CN102526148A - New use of erigeron breviscapus extract for preparation of medicaments - Google Patents
New use of erigeron breviscapus extract for preparation of medicaments Download PDFInfo
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Abstract
The invention discloses the use of erigeron breviscapus extract for the preparation of medicaments for inhibiting beta-amyloid peptide accumulation and fibril formation. The erigeron breviscapus extract is total phenol extract prepared by extracting the whole plant of erigeron breviscapus, and contains flavonoids compounds and caffeoylquinic acid esters compounds. Experimental researches show that the erigeron breviscapus extract can remarkably inhibit the accumulation of A beta1-42, intracellularly improve apoptosis and inflammation induced by the A beta1-42 and reduce intracellular oxidative stress by clearing reactive oxygen species (ROS) such as malondialdehyde (MDA) so as to achieve the effect of protecting nerve cells and improve the activity of the nerve cells; in addition, the erigeron breviscapus extract has low toxicity to the nerve cells; and therefore, the erigeron breviscapus extract can be used for the preparation of the medicaments for treating or preventing related diseases caused by the beta-amyloid peptide accumulation and the fibril formation.
Description
Technical field
The present invention relates to Herba Erigerontis extract and suppress the purposes in beta-amyloid polypeptide 1-gathering and the fibroplastic medicine, belong to technical field of Chinese medicines in preparation.
Background technology
Alzheimer's disease (Alzheimers Disease; AD) be a kind of old people's of betiding constitutional central nervous system degenerative disorders; Its main pathological characters comprises that brain is local; Especially Hippocampus and cortical neuron degeneration change, neurofibrillary tangles and extracellular senile plaque deposition in the cell.The sickness rate of AD is high, has brought a lot of inconvenience for patient's live and work, has caused heavy social burden and financial burden for individual, family, society.The pathogeny of research AD discloses its pathophysiological process, and the exploitation that provides further therapy apparatus can reach novel drugs has important social and is worth and economic worth, and important Research Significance is arranged.
Pathology damage process about AD has proposed a lot of hypothesis (Kaltschmidt B, et al.Proc Natl Acad Sci USA, 1999,96 (16): 9409-9414).The neurodegenerative diseases hypothesis that axoplasm transportation obstacle causes thinks that it is the inducement of AD that associated gene mutation causes attitude structural change of Tau protein aggregation and changing function.The cholesterol transformant doctrine thinks that then it is the key reason that causes AD pathological changes such as synaptic plasticity infringement, deterioration of neurons that the cholesterol stable state changes, and variations such as amyloid plaques, Tau phosphorylation and cytoskeleton, oxidative pressure all are the compensation responses of pin brain inner cholesterol dynamic variation.A β (β-amyloid pepide, beta-amyloid polypeptide 1-) hypothesis thinks, to be a kind of express because genetic flaw directly or indirectly changes amyloid precursor protein (APP) AD or the proteolysis process influence the stable pathology syndrome of A beta peptide aggregation; Balance between A β produces and removes changes gradually, and the A β accumulation of state of aggregation causes consecutive complex reaction, comprises the variation of synapse/projection; The Tau protein phosphorylation; Mediator is lost, and neuronal function imbalance, death finally appear in gliosis and inflammatory reaction etc.; Speckle forms, and neurofibril twines long-pending grade for pathological phenomenon.
Go deep into along with what AD was studied, the A beta hypothesis that takes place about disease has obtained deep development, and more and more evidences shows that A β possibly be the constitutional pathology factor that AD takes place.At first almost in all patients' AD brain, all found changes such as a large amount of amyloid plaques depositions and teleneuron degeneration, and directly be directly proportional with the mental extent of damage in the quantity of the key area speckle relevant with learning and memory.The main toxic component of senile plaque is the beta amyloid peptide that amyloid precursor (APP) produces, and early stage A β dispersivity speckle is similar to cholesterol fat stricture of vagina, and sophisticated senile plaque is similar with atheromatous plaque.Other human amyloidogenic diseases; Often just can successfully treat this type disease as long as suppress the generation of pathogenic starch peptide; Also bring hope, just might find the method for treatment AD in case illustrate the incidence and development mechanism of A β, even untie the answer to a riddle of human learning and memory to research worker.Therefore, if can: 1. suppress the formation of A β peptide; 2. suppress the gathering (neurotoxicity that suppresses A β) of A β, quicken degraded and the removing of A β; Just can alleviate AD patient's symptom, even reach the sick purpose of treatment AD.
Simultaneously, A beta peptide aggregation and fiber form can also cause vascular amyloid pathological changes, and then the illness of grading in bringing out.So far, do not find as yet and can effectively effect a radical cure the medicine of vascular amyloid pathological changes.
Herba Erigerontis is a Compositae Herba Erigerontis aceris platymiscium Erigeron breviscapus (Vant.) Hand.-Mazz. (Erigeron breviscapus), can expelling cold and relieving exterior syndrome, and expelling wind and removing dampness, activating collaterals to relieve pain.Be usually used in headache due to common cold, toothache, stomachache, rheumatalgia, the paralysis that cerebrovascular accident causes etc.Be main often clinically with Herba Erigerontis, in conjunction with other integrative medicine therapy, back something lost such as treatment hypertensive cerebral hemorrhage, cerebral thrombosis, cerebral embolism, polyneuritis, chronic arachnoiditis paralysed disease.Existing a plurality of patents are around the application (Chinese invention patent ZL03117754, ZL01115358.X, ZL0213750.X, ZL03117753.0 etc.) of Herba Erigerontis at the treatment treating cardiac and cerebral vascular diseases; Simultaneously; Also be used to treat vascular senile dementia report (Li Fuhui, the clinical research of Herba Erigerontis injection associating piracetam treatment vascular dementia, Chinese practical sacred disease magazine relevant for Herba Erigerontis; 2011,14:10-13).
But suppress that beta-amyloid polypeptide 1-is assembled and fiber forms activity and is used for anti senile dementia drug based on the beta-amyloid polypeptide 1-hypothesis and all do not appear in the newspapers about Herba Erigerontis.
Summary of the invention
The objective of the invention is to: the new purposes of a kind of Herba Erigerontis extract in the preparation medicine is provided.Research shows that Herba Erigerontis extract has significant inhibitory effect to the gathering of A β, and the beta induced neurocyte toxicity of A is had good protective action, can be used for preparation and suppresses beta-amyloid polypeptide 1-gathering and fibroplastic medicine.
Technical scheme of the present invention: Herba Erigerontis extract suppresses the purposes in beta-amyloid polypeptide 1-gathering and the fibroplastic medicine in preparation.
Herba Erigerontis extract also can be used for preparing treatment or prevention is assembled owing to beta-amyloid polypeptide 1-and the medicine of the disease that fiber formation causes.
Aforesaid Herba Erigerontis extract is the total phenols extract that contains flavone compound and caffeoyl quinic acid ester type compound that is extracted preparation by the herb of feverfew Herba Erigerontis (Erigeron breviscapus).
Aforementioned Herba Erigerontis extract is preparation like this: get the Herba Erigerontis herb, pulverize, extract 2～3 times with lower alcohol solvent; Merge extractive liquid,, concentrating under reduced pressure reclaims solvent, concentrated solution dilute with water; Filter, phenylethylene macroporous adsorbent resin on the filtrating is after water elution is extremely colourless; Alcoholic solution eluting with 30%～95%, elution volume are 3～20 times of column volumes; Eluent concentrates, and using 10% sodium hydroxide solution adjust pH is 7.0～7.5, and spray drying gets pale brown toner end, i.e. Herba Erigerontis total phenols extract then.
Aforementioned Herba Erigerontis extract also can prepare like this: get the Herba Erigerontis herb, pulverize, extract 2～3 times merge extractive liquid, with lower alcohol solvent; Concentrating under reduced pressure reclaims solvent, and the concentrated solution dilute with water is earlier with No. 120 gasoline extraction defats; Water layer is with ethyl acetate extraction 3～4 times, and the combined ethyl acetate part concentrates; Remove and desolvate, get pale brown toner end, i.e. Herba Erigerontis total phenols extract.
Used lower alcohol was methanol or ethanol when aforementioned Herba Erigerontis extract prepared.
The content of scutellarin is 0.1%～50% in the flavone compound that contains in the aforementioned Herba Erigerontis extract.
The content of total caffeoyl quinic acid ester is 10%～99% in the caffeoyl quinic acid ester type compound that contains in the aforementioned Herba Erigerontis extract.
Contain 4 in the aforementioned caffeoyl quinic acid ester type compound, 5-dicaffeoyl-quinic acid ester, 3,5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1,5-dicaffeoyl-quinic acid ester and Erigeroster B.
In order to ensure effect of the present invention, the applicant has carried out pharmacological experiment study to described Herba Erigerontis extract, and is specific as follows:
1, Herba Erigerontis extract and wherein main component to the accumulative inhibitory action of beta-amyloid polypeptide 1-
A β
1-42Lyophilized powder adds PBS (pH=7.4) buffer solution of 50mM again with a small amount of 0.1% ammonia solvent, is made into the A β of 1mM
1-42Storing solution, the PBS of reuse 50mM (pH=7.4) buffer solution dilutes, and is made into to contain A β
1-42The solution of 45 μ M; The following sample that perhaps adds 100 μ g/mL respectively: Herba Erigerontis extract, scutellarin, Erigeroster B, 4,5-dicaffeoyl-quinic acid ester, 3,5-dicaffeoyl-quinic acid ester, 1; 3-dicaffeoyl-quinic acid ester, 1; 5-dicaffeoyl-quinic acid ester, cofabrication 18 parts of every kind of sample solution, every part of volume 200 μ L.Different sample solutions are respectively got 2 parts and under 37 ℃ of water-baths, were hatched 0,1,2,4,6,8,12,24,36 hour respectively.Hatch regulation during the moment, take out sample solution, with ice bath cooling quencher aggreation.The PBS buffer 200 μ L that add the fluorescein ThT that contains 3 μ M then, mix homogeneously is measured its fluorescent value at once on the F-4600 spectrofluorophotometer.Excitation wavelength is 445 λ m, and emission wavelength is 490 λ m, and each sample is got 2 parts of measured in solution on the time point, averages.
Shown in accompanying drawing 1, A β
1-42Solution begins to form aggregation in solution after hatching different time under 37 ℃ of water-baths, add ThT in the system after, with accumulative A β
1-42In conjunction with, excite down at 445 λ m light, produce the emission light of absorption maximum in 490 λ m places, its fluorescent value is along with A β
1-42The increase of concentration class and increasing.After arriving certain hour, to assemble fully basically, fluorescent value is also basicly stable.Can find out that from Fig. 1 after 12 hours, gathering reaches balance basically.
When containing certain density agglutination inhibitor in the sample solution, A β
1-42Aggregation extent is suppressed, and fluorescent value significantly descends.Can find out that from accompanying drawing 1 Herba Erigerontis extract can significantly suppress A β
1-42Gathering, and, the main component of Herba Erigerontis extract (scutellarin, Erigeroster B, 4; 5-dicaffeoyl-quinic acid ester, 3; 5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1,5-dicaffeoyl-quinic acid ester) inhibitory action in various degree all arranged.
Originally experiment showed, that Herba Erigerontis extract can significantly suppress A β
1-42The gathering of (being beta-amyloid polypeptide 1-) is a kind of A β
1-42Agglutination inhibitor.
2, Herba Erigerontis extract is to the toxicity test of neurocyte
Get be in exponential phase the PC12 cell inoculation in 96 orifice plates, plate is put in 37 ℃, 5%CO
2Cultivate in the incubator.Experiment is divided into normal control group, sample effect group.Normal group adds corresponding solvent behind the 24h, and sample sets adds 10 each samples of μ l, puts and abandons culture fluid in the incubator behind the 24h; Every hole adds fresh 1640 culture medium, 90 μ l; Normal group adds corresponding solvent, behind 24h, detects with mtt assay, surveys the light absorption value in the every hole of 570nm wavelength with ELIASA.Parallel 3 holes of each concentration in the experiment, experiment repetition 3 times.Suppression ratio according to formula calculation sample pair cell:
Sample is to PC12 cell inhibiting rate=(normal group absorbance one sample sets absorbance)/normal group absorbance * 100%
Sample sets adopts Herba Erigerontis extract respectively, and result of the test is referring to accompanying drawing 2.It is thus clear that Herba Erigerontis extract does not show significant cytotoxicity to the PC12 cell, can be applied to A beta peptide aggregation inhibitor safely.
3, Herba Erigerontis extract is to the Cytotoxic protective effect of the inductive PC12 of beta-amyloid polypeptide 1-
The take the logarithm PC12 cell of trophophase is blown and beaten into single cell suspension, is inoculated on 96 well culture plates; Add variable concentrations Herba Erigerontis extract, scutellarin, Erigeroster B, 4 respectively; 5-dicaffeoyl-quinic acid ester, 3,5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1; 5-dicaffeoyl-quinic acid ester sample pretreatment 24h adds 10 μ l, 10 μ molL with model group more simultaneously
-1A β
1-42, continue to cultivate 24h.After having cultivated, every hole adds MTT 20 μ l (final concentration 5mg/ml), hatches 4 hours for 37 ℃, adds three liquid, 50 μ l again, puts in the incubator and spends the night, and measures the light absorption value (OD value) in the every hole of wavelength 570nm wavelength with ELIASA.Calculate the cells survival rate according to formula:
Survival rate=(each processed group absorbance one blank control group absorbance)/(matched group absorbance-blank control group absorbance) * 100%
Visible by accompanying drawing 3, Herba Erigerontis extract and wherein main component can both reduce A β significantly
1-42To the toxic action of neurocyte, particularly Herba Erigerontis extract and Erigeroster B, 3, the effect of 5-dicaffeoyl-quinic acid ester etc. is obvious, and significant neuroprotective is arranged.
4, Herba Erigerontis extract is to producing the scavenging action of MDA in the inductive PC12 cell of beta-amyloid polypeptide 1-
The take the logarithm PC12 cell of trophophase is inoculated on 96 well culture plates, adds variable concentrations Herba Erigerontis extract, scutellarin, Erigeroster B, 4 respectively; 5-dicaffeoyl-quinic acid ester, 3; 5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1,5-dicaffeoyl-quinic acid ester; Pretreatment 24h adds 10 μ l10 μ molL with model group more simultaneously
-1A β
1-42, continue to cultivate 24h and measure.During mensuration, each group cell with piping and druming pipe piping and druming sucking-off, is placed the centrifuge tube of 1.5ml, the centrifugal 10min of 1600r abandons supernatant, washes 2 times with the PBS buffer of pre-cooling then, discards residual PBS.With cell precipitation place 4 ℃ subsequent use.In each group cell precipitation, add the non-DC lysate of 100 μ l pre-coolings, it is dispelled with the rifle head, let the abundant mixing of cell pyrolysis liquid and cell, place 4 ℃ of cracking 30min then.After lysis was good, the centrifugal 10min of 1600r got 100 μ l supernatants and shifts the mensuration of in a new centrifuge tube, carrying out index.
Take by weighing an amount of TBA, using TBA preparation liquid to be mixed with concentration is 0.37% TBA storage liquid.The TBA storage liquid room temperature for preparing keeps in Dark Place.To promote the dissolving of MDA testing liquid, the MDA testing liquid for preparing must use the same day through supersound process.
Suitably solution is as blank in centrifuge tube, to add 0.1ml homogenate, lysate or PBS etc., and the above-mentioned variable concentrations standard substance of adding 0.1ml are used for the production standard curve, adds the 0.1ml sample and is used for measuring; Add 0.2ml MDA testing liquid subsequently.
Visible by accompanying drawing 4, Herba Erigerontis extract and wherein main component all can significantly reduce PC12 cell endogenous cause of ill and receive A β
1-42The products of oxidative stress MDA that stimulates and raise.Wherein with Herba Erigerontis extract and Erigeroster B, 3,5-dicaffeoyl-quinic acid ester etc. are the most remarkable.
Experimental result shows that Herba Erigerontis extract can effectively be removed the neurocyte endogenous cause of ill and receive A β
1-42The products of oxidative stress MDA that stimulates and raise, Herba Erigerontis extract possibly pass through antioxidation, reaches protecting neuron from acute.
5, Herba Erigerontis extract is to the influence of caspase-3/7 protein expression in the inductive PC12 cell of beta-amyloid polypeptide 1-
The take the logarithm PC12 cell of trophophase is inoculated on 96 well culture plates, adds variable concentrations Herba Erigerontis extract, scutellarin, Erigeroster B, 4 respectively; 5-dicaffeoyl-quinic acid ester, 3; 5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1,5-dicaffeoyl-quinic acid ester; Pretreatment 24h adds 10 μ l10 μ molL with model group more simultaneously
-1A β
1-42, continue to cultivate 24h.During mensuration, with Caspase-Glo
TMBuffer adds Caspase-Glo
TMIn the substrate reagent bottle, put upside down mixing and thoroughly dissolve, be made into Caspase-Glo up to substrate
TMReagent.96 orifice plates that will contain cultured cell take out equilibrium at room temperature from incubator; Simultaneously also the Caspase-Glo for preparing
TMThe reagent equilibrium at room temperature.In cell culture, add isopyknic reagent, mix 30s, incubated at room 30min with the 300-500rpm light shaking.Sample panel is put into GloMax
TMDetect in the luminous detection appearance.
Visible by accompanying drawing 5; Herba Erigerontis extract can significantly reduce the neurocyte endogenous cause of ill and stimulated and the remarkable caspase-3/7 protein expression that raises by beta-amyloid polypeptide 1-, shows that Herba Erigerontis extract maybe be through inducing neuronal apoptosis to play neuroprotective to blocking-up or inhibition beta-amyloid polypeptide 1-.
6, Herba Erigerontis extract is to the influence of NF-κ b protein expression in the inductive PC12 cell of beta-amyloid polypeptide 1-
The take the logarithm PC12 cell of trophophase is inoculated on 96 well culture plates, adds variable concentrations Herba Erigerontis extract and main component (scutellarin, Erigeroster B, 4 respectively; 5-dicaffeoyl-quinic acid ester, 3; 5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1,5-dicaffeoyl-quinic acid ester); Pretreatment 24h adds 10 μ l, 10 μ molL with model group more simultaneously
-1A β
1-42, continue to cultivate 24h and measure.Each group cell with piping and druming pipe piping and druming sucking-off, is placed the centrifuge tube of 1.5ml, and the centrifugal 10min of 1600r abandons supernatant, washes 2 times with the PBS buffer of pre-cooling then, discards residual PBS.With cell precipitation place 4 ℃ subsequent use.In each group cell precipitation, add the non-DC lysate of 100 μ l pre-coolings, it is dispelled with the rifle head, let the abundant mixing of cell pyrolysis liquid and cell, place 4 ℃ of cracking 30min then.After lysis was good, the centrifugal 10min of 1600r got 100 μ l supernatants and shifts the mensuration of in a new centrifuge tube, carrying out index.
With the blank value zeroing, the 450nm wavelength is measured the absorbance in each hole in regular turn.Mensuration should be after adding stop buffer be carried out with interior in 15 minutes.
Visible by accompanying drawing 6, Herba Erigerontis extract and wherein main component can significantly lower the NF-κ b protein expression that PC12 cell endogenous cause of ill beta-amyloid polypeptide 1-is induced and significantly increase.The result shows that Herba Erigerontis extract maybe be through suppressing A β
1-42To the inflammatory stimulus of neurocyte and reach neuroprotective.
Above The pharmacological results shows that Herba Erigerontis extract can significantly suppress A β
1-42Gathering, and in cell, improve because of A β
1-42Induce apoptosis, the inflammation of generation,, reduce oxidative stress in the cell, thereby reach, increase the neurocyte vigor protecting neuron from acute through removing ROS (like MDA); Simultaneously, Herba Erigerontis extract itself is very little to neurocyte toxicity; So Herba Erigerontis extract can be used for because beta-amyloid polypeptide 1-is assembled and fiber forms in the treatment or prophylactic agent preparation of the relevant disease that causes.
Description of drawings
Fig. 1 be Herba Erigerontis extract and wherein main component to beta-amyloid polypeptide 1-(A β
1-42) accumulative inhibitory action curve chart;
Fig. 2 is the cytotoxic effect sketch map of Herba Erigerontis extract to the PC12 neurocyte;
Fig. 3 be Herba Erigerontis extract and wherein main component to beta-amyloid polypeptide 1-(A β
1-42) the Cytotoxic protective effect design sketch of inductive PC12;
Fig. 4 be Herba Erigerontis extract and wherein main component to beta-amyloid polypeptide 1-(A β
1-42) the impact effect figure of MDA in the inductive PC12 cell;
Fig. 5 be Herba Erigerontis extract and wherein main component to beta-amyloid polypeptide 1-(A β
1-42) Caspase-3/7 expresses in the inductive PC12 cell impact effect figure;
Fig. 6 be Herba Erigerontis extract and wherein main component to beta-amyloid polypeptide 1-(A β
1-42) variation of Nf-κ b content is expressed in the inductive PC12 cell impact effect figure.
In Fig. 1, Fig. 3-Fig. 6: 0-A β
1-42The 1-Herba Erigerontis extract; The 2-scutellarin; The 3-Erigeroster B; 4-4,5-dicaffeoyl-quinic acid ester; 5-3,5-dicaffeoyl-quinic acid ester; 6-1,3-dicaffeoylquinic acid ester; 7-1,5-dicaffeoyl-quinic acid ester.
The specific embodiment
Embodiments of the invention 1: the preparation of Herba Erigerontis extract
Get Herba Erigerontis herb 5kg, pulverize, add about 15 liters of 70% ethanol, be as the criterion to flood medical material and to exceed slightly; Reflux 1 hour, inclining liquid, continue to add an amount of 70% ethanol, repeats same operation, extracts 3 times, at last-inferior medicinal residues are filtered.Merging filtrate, 40～60 ℃ are evaporated to about 5 liters of volume, and concentrated solution is diluted with water to 10 liters, filters, and removes filtering residue.Filtrating is adsorbed distribution on pretreated AB-8 macroporous adsorptive resins, earlier with 30 premium on currency eluting, and 20 liter of 80% ethanol eluting of reuse.80% ethanol eluent is concentrated into about 1 liter, and using 10% sodium hydroxide solution adjust pH is about 7.0, and spray drying gets pale brown toner end, must measure to be that 126g, yield are 2.52% (in Herba Erigerontis herb raw material).This powder is Herba Erigerontis extract I., quantitative analysis qualitative through HPLC; Contain flavonoid component and caffeoyl quinic acid esters component among the Herba Erigerontis extract I; Wherein main flavonoid component scutellarin content is 10.5%; In the caffeoyl quinic acid esters component 4,5-dicaffeoyl-quinic acid ester, 3,5-dicaffeoyl-quinic acid ester and Erigeroster B content are respectively 5.6%, 4.1% and 12.8%.
Embodiments of the invention 2: the preparation of Herba Erigerontis extract
Get Herba Erigerontis herb 5kg, pulverize, add about 15 liters of 70% ethanol, be as the criterion to flood medical material and to exceed slightly; Reflux 1 hour, inclining liquid, continues to add an amount of 70% ethanol, repeats same operation, extracts 3 times, for the last time medicinal residues is filtered.Merging filtrate, 40～60 ℃ are evaporated to about 5 liters of volume, and concentrated solution is diluted with water to 10 liters; Earlier with No. 120 gasoline extraction defats, water layer is with ethyl acetate extraction 3-4 time, combined ethyl acetate part; Concentrating under reduced pressure is removed ethyl acetate, gets pale brown toner end; Must measure and be that 138g, yield are 2.76% (in Herba Erigerontis herb raw material).This powder is Herba Erigerontis extract II., quantitative analysis qualitative through HPLC; Contain flavonoid component and caffeoyl quinic acid esters component among the Herba Erigerontis extract II; Wherein main flavonoid component scutellarin content is 6.5%; In the caffeoyl quinic acid esters component 4,5-dicaffeoyl-quinic acid ester, 3,5-dicaffeoyl-quinic acid ester and Erigeroster B content are respectively 7.4%, 6.2% and 15.6%.
Embodiments of the invention 3: the separation of main component in the Herba Erigerontis extract
Get Herba Erigerontis extract I 50g, cross sephadex LH-20 gel chromatography column, methanol-water solution gradient eluting (0% → 100%) gets 3 parts, and each part is carried out the ODS column chromatography more respectively, respectively with methanol-water solution gradient eluting (30% → 100%).Obtain chemical compound 1 from first, obtain 2, the three parts of chemical compound from second portion and obtain two positions respectively, further carry out purification again, obtain chemical compound 3-6 respectively with HPLC.Chemical compound 1-6 is accredited as scutellarin, 4 respectively, 5-dicaffeoyl-quinic acid ester, 3,5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1,5-dicaffeoyl-quinic acid ester, Erigeroster B.
Embodiment 4: the application of Herba Erigerontis extract
The preparation of medicinal tablet: get the Herba Erigerontis extract I 100g, starch 50g, 10% starch slurry 10g and the magnesium stearate 2g that make among the embodiment 1; Behind Herba Erigerontis extract I and starch mix homogeneously, add 10% starch slurry and process soft material, cross 14 mesh sieves and granulate, dry under 70-80 ℃ of temperature, cross 12 mesh sieve granulate, after adding magnesium stearate and mixing, be pressed into 1000, promptly get tablet.Every contains Herba Erigerontis extract I 100mg.Said preparation can be used for treating or prevents because beta-amyloid polypeptide 1-is assembled and fiber forms the senile dementia that causes.
Embodiment 5: the application of Herba Erigerontis extract
The preparation of medicinal tablet: get the Herba Erigerontis extract I 50g that makes among the embodiment 1, the Herba Erigerontis extract II 50g that makes among the embodiment 2, starch 50g, 10% starch slurry 10g and magnesium stearate 2g; Behind Herba Erigerontis extract I and II and starch mix homogeneously, add 10% starch slurry and process soft material, cross 14 mesh sieves and granulate, dry under 70-80 ℃ of temperature, cross 12 mesh sieve granulate, after adding magnesium stearate and mixing, be pressed into 1000, promptly get tablet.Every contains Herba Erigerontis extract I and each 50mg of II.Said preparation can be used for treating or prevents because beta-amyloid polypeptide 1-is assembled and fiber forms the senile dementia that causes.
Embodiment 6: the application of Herba Erigerontis extract
The preparation of medicament capsule: get the Herba Erigerontis extract II 100g, starch 50g and the magnesium stearate 2g that make among the embodiment 2; Behind Herba Erigerontis extract II and 80 ℃ of exsiccant starch and magnesium stearate mix homogeneously, be distributed into 1000 capsules, promptly get capsule.Every capsules contains Herba Erigerontis extract II 100mg.Said preparation can be used for treating or prevents because beta-amyloid polypeptide 1-is assembled and fiber forms the disease that causes.
Claims (9)
1. Herba Erigerontis extract suppresses the purposes in beta-amyloid polypeptide 1-gathering and the fibroplastic medicine in preparation.
2. Herba Erigerontis extract is preparing treatment or prevention because the purposes in the medicine of the disease that beta-amyloid polypeptide 1-gathering and fiber formation cause.
3. according to the purposes of claim 1 or 2 said Herba Erigerontis extracts, it is characterized in that: described Herba Erigerontis extract is the total phenols extract that contains flavone compound and caffeoyl quinic acid ester type compound that is extracted preparation by the herb of feverfew Herba Erigerontis.
4. according to the purposes of the said Herba Erigerontis extract of claim 3, it is characterized in that: described Herba Erigerontis extract is preparation like this: get the Herba Erigerontis herb, pulverize; Extract 2～3 times with lower alcohol solvent, merge extractive liquid,, concentrating under reduced pressure reclaims solvent; The concentrated solution dilute with water filters phenylethylene macroporous adsorbent resin on the filtrating; After water elution was extremely colourless, the alcoholic solution eluting with 30%～95%, elution volume were 3～20 times of column volumes; Eluent concentrates, and using 10% sodium hydroxide solution adjust pH is 7.0～7.5, and spray drying gets pale brown toner end, i.e. Herba Erigerontis total phenols extract then.
5. according to the purposes of the said Herba Erigerontis extract of claim 3, it is characterized in that: described Herba Erigerontis extract is preparation like this: get the Herba Erigerontis herb, pulverize, extract 2～3 times with lower alcohol solvent; Merge extractive liquid,, concentrating under reduced pressure reclaims solvent, and the concentrated solution dilute with water is earlier with No. 120 gasoline extraction defats; Water layer is with ethyl acetate extraction 3～4 times, and the combined ethyl acetate part concentrates; Remove and desolvate, get pale brown toner end, i.e. Herba Erigerontis total phenols extract.
6. according to the purposes of claim 4 or 5 said Herba Erigerontis extracts, it is characterized in that: used lower alcohol was methanol or ethanol when Herba Erigerontis extract prepared.
7. according to the purposes of the said Herba Erigerontis extract of claim 3, it is characterized in that: the content of scutellarin is 0.1%～50% in the said flavone compound.
8. according to the purposes of the said Herba Erigerontis extract of claim 3, it is characterized in that: the content of total caffeoyl quinic acid ester is 10%～99% in the said caffeoyl quinic acid ester type compound.
9. the purposes of said Herba Erigerontis extract according to Claim 8; It is characterized in that: contain 4 in the said caffeoyl quinic acid ester type compound; 5-dicaffeoyl-quinic acid ester, 3; 5-dicaffeoyl-quinic acid ester, 1,3-dicaffeoyl-quinic acid ester, 1,5-dicaffeoyl-quinic acid ester and Erigeroster B.
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| CN111067926A (en) * | 2020-01-14 | 2020-04-28 | 仲恺农业工程学院 | Method for extracting and enriching total flavonoids and quinic acid ester compounds in rhinacanthus nasutus |
| CN116509916A (en) * | 2023-06-15 | 2023-08-01 | 云南德彩堂生物医药科技有限公司 | Erigeron breviscapus active site liposome, and preparation method and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103110680A (en) * | 2013-02-27 | 2013-05-22 | 黄睿 | Preparation method of total phenolic acid of erigeron breviscapus |
| CN105560227A (en) * | 2015-12-30 | 2016-05-11 | 神威药业集团有限公司 | Neuroprotection use and medicine of Dandengtongnao active component Erigoster B |
| CN111067926A (en) * | 2020-01-14 | 2020-04-28 | 仲恺农业工程学院 | Method for extracting and enriching total flavonoids and quinic acid ester compounds in rhinacanthus nasutus |
| CN111067926B (en) * | 2020-01-14 | 2021-12-28 | 仲恺农业工程学院 | Method for extracting and enriching total flavonoids and quinic acid ester compounds in rhinacanthus nasutus |
| CN116509916A (en) * | 2023-06-15 | 2023-08-01 | 云南德彩堂生物医药科技有限公司 | Erigeron breviscapus active site liposome, and preparation method and application thereof |
| CN116509916B (en) * | 2023-06-15 | 2024-04-19 | 云南德彩堂生物医药科技有限公司 | Erigeron breviscapus active site liposome, and preparation method and application thereof |
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