CN103393640A - Application of Sarcaboside B to antidepressant medicament - Google Patents
Application of Sarcaboside B to antidepressant medicament Download PDFInfo
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- CN103393640A CN103393640A CN2013102625756A CN201310262575A CN103393640A CN 103393640 A CN103393640 A CN 103393640A CN 2013102625756 A CN2013102625756 A CN 2013102625756A CN 201310262575 A CN201310262575 A CN 201310262575A CN 103393640 A CN103393640 A CN 103393640A
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Abstract
The invention discloses application of Sarcaboside B to antidepressant medicaments. The invention provides application of Sarcaboside B to antidepressant medicaments, and the Sarcaboside B in the invention can be used as a medicament for prevention or treatment of depression. The application of Sarcaboside B to preparation of medicaments for resisting depression involved in the invention is disclosed for the first time. As the Sarcaboside B has a novel skeleton type and unimaginably strong activity in resisting depression, no other compound can give any enlightenment. The invention has outstanding substantive distinguishing features and shows substantial progress in application to antidepressant medicaments.
Description
Technical field
The present invention relates to medical technical field, is exactly the new purposes of Sarcaboside B in antidepressant drug.
Background technology
Depression is a kind of common mood disorders, can be caused by a variety of causes, and is low as main clinical characteristics take remarkable and lasting mental state, and mental state is low unbecoming with its situation, and suicidal thought and behavior can appear in severe patient.Majority of cases has the tendency of outbreak repeatedly, and the great majority that at every turn show effect can be alleviated, and part can have residual symptoms or transfer to chronic.
Depression has at least the patient of 10 % maniac access can occur, and should be diagnosed as the two-phase obstacle this moment.Our depression of often saying, refer to major depression (major depression) clinically in fact in addition, has 16% people affected by it in certain period throughout one's life in the crowd.Suffer from depression except paying serious emotion and social costs, economic cost is also huge.According to World Health Organization's statistics, depression has become the large illness in the world the 4th, expects the year two thousand twenty, may become the second largest disease that is only second to coronary heart disease.
the compound S arcaboside B that the present invention relates to is one and delivered (Li in 2012, X. et al., 2012. Two New-Skeleton Compounds from Sarcandra glabra. Helvetica Chimica Acta 95 (6), 998-1002.) New skeleton compound, this compound has brand-new framework types, there is no at present the report about activity, belong to open first for the purposes of Sarcaboside B in preparing antidepressant drug that the present invention relates to, because framework types belongs to brand-new framework types, and its antidepressant activity is unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, be used for simultaneously antidepressant drug and obviously have significant progress.
Summary of the invention
The purpose of this invention is to provide the purposes of Sarcaboside B in antidepressant drug.The present invention has the function of relieving anxiety and stress well.The inventor has wide practical use by studies show that this medicine in prevention or controlling on antidepressant.
Described compound S arcaboside B structure is as shown in formula I:
Formula I
It is open first that the purposes of Sarcaboside B in preparing antidepressant drug that the present invention relates to belongs to, because framework types belongs to brand-new framework types, and its antidepressant activity is unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for simultaneously antidepressant drug and obviously have significant progress.
The specific embodiment
The preparation method of compound S arcaboside B involved in the present invention is referring to document (Li, X. et al., 2012. Two New-Skeleton Compounds from Sarcandra glabra. Helvetica Chimica Acta 95 (6), 998-1002.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but by claim, be limited.
Embodiment 1: the preparation of compound S arcaboside B tablet involved in the present invention:
Get 20 and digest compound Sarcaboside B, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound S arcaboside B capsule involved in the present invention:
Get 20 and digest compound Sarcaboside B, add the conventional adjuvant such as starch 180 grams that prepare capsule, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Below for the present invention, can be used as the experiment situation of antidepressant drug.
1, Tail suspension test
1.1 animal
40 of healthy SD rats, male, cleaning level, body weight 180 ~ 200g; 40 of healthy kunming mices, male, cleaning level, body weight 18 ~ 22 grams.Sub-cage rearing, 4, every cage.18 ~ 29 ℃ of room temperatures, relative humidity 40% ~ 70%, the well-ventilated, environment is quiet, drinks cold boiled water.
1.2 medicine and reagent
Positive drug is fluoxetine Hydrochloride (prozac), it is a kind of selective serotonin reuptake inhibitor, its effectively inhibitory neuron absorb 5-hydroxy tryptamine from synaptic space, increasing can be for the actual this neurotransmitter that utilizes in gap, thereby improve affective state, treatment inhibition mental disorder.Spain Lilly S.A. company, quantity is 20mg/d.
1.3 animal grouping and processing
40 kunming mices are divided into 5 groups at random, every group of 8 animals.Specifically be grouped as follows: (1) blank group; (2) Sarcaboside B high dose group (5mg/Kg); (3) dosage group (1mg/Kg) in Sarcaboside B; (4) Sarcaboside B low dose group (0.2mg/Kg); (5) fluoxetine Hydrochloride group.This experimental result judgement is the band subjectivity easily, for reducing this experiment of error, adopts blind method.Concrete group and gastric infusion are responsible for by the special messenger, and the experimental index tester is ignorant in advance.Mice is hung upside down on the cross bar of distance ground 60cm (European Journal of Pharmacology 2001,415:197).The fixedly site of mice is apart from tail 1cm place slightly.Observe 6min, record mice and stop struggling, body is the dead time of relaxation state.
Experimental result represents with mean+/-standard error, with the t inspection statistics, processes.
The impact of table 1 Sarcaboside B on Tail suspension test
Annotate: with the blank group, compare * p＜0.05, * * p＜0.01.
Tail suspension test is classical screening antidepressants experimental model.Mouse tail suspension after a period of time, presents desperate state, stops struggling, and the time of record this moment is " dead time ".Effectively antidepressants can make the dead time of mouse tail suspension shorten.This experiment shows that Sarcaboside B has antidepressant effect.By as seen from Table 1, compare with the blank group, after mouse tail suspension is motionless, the motionless time shorten of accumulative total in fluoxetine Hydrochloride group 6min, difference has statistical significance; The time shorten of the cumulative motionless state of Sarcaboside B, difference has statistical significance.
2, force the rats'swimming experiment
2.1 animal
40 of healthy SD rats, male, cleaning level, body weight 180 ~ 200g; 40 of healthy kunming mices, male, cleaning level, body weight 18 ~ 22 grams.Sub-cage rearing, 4, every cage.18 ~ 29 ℃ of room temperatures, relative humidity 40% ~ 70%, the well-ventilated, environment is quiet, drinks cold boiled water.
2.2 medicine and reagent
Positive drug is fluoxetine Hydrochloride (prozac), it is a kind of selective serotonin reuptake inhibitor, its effectively inhibitory neuron absorb 5-hydroxy tryptamine from synaptic space, increasing can be for the actual this neurotransmitter that utilizes in gap, thereby improve affective state, treatment inhibition mental disorder.Spain Lilly S.A. company, specification: 20mg/ sheet, quantity are 20mg/d.
2.3 animal grouping and processing
40 kunming mices are divided into 5 groups at random, every group of 8 animals.Specifically be grouped as follows: (1) blank group; (2) Sarcaboside B high dose group (5mg/Kg); (3) dosage group (1mg/Kg) in Sarcaboside B; (4) Sarcaboside B low dose group (0.2mg/Kg); (5) fluoxetine Hydrochloride group.This experimental result judgement is the band subjectivity easily, for reducing this experiment of error, adopts blind method.Concrete group and gastric infusion are responsible for by the special messenger, and the experimental index tester is ignorant in advance.
Swimming device is made (European Journal of Pharmacology2003,461:99) by transparent organic glass.High 40cm, internal diameter 18cm, depth of water 20cm, water temperature is 25 ℃.Before formal experiment, with rat at working in water 15min.After 24 hours, rat is placed in water, records the rat dead time in 5min.Standard is the little volume body of rat, is floating state, surfaces in nostril.
The impact of table 2 Sarcaboside B on the experiment of mice forced swimming
Annotate: with the blank group, compare * p＜0.05, * p＜0.01.
Force the rats'swimming experiment to be classical screening antidepressants experimental model.Effectively antidepressants can make the dead time of rats'swimming shorten.This experiment shows that Sarcaboside B has antidepressant effect.By as seen from Table 2, to compare with the blank group, fluoxetine Hydrochloride group rat motionless time in Plastic Drum went swimming 5min obviously shortens, and difference has significant statistical significance (P＜0.01); Each group of Sarcaboside B can significantly shorten the time of cumulative motionless state in rat 5min.
3 conclusions
More than experimental results show that: Sarcaboside B has obvious antidepressant effect, thereby, can and treat antidepressant medicine for the preparation of prevention.
Claims (1)
1.Sarcaboside the application of B in antidepressant drug, described compound S arcaboside B structure as
Formula IShown in:
Formula I.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2013102625756A CN103393640A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B to antidepressant medicament |
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| CN2013102625756A CN103393640A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B to antidepressant medicament |
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Application publication date: 20131120 |