CN104606217A - Application of catalpol in preparation of antidepressant medicine - Google Patents
Application of catalpol in preparation of antidepressant medicine Download PDFInfo
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- CN104606217A CN104606217A CN201510039946.3A CN201510039946A CN104606217A CN 104606217 A CN104606217 A CN 104606217A CN 201510039946 A CN201510039946 A CN 201510039946A CN 104606217 A CN104606217 A CN 104606217A
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Abstract
The invention discloses application of catalpol in the preparation of an antidepressant medicine. The catalpol can be used as the antidepressant medicine for preventing and treating depression. A mouse forced swimming test (FST), a mouse tail suspension test (TST) and a rat chronic unpredictable mild stress (CUMS) test prove that the catalpol has an obvious antidepressant effect, the antidepressant activity of the catalpol reaches or exceeds that of the anti-depression western medicine fluoxetine commonly used in the clinic, and the catalpol can be used for preparing the medicine for preventing and treating depression.
Description
Technical field
The present invention relates to anti-depression drug, specifically belong to a kind of novelty teabag of native compound catalpol.
Background technology
Depression belongs to the one of mental state (emotion) obstacle, and main manifestations is depressed for presenting significantly and enduringly, and slight person shows as dysphoria, interest blank, and severe patient can be overwhelmed with sorrow, pessimistic desperate, often has suicidal tendency.Depression is the common mental sickness of a class serious harm human physical and mental health, and World Health Organization (WHO) has been classified as one of ten large heavy diseases.Along with socioeconomic fast development, the quickening of rhythm of life, the pressure of people increases, and various emotion is impacted and strengthened, and causes depression rate to increase year by year.Depression is known as " epidemic diseases of 21st century ".
At present, the drug main of Cure of depression will selectively serotonin reuptake inhibitors, serotonin and NRI, oxidase inhibitor and tricyclic antidepressant.Modern medicine is a lot of to the research of depression, but still not bery clear and definite to its pathogenesis, and the medicine of existing Cure of depression is many is subject to serious restriction due to reasons such as untoward reaction are more, expensive.In recent years, Chinese medicine more and more gets more and more people's extensive concerning for the treatment of depression.Acupuncture, Chinese herbal medicine are used for the treatment of depression and anxiety neurosis also causes the attention of height in states such as America and Europes.Therefore, from Chinese herbal medicine, excavate the native compound with good antidepressant effect is the important channel finding to have the antidepressants of good therapeutical effect.
Catalpol (Catalpol) has another name called catalpinoside, and being fresh from scrophulariaceae rehmannia glutinosa plant or the micromolecule iridoid that extracts dried root, is the principle active component of Radix Rehmanniae, molecular formula C
15h
22o
10, molecular weight is 362.33 DEG C, fusing point 207 ~ 209 DEG C, soluble in water.
Catalpol be distributed widely in Metachlamydeae, Loganiaceae Herba Buddlejae Lindleyanae belong to, Scrophulariaceae bubble Chinese parasol tree belong to and the plant such as Radix Rehmanniae genuss, bavin Wei section Cinnamomum, Orobanchaceae Cistanche deserticola, Plantaginaceae Plantago in, raw material sources and enrich.Modern study shows, catalpol has the multiple pharmacological effect such as anti-apoptotic, antioxidation, antitumor, blood sugar lowering, protection cardiovascular.But catalpol have not been reported preparing in prevention and therapy antidepressant agents.
Summary of the invention
The object of the present invention is to provide the novelty teabag of catalpol.
Catalpol provided by the invention is preparing the application in antidepressant drug.
Described medicine can be made up of catalpol and pharmaceutically acceptable carrier.Described carrier comprises: the conventional pharmaceutical adjuvants such as starch, dextrin or cyclodextrin and various Chemical modified cyclodextrin, sucrose.
Described medicine is oral formulations, injection or local administration preparation.Described oral formulations is tablet, effervescent tablet, capsule, liposome, capsule of nano, hard capsule, nanometer oral liquid or micropill.Described injection is injection dosage form or freeze-dried powder injection type.Described local administration preparation is ointment, spray or patch.
The present invention take fluoxetine as positive drug, carries out evaluating drug effect, filter out antidepressant optimal dose simultaneously by mouse tail suspension and swimming test to catalpol.Experimental result shows, this compound obviously can reduce the dead time in Mouse Forced Swim Test and rat force swimming test, the body weight of the chronic gentleness of remarkable increase unpredictable depression model sucrose solution consumption and rat, the autonomic activities number of times of rat can also be improved, show that it has obvious antidepressant effect, antidepressant activity meets or exceeds clinical conventional antidepressant Western medicine fluoxetine.
Accompanying drawing explanation
Fig. 1 catalpol is on the impact of CUMS rat sucrose solution preference rate
Detailed description of the invention
In order to further describe in detail the present invention, provide following specific embodiment, but only as illustrating the present invention, instead of in order to limit the scope of the invention.
Embodiment 1 catalpol antidepressant pharmacodynamic experiment
The present invention adopts the gentle unpredictability of Mouse Forced Swim Test (Forced swimming test), rat force swimming test (Tail suspensiontest) and rat chronic program (CUMS) stress verify the antidepressant effect of catalpol.
1.1 laboratory animals and administration
Laboratory animal is that (Beijing dimension tonneau China animal experimental center provides healthy ICR mice, and the quality certification is numbered: SCXK (capital) 2014-0003), male, 18 ~ 22g; (Beijing dimension tonneau China animal experimental center provides SD rat, the quality certification is numbered: SCXK (capital) 2014-0012), male, 180 ~ 200g raises in University Of Shanxi's Experimental Animal Center, experimental session keeps freely drinking water and taking food, feeding environment temperature is 22 ± 2 DEG C, and adaptability is fed after 3 ~ 5 days and tested.Positive control drug is fluoxetine Hydrochloride (7.5mg/kg), and investigational agent is the basic, normal, high dosage of catalpol (50mg/kg, 100mg/kg and 200mg/kg).
1.2. experimental technique
1.2.1 Mouse Forced Swim Test
Mice administration was tested after 1 hour, be placed on high 20cm, in the lucite cylinder of diameter 10cm, wherein put into the water of 22 ± 2 DEG C, height 15cm, each operation one, and the swimming behavior recording mice in 6min with animal behavior video analytic system (Jiliang Software Sci-Tech Co., Ltd., Shanghai), analyze the accumulative dead time (s) of mouse forced swimming test in rear 4min.Dead time is judged as that animal stops struggling in water, in floating state, only has tiny limb motion to float on the surface to keep head.
1.2.2 rat force swimming test
Mice administration was tested after 1 hour, and its tail point 1cm place is pasted hang upside down, each operation one, with the desperate behavior of mice in animal behavior video analytic system record 6min, and the accumulative dead time (s) after analyzing in 4min.Judge that motionless standard is that mice stops struggling, in lent inverted hang state, transfixion.
1.2.3 the gentle unpredictability stress tests of rat chronic
SD rat is divided into 6 groups at random, often organizes 12, and blank group does not give any stimulation, drinking-water of normally taking food.Respectively the random acceptance of group 28 days unpredictability gentlenesses stress for all the other, comprise frozen water swimming (4 DEG C, 5min), tail 2min, foot shock (36V voltage is pressed from both sides, each 10s, every minor tick 15s, totally 10 times), thermostimulation (45 DEG C, 10min), concussion 2min, fasting 24h, prohibit water 24h.Give a kind of stimulation every day, often kind stimulates random use 3 times.The 14th day stress at the end of, fluoxetine group and catalpol each dosage group start gavage and give corresponding medicine.Blank group and model group then give isopyknic normal saline.Test start and experiment the 7th day, the 14th day, the 21st day and the 28th day time measure body weight and the 1% sucrose water consumption in 24 hours of every rat.Administration in the 28th day after 1 hour, (inwall is black rat to be placed in self-control Open-field activities test box, bottom white line is divided into 25 lattice) central authorities, with the autonomic activities behavior of animal behavior video analytic system record rat, analytic statistics rat passes through lined and upright number of times.
1.3. experimental result
Mouse Forced Swim Test the results are shown in Table 1, result shows, in catalpol, dosage and high dose group compare with blank group, dead time all significantly reduces, there is statistical significance (P < 0.05, P < 0.01), and compare no significant difference with fluoxetine group.
Table 1 Mouse Forced Swim Test dead time (s)
Compare with blank group: * P < 0.05, * * P < 0.01
Rat force swimming test the results are shown in Table 2, result shows, in catalpol, dosage and high dose group compare with blank group, dead time all significantly reduces, there is statistical significance (P < 0.05, P < 0.01), and compare no significant difference with fluoxetine group.
Table 2 rat force swimming test dead time (s)
Compare with blank group: * P < 0.05, * * P<0.01
In the slow stress tests of rat 24 hours, 1% sucrose water preference rate (sucrose solution consumption rate) the results are shown in Figure 1, and result shows, each group rat sucrose solution consumption there was no significant difference before experiment.Increase gradually in experiment the 7th day, the 14th day, the 21st day and 28 days blank control rats sucrose solution preference rates, but there was no significant difference.The basic, normal, high dosage group of model group, fluoxetine group, catalpol stress the 14th day time sucrose solution preference rate be all significantly less than blank group consumption.Compare with model group, when experiment the 21st day, fluoxetine group, catalpol high dose group, middle dosage group and low dose group and model group had significant difference (* P < 0.05, * * P < 0.01).When experiment 28 days, fluoxetine group, catalpol high dose group, middle dosage group and low dose group and model group have significant difference (* P < 0.05, * P < 0.01), and in fluoxetine group and catalpol dosage group close to blank group.
The slow stress tests of rat on the impact of body weight in table 3, result shows, each group rat body weight no significant difference (P > 0.05) before experiment, the 7th day after the test, the 14th day, the 21st day and the 28th day blank group control rats body weight obviously increases, and each stress group accept stress stimulation after 28 days body weight all have increase in various degree compared with before experiment, but there was no significant difference; When experiment 21 days, fluoxetine group, catalpol high dose group, middle dosage group and low dose group and model group had significant difference (* P < 0.05, * * P < 0.01).When experiment 28 days, fluoxetine group and catalpol high dose group rat body weight were closest to blank group rat body weight, and compared with model group and have significant difference (* P < 0.05, * * P < 0.01).
Table 3 catalpol is on the impact of CUMS rat body weight
Compare with model group: * P < 0.05, * * P<0.01
Open field test the results are shown in Table 4, catalpol successive administration is after 14 days, result shows, the behavioral indexes of each administration group is all higher than model group, and have significant difference (* P < 0.05, * P < 0.01), wherein in positive drug group and catalpol the behavioral indexes of dosage group closest to blank group, and there was no significant difference between the two.
Lined quantity and upright number of times is passed through in the experiment of table 4 rat spacious field
Compare with model group: * P < 0.05, * * P<0.01
Above experimental result shows, the catalpol related in the present invention significantly can reduce the dead time in mouse forced swimming test and the test of outstanding tail, also sucrose solution consumption and the body weight increment of chronic gentle unpredictability Stress model rat can be increased, and the autonomic activities of rat can be improved, therefore can think that this compound has significant antidepressant effect, especially best with middle dose effect, may be used for the medicine preparing Cure of depression.
The preparation of embodiment 2 capsule
Get the appropriate 200g of catalpol, then add starch 800g, mix homogeneously, with 10% starch slurry soft material, cross 14 mesh sieves and granulate, in 70 ~ 80 DEG C of dryings, 16 mesh sieve granulate, load in snap fit capsule, obtain capsule.
The preparation of embodiment 3 tablet
Get catalpol 200g, then add starch 800g, mix homogeneously, with 10% starch slurry soft material, cross 14 mesh sieves and granulate, 70 ~ 80 DEG C of dryings, 16 mesh sieve granulate, add 0.5% magnesium stearate 3g mixing, tabletting, sugar coating, subpackage, obtained tablet.
The preparation of embodiment 4 granule
Get catalpol 50g, then add sucrose fine 450g, dextrin 100g, with 70% ethanol soft material, cross 14 mesh sieves and granulate, 50 ~ 60 DEG C of dryings, 16 mesh sieve granulate obtain granule.
The preparation of embodiment 5 injection
Get catalpol 50g, add sodium chloride 200g again, add water for injection, stirring makes it dissolve, regulate pH (6.8 ~ 7.0) with 10% bicarbonate aqueous solution, inject water to 1000ml, then filter with 0.22 μm of microporous filter membrane, subpackage embedding (2ml/ bottle), 100 DEG C of bacterium 30 minutes and get final product.
The preparation of embodiment 6 ointment
9.0g glycerol, 0.1g sodium benzoate are dissolved in 60ml distilled water, then add 3.0g methylcellulose, stir, be placed to gel, obtain water-soluble ointment base; Put into 15g catalpol, stir and get final product.
Claims (6)
1. catalpol is preparing the application in antidepressant drug.
2. catalpol as claimed in claim 1 is preparing the application in antidepressant drug, and it is characterized in that, described medicine is made up of catalpol and pharmaceutically acceptable carrier.
3. catalpol as claimed in claim 1 is preparing the application in antidepressant drug, and it is characterized in that, described medicine is oral formulations, injection or local administration preparation.
4. catalpol as claimed in claim 3 is preparing the application in antidepressant drug, and it is characterized in that, described oral formulations is tablet, effervescent tablet, capsule, liposome, capsule of nano, hard capsule, nanometer oral liquid or micropill.
5. catalpol according to claim 3 is preparing the application in antidepressant drug, it is characterized in that, described injection is injection dosage form or freeze-dried powder injection type.
6. catalpol as claimed in claim 3 is preparing the application in antidepressant drug, and it is characterized in that, described local administration preparation is ointment, spray or patch.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201510039946.3A CN104606217A (en) | 2015-01-27 | 2015-01-27 | Application of catalpol in preparation of antidepressant medicine |
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| CN201510039946.3A CN104606217A (en) | 2015-01-27 | 2015-01-27 | Application of catalpol in preparation of antidepressant medicine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115252749A (en) * | 2022-03-26 | 2022-11-01 | 吉林大学 | Application of aconite root preparation for regulating middle warmer as antidepressant targeting medicine |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101579319A (en) * | 2009-06-12 | 2009-11-18 | 西南大学 | Medical prescription of catalpol freezing-drying powder for injection and preparation method |
| CN102008497A (en) * | 2010-11-03 | 2011-04-13 | 南京中医药大学 | Application of catalpol in preparing drug for treating cardiac failure disease |
-
2015
- 2015-01-27 CN CN201510039946.3A patent/CN104606217A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101579319A (en) * | 2009-06-12 | 2009-11-18 | 西南大学 | Medical prescription of catalpol freezing-drying powder for injection and preparation method |
| CN102008497A (en) * | 2010-11-03 | 2011-04-13 | 南京中医药大学 | Application of catalpol in preparing drug for treating cardiac failure disease |
Non-Patent Citations (1)
| Title |
|---|
| 王君明 等: "地黄醇提物及其药渣水提物抗抑郁作用的比较研究", 《中国药学杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115252749A (en) * | 2022-03-26 | 2022-11-01 | 吉林大学 | Application of aconite root preparation for regulating middle warmer as antidepressant targeting medicine |
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Application publication date: 20150513 |
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