, comprises the following steps: Herba Paederiae petroleum ether diafiltration, first soak 18-36h with petroleum ether, diafiltration is extracted into 3-8 times of medical material amount, reclaim residue, volatilize the petroleum ether in residue, use 70%-90% ethanol extraction, extracting solution concentrates to obtain ethanol concentrated solution, relative density is 1.15-1.20, then uses and the isopyknic ethyl acetate extraction of ethanol concentrated solution, pours out upper strata, concentrate drying, obtains ethyl acetate extract.
The present invention also provides the preparation containing the ethyl acetate extract of Herba Paederiae, is made up of Herba Paederiae ethyl acetate extract and pharmaceutically acceptable carrier or diluent.
The present invention also provides the ethyl acetate extract of Herba Paederiae or the application in the medicine of preparation control senile dementia containing the preparation of the ethyl acetate extract of Herba Paederiae.
The herb that the use position of described Herba Paederiae is Herba Paederiae.
Described pharmaceutically acceptable carrier or diluent refer to the pharmaceutical carrier of pharmaceutical field routine, are selected from one or more in filler, binding agent, disintegrating agent, lubricant, suspending agent, wetting agent, solvent, surfactant or correctives.
Described filler is selected from starch, sucrose, lactose, mannitol, sorbitol, xylitol, microcrystalline Cellulose or glucose etc.;
Described binding agent is selected from cellulose derivative, alginate, starch, dextrin, gelatin or polyvinylpyrrolidone etc.;
Described disintegrating agent is selected from microcrystalline Cellulose, carboxymethyl starch sodium, crospolyvinylpyrrolidone, low-substituted hydroxypropyl cellulose or cross-linking sodium carboxymethyl cellulose;
Described lubricant is selected from stearic acid, Polyethylene Glycol, calcium carbonate, sodium bicarbonate, micropowder silica gel, Pulvis Talci or magnesium stearate;
Described suspending agent is selected from micropowder silica gel, Cera Flava, cellulose, solid polyethylene glycol;
Described wetting agent is selected from glycerol, tween 80, ethyoxyl castor oil hydrogenated or lecithin;
Described solvent is selected from ethanol, liquid polyethylene glycol, isopropyl alcohol, tween 80, glycerol, propylene glycol or vegetable oil, and described vegetable oil is selected from soybean oil, Oleum Ricini, Oleum Arachidis hypogaeae semen, mediation wet goods;
Described surfactant is selected from smooth or Polysorbate (tween) of dodecylbenzene sodium sulfonate, stearic acid, Pluronic F68, fatty acid Pyrusussuriensis etc.;
Described correctives is selected from aspartame, Sucralose, essence, citric acid or saccharin sodium.
Described preparation is tablet, dragee, capsule, injection, solution, emulsion, ointment, emulsifiable paste, inhalant, aerosol or suppository.
The extract of Herba Paederiae provided by the invention has the following advantages:
1, the invention provides the ethyl acetate extract of Herba Paederiae, can be by after ethanol extraction, ethyl acetate extraction obtains; Also can, by petroleum ether lixiviate, after ethanol extraction, be extracted with ethyl acetate, obtain.
2, the ethyl acetate extract of Herba Paederiae can significantly suppress the activity of butyrylcholine esterase in AD model, and therefore, the ethyl acetate extract of Herba Paederiae can be for the preparation of the medicine of senile dementia prevention and cure.
Detailed description of the invention
Following examples are used for illustrating the present invention, but are not used for limiting the scope of the invention.
Embodiment 1: the ligroin extraction of Herba Paederiae
Getting the herb of Herba Paederiae pulverizes, cross No. two sieves (particle diameter be 850 μ m), get 500 grams of coarse powder, with after petroleum ether immersion 24h, diafiltration is extracted into percolate (being equivalent to 5 times of medical material amounts) of light color, collects percolate, and it is 1.15-1.20 that percolate is evaporated to relative density, spraying is dry, obtains ligroin extraction 8.54g.
Embodiment 2: the ethanol of Herba Paederiae and ethyl acetate extract
Getting the herb of Herba Paederiae pulverizes, particle diameter 500 μ m, get 500 grams of coarse powder, with after petroleum ether immersion 16h, diafiltration is extracted into percolate color and shoals (being equivalent to 5 times of medical material amounts), collect residue and percolate, residue is volatilized to petroleum ether, with 80% ethanol extraction 2 times of 3 times of amount volumes, each 2 hours, merge extracted twice liquid, be evaporated to without alcohol taste (relative density is 1.15-1.20), obtain ethanol concentrated solution, used the ethyl acetate extraction with ethanol concentrated solution equivalent (volume), emit lower floor, be concentrated into and do as ethanol extraction; Pour out upper strata, be concentrated into dryly, obtain 1.20g ethyl acetate extract (yield is 0.24%).
Embodiment 3: the ethanol of Herba Paederiae and ethyl acetate extract
Getting the herb of Herba Paederiae pulverizes, particle diameter 850 μ m, get 500 grams of coarse powder, with after petroleum ether immersion 24h, diafiltration is extracted into percolate color and shoals (being equivalent to 5 times of medical material amounts), collect residue and percolate, residue is volatilized to petroleum ether, with 80% ethanol extraction 2 times of 3 times of amount volumes, each 2 hours, merge extracted twice liquid, be evaporated to without alcohol taste (relative density is 1.15-1.20), obtain ethanol concentrated solution, use the ethyl acetate extraction with ethanol concentrated solution equivalent (volume), emit lower floor, be concentrated into and do as ethanol extraction; Pour out upper strata, be concentrated into dryly, obtain 1.50g ethyl acetate extract (yield is 0.3%).
Embodiment 4: the ethyl acetate extract of Herba Paederiae
Getting the herb of Herba Paederiae pulverizes, particle diameter 250 μ m, get 500 grams of coarse powder, with after petroleum ether immersion 36h, diafiltration is extracted into percolate color and shoals (being equivalent to 5 times of medical material amounts), collect residue and percolate, residue is volatilized to petroleum ether, with 80% ethanol extraction 3 times of 5 times of amount volumes, each 1.5 hours, merge three times extracting solution, be evaporated to without alcohol taste (relative density is 1.15-1.20), obtain ethanol concentrated solution, use the ethyl acetate extraction with ethanol concentrated solution equivalent (volume), emit lower floor, be concentrated into and do as ethanol extraction; Pour out upper strata, be concentrated into dryly, obtain 1.40g ethyl acetate extract (yield is 0.28%).
Embodiment 5: the ethanol extraction of Herba Paederiae and ethyl acetate extract
Getting the herb of Herba Paederiae pulverizes, particle diameter 250 μ m, get 350 grams of coarse powder, with 80% ethanol extraction 2 times of 6 times of amount volumes, each 2 hours, merge extracted twice liquid, be evaporated to without alcohol taste (relative density is 1.15-1.20), obtain ethanol concentrated solution, use the ethyl acetate extraction with ethanol concentrated solution equivalent (volume), emit lower floor, be concentrated into and do as ethanol extraction; Pour out upper strata, be concentrated into dryly, obtain 3.50g ethyl acetate extract (yield is 0.7%).
Embodiment 6: the tablet that contains the ethyl acetate extract of Herba Paederiae
1, composition: ethyl acetate extract (the method preparation of the embodiment 3) 50g of Herba Paederiae, starch 15g, microcrystalline Cellulose 20g, magnesium stearate 6g.
2, preparation method: take supplementary material according to proportioning, according to the equivalent method mix homogeneously that progressively increases, direct compression.
Embodiment 7: the water extract of Herba Paederiae
Herba Paederiae herb is boiled 3 times with the decocting of 6 times of amounts, and extraction time is respectively 2,1.5,1.5 hours, united extraction thing, the concentrated water extract that obtains of extracting solution.
Experimental example 1: Herba Paederiae active site suppresses active mensuration to butyrylcholine esterase
1, experimental principle
Butyrylcholine esterase (BuChE) hydrolysis BuCh (BuCh) generates choline and butanoic acid, choline can with sulfydryl developer 5, two nitrobenzoic acid (DTNB) reactions of 5-bis-sulfur generate TNB yellow compound, carry out colorimetric assay according to shade, the quantity of hydrolyzate choline can be reacted the vigor of BuChE.
2, Experimental agents: BuChE, substrate B uCh, developer DTNB, all purchased from Acros company; Tetra isopropyl octamethylphyropyosphoramide (Iso-OMPA), purchased from SIGMA company; Dimethyl sulfoxide (DMSO), purchased from Shanghai City Xin Cheng Chemical Co., Ltd..
3, experiment grouping and method
Grouping: sample sets: numbering DF9550-9603, certainly preparation;
Positive control drug: tetra isopropyl octamethylphyropyosphoramide (Iso-OMPA);
Herba Paederiae ligroin extraction group: product prepared by embodiment 1, (get appropriate ligroin extraction DMSO and dissolve, being diluted with water to concentration is 50 μ L/mL);
Herba Paederiae ethanol extraction group: ethanol extraction prepared by embodiment 3, (get appropriate ethanol extraction DMSO and dissolve, being diluted with water to concentration is 50 μ L/mL)
Herba Paederiae ethyl acetate extract group: ethyl acetate extract prepared by embodiment 3, (get appropriate ethyl acetate extract DMSO and dissolve, being diluted with water to concentration is 50 μ L/mL)
Herba Paederiae water extract group: product prepared by embodiment 7, (get suitable quantity of water extract DMSO and dissolve, being diluted with water to concentration is 50 μ L/mL)
In enzyme reaction system, finite concentration testing compound and BuChE are suspended in (pH7.2) in reaction buffer, add quantitative substrate B uCh and developer DTNB, and 37 ° of C were hatched after 60 minutes, measure light absorption value at wavelength 412nm.The amount that the light absorption value of reaction system consumes BuCh in can reflection system.Can the suppression ratio of computerized compound to BuChE activity according to the change of light absorption value.
3, experimental result: in table 1
Table 1.: the inhibitory action of the each position of Herba Paederiae to butyrylcholine esterase vigor
| Group | Concentration | Suppression ratio % | IC50（ug/mL） |
| Tetra isopropyl octamethylphyropyosphoramide (ISO-OMPA) | 50 | 94.43 | 8.95 |
| Herba Paederiae ligroin extraction | 50 | 15.40 | —— |
| Herba Paederiae ethanol extraction | 50 | 40.04 | —— |
| Herba Paederiae ethyl acetate extract | 50 | 66.92 | 12.415 |
| Herba Paederiae water extract | 50 | 11.45 | —— |
Table 1 result shows: the ethyl acetate extract of Herba Paederiae provided by the invention has stronger butyrylcholine esterase inhibitory action.
Equally, ethyl acetate extract prepared by additive method provided by the invention is tested, and the ethyl acetate extract that effect and embodiment 3 provide is similar.
Conclusion: the ethyl acetate extract of Herba Paederiae can significantly suppress the activity of butyrylcholine esterase in AD model, therefore, the ethyl acetate extract of Herba Paederiae can be for the preparation of the medicine of senile dementia prevention and cure.
Although, above use general explanation, detailed description of the invention and test, the present invention is described in detail, on basis of the present invention, can make some modifications or improvements it, and this will be apparent to those skilled in the art.Therefore, these modifications or improvements without departing from theon the basis of the spirit of the present invention, all belong to the scope of protection of present invention.
Claims (6)
1. the extract of a Herba Paederiae, this extract is the ethyl acetate extract of Herba Paederiae, and the ethyl acetate extract of described Herba Paederiae is prepared by following methods: Herba Paederiae soaks 18-36h with petroleum ether, and diafiltration is extracted into 3-8 times of medical material amount, reclaim residue, volatilize the petroleum ether in residue, use 70%-90% ethanol extraction, extracting solution concentrates to obtain ethanol concentrated solution, relative density is 1.15-1.20, be extracted with ethyl acetate, pour out upper strata, obtain ethyl acetate extract.
2. ethyl acetate extract according to claim 1, it is characterized in that, the ethyl acetate extract of Herba Paederiae is prepared by following methods: Herba Paederiae soaks 24h with petroleum ether, diafiltration is extracted into 5 times of medical material amounts, obtain residue and percolate, the petroleum ether of residue is volatilized, the ethanol extraction that is 80% by 3 times of amount volumetric concentrations 2 times, each 2 hours, merge extracted twice liquid, be evaporated to 1.15-1.20, obtain ethanol concentrated solution, with extracting with the ethyl acetate of ethanol concentrated solution equivalent, pour out upper strata, obtain ethyl acetate extract.
3. prepare the method for the extract described in claim 1 or 2 for one kind, it is characterized in that, the method comprises the following steps: get Herba Paederiae petroleum ether and soak 18-36h, diafiltration is extracted into 3-8 times of medical material amount, reclaim residue, volatilize petroleum ether, use 70%-90% ethanol extraction, extracting solution concentrates to obtain ethanol concentrated solution, relative density is 1.15-1.20, be extracted with ethyl acetate, pour out upper strata, obtain ethyl acetate extract.
4. containing the preparation of extract described in claim 1 or 2, it is characterized in that, described preparation is to be made up of the ethyl acetate extract of Herba Paederiae and pharmaceutically acceptable carrier or diluent.
5. preparation according to claim 4, is characterized in that, described preparation is tablet, dragee, capsule, injection, solution, emulsion, ointment, emulsifiable paste, inhalant, aerosol or suppository.
6. the application of the preparation containing Herba Paederiae ethyl acetate extract described in the extract described in claim 1 or 2 or claim 4 or 5 in the medicine of preparation control senile dementia.
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| CN115137676B (en) * | 2021-03-30 | 2024-03-26 | 海南师范大学 | Paederia scandens extract and application thereof in preparing toothpaste |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101129524A (en) * | 2007-09-18 | 2008-02-27 | 蒋毅 | Paederia extractive and medical use of the same |
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| CN101129524A (en) * | 2007-09-18 | 2008-02-27 | 蒋毅 | Paederia extractive and medical use of the same |
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| Title |
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| 丹皮乙醇提取物的抗糖尿病活性研究;李盼盼等;《中国动物保健》;20120228;第14卷(第2期);19-20 * |
| 李盼盼等.丹皮乙醇提取物的抗糖尿病活性研究.《中国动物保健》.2012,第14卷(第2期),19-20. |
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