CN102872051B - Application of gypensapogenin A to antidepressant drugs - Google Patents
Application of gypensapogenin A to antidepressant drugs Download PDFInfo
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- CN102872051B CN102872051B CN 201210418183 CN201210418183A CN102872051B CN 102872051 B CN102872051 B CN 102872051B CN 201210418183 CN201210418183 CN 201210418183 CN 201210418183 A CN201210418183 A CN 201210418183A CN 102872051 B CN102872051 B CN 102872051B
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Abstract
The invention discloses application of gypensapogenin A to antidepressant drugs. Gypensapogenin A involved in the invention can be used as an antidepressant drug. The application of gypensapogenin A to the preparation of the antidepressant drugs is firstly publicized, the skeleton type is brand-new, the antidepressant activity is unexpectedly strong and the possibility of giving any revelation by other compounds does not exist, so that prominent substantive features are provided and a remarkable progress in the prevention of depression is made at the same time.
Description
Technical field
The present invention relates to medical technical field, exactly is the new purposes of Gypensapogenin A in antidepressant drug.
Background technology
Depression is a kind of common mood disorders, can be caused by a variety of causes, and low with remarkable and lasting mental state is main clinical characteristics, and mental state is low unbecoming with its situation, and suicidal thought and behavior can appear in severe patient.Most cases have the tendency of outbreak repeatedly, and the great majority that at every turn show effect can be alleviated, and part can have residual symptom 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 refers to serious symptom depression (major depression) clinically in fact in addition, has 16% people influenced by it in certain period throughout one's life among the crowd.Suffer from depression except paying serious emotion and social costs, economic cost also is huge.According to World Health Organization's statistics, depression has become the world's the 4th big illness, expects the year two thousand twenty, may become the second largest disease that is only second to coronary heart disease.
The chemical compound Gypensapogenin A that the present invention relates to is one and delivered (Li in 2012, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178.) new framework compound, this chemical compound has brand-new framework types, present purposes only relates to the cytotoxic activity (Li of human tumor cell line, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178.), belong to open first for the purposes of the Gypensapogenin A that the present invention relates in the preparation antidepressant drug, because framework types belongs to brand-new framework types, and its antidepressant activity is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for antidepressant drug simultaneously and obviously have obvious improvement.
Summary of the invention
The purpose of this invention is to provide the purposes of Gypensapogenin A 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 antidepressant.
Described chemical compound Gypensapogenin A structure is shown in formula I:
The purposes of the Gypensapogenin A that the present invention relates in the preparation antidepressant drug belongs to open first, because framework types belongs to brand-new framework types, and its antidepressant activity is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for antidepressant drug simultaneously and obviously have obvious improvement.
The specific embodiment
The preparation method of chemical compound Gypensapogenin A involved in the present invention is referring to document (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178. and Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45 (3): 167-171.).
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 limited by claim.
Embodiment 1: the preparation of chemical compound Gypensapogenin A tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of chemical compound Gypensapogenin A capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin A, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Below can be used as the experiment situation of antidepressant drug for the present invention.
1, mouse tail suspension experiment
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 in every cage.18 ~ 29 ℃ of room temperatures, relative humidity 40% ~ 70%, the well-ventilated, cold boiled water is drunk in the environment peace and quiet.
1.2 medicine and reagent
Positive drug is fluoxetine Hydrochloride (prozac), it is a kind of selective serotonin reuptake inhibitor, it can suppress neuron effectively and absorb 5-hydroxy tryptamine from synaptic space, increasing can be for the actual this neurotransmitter that utilizes in the gap, thereby improve affective state, treatment inhibition mental disorder.Spain Lilly S.A. company, clinical consumption 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) Gypensapogenin A high dose group (5mg/Kg); (3) dosage group (1mg/Kg) among the Gypensapogenin A; (4) Gypensapogenin A low dose group (0.2mg/Kg); (5) fluoxetine Hydrochloride group.This experimental result is judged easily band subjectivity, adopts blind method for reducing this experiment of error.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, the record mice stops to struggle, and body is the dead time of relaxation state.
Experimental result is represented with mean+/-standard error, handles with the t inspection statistics.
The influence of the mouse tail suspension experiment of table 1 Gypensapogenin A
Annotate: compare * p＜0.05, * * p＜0.01 with the blank group.
The mouse tail suspension experiment is classical screening antidepressants experimental model.Mouse tail suspension presents desperate state after a period of time, stops to struggle, 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 Gypensapogenin A has antidepressant effect.By table 1 as seen, compare with the blank group, after mouse tail suspension was motionless, the motionless time of accumulative total shortened in the fluoxetine Hydrochloride group 6min, and difference has statistical significance; Add up time of motionless state of Gypensapogenin A shortens, and 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 in every cage.18 ~ 29 ℃ of room temperatures, relative humidity 40% ~ 70%, the well-ventilated, cold boiled water is drunk in the environment peace and quiet.
2.2 medicine and reagent
Positive drug is fluoxetine Hydrochloride (prozac), it is a kind of selective serotonin reuptake inhibitor, it can suppress neuron effectively and absorb 5-hydroxy tryptamine from synaptic space, increasing can be for the actual this neurotransmitter that utilizes in the gap, thereby improve affective state, treatment inhibition mental disorder.Spain Lilly S.A. company, specification: 20mg/ sheet, clinical consumption 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) Gypensapogenin A high dose group (5mg/Kg); (3) dosage group (1mg/Kg) among the Gypensapogenin A; (4) Gypensapogenin A low dose group (0.2mg/Kg); (5) fluoxetine Hydrochloride group.This experimental result is judged easily band subjectivity, adopts blind method for reducing this experiment of error.Concrete group and gastric infusion are responsible for by the special messenger, and the experimental index tester is ignorant in advance.
Swimming device by transparent organic glass make (European Journal of Pharmacology2003,461:99).High 40cm, internal diameter 18cm, depth of water 20cm, water temperature is 25 ℃.Before the formal experiment, with rat at working in water 15min.After 24 hours, rat is placed water, the rat dead time among the record 5min.Standard is the little volume body of rat, is floating state, surfaces in the nostril.
The influence of the mice forced swimming experiment of table 2 Gypensapogenin A
Annotate: compare * p＜0.05, * p＜0.01 with the blank group.
Force the rats'swimming experiment to be classical screening antidepressants experimental model.Effectively antidepressants can make rats'swimming immobility time shorten.This experiment shows that Gypensapogenin A has antidepressant effect.By table 2 as seen, with the blank group relatively, fluoxetine Hydrochloride group rat is swum in Plastic Drum, and the motionless time obviously shortens in the 5min, difference has significant statistical significance (P＜0.01); Each group of Gypensapogenin A can significantly shorten the time of the motionless state that adds up in the rat 5min.
3 conclusions
More than experimental results show that: Gypensapogenin A has tangible antidepressant effect, thereby, can and treat antidepressant medicine for the preparation of prevention.
Claims (1)
1.Gypensapogenin A is in the application of preparation in the antidepressant drug, described chemical compound Gypensapogenin A structure as
Formula IShown in:
Formula I.
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