CN1149989C - Application of skullcap stem and leaf general flavone and wild baicalin in preparing dementia resisting medicine - Google Patents
Application of skullcap stem and leaf general flavone and wild baicalin in preparing dementia resisting medicine Download PDFInfo
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- CN1149989C CN1149989C CNB02102233XA CN02102233A CN1149989C CN 1149989 C CN1149989 C CN 1149989C CN B02102233X A CNB02102233X A CN B02102233XA CN 02102233 A CN02102233 A CN 02102233A CN 1149989 C CN1149989 C CN 1149989C
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Abstract
The present invention discloses the novel pharmaceutical application of scutellaria stem-leaf total flavonoids and the scutellarin thereof, i.e. the stem and leaf of scutellaria are adopted to prepare an extraction with a total flavonoid content of not less than 50% as a medicament for treating dementia and the extraction with a scutellarin content of not less than 98% as a medicament for treating dementia. The two medicaments and the agents thereof can represent the shapes of tablets, capsules, dripping pills, oral medicinal liquids, injections, etc. The application using the special polyhydric structure of scutellaria stem-leaf total flavonoids has the characteristics of strong reducibility and antagonism towards free radicals. The obvious medical care effect obtained by perennial animal experiment researches can prove that the medicaments have reliable anti-dementia functions. The medicaments have the advantages of obvious pathology function, positive clinic curative effect, safety, low toxicity, plentiful resource and low cost, and thus, the medicaments have integral effects exceeding that of an existing anti-senile dementia medicament.
Description
Technical field: the invention belongs to the drug development technical field, relate in particular to the new medical use of Caulis et Folium Scutellariae total flavones and scutellarin thereof.
Background technology: dementia belongs to the neurodegenerative diseases that multi-pathogenesis participates in.At present, it has become the commonly encountered diseases and the frequently-occurring disease of elderly population, is the great fatal disease that is only second to the heart, cerebrovascular and tumor etc.Since the eighties, the dull-witted medicine of a series of treatments has appearred, wherein especially with cholinesterase inhibitor (ChEI) Tacrine, E both at home and abroad
2020Deng synthetic drug is representative, low or toxic and side effects limits use (Giacobini E greatly yet owing to them or because of bioavailability, Cuadra G.Second and third generation cholinesteraseinhibitors:from preclinical studies to clinical efficacy.In:Giacobini E, Becker R, editors.Alzheimer Disease:Therapeutic Strategies.Boston:Birkhauser 1994:155～171).In the face of the rapid increase of alzheimer disease number of the infected, development, exploitation antidementia agent efficient, low toxicity are the focuses that international the world of medicine, pharmacy industry are paid close attention to.
The application finds that by research for many years its stem leaf total flavones of Chinese herbal medicine Radix Scutellariae (Scutellaria baicalensis Georgi) has tangible dementia effect.The Radix Scutellariae tradition is used as medicine with root, and output is that the stem and leaf of root several times is then passed into disuse for a long time.Put down in writing according to Chinese patent CN1260189A disclosed " application of Caulis et Folium Scutellariae in pharmacy ": what Hebei province's " scientific and technical research achievement communique " in 1991 and the 101st phase " Chinese technological achievement complete works " included discloses the medical value of Caulis et Folium Scutellariae respectively about " plant of Caulis et Folium Scutellariae total flavones and pharmacological research ", the main component that confirms Caulis et Folium Scutellariae is a flavone compound, content about 5%; The main component of determining the Caulis et Folium Scutellariae total flavones is scutellarin (Scutellarin), and content is about 16%, and (main component is a baicalin, Baicalin) notable difference is arranged with the contained flavone of scutellariae,radix; Find that the Caulis et Folium Scutellariae total flavones has blood fat reducing, expansion cardiovascular and cerebrovascular vessel, increases the effect that cardiovascular and cerebrovascular vessel flow, arrhythmia and anticoagulation, blood pressure lowering etc. are prevented and treated cardiovascular and cerebrovascular disease widely.But, about the Caulis et Folium Scutellariae effective ingredient have analgesia, antiinflammatory, analgesic Pharmacological action study do not see as yet have open.Therefore, this patent application disclose that Caulis et Folium Scutellariae or its total flavones have analgesia as producing, the application technology of antiinflammatory, analgesic function medicament aspect.This shows that about the application of Caulis et Folium Scutellariae in producing the dementia resisting medicine, prior art is not seen as yet to be had openly.
Summary of the invention:
The objective of the invention is: at the defective of existing dementia resisting medicine and the potentiality to be exploited of Caulis et Folium Scutellariae, providing a kind of is raw material with the Caulis et Folium Scutellariae, produces the new way of the dementia resisting medicine of efficient, low toxicity.
Technical solution of the present invention is:
The Caulis et Folium Scutellariae total flavones is as the application of preparation dementia resisting medicine, and it is characterized in that: in the Caulis et Folium Scutellariae extract, its general flavone content is not less than 50%, is used to prepare the dementia resisting medicine.
The Caulis et Folium Scutellariae scutellarin is as the application of preparation dementia resisting medicine, and it is characterized in that: in the Caulis et Folium Scutellariae extract, its scutellarin content is not less than 90%, is used to prepare the dementia resisting medicine.
The present invention has the advantages that according to the special polyhydroxy structure of Caulis et Folium Scutellariae total flavones stronger reproducibility can be resisted free radical; prediction verifies by the neuroprotective testing experiment whether it has the dementia effect; thereby a series of scientific experimentations have been done; through experimentation for many years, obtain following achievement:
1, medicine oxygen lack resistant function:
1. the anti-anoxia in mice effect of Caulis et Folium Scutellariae total flavones, 50,100 and the total flavones medicine continuous irrigation stomach mice of 200mg/kg after 14 days, lumbar injection KCN 10mg/kg or 200mg/kg NaNO
2Or joint vagal bilateral common carotid arteries of band or broken end, found that total flavones obviously prolongs the time-to-live of mice under the above-mentioned condition, shows that the Caulis et Folium Scutellariae total flavones has the effect of obvious antagonism anoxia in mice.
2. the anti-anoxia in mice effect of scutellarin, 37.5,75, the scutellarin subcutaneous injection mice of 150mg/kg is after 7 days, lumbar injection KCN 10mg/kg found that scutellarin obviously prolongs KCN and causes mouse diing time, shows that scutellarin has obvious anti-anoxia in mice effect.
2, medicine improves the normal mouse memory:
1. the Caulis et Folium Scutellariae total flavones improves mouse memory, 50,100, the medicine of 200mg/kg and piracetam (200mg/kg) continuous irrigation stomach mice are after 7 days, carry out the water maze test, find that the reach home incubation period of platform and the number of times that enters cecum of medicine three dosage group mices obviously reduces, show that medicine has the raising memory effect, the piracetam effect is then not obvious.
2. 37.5,75, the scutellarin subcutaneous injection mice of 150mg/kg is after 7 days, carries out the water maze test, finds that the reach home incubation period of platform and the number of times that enters cecum of three dose drug group mices obviously reduces, and shows that medicine has the raising memory effect.
3, Caulis et Folium Scutellariae total flavones medicine improves that pentobarbital sodium produces the mouse memory acquired disturbance and sodium nitrite causes that mouse memory keeps obstacle:
50,100, the Caulis et Folium Scutellariae total flavones medicine continuous irrigation stomach mice of 200mg/kg is 7 days, since the 8th day, before water maze test 60min, irritate and feed each medicine, inject pentobarbital sodium 15mg/kg before the 30min on an empty stomach, the reach home incubation period of platform and the number of times that enters cecum of water maze test result medicine group mice obviously reduces than model group, shows that medicine has the effect that improves the mouse memory acquired disturbance that pentobarbital sodium produces.The same medicine 50,100 and 200mg/kg irritated the stomach mice 7 days (day once), 1h after the 8th administration, carry out water maze training (continuation administration), train every day twice, when all mices arrive the incubation period＜20s of platforms, enter number of times＜2 o'clock of cecum, i.e. mice training is up to standard can be remembered and consolidate the obstacle experiment.Mice up to standard after training, lumbar injection 120mg/kg NaNO immediately
2, behind the 24h, carry out water maze test, found that the number of times that medicine group mice is reached home time incubation period and enters cecum obviously reduces than model group, showing that medicine has improves sodium nitrite and causes that mouse memory keeps the effect of obstacle.
4, Caulis et Folium Scutellariae total flavones medicine antagonism mice naturally-aged, d-galactose cause old and feeble effect:
Aged Mice hypomnesis, immunity reduction, neurocyte pathological change, free radical system ANOMALOUS VARIATIONS.Aged Mice was irritated stomach medicine 50,100 and 200mg/kg after 21 days, carried out the water maze test, found that medicine group mice reaches home platform incubation period and enter the cecum number of times and significantly reduce than old model group mice; Compare with the model group mice, MDA reduces in medicine group mouse cortex, Hippocampus and the serum, and SOD is active to raise; The neural pyramidal cell of medicine group mouse cortex, Hippocampus is full, be various state, nerve fiber is elongated, nuclear understain placed in the middle etc.; Medicine group mouse thymus increases than Aged Mice thymic weight.Show that medicine has a series of ANOMALOUS VARIATIONS that the antagonism naturally-aged causes.
50,100, the 200mg/kg medicine is irritated the stomach mice, lumbar injection D-galactose 120mg/kg is 42 days simultaneously, carried out water maze test (continuing to give D-galactose and medicine) since 43 days, continuous 5 days, the samely do that cortical cell is observed, spleen index is measured, found that medicine group mice reaches home incubation period and enter the cecum number of times and obviously reduce than model group; The cortex pyramidal cell is full to be that various states, nerve fiber are elongated, nuclear understain placed in the middle etc.; Spleen index increases.Show that medicine has antagonism D-galactose and causes old and feeble effect.
Compared with prior art, the Caulis et Folium Scutellariae total flavones is as the medicine of treatment dementia, and not only pharmacological action is outstanding, and clinical efficacy is sure, and safety and low toxicity, and aboundresources are with low cost, and whole structure estimates to surpass the medicine of at present existing anti-ageing year dementia.
Description of drawings:
The specific embodiment: the present invention is elaborated below in conjunction with embodiment.
Embodiment 1, the preparation of Caulis et Folium Scutellariae total flavones medicine: get the clean dried Caulis et Folium Scutellariae, 10 times of decocting in water 1hr, filter, 8 times of water of medicinal residues boil 1hr again, filter, merge filtrate twice, it is centrifugal suitably to concentrate the back, and supernatant is transferred about PH2, macroporous resin adsorption, the washed several times with water removal of impurity, dress chromatographic column, be higher than 85% ethanol elution, the eluent decompression recycling ethanol is drying to obtain the Caulis et Folium Scutellariae total flavones, and wherein general flavone content is not less than 50%.Adopt routine techniques to make tablet, capsule, drop pill, oral liquid and injection etc. then.
Embodiment 2, the preparation of Caulis et Folium Scutellariae scutellarin: total flavones is carried out repeatedly recrystallization with methanol, get scutellarin, its scutellarin content is not less than 90%.
Adopt the Caulis et Folium Scutellariae total flavones and the scutellarin medicine of such scheme preparation to be used for the treatment of dementia.
Claims (1)
1, scutellarin is as the application of preparation dementia resisting medicine in the Caulis et Folium Scutellariae total flavones, and it is characterized in that: in the Caulis et Folium Scutellariae extractive total flavone, scutellarin content is not less than 90%, is used to prepare the dementia resisting medicine.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB02102233XA CN1149989C (en) | 2002-01-05 | 2002-01-05 | Application of skullcap stem and leaf general flavone and wild baicalin in preparing dementia resisting medicine |
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| Application Number | Priority Date | Filing Date | Title |
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| CNB02102233XA CN1149989C (en) | 2002-01-05 | 2002-01-05 | Application of skullcap stem and leaf general flavone and wild baicalin in preparing dementia resisting medicine |
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| CN1383818A CN1383818A (en) | 2002-12-11 |
| CN1149989C true CN1149989C (en) | 2004-05-19 |
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| CNB02102233XA Expired - Fee Related CN1149989C (en) | 2002-01-05 | 2002-01-05 | Application of skullcap stem and leaf general flavone and wild baicalin in preparing dementia resisting medicine |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100378089C (en) * | 2005-02-23 | 2008-04-02 | 吉林省东北亚药业股份有限公司 | Process for extracting total flavone from stem and leaf of scutellaria |
| CN100422199C (en) * | 2005-04-15 | 2008-10-01 | 长沙世唯科技有限公司 | Extractive from specific part of skullcap, preparation method and application |
| CN100435814C (en) * | 2006-03-27 | 2008-11-26 | 承德医学院中药研究所 | Scullcap stem and leaf injection powder and its preparing method |
| CN102000101A (en) * | 2010-10-28 | 2011-04-06 | 天津中医药大学 | Application of scutellarin to treatment of microglia-mediated diseases |
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