CN104147027A - New application of resveratrol derivative - Google Patents

New application of resveratrol derivative Download PDF

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Publication number
CN104147027A
CN104147027A CN201410412153.7A CN201410412153A CN104147027A CN 104147027 A CN104147027 A CN 104147027A CN 201410412153 A CN201410412153 A CN 201410412153A CN 104147027 A CN104147027 A CN 104147027A
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verakanol derivative
structural formula
derivative
verakanol
molecular structural
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CN201410412153.7A
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Chinese (zh)
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安树君
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Individual
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Abstract

The invention relates to a new application of a resveratrol derivative, the resveratrol derivative has effect to prevent reversible dementia, a molecule structural formula of the resveratrol derivative is as follows, a molecular formula of the resveratrol derivative with the above molecule structural formula is C20H22O9, the molecular weight is 406, degree of unsaturation n is 10, and a name of the is 3'-hydroxy resveratrol, 4'-O-beta-D-pyranoglucoside. According to the resveratrol derivative with the above molecule structural formula, the high purity compound prevent reversible dementia, the curative effect is obvious, the resveratrol derivative has no toxicity, no side effect, and is suitable for popularization and application.

Description

A kind of new purposes of Verakanol derivative
Technical field
The present invention relates to medical technical field, relate in particular to a kind of new purposes of Verakanol derivative.
Background technology
Vascular dementia (vasculardementia, VD) is because of the intelligence due to cerebrovascular disease and the clinical syndrome of cognitive disorder, is only dementia of preventing and treating in alzheimer disease, is called as cataphrenia.The traditional Chinese medical science is early recognized dementia, but there is no at present the Chinese medicine preparation of the prevention VD that active constituent content is high, curative effect is sure, can promote the use of.
Summary of the invention
For above problem, the invention provides the new purposes of a kind of Verakanol derivative aspect prevention cataphrenia.
Concrete technical scheme of the present invention is as follows:
The new purposes of above-mentioned Verakanol derivative, has the effect of prevention cataphrenia, and the molecular structural formula of described Verakanol derivative is as follows:
The molecular formula of the Verakanol derivative of above-mentioned molecular structural formula is C20H22O9, and molecular weight is 406, degree of unsaturation n=10, and its title is 3 '-hydroxyl resveratrol, 4 '-O-β-D-glucopyanoside.
The new purposes of described Verakanol derivative, wherein: the Verakanol derivative of described molecular structural formula, its low dosage extract has preventive effect to the damage in learning and memory of vascular dementia rats.
The new purposes of described Verakanol derivative, wherein: the Verakanol derivative of described molecular structural formula, its administration is intended to the initial stage of the slow forming process of vascular dementia it is carried out to pharmaceutical intervention, thus the damage in learning and memory after prevention vascular dementia forms.
The new purposes of described Verakanol derivative, wherein: the Verakanol derivative of described molecular structural formula, it can be from natural drug as extracted or synthetic the Chinese medicines such as Radix Rhei emodi, Rheum hotaoense C. Y. Cheng et C. T. Kao, Rheum officinale, Rheum tanguticum and Rhizoma Polygoni Cuspidati, Radix Polygoni Multiflori.
Beneficial effect:
The new purposes of Verakanol derivative of the present invention is mainly reflected in, the Verakanol derivative providing of above-mentioned molecular structural formula has can effectively prevent cataphrenia, wherein, by behavioristics, detect, observe in above-mentioned molecular structural formula Verakanol derivative, low dose group has preventive effect to the damage in learning and memory of vascular dementia rats, evident in efficacy and have no side effect, be suitable for propagation and employment.
The specific embodiment
The Verakanol derivative the present invention relates to is mainly from plant, can be from natural drug as extracted the Chinese medicines such as Radix Rhei emodi, Rheum hotaoense C. Y. Cheng et C. T. Kao, Rheum officinale, Rheum tanguticum and Rhizoma Polygoni Cuspidati, Radix Polygoni Multiflori, and also can synthetic.
The structural formula of the Verakanol derivative the present invention relates to is as follows:
The molecular formula of the Verakanol derivative of above-mentioned molecular structural formula is C20H22O9, and molecular weight is 406, degree of unsaturation n=10, its name is called 1-(3,5-dihydroxyphenyl)-2-(3,4-dihydroxyphenyl) ethylene, 4 '-O-β-D-glucopyanoside or cry 3,3 ', 4 ', 5-tetrahydroxystilbene, 4 '-O-β-D-glucopyanoside, again or be 3 '-hydroxyl resveratrol, 4 '-O-β-D-glucopyanoside.
For the extract of Verakanol derivative that the proves above-mentioned molecular structural formula preventive effect to vascular dementia rats damage in learning and memory, inventor adopts the method (2-VO) of permanent ligation bilateral common carotid arteries, make vascular dementia rats model, by shuttle box, test the learning and memory in rats ability of respectively organizing that detects.
Below in conjunction with specific embodiment, the new purposes of Verakanol derivative of the present invention is made to further proof:
One, materials and methods
(1) choice experiment animal
130 of adult healthy Wistar male rats (12～14 week age), body weight 300g～350g.
(2) experimental drug and reagent
C drug extract: Kunming Rui Pu Bioisystech Co., Ltd provides, content: Dihydroergotoxine Tianjin Hua Jin pharmaceutical factory and Novartis Pharma Schweiz AG's co-production, lot number: 060167;
Folium Ginkgo: Hunan Warrant Pharmaceutical Co., Ltd. produces, lot number: 060101.
(3) foundation of creation
The preoperative 12h fasting of rat, 4h prohibit water, with 10% chloral hydrate (0135ml/100g) intraperitoneal injection of anesthesia, lie on the back fixing, throat portion unhairing sterilization tailing edge neck medisection, the separated left and right side common carotid artery (noting not injuring vagus nerve) that exposes, cover is with/No. 00 dual ligation of silk thread, layer-by-layer suture; Rats in sham-operated group is except not ligation common carotid artery, all the other same model group; In art, rat anus temperature remains on 3615e～3715e, and art is complete gives benzylpenicillin sodium for injection aqueous solution appropriate local coating, puts into cage and raises, and lumbar injection penicillin sodium 200,000 U/ of every days, is used in conjunction 3d, and control is infected.
(4) laboratory animal grouping and administration
Latter 1 week of above-mentioned steps (3) modeling operation, to survive rat (survival rate is 50% left and right) and be divided at random 6 groups, every group 10, be model group (Model, normal saline 10ml/kg), Verakanol derivative extract high dose group (TMH, 310g crude drug/kg), dosage group (TMM in Verakanol derivative extract, 115g crude drug/kg), Verakanol derivative extract low dose group (TML, 0175g crude drug/kg), Western medicine positive control Dihydroergotoxine group (XDZ, 016mg/kg), Chinese medicine positive control Folium Ginkgo group (YXY, 40mg/kg); Separately add 10 of sham operated rats (Sham, normal saline 10ml/kg); Each organizes gastric infusion 1 time every day, continuous 8 weeks.
(5) learning and memory function detects
Adopt rat shuttle box to detect the ability of learning and memory of respectively organizing rat, at above-mentioned steps (5) successive administration, after 8 weeks, start to detect, every day 1 time, continuously 7d; Systematic parameter is made as cycle-index 20 times, interval time 5s, buzzing time 5s, electric shock time 10s; Record the number of times that gets shocked of every rat, the total time getting shocked and the total time of initiatively escaping (note: in 1 circulation, initiatively escape if occur after buzzing 2s, this active be designated as/3s of escape time; If do not occur, initiatively do not escape, active be designated as/0s of escape time).
(6) statistical data is processed
Application SPSS13.0ForWindows statistical software, relatively adopts variance analysis between many groups, result all represents with X ± S.
Two, result
The impact of the extract of the Verakanol derivative of above-mentioned molecular structural formula on vascular dementia rats learning and memory function, in Table 1～3:
Table 1 rat shuttle box experiment number of shocks test result (X ± S)
Group The1stday The2nd?day The3 rdday The4 thday The5 thday The6 thday The7 thday
Sham 14.4±3.40 15.0±3.28 14.±41.74 13.2±5.61 10.22±2.99 8.78±2.90 6.78±2.73
Model 14.8±2.30 16.3±1.89 15.4±2.07 15.5±2.12 15.50±2.72* 14.30±3.95 14.1±4.18*
TMH 14.1±3.64 15.0±2.73 15.4±2.07 14.1±3.98 12.25±1.98# 12.37±2.07 10.88±2.03
TMM 14.8±1.97 14.6±3.20 13.4±3.91 12.6±5.68 10.5±4.19## 10.3±2.00# 9.33±2.45
TML 14.5±2.51 15.2±1.58 12.4±5.59 14.1±3.48 11.71±4.31 11.00±4.32 8.00±3.06
XDZ 14.0±2.73 13.2±3.53 14.5±2.98 15.3±2.13 12.75±4.37 11.2±2.38# 10.00±2.83
YXY 14.2±1.99 14.9±3.05 14.3±2.87 14.6±2.83 15.67±2.29 13.67±3.61 9.78±5.40
Note: with Sham comparison, * P<0.001; With Model comparison, #P<0.05, ##P<0.01, ###P<0.001.
Table 1 demonstration, with the increase of training natural law, number of shocks is on a declining curve; 4d before training, model group and sham operated rats comparison, administration group and model group comparison, number of shocks there are no significant difference; From 5d, between group, relatively there is significant difference; To training 7d, Model and Sham comparison, number of shocks significantly increases (P<0.001); With Model comparison, the number of shocks that administration group TMM (P<0.01), TML (P<0.001), XDZ (P<0.05), YXY (P<0.01) are four groups all has minimizing in various degree.
Table 2 rat shuttle box experiment electric shock time test result (X ± S)
Group The1stday The2nd?day The3 rdday The4 thday The5 thday The6 thday The7 thday
Sham 74.56±16.72 80.88±25.36 67.5±24.56 59.67±38.35 59.56±21.42 48.2±20.11 29.8±23.16
Model 87.30±22.25 104.2±33.91 85.2±33.54 107.7±36.78 91.60±29.40 92.0±37.25 84.7±34.75
TMH 104.8±47.77 110.3±43.40 81.7±38.24 90.38±42.60 78.63±29.79 79.8±32.57 69.1±20.88
TMM 95.78±19.29 99.56±26.74 67.4±42.19 87.78±47.10 74.11±22.47 60.6±26.54 52.2±18.34
TML 79.14±27.69 105.1±58.31 60.1±38.03 66.57±29.14 62.86±24.48 57.8±23.80 46.5±21.36
XDZ 75.13±22.91 96.38±29.81 70.7±41.10 63.63±22.53 74.75±34.40 63.2±25.73 51.5±23.10
YXY 83.89±30.51 80.78±30.00 69.3±39.20 68.33±39.95 68.56±36.67 62.0±33.86 50.7±48.17
Note: with Sham comparison, * P<0.05, * * P<0.01, * * * P<0.001; Compare #P<0.05 with Model.
Table 2 demonstration, with the increase of training natural law, the electric shock time is on a declining curve; 3d before training, model group and sham operated rats comparison, administration group and model group comparison, difference that the electric shock time, there are no significant; From 4d, between group, relatively there is significant difference; To training 7d, Model and Sham comparison, the electric shock time significantly increases (P<0.001); With Model comparison, the electric shock time that administration group TMM, TML, XDZ, YXY are tetra-groups all reduces (P<0.05).
Time test result (X ± S) is initiatively escaped in the experiment of table 3 rat shuttle box
aGroup The1stday The2nd?day The3 rdday The4 thday The5 thday The6 thday The7 thday
Sham 17.7±11.18 16.5±11.13 18.89±6.53 22.3±18.01 30.33±9.06 32.33±9.54 36.00±7.94
Model 18.20±9.44 11.70±5.77 16.50±8.20 14.30±6.88 14.50±8.10 17.0±12.44 19.3±11.09
TMH 19.2±11.66 17.38±8.52 17.7±12.13 19.6±12.35 24.62±5.85 25.50±8.83 25.63±7.76
TMM 17.56±7.63 18.4±11.89 22.2±13.63 23.1±18.17 32.3±14.17 30.22±7.74 29.4±10.08
TML 18.14±8.30 17.1±16.94 25.5±18.42 20.8±12.25 29.0±15.29 30.8±13.80 30.7±10.58
XDZ 19.75±8.28 17.38±5.40 19.6±11.39 15.87±7.92 24.1±15.81 29.50±6.91 29.63±7.48
YXY 20.44±7.35 23.4±12.08 19.7±10.64 17.78±9.98 15.56±8.83 19.3±11.78 28.2±15.34
Note: with Sham comparison, * P<0.01, * * P<0.001; With Model comparison, #P<0.05, ##P<0.01.
Table 3 demonstration, with the increase of training natural law, initiatively the escape time is in rising trend; 4d before training, model group and sham operated rats comparison, administration group and model group comparison, difference that the active escape time, there are no significant; From 5d, between group, relatively there is significant difference; To training 7d, Model and Sham comparison, initiatively the escape time significantly reduces (P<0.001); With Model comparison, the time of initiatively escaping of administration group TMM, TML, XDZ3 group all increases (P<0.05).
Wherein, the experiment of the present embodiment Verakanol derivative used is extracted by natural Chinese medicines, and the experimentation of the extract of this Verakanol derivative aspect vascular dementia has no report.Damage in learning and memory is the core symptom of VD clinical manifestation, therefore, also becomes the key of judgement VD model success or not.According to VD, can be caused by long-term Cerebral hypoperfusion clinically, we adopt the method (2-VO) of permanent ligation bilateral common carotid arteries to copy the VD model of rat.This experimentation shows, latter the 9th week of modeling operation, compared with sham operated rats, there is obvious damage in learning and memory (P<0.001) in model group, illustrate that this animal model making is extremely successful, consistent with lot of documents report, proving again the reliability of 2-VO method VD model.
The present embodiment is prevention administration, and the time point of administration fixes on modeling and performs the operation after 1 week, be intended to the initial stage of the slow forming process of VD it is carried out to pharmaceutical intervention, thus the damage in learning and memory after prevention VD forms.Shuttle box is a kind of important method in behavioristics's detection method, and it,, by detecting active escape reaction and the passive escape reaction of rat, carrys out the ability of learning and memory of objective reaction rat.The present embodiment is by training the shuttle box of the continuous 7d of rat, each group has shown the difference of ability of learning and memory, compared with sham operated rats, there is significant damage in learning and memory in model group, in large Rhizoma Chuanxiong drop pill, low dose group improves significantly compared with model group learning and memory function, low dose group has preventive effect to the damage in learning and memory of VD rat, and effect is slightly better than positive control drug hydergine group and Folium Ginkgo group.
Wherein, above three experimental results show: with model group comparison, the extract doses group number of shocks of the Verakanol derivative of above-mentioned molecular structural formula obviously reduces (P<0.01), electric shock time decreased (P<0.05), initiatively the escape time increases (P<0.05); The Verakanol derivative low dose group number of shocks of said structure formula significantly reduces (P<0.001), electric shock time decreased (P<0.05), initiatively the escape time increases (P<0.05).
The new purposes of Verakanol derivative of the present invention is embodied in, in the extract of the Verakanol derivative of above-mentioned molecular structural formula, low dose group has preventive effect to the damage in learning and memory of vascular dementia rats, good effect and having no side effect, is suitable for propagation and employment.

Claims (4)

1. a new purposes for Verakanol derivative, has the effect of prevention cataphrenia, and the molecular structural formula of described Verakanol derivative is as follows:
The molecular formula of the Verakanol derivative of above-mentioned molecular structural formula is C20H22O9, and molecular weight is 406, degree of unsaturation n=10, and its title is 3 '-hydroxyl resveratrol, 4 '-O-β-D-glucopyanoside.
2. the new purposes of Verakanol derivative as claimed in claim 1, is characterized in that: the Verakanol derivative of described molecular structural formula, its low dosage extract has preventive effect to the damage in learning and memory of vascular dementia rats.
3. the new purposes of Verakanol derivative as claimed in claim 1, it is characterized in that: the Verakanol derivative of described molecular structural formula, its administration is intended to the initial stage of the slow forming process of vascular dementia it is carried out to pharmaceutical intervention, thus the damage in learning and memory after prevention vascular dementia forms.
4. the new purposes of Verakanol derivative as claimed in claim 1, it is characterized in that: the Verakanol derivative of described molecular structural formula, it can be from natural drug as extracted or synthetic the Chinese medicines such as Radix Rhei emodi, Rheum hotaoense C. Y. Cheng et C. T. Kao, Rheum officinale, Rheum tanguticum and Rhizoma Polygoni Cuspidati, Radix Polygoni Multiflori.
CN201410412153.7A 2014-08-20 2014-08-20 New application of resveratrol derivative Pending CN104147027A (en)

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1347699A (en) * 2001-10-30 2002-05-08 首都医科大学宣武医院 Use of stilbene glycoside in treating dementia
WO2010022140A1 (en) * 2008-08-19 2010-02-25 Knopp Neurosciences, Inc. Compositions and methods of using (r)-pramipexole
CN102526227A (en) * 2012-01-13 2012-07-04 西藏金哈达药业有限公司 Use of Rheum emodi extract for preparing drugs for preventing and treating fatty liver diseases
CN102958516A (en) * 2009-02-20 2013-03-06 N.V.努特里西阿公司 Use of resveratrol or another hydroxylated stilbene for preserving cognitive functioning

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1347699A (en) * 2001-10-30 2002-05-08 首都医科大学宣武医院 Use of stilbene glycoside in treating dementia
WO2010022140A1 (en) * 2008-08-19 2010-02-25 Knopp Neurosciences, Inc. Compositions and methods of using (r)-pramipexole
CN102958516A (en) * 2009-02-20 2013-03-06 N.V.努特里西阿公司 Use of resveratrol or another hydroxylated stilbene for preserving cognitive functioning
CN102526227A (en) * 2012-01-13 2012-07-04 西藏金哈达药业有限公司 Use of Rheum emodi extract for preparing drugs for preventing and treating fatty liver diseases

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