CN103027916A - Application of Houttuynoid D in preparation of antidepressant drug - Google Patents
Application of Houttuynoid D in preparation of antidepressant drug Download PDFInfo
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- CN103027916A CN103027916A CN2012104704283A CN201210470428A CN103027916A CN 103027916 A CN103027916 A CN 103027916A CN 2012104704283 A CN2012104704283 A CN 2012104704283A CN 201210470428 A CN201210470428 A CN 201210470428A CN 103027916 A CN103027916 A CN 103027916A
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- houttuynoid
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Abstract
The invention discloses application of Houttuynoid D in preparation of an antidepressant drug. The invention provides the use of Houttuynoid D in the antidepressant drug. The Houttuynoid D disclosed by the invention can be used as the drug for preventing or treating depression. The use of the Houttuynoid D disclosed by the invention in the preparation of the antidepressant drug is firstly disclosed. The framework type is a brand-new framework type and has an unexpected strong effect of restraining the bacterial activity, and so the Houttuynoid D is impossibly reveled by other compounds, and has outstanding substantial characteristics. Meanwhile, the Houttuynoid D has significant progress in antidepressant drug.
Description
Technical field
The present invention relates to medical technical field, exactly is the new purposes of Houttuynoid D 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 repeatedly tendency of outbreak, 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 refers to major depression (major depression) clinically in fact in addition, has 16% people affected 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 large illness, expects the year two thousand twenty, may become the second largest disease that is only second to coronary heart disease.
The compound H outtuynoid D that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Houttuynoid D, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to DEF(Cai, J. Y. et al., 2012. Houttuynoid D, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Houttuynoid D 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 simultaneously antidepressant drug and obviously have significant progress.
Summary of the invention
The purpose of this invention is to provide the purposes of Houttuynoid D in antidepressant drug.The present invention has the well function of relieving anxiety and stress.The inventor has wide practical use by studies show that this medicine in prevention or controlling antidepressant.
Described compound H outtuynoid D structure is shown in formula I:
The purposes of the Houttuynoid D 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 simultaneously antidepressant drug and obviously have significant progress.
The specific embodiment
The preparation method of compound H outtuynoid D involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Houttuynoid D, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 compound H outtuynoid D tablet involved in the present invention:
Get 20 and digest compound Houttuynoid D, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid D capsule involved in the present invention:
Get 20 and digest compound Houttuynoid D, 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, 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 in 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 from synaptic space, absorb 5-hydroxy tryptamine, 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, 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) Houttuynoid D high dose group (5mg/Kg); (3) dosage group (1mg/Kg) among the Houttuynoid D; (4) Houttuynoid D 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 represents with mean+/-standard error, processes with the t inspection statistics.
Table 1 Houttuynoid D is on the impact of Tail suspension test
Annotate: compare * p＜0.05, * * p＜0.01 with the blank group.
Tail suspension test 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 Houttuynoid D 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 the fluoxetine Hydrochloride group 6min, difference has statistical significance; The time shorten of the cumulative motionless state of Houttuynoid D, 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, 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 from synaptic space, absorb 5-hydroxy tryptamine, 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, 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) Houttuynoid D high dose group (5mg/Kg); (3) dosage group (1mg/Kg) among the Houttuynoid D; (4) Houttuynoid D 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 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 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.
Table 2 Houttuynoid D is on the impact of mice forced swimming experiment
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 the dead time of rats'swimming shorten.This experiment shows that Houttuynoid D 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 Houttuynoid D can significantly shorten the time of cumulative motionless state in the rat 5min.
3 conclusions
More than experimental results show that: Houttuynoid D has obvious antidepressant effect, thereby, can and treat antidepressant medicine for the preparation of prevention.
Claims (1)
1.Houttuynoid D is in the application of preparation in the antidepressant drug, described compound H outtuynoid D structure as
Formula IShown in:
Formula I.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2012104704283A CN103027916A (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid D in preparation of antidepressant drug |
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| CN2012104704283A CN103027916A (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid D in preparation of antidepressant drug |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105267189A (en) * | 2015-10-29 | 2016-01-27 | 淄博齐鼎立专利信息咨询有限公司 | Application of Haloroquinone in preparation of antidepressant drugs |
-
2012
- 2012-11-19 CN CN2012104704283A patent/CN103027916A/en not_active Withdrawn
Non-Patent Citations (1)
| Title |
|---|
| SHAO-DAN CHEN，ET AL: "Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata", 《ORGANIC LETTERS》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105267189A (en) * | 2015-10-29 | 2016-01-27 | 淄博齐鼎立专利信息咨询有限公司 | Application of Haloroquinone in preparation of antidepressant drugs |
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Application publication date: 20130410 |