CN104840527A - Composition containing tenuifoliside and ginsenoside - Google Patents
Composition containing tenuifoliside and ginsenoside Download PDFInfo
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- CN104840527A CN104840527A CN201510216169.5A CN201510216169A CN104840527A CN 104840527 A CN104840527 A CN 104840527A CN 201510216169 A CN201510216169 A CN 201510216169A CN 104840527 A CN104840527 A CN 104840527A
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- ginsenoside
- radix polygalae
- sugar ester
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Abstract
The invention provides a composition containing tenuifoliside and ginsenoside. The composition is formed by tenuifoliside and ginsenoside in a weight ratio in a range of 0.5:0.5 to 0.11:0.89. Single effective tenuifoliside and ginsenoside are extracted from tenuifoliside and ginsenoside medicine materials, and both reach more than 50%. The composition can be applied to preparation of medicine for treating and improving depression. Two effective parts are combined, and accordingly, the mouse yohimbine toxicity is enhanced apparently, and the mouse forced swimming unmovable time is shortened apparently. By combining the two effective parts, the effect is enhanced compared with the effect of single use of any one part. By means of the composition, medicine definitive in curative effect and slight in adverse reaction is provided for treating and improving depression.
Description
Technical field
The invention belongs to natural drug composition, the compositions particularly relating to Radix Polygalae sugar ester and ginsenoside and the purposes for the treatment of in preparation and improving in antidepressant agents thereof.
Background technology
Depression is also known as depressive disorder, low for main clinical characteristics with remarkable and lasting mental state, is the main Types of mood disorders.World Health Organization's investigation statistics is analyzed, and the incidence rate of global depression is about 53.1%, and in developed country close to about 60%, 2002 years existing more than 8,900 ten thousand people of global Serious depression patient, and the patients with depression in the whole world reaches 3.4 hundred million.In the adult population of 18 years old, patients with depression just increases with the speed of annual 41.3%.Depression also allows of no optimist in the situation of China, and current depression is approximately 24% at the sickness rate of China, and some areas Epidemiological study data shows, depression prevalence is about about 29-35%, close with developed country.World Health Organization (WHO) predicts, to the year two thousand twenty, depression will become the second largest class pandemic after cardiovascular disease.Depression is one of important hazard factor of committing suiside, and the suicide of 90% is relevant with depression.Meanwhile, depression often occurs together cardiovascular and cerebrovascular disease, diabetes, Alzheimer and tumor etc.
There is series of problems in antidepressant chemicals, as slow in onset, easily recurrence and many untoward reaction etc.At present, the research and development of antidepressant drug have been turned to traditional medicine field by people more.Radix Polygalae is milk wort Radix Polygalae
polygala tenuifoliaor ovum leaf Radix Polygalae Willd.
polygala sibirical. dry root, has effect of Fructus Alpiniae Oxyphyllae of calming the nerves, restoring normal coordination between the heart and kidney, eliminating phlegm for diminishing swelling, be clinically used for the treatment of insomnia and dreamful sleep, forgetful palpitation with fear that disarmony between the heart and kidney causes, mind be in a trance, expectoration is not well, sore swollen toxin, breast swell and pain.Chemical constitution study shows: chemical composition contained by Radix Polygalae is mainly saponin, sugar ester, ketone, alkaloid and fatty wet goods.Modern pharmacology research shows: polygalic acid has the effect of expelling phlegm for arresting cough, is also the major toxicity composition (having obvious gastric irritation effect and haemolysis) of Radix Polygalae; Radix Polygalae ketone has the effect of antifungal and pain relieving; Radix Polygalae sugar ester is considered to the antidepressant material base of Radix Polygalae.Radix Ginseng is Araliaceae Radix Ginseng
panax ginsengc. the dry root welding technology of A. Mey..Have strongly invigorating primordial QI, multiple arteries and veins takes off admittedly, and invigorating the spleen to benefit the lung, promotes the production of body fluid and nourish blood, Fructus Alpiniae Oxyphyllae of calming the nerves, clinical in weak body and prostration, cold extremities faint pulse, insufficiency of the spleen lack of appetite, and the deficiency of the lung is breathed with cough, and Tianjin wound is thirsty, and interior-heat is quenched one's thirst, deficiency of qi and blood, prolonged illness weakness with emaciation, palpitation with fear insomnia, sexual impotence cold womb.Chemical constitution study shows, Radix Ginseng contains the compositions such as saponins, saccharide, volatile ingredient, organic acid and ester thereof, protein, enzyme, sterol and glycosides, polypeptide class, nitrogen-containing compound, lignin, flavonoid, vitamins, inorganic elements.Wherein, principle active component is ginsenoside and ginseng polysaccharide.Modern pharmacology research shows: Radix Ginseng effect of disease in central nervous system is relevant with ginsenoside.Radix Polygalae and Radix Ginseng clinically frequent compatibility are applied to the treatment of depression, and it represents prescription as Kaixin San, sedate piller etc., in zoopery and clinical research, all show good antidepressant effect.
Summary of the invention
An object of the present invention is to provide Radix Polygalae sugar ester and Panaxsaponin composition, compositions consist of Radix Polygalae sugar ester: the weight ratio of ginsenoside is 0.5:0.5 ~ 0.11:0.89, and Radix Polygalae sugar ester and ginsenoside are the effective site extracting single tool activity from Chinese medicine polygala root and Radix Ginseng.
Another object of the present invention is to provide the application of said composition in the medicine preparing Cure of depression.
Another object of the present invention is to provide said composition and is preparing the application improved in the medicine of depression.
Dosage form prepared by described compositions and pharmaceutical excipient, mainly comprises liquid preparation and solid preparation.Solid preparation mainly comprises granule, tablet, capsule (containing soft capsule), drop pill.Liquid preparation mainly comprises oral liquid and injecting fluid preparation.
The form of medication of described preparation mainly comprises oral administration or parenterai administration.
Compositions of the present invention medical material Radix Polygalae used and Radix Ginseng clinically frequent compatibility are applied to the treatment of depression, have the Chinese medical theory basis that experienced by long-term prescription confirmation of China's uniqueness.Said composition can solve in such disease treatment, obviously lacks the problem of the medicine that curative effect is affirmed, untoward reaction is slight.Prove through animal pharmacodynamic experiment, said composition has following effect: (1) significantly strengthens the toxicity of mice Yohimbine.(2) significantly the mouse forced swimming test dead time is shortened.Two kinds of effective sites are share, more remarkable than the effect of alone wherein any one, not simply act on superposition.This compositions toxicological effect result of study shows, the Mouse Acute Toxicity result of study that two kinds of effective site is share, similar with alone wherein any one, does not all occur dead and obvious poisoning symptom.The present invention extracts single effective site Radix Polygalae sugar ester and ginsenoside from Radix Polygalae and ginseng crude drug, respectively reaches 50 more than %.
Detailed description of the invention
Following examples further illustrate of the present invention, instead of limitation of the present invention.
embodiment 1: the preparation method of Radix Polygalae sugar ester of the present invention and ginsenoside
(1) the Radix Polygalae sugar ester effective site that the present invention is used, obtain see patent No. method disclosed in 201410215399.5: take Polygala tenuifolia as raw material, alcoholic solution circumfluence method is adopted to extract, be specially: with 70 % alcoholic solution of Polygala tenuifolia quality 10 times amount for Extraction solvent, reflux, extract, 3 times, each 1.5 h, merge extractive liquid, be evaporated to without alcohol taste (60 DEG C), obtain Radix Polygalae extract.D130 macroporous resin is adopted to carry out purification to the Radix Polygalae extract of gained.The concentration of sample solution is for containing crude drug 0.25 g/ml, and loading speed is 2 Bv/h, and applied sample amount is 4 Bv; First rinse with the water of 5 Bv in elution process, washing speed is 4 Bv/h, and then carry out eluting with the alcoholic solution that the concentration of 5 Bv is 20 %, elution speed is 2 Bv/h, then carry out eluting with the alcoholic solution that the concentration of 6 Bv is 35 %, elution speed is 2 Bv/h.35 % alcoholic solution eluents, are evaporated to without alcohol taste (60 DEG C), obtain sugar esters enrichment positions.The sugar esters enrichment positions of method to gained of liquid-liquid extraction is adopted to carry out purification.Sugar ester enrichment positions adds aqueous dispersion and obtains sample liquid, and concentration is for containing sugar ester 6.81 mg/ml, and extractant is ethyl acetate, extraction times 3 times, and each extractant consumption is 3 times of sample liquid amounts.Combined ethyl acetate layer; be evaporated to dry (60 DEG C); obtain Radix Polygalae sugar ester effective site (analyze through HPLC, tenuifoliside A, tenuifoliside B, tenuifoliside C and 3',6-disinapoylsucrose content sum are 64.84%).
(2) ginsenoside's effective site that the present invention is used, prepare by the following method: get Radix Ginseng 300 g, be cut into sheet, add 8 times of water gagings, decoct twice, 2 hours first times, second time 1.5 hours, decoct and filter, merging filtrate, by D101 type macroporous adsorbent resin (column volume is 300 mL), water elution is to colourless, use 60% ethanol elution again, collect 60% ethanol elution, loading and elution speed are 2 Bv/h), it is 1.06(80 DEG C that filtrate is concentrated into relative density) clear paste, dry, pulverize, obtain ginsenoside (to analyze through HPLC, content of ginsenoside is 73.48 %).
embodiment 2: the maximum tolerated dose experiment of the present composition
(1) materials and methods
Radix Polygalae sugar ester and ginsenoside obtain with reference to embodiment 1 method, are made into suspension with 0.5% sodium carboxymethyl cellulose.Before use according to Radix Polygalae sugar ester: ginsenoside's weight ratio is respectively 0.5:0.5 and 0.11:0.89, mixing becomes compositions.
Adopt Cmax, maximum administration capacity 0.4 mL/10 g/ gastric infusion, one day administered twice, interval 6 h, observe the body weight of mice in the administration same day and two weeks subsequently and various symptom.
(2) result:
The mouse stomach administration same day and next day, all there is not death in all administration groups, has no apparent ill symptoms in two weeks subsequently.Within two weeks subsequently, have no apparent bad present situation.
(3) conclusion:
Mouse stomach gives 160mg/kg compositions and the single extract of two medical materials, does not occur death and the reaction of other overt toxicity.
embodiment 3: mice Yohimbine toxicity Enhancement test
(1) materials and methods:
Radix Polygalae sugar ester and ginsenoside obtain, according to Radix Polygalae sugar ester: ginsenoside weight ratio 0.11:0.89 with reference to embodiment 1 method.
Yohimbine Hcl: Aladdin Chemistry Co., Ltd. lot number: 29107.Normal saline: Hangzhou Ninth Heaven animal health-care product company limited lot number: 2014071901.
Male ICR mouse, cleaning grade, body weight 18 ~ 24g, gives mice standard pellet and pure drinking-water between feeding period.If solvent control group, fluoxetine positive drug control group (20 and 40 mg/kg), Radix Polygalae sugar ester group (2.5,5 and 10 mg/kg), ginsenoside's group (20,40 and 80 mg/kg), Radix Polygalae sugar ester and Panaxsaponin composition group (11.25 and 22.5 mg/kg), intraperitoneal injection.Give test medicine or solvent, the Yohimbine (25 mg/kg) of subcutaneous injection sublethal dose after 0.5 h.Observe tested group and control group mice mortality rate in 24 h.
(2) result
Experimental result is in table 1, and Radix Polygalae sugar ester (10 and 20 mg/kg) is alone, ginsenoside (80 and 120 mg/kg) is alone, and Radix Polygalae sugar ester and ginsenoside share (11.25 and 22.5 mg/kg) all significantly can strengthen the toxicity of mice Yohimbine.
(3) conclusion
Radix Polygalae sugar ester and Panaxsaponin composition group (11.25 and 22.5 mg/kg) significantly can strengthen the lethal effect of Yohimbine, more remarkable than alone arbitrary effective site effect.
embodiment 4: mouse forced swimming test
(1) materials and methods:
Radix Polygalae sugar ester and ginsenoside obtain, according to Radix Polygalae sugar ester: ginsenoside weight ratio 0.5:0.5 with reference to embodiment 1 method.
Fluoxetine Hydrochloride: Li Lai Suzhou pharmaceutical Co. Ltd.Normal saline: Hangzhou Ninth Heaven animal health-care product company limited lot number: 2014071901.
Male ICR mouse, cleaning grade, body weight 18 ~ 24g, starts experiment, gives mice standard pellet and pure drinking-water between feeding period after conforming 1 week.If solvent control group, fluoxetine positive drug control group (50 mg/kg), Radix Polygalae sugar ester group (25,50 and 100 mg/kg), ginsenoside's group (50 and 100 mg/kg), Radix Polygalae sugar ester and Panaxsaponin composition group (5,100 and 200 mg/kg), gastric infusion one week.
After experimental day is placed in experiment room, place adapts to 1 h, give test medicine or solvent 1h, be placed in fiberglass, observe the mouse forced swimming test dead time, observing time is 6 min altogether, the dead time in 4 min after record.
(2) result:
Experimental result is in table 2, and Radix Polygalae sugar ester (100 mg/kg) is alone, ginsenoside (100 mg/kg) is alone, and Radix Polygalae sugar ester and ginsenoside share (50+50 and 100+100 mg/kg) all can significantly shorten the ICR mouse forced swimming test dead time.
(3) conclusion:
Radix Polygalae sugar ester and Panaxsaponin composition group (50+50 and 100+100 mg/kg) can significantly shorten the ICR mouse forced swimming test dead time, more remarkable than alone arbitrary effective site effect.
Claims (4)
1. a Radix Polygalae sugar ester and Panaxsaponin composition, it is characterized in that, compositions consist of Radix Polygalae sugar ester: the weight ratio of ginsenoside is 0.5:0.5 ~ 0.11:0.89, and described Radix Polygalae sugar ester and ginsenoside are the effective site extracting single tool activity from Chinese medicine polygala root and Radix Ginseng.
2. Radix Polygalae sugar ester according to claim 1 and the application of Panaxsaponin composition in the medicine preparing Cure of depression.
3. Radix Polygalae sugar ester according to claim 1 and Panaxsaponin composition are preparing the application improved in the medicine of depression.
4. apply according to Claims 2 or 3, it is characterized in that, described medicine is made up of compositions and pharmaceutical excipient, and the dosage form of described medicine is liquid preparation and solid preparation.
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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KR20180027216A (en) * | 2016-09-06 | 2018-03-14 | 주식회사 엘지생활건강 | Composition for skin improvement containing tenuifoliside A |
CN109432181A (en) * | 2018-12-19 | 2019-03-08 | 泓博元生命科技(深圳)有限公司 | Alleviate the composition and the preparation method and application thereof of depression |
CN109620863A (en) * | 2018-12-19 | 2019-04-16 | 泓博元生命科技(深圳)有限公司 | A kind of composition and the preparation method and application thereof for alleviating depression |
CN113491727A (en) * | 2020-04-02 | 2021-10-12 | 中国医学科学院药用植物研究所 | Traditional Chinese medicine composition for treating depression and preparation method thereof |
CN116159101A (en) * | 2020-06-24 | 2023-05-26 | 鲁南新时代生物技术有限公司 | Traditional Chinese medicine composition and preparation method and application thereof |
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CN104027403A (en) * | 2014-05-21 | 2014-09-10 | 浙江大学 | Method for preparing polygala glycolipid effective part |
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CN104027403A (en) * | 2014-05-21 | 2014-09-10 | 浙江大学 | Method for preparing polygala glycolipid effective part |
Non-Patent Citations (2)
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Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20180027216A (en) * | 2016-09-06 | 2018-03-14 | 주식회사 엘지생활건강 | Composition for skin improvement containing tenuifoliside A |
KR102664892B1 (en) | 2016-09-06 | 2024-05-09 | 주식회사 엘지생활건강 | Composition for skin improvement containing tenuifoliside A |
CN109432181A (en) * | 2018-12-19 | 2019-03-08 | 泓博元生命科技(深圳)有限公司 | Alleviate the composition and the preparation method and application thereof of depression |
CN109620863A (en) * | 2018-12-19 | 2019-04-16 | 泓博元生命科技(深圳)有限公司 | A kind of composition and the preparation method and application thereof for alleviating depression |
CN113491727A (en) * | 2020-04-02 | 2021-10-12 | 中国医学科学院药用植物研究所 | Traditional Chinese medicine composition for treating depression and preparation method thereof |
CN116159101A (en) * | 2020-06-24 | 2023-05-26 | 鲁南新时代生物技术有限公司 | Traditional Chinese medicine composition and preparation method and application thereof |
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Application publication date: 20150819 |