CN1830458A - New use of tribulus terrestris extraction - Google Patents
New use of tribulus terrestris extraction Download PDFInfo
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- CN1830458A CN1830458A CNA2005100243358A CN200510024335A CN1830458A CN 1830458 A CN1830458 A CN 1830458A CN A2005100243358 A CNA2005100243358 A CN A2005100243358A CN 200510024335 A CN200510024335 A CN 200510024335A CN 1830458 A CN1830458 A CN 1830458A
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Abstract
An application of the extract of puncturevine caltrop fruit in preparing the medicine, health-care products, or food for preventing and treating depression is disclosed.
Description
Technical field
The present invention relates to a kind of new purposes of tribulus terrestris extraction.
Background technology
The Chinese medicine Fructus Tribuli is the dry mature fruit of zygophyllaceae (Zygophyllaceae), Tribulus (Tritulus) plant Fructus Tribuli (Tritulus terrestris), has another name called Fructus Tribuli, Fructus Atriplicis Sibiricae, Fructus Tribuli, hard Fructus Tribuli.Nature and flavor suffering, hardship, tepor, slightly poisonous, go into liver, lung meridian, have diffusing wind, make eye bright, the effect of the therapeutic method to keep the adverse QI flowing downwards, promoting the circulation of blood, the kidney invigorating and essence nourishing.Fructus Tribuli has long medication history in that China is among the people, and Shennong's Herbal is classified top grade medicine as with " Fructus Tribuli ", says its " main stagnant blood, broken crux is gathered, sore throat, breast is difficult, obeys longue meat for a long time, makes eye bright, and makes light of one's life by commiting suicide ".Chinese Pharmacopoeia is put down in writing its function, and " the suppressing the hyperactive liver resolving depression, promoting blood circulation by removing wind makes eye bright, and is antipruritic.It is dizzy to be used to have a headache, distending pain in the chest and hypochondrium, breast closes acute mastitis, conjunctival congestion cataracta, rubella pruritus ".
In recent years, various countries do not end to this plant research.Studies show that, tribulus terrestris extraction comprises compositions such as Fructus Tribuli steroidal saponin (Saponin), flavone, polysaccharide and alkaloid, wherein, can by the distinct methods extraction separation to main component be saponin (Jin Jingling etc. the macroporous adsorbent resin method is extracted puncture vine total saponin. Yanbian University's medical journal .3 month, 1999.22 (1): 29-31), flavonoid (Shi Qin etc. the content of 3 kinds of hydrolysis flavone aglycone of rp-hplc determination Fructus Tribuli class. pharmaceutical analysis impurity; 1999,19 (2): 75~78 or Wu Qiongshi etc. content of total flavone is measured in the puncturevine herb. ACAD J GCP; 1998,14 (4): 273~275) or polysaccharide (Shi Qin etc. the content of polysaccharide in the colorimetric method for determining Fructus Tribuli. China Medicine University's journal; 1997,28 (5): tribulus terrestris extraction 291~293).External is that development of raw materials has gone out to be used for " Tribustan " of sexual function improving and the preparations such as " Tribusaponin " of " Vitanone " and vessel softening with the Fructus Tribuli, and China is that development of raw materials goes out " Xinnao Shutong " treatment cardiovascular disease with the stem and leaf of Fructus Tribuli also.But do not treat the report of depression so far relevant for tribulus terrestris extraction.
Summary of the invention
The technical problem to be solved in the present invention promptly is above-mentioned problem, and a kind of new purposes of tribulus terrestris extraction is provided, i.e. the purposes of tribulus terrestris extraction in medicine, health food or the food of preparation treatment or prevention depression.
According to the present invention, the same Chinese Pharmacopoeia of term Fructus Tribuli is meant the Fructus Tribuli fruit.And tribulus terrestris extraction of the present invention is meant that the various crude extracts that extract are (after the extraction such as water or ethanol from the fruit of plant Fructus Tribuli, no longer further separation and purification and making comprises multiple compositions such as steroid saponin, flavonoid, polysaccharide and alkaloid) or the Fructus Tribuli steroidal saponin extract of various purity (above-mentioned crude extract through variously differently separate, purification steroidal saponin method makes); Wherein, the tribulus terrestris extraction of total steroid saponin class weight content 〉=50%, the present invention abbreviates Fructus Tribulus total saponins again as, and it contains total spirostanol saponin of Fructus Tribuli and the total furostanol of Fructus Tribuli.
According to the present invention, preferred tribulus terrestris extraction is a Fructus Tribulus total saponins.
Wherein, the active component of above-mentioned medicine can also contain other the treatment or the active substance of prevention depression except that tribulus terrestris extraction or its total saponins, as being used for antidepressant various kinds of drug at present, and for example fluoxetine, paroxetine or Sertraline etc.
This medicine or health product can be tablet, granule, pill, powder, capsule, oral liquid, suspension or Emulsion etc.
Positive progressive effect of the present invention is: the present invention studies the tribulus terrestris extraction antidepressant activity by the rat depression model, and has measured the content of rat brain neurotransmitter.The result shows that tribulus terrestris extraction can obviously improve the depressive state of rat, wherein high dose group Fructus Tribulus total saponins (200mg/kg) can also obviously improve (5-hydroxy tryptamine) content of 5-HT in the rat brain and 5-HIAA (5-hydroxyindoleacetic acid) content, so its effective active composition is a total saponins.Therefore, tribulus terrestris extraction of the present invention, especially Fructus Tribulus total saponins can be used to prepare antidepressant medicine, health food or food, also can be used for the auxiliary treatment of depressive patients.
The specific embodiment
Further specify the present invention with embodiment and effect embodiment below.Wherein Fructus Tribuli crude extract and Fructus Tribulus total saponins can be the commercially available prod.
The preparation of embodiment 1 Fructus Tribuli crude extract
Get raw material Fructus Tribuli fruit 1kg, five times of water reflux, extract, 3 times, each 1 hour, extracting solution promptly got the Fructus Tribuli crude extract through spray drying.After measured, this Fructus Tribuli crude extract contains total saponins class 20% (vanillin-perchloric acid method), contains polysaccharide 2%, contains total flavonoid 1%.
The preparation of embodiment 2 Fructus Tribulus total saponins
Get raw material Fructus Tribuli fruit 1kg, with octuple amount 75% alcohol reflux 3 times, each 2.5 hours, extracting solution merged, and filtered, filtrate (temperature is less than 10 ℃) was in the cool placed 12 hours, 4000 rev/mins after centrifugal 5 minutes, get supernatant, reclaim ethanol, be concentrated into dry extract, water is dissolved into behind the solution through macroporous adsorptive resins (HPD100).Behind the upper prop, wash with water earlier after colourless, reuse 30% ethanol is washed till colourless, uses 70% ethanol elution then, collects eluent, reclaims ethanol to there not being the alcohol flavor, is spray dried to dry powder, promptly gets Fructus Tribulus total saponins, and its purity is 60%.
The preparation of embodiment 3 Fructus Tribuli total flavones
Fructus Tribuli fruit 1kg, with 5 times of water gaging reflux, extract, 3 times, behind ethanol precipitation, the elimination precipitation, polyamide column filtrate on, after colourless, with the acetone eluting, collection acetone eluent volatilizes acetone, is drying to obtain Fructus Tribuli fruit total flavones with water elution.The above-mentioned document of assay reference (Shi Qin etc. the content of 3 kinds of hydrolysis flavone aglycone of rp-hplc determination Fructus Tribuli class. pharmaceutical analysis impurity; 1999,19 (2): 75~78 and Wu Qiongshi etc. content of total flavone is measured in the puncturevine herb. ACAD J GCP; 1998,14 (4): 273~275), its purity is 52% after measured.
The preparation of embodiment 4 Fructus Tribuli polysaccharide
According to above-mentioned document (Shi Qin etc. the content of polysaccharide in the colorimetric method for determining Fructus Tribuli. China Medicine University's journal; 1997,28 (5): 291~293) preparation.
Fructus Tribuli fruit 1kg, behind 95% alcohol reflux, residue boils 3 times with the decocting of 3 times of amounts, and each 1h merges aqueous extract.Water intaking extract 1500mL adds chloroform 300 extracting solution.Water intaking extract 1500mL adds chloroform 300mL, n-butyl alcohol 100mL, and magnetic agitation 10-15h puts in the separatory funnel, places and makes layering, removes chloroform layer (containing protein).Then water layer is put the 72h that dialyses in the bag filter (removing small molecular weight impurity and organic solvent).Dialysis with the dialysis solution lyophilization, obtains purified Fructus Tribuli polysaccharide after finishing.
Effect embodiment 1 tribulus terrestris extraction and Fructus Tribulus total saponins are to depression model rat antidepressant effect-forced swimming experiment
1. modeling: wistar rat (200-220g) is put into the glass circle cylinder of internal diameter 20cm, high 40cm, 1 in every cylinder, depth of water 24cm in the cylinder, 28 ℃-29 ℃ of water temperatures (every cylinder water is only used 1 time).Tested first day, every rat is swum 15min in advance, takes out subsequently, dries under lamp, puts into cage, tests behind the 24h.Rat is reentered in the water vat, observes 5min continuously, and the accumulative total rat stops to struggle, be floating erectility, only once in a while the persistent period (dead time) of limb motion to keep head to keep afloat, continuous 16 days forced swimmings arranged in water.Surpass 150s person with the dead time and be decided to be the depression model animal.
2. gastric infusion: as sample, divide high dose group (200mg/kg) and low dose group (100mg/kg) with the Fructus Tribulus total saponins of the Fructus Tribuli crude extract of embodiment 1, embodiment 2; Organize (4.5mg/kg) in contrast with sertraline hydrochloride (Shanghai Institute of Pharmaceutical Industry's production); With the normal saline is blank (5ml/ only).24h, 5h before the dead time, 1h gastric infusion are measured in every rat administration 3 times.
3. swimming test: carry out the forced swimming experiment by step requirement 1. behind the gastric infusion, non-swimming time in every wistar rat 5min of meter record the results are shown in Table 1.
4. monitoring: swimming finishes the back and puts to death rat, take out brain, adopt monoamine neurotransmitter in the fluorescence spectrometry rat brain, 5-hydroxy tryptamine (5-HT) (sigma provides), 5-hydroxyindoleacetic acid (5-HIAA) (sigma provides), dopamine (DA) (sigma provides) and norepinephrine (NA) (sigma provides) the results are shown in Table 2.
The table 1 wistar rat forced swimming dead time
Group | Dosage (mg/kg) | Dead time in 5 minutes (s) |
The blank group of high dose crude extract group low dosage crude extract group high dose saponin group low dosage saponin group Sertraline group normal saline | 200 100 200 100 4.5 5ml/ only | 70.17±15.06 * 74.59±9.58 * 62.56±4.74 * 87.92±12.54 * 57.23±1.91 * 195.53±24.48 |
Compare with the blank group
*P<0.01
Neurotransmitter in the table 2 fluorescence spectrometry wistar rat brain
Group | Dosage (mg/kg) | 5-HT content ug/g cerebral tissue | 5-HIAA content ug/g cerebral tissue | DA content ug/g cerebral tissue | NE content ug/g cerebral tissue |
The blank group of high dose crude extract group low dosage crude extract group high dose saponin group low dosage saponin group Sertraline group | 200 100 200 100 4.5 5ml/ only | 1.00±0.13 * 0.58±0.16 0.72±0.13 ** 0.66±0.18 0.96±0.16 * 0.57±0.09 | 0.44±0.08 0.54±0.34 0.76±0.17 * 0.48±0.16 0.54±0.18 0.40±0.15 | 0.74±0.61 0.45±0.20 0.41±0.12 0.63±0.29 0.90±0.27 0.67±0.29 | 0.49±0.05 0.56±0.09 0.60±0.18 0.48±0.06 0.45±0.02 0.52±0.09 |
Compare with the blank group
*P<0.01,
*P<0.05
The comparison of effect embodiment 2 antidepressant effects
Get ICR mice (20-22g), the Fructus Tribulus total saponins (143.6mg/kg) that makes respectively with embodiment 2,3 and 4, Fructus Tribuli polysaccharide (14.4mg/kg), Fructus Tribuli total flavonoid (7.2mg/kg) as sample, Sertraline organize (5.92mg/kg) in contrast, normal saline is blank (0.5ml/ only), continuous irrigation stomach 14 days, after irritating stomach on the 14th day, forced swimming 6 minutes, calculate non-swimming time in back 4 minutes, the results are shown in Table 3.Wherein, be about 10: 1: 0.5 in the ratio that contains saponin, polysaccharide and flavonoid in the Fructus Tribuli crude extract that extracts among the embodiment 1, and set the dose ratio of above-mentioned three in the test.
The table 3 ICR mice forced swimming dead time
Group | Dosage (mg/kg) | Dead time (s) in back 4 minutes |
The blank group of Fructus Tribulus total saponins group polysaccharide group flavonoid group Sertraline group normal saline | 143.6 14.4 7.2 5.92 0.5ml/ only | 106.70±11.41 * 181.51±14.50 166.68±5.99 116.84±11.73 * 177.78±10.30 |
Compare with the blank group
*P<0.01
Above-mentioned effect embodiment 1,2 studies the tribulus terrestris extraction antidepressant activity by the rat depression model, and has measured the content of rat brain neurotransmitter.The result shows that tribulus terrestris extraction can obviously improve the depressive state of rat, wherein high dose group Fructus Tribulus total saponins (200mg/kg) can also obviously improve (5-hydroxy tryptamine) content of 5-HT in the rat brain and 5-HIAA (5-hydroxyindoleacetic acid) content, but the content to DA, NE does not have influence, and its exercising result and the 3rd class antidepressants Sertraline are similar.Further by the antidepressant activity research to flavone component in the Fructus Tribuli and polysaccharide component, the result shows neither have antidepressant effect.
Claims (2)
1, the purposes of tribulus terrestris extraction in medicine, health food or the food of preparation treatment or prevention depression.
2, purposes as claimed in claim 1 is characterized in that this tribulus terrestris extraction is a Fructus Tribulus total saponins.
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102258545A (en) * | 2010-05-27 | 2011-11-30 | 上海中医药大学 | Application of tribulus terrestris total sapogenin extract to preparation of medicaments, health-care food or food for preventing and treating depression |
CN102657819A (en) * | 2012-05-16 | 2012-09-12 | 高新华 | Drug combination for treating dysthymic disorder |
CN102846693A (en) * | 2012-09-13 | 2013-01-02 | 北京康比特体育科技股份有限公司 | Composition used for relieving exercise-induced fatigue, and preparation method and application thereof |
CN115448990A (en) * | 2022-09-03 | 2022-12-09 | 陈均全 | Polysaccharide from natural sources and application of polysaccharide to whitening and moisturizing cosmetics |
-
2005
- 2005-03-11 CN CNB2005100243358A patent/CN100444849C/en not_active Expired - Fee Related
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102258545A (en) * | 2010-05-27 | 2011-11-30 | 上海中医药大学 | Application of tribulus terrestris total sapogenin extract to preparation of medicaments, health-care food or food for preventing and treating depression |
CN102657819A (en) * | 2012-05-16 | 2012-09-12 | 高新华 | Drug combination for treating dysthymic disorder |
CN102657819B (en) * | 2012-05-16 | 2013-07-03 | 高新华 | Drug combination for treating dysthymic disorder |
CN102846693A (en) * | 2012-09-13 | 2013-01-02 | 北京康比特体育科技股份有限公司 | Composition used for relieving exercise-induced fatigue, and preparation method and application thereof |
CN115448990A (en) * | 2022-09-03 | 2022-12-09 | 陈均全 | Polysaccharide from natural sources and application of polysaccharide to whitening and moisturizing cosmetics |
CN115448990B (en) * | 2022-09-03 | 2024-06-07 | 广州市万千粉丝化妆品有限公司 | Polysaccharide from natural sources and application of polysaccharide to whitening and moisturizing cosmetics |
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