CN101569658A - Application of total flavone of scutellaria barbata for preparing anti-dementia medicine - Google Patents
Application of total flavone of scutellaria barbata for preparing anti-dementia medicine Download PDFInfo
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- CN101569658A CN101569658A CNA2009100746868A CN200910074686A CN101569658A CN 101569658 A CN101569658 A CN 101569658A CN A2009100746868 A CNA2009100746868 A CN A2009100746868A CN 200910074686 A CN200910074686 A CN 200910074686A CN 101569658 A CN101569658 A CN 101569658A
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- scutellaria barbata
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Abstract
The anti-dementia medicine prepared from scutellaria barbata is invented for making up for a deficiency of clinical anti-dementia medicines. A series of experimental studies for years verify that the total flavone of the scutellaria barbata has obvious function of nerve protection, anti-dementia and memory improvement. The invention comprises the following steps of: pulverizing clean scutellaria barbata; carrying out the inverse flow of ethanol 20 times as much as the scutellaria barbata for 1 hour and filtering; carrying out the inverse flow of ethanol 20 times as much as dregs for 1 hour and filtering again; mixing the filtrate obtained twice; thoroughly recycling the ethanol after 60-DEG C decompression; adsorbing chlorophyll by adding 3% calcium carbonate to the residual liquid; standing for a night; carrying out suction filtration; regulating the filtrate to a pH value of 2 or so with acid; and obtaining the total flavone extract by centrifugal precipitation, 60-DEG C drying and the like. In the total flavone extract, the total content of the flavone is not less than 70% and can be prepared into tablets, capsules, oral liquid or injection. The Scutellaria barbata is abundant in nature or can be cultivated artificially with low cost, and the quality of the artificially-cultivated medicinal material is similar to the natural. The experiment proves that the anti-dementia medicine prepared from the total flavone of scutellaria barbata has positive clinical function, high efficiency and low toxicity, thereby having wide development foreground.
Description
Technical field:
The invention belongs to the drug development technical field, relate in particular to the new medical use of Chinese herbal medicine Herba Scutellariae Barbatae and the preparation of Herba Scutellariae Barbatae total flavones thereof.
Technical background:
Enter 21st century, alzheimer disease has become commonly encountered diseases and frequently-occurring disease, serious threat health in human old age.Since the eighties in last century, carried out the dull-witted drug research of a series of treatments both at home and abroad, all can delay the development process of senile dementia disease as VitE, selegiline (using 2 years), not improve patient's memory and improve the patient and finish the brainwork ability but observe; Ginkgo agent EGB7616 in Germany, Britain as the listing of the dull-witted medicine of treatment, its mechanism of action has antioxidation, removing free radical, cerebral blood flow increasing with ingredient, it is relevant to improve brain function; Cholinergic drug (Tacrine, E in addition
2020, Huperzine-A) also improve amnemonic effect (Tariot PN from suppressing the cholinesterase activity performance, Federoff HJ.Currenttreatment for Alzheimer disease and future prospects[J] .Alzhei Dis Assoc Disor, 2003,17 (Suppl 4): S105-13), or the like.Although occur a series of antidementia agents both at home and abroad, still can not satisfy global dementia human needs.Therefore, more efficient, the low toxicities of development, exploitation, the antidementia agent that the mechanism of action is clear and definite are still the focus that international the world of medicine, pharmacy industry pay close attention to.
Summary of the invention:
The objective of the invention is at the dull-witted medicine deficiency of treatment, exploitation motherland medical treasure-house, a kind of resourceful Chinese herbal medicine is provided---Herba Scutellariae Barbatae is as the new way of preparation dementia resisting medicine, and the clinical effect of producing with Herba Scutellariae Barbatae total flavones certainly, the dementia Chinese medicine preparation of high-efficiency low-toxicity.
Herba Scutellariae Barbatae (Scutellaria barbata D.Don) is traditional Chinese herbal medicine, except that wild, artificial implantation is arranged also.The document record is arranged, and Herba Scutellariae Barbatae contains the number of chemical composition, based on flavonoid and diterpene-kind compound, also contains alkaloid, steroidal and polysaccharide etc.Its aerial parts flavonoid glycoside content is maximum, accounts for 2.31% of medical material, and scutellarin maximum effective active composition that is the Herba Scutellariae Barbatae flavones content accounts for medical material 5.28%.And find that artificial implantation quality and natural crude drugs quality are approaching.Having pharmacological literature report Herba Scutellariae Barbatae or its to extract composition has analgesic, antibiotic, mutation, antioxidation, hepatoprotective and the vascular endothelial function infringement that diabetes cause is had effects such as protection.Be used for the treatment of gastropathy, prostatosis and tumor etc. according to another each prescription decoction of clinical report.And treat the experience that has a poor memory also useful Herba Scutellariae Barbatae among the people.But whether have neuroprotective about the Herba Scutellariae Barbatae flavone and do not see that with the amnemonic effect of improvement bibliographical information is arranged.
The present invention is from the nineties later stage in last century, and we begin the Herba Scutellariae Barbatae medical material is carried out systematic study, finds that its contained flavone compound is based on scutellarin; Pharmaceutical research find Herba Scutellariae Barbatae extract composition have multiple pharmacotoxicological effect (Zou Zhenlei, Wu Qinan. precious traditional Chinese medical science traditional Chinese medicines Nanjing University of Traditional Chinese Medicine 2005,16 (2) when chemical constituent of Herba Scutellariae Barbatae and Advance on Pharmacological Activities: 149-150).Afterwards, we were according to experience and Herba Scutellariae Barbatae flavone construction features that useful Herba Scutellariae Barbatae treatment among the people has a poor memory, predicted character performance neuroprotective that it may be by the polyhydroxy reproducibility and to the effect of dementia.By a series of simulation alzheimer disease body inside/outside models, on laboratory animal integral level and cellular level, set forth the Herba Scutellariae Barbatae flavone and improve dysmnesia dementia effect and mechanism of action thereof.Again through a series of pharmacodynamic studies, confirm the Herba Scutellariae Barbatae flavone have tangible neuroprotective, to dementia with improve memory impairments.Therefore, technical scheme of the present invention is:
Herba Scutellariae Barbatae is as the purposes of preparation dementia resisting medicine.
Herba Scutellariae Barbatae total flavones is characterized in that as the purposes of preparation dementia resisting medicine general flavone content is not less than 70%, is prepared into tablet, capsule, oral liquid or injection.
Herba Scutellariae Barbatae total flavones preparation technology is as follows: the clean dried Herba Scutellariae Barbatae is pulverized, and 20 times of alcohol reflux 1hr filter, 10 times of ethanol of medicinal residues 1hr that refluxes again, filter, merge filtrate twice, ethanol is thoroughly reclaimed in 60 ℃ of decompressions, debris adds 3% titanium pillaring solution chlorophyll, placement is spent the night, sucking filtration, and filtrate is transferred about PH2 with acid, centrifugation is drying to obtain total flavones for 60 ℃, and content of total flavone is not less than 70% in the sample.
Adopt the Herba Scutellariae Barbatae total flavones of above-mentioned prepared, the pharmacodynamic experiment result is as follows:
1, the anti-mouse brain anoxia functions of medicine: 25,50 and the medicine continuous irrigation stomach mice of 100mg/kg after 10 days, lumbar injection 200mg/kg NaNO
2Or broken end, found that medicine obviously prolongs the mice time-to-live under the above-mentioned condition, shows that Herba Scutellariae Barbatae total flavones has obvious antagonism mouse brain anoxia functions.
2, medicine improves alcohol induced mouse memory and reproduces obstacle: 25,50 and the medicine continuous irrigation stomach of 100mg/kg 7 days, alcohol induced mouse memory is reproduced obstacle have obvious improvement effect, 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, and shows that medicine can improve alcohol induced mouse memory and reproduce obstacle.
3, medicine improves that pentobarbital sodium produces the mouse memory acquired disturbance and sodium nitrite causes that mouse memory keeps obstacle: 25,50 and 100mg/kg medicine continuous irrigation stomach 7 days, since the 8th day, before water maze test 60min, irritate each medicine of stomach, lumbar injection pentobarbital sodium 15mg/kg before the 30min, 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.
4, medicine obviously shortens ovariectomized rat Morris water maze operation incubation period, increases the number of times of spanning platform and at the swimming time of platform area; Reduce the expression of short apoptogene Bax of removal ovary rat layer and P53 and increase and press down apoptogene Bcl-2 expression; The content of GSH-Px vigor and NO improves the oxidative damage that energy and radical pair neurocyte cause in downward modulation removal ovary rat rat layer, hippocampal tissue MDA content, rise cortex and the hippocampal tissue; Improve removal ovary rat blood serum E2 level, reduce the weight increase rate and increase fallopian tube uterus, spleen and thymus index.
Adopt the Herba Scutellariae Barbatae total flavones of above-mentioned prepared, the toxicological experiment result is as follows:
1, the chmice acute toxicity test of research medicine, lumbar injection 8300-10000mg/kg observes a week after the administration, calculates LD50=9612.52-8608.8mg/kg, and dead mice becomes celestial and does not see that organ obviously changes.
2, the long term toxicity test of research medicine was irritated stomach rat 2.0,1.0,0.5g/kg medicine three months, and control rats is given isopyknic drug solvent.
(1) three dosed administration group rat behavior, appetite are similar to matched group with body weight gain.
(2) electrocardiogram, the rhythm of the heart are not had obvious influence, but the effect of slight decreased heart rate is arranged.
(3) administration treated animal Serum ALT/GPT, albumin, TTT etc. do not have obviously change.
(4) medicine does not have obvious influence to RBC, WBC and Hb and blood urea nitrogen in the rat blood, and prompting does not have obvious influence to blood and renal function.
(5) histopathologic examination, the tissue of each organ of administration group does not have obvious pathological change.The maximal dose of medicine gastric infusion (capacity) can not surpass 2g/kg, if surpass this dosage, suspension is too thick, can't administration, so do not increase dosage.From this experiment gained data, as can be seen, may be except that heavy dose influential to liver function, do not see other tangible toxicity.Therefore think under used dosage situation it is comparison safety.
The basic consumption of medicine provided by the invention is 2.8-11.2mg/kg, day clothes 1 time, and this dosage is determined according to zooperal effective dose.
Compared with prior art, the present invention develops motherland's medical treasure-house, has found the new way of a preparation dementia resisting medicine, promptly utilizes Herba Scutellariae Barbatae to prepare dementia resisting medicine.Herba Scutellariae Barbatae is ABUNDANT NATUREAL RESOURSES not only, but and also artificial implantation, with low cost, and the quality of medicinal material of wild and artificial implantation is close.Experiment showed, that the dementia preparation clinical effect for preparing with Herba Scutellariae Barbatae total flavones is affirmed, high-efficiency low-toxicity, have the wide development prospect.
The specific embodiment:
Below in conjunction with embodiment the present invention is elaborated.
Embodiment 1, and Herba Scutellariae Barbatae is as the purposes of preparation dementia resisting medicine.
Embodiment 2, get the clean dried Herba Scutellariae Barbatae, pulverize, 20 times of alcohol reflux 1hr filter, 10 times of ethanol of medicinal residues 1hr that refluxes again, filter, merge filtrate twice, ethanol is thoroughly reclaimed in 60 ℃ of decompressions, debris adds 3% titanium pillaring solution chlorophyll, and placement is spent the night, sucking filtration, filtrate is transferred about PH2 with acid, 60 ℃ of dryings of centrifugation get total flavones, and its content of total flavone is not less than 70%.Adopt routine techniques to be prepared into clinical medicaments such as tablet, capsule, oral liquid or injection again.
Claims (2)
1, Herba Scutellariae Barbatae is as the purposes of preparation dementia resisting medicine.
2, Herba Scutellariae Barbatae total flavones is characterized in that as the purposes of preparation dementia resisting medicine general flavone content is not less than 70%, is prepared into tablet, capsule, oral liquid or injection.
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| CNA2009100746868A CN101569658A (en) | 2009-06-04 | 2009-06-04 | Application of total flavone of scutellaria barbata for preparing anti-dementia medicine |
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| CNA2009100746868A CN101569658A (en) | 2009-06-04 | 2009-06-04 | Application of total flavone of scutellaria barbata for preparing anti-dementia medicine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102688291A (en) * | 2012-06-01 | 2012-09-26 | 康阳润和（北京）医药科技有限公司 | Sculellaria barbata general flavone compound, oral preparations prepared from Sculellaria barbata general flavone compound and preparation methods respectively for Sculellaria barbata general flavone compound and oral preparations |
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2009
- 2009-06-04 CN CNA2009100746868A patent/CN101569658A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102688291A (en) * | 2012-06-01 | 2012-09-26 | 康阳润和（北京）医药科技有限公司 | Sculellaria barbata general flavone compound, oral preparations prepared from Sculellaria barbata general flavone compound and preparation methods respectively for Sculellaria barbata general flavone compound and oral preparations |
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Open date: 20091104 |