CN1548132A - Common jujube seed extract and its use - Google Patents
Common jujube seed extract and its use Download PDFInfo
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- CN1548132A CN1548132A CNA031310605A CN03131060A CN1548132A CN 1548132 A CN1548132 A CN 1548132A CN A031310605 A CNA031310605 A CN A031310605A CN 03131060 A CN03131060 A CN 03131060A CN 1548132 A CN1548132 A CN 1548132A
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- ziziphi spinosae
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Abstract
The present invention is one kind of common jujube seed extract and its application in inhibiting tumor growth. The present invention features that common jujube seed as material is extracted with solvent including alkyl dichloride and the extractive is used as effective component in preparing selective antitumor cell medicine. Research shows that it has toxicity on tumor cell as high as 2-10 times that on common cell and has especially even high effect on melanoma cell. Therefore, the present invention may be used as medicine specially for inhibiting melanoma cell.
Description
Technical field
The present invention is extract of a plant material and uses thereof, and specifically a kind of extract of Semen Ziziphi Spinosae is used for the growth that selectivity suppresses tumor cell.
Background technology
Semen Ziziphi Spinosae is as the dry mature seed of the Rhamnaceae plant Ziziphi Spinosae of medicine-food two-purpose, and Chinese Pharmacopoeia version in 2000 is recorded, function with cure mainly to tonifying liver, mind calming, arresting sweating, promote the production of body fluid.It is thirsty to be used for restlessness of asrhenia type and insomnia, the empty hyperhidrosis of palpitation with fear dreaminess, body, Tianjin wound.Contain fatty oil (about 32%) in the known acid Semen Ziziphi Spinosae, materials such as Saponin (jujuboside), flavone (spinosin), ferulic acid, triterpenoid compound, organic acid, monosaccharide, polysaccharide, trace element, aminoacid, Vc, protein.Pharmacological action comprises (1) effect to nervus centralis; (2) to cardiovascular effect; (3) to Immune Effects; (4) blood fat reducing; (5) protect scald, antiradiation and prevention altitude sickness etc.
Can from Semen Ziziphi Spinosae, obtain different active components with different extraction separation methods, preparing the herbal mixture of multiple efficacies and health product thus is that the U.S. originates in wild Radix Panacis Quinquefolii and China property natural plants Fructus Jujubae, Semen Ziziphi Spinosae, Radix Ophiopogonis etc. as the Main Ingredients and Appearance of " the peaceful and prosperous power of English adds ", be used for driving away tired, improve sleep, recover natural immunity, promote the holistic health level comprehensively.The prescription that " Chinese and Western Bao oral liquid " introduced is aminoacids complex, Semen Ziziphi Spinosae, Semen Platycladi, Radix Asparagi, Radix Polygalae, Concha Margaritifera, Radix Rehmanniae etc., be applicable to poor sleep in evening, bad, the fatigable crowd of mental status on daytime, especially be fit to old people and the huge white collar class of operating pressure.But there is not Semen Ziziphi Spinosae extract to have the report of selectivity tumor promotion as yet.
Tumor is a kind of disease of serious harm human health, and treatment measure at present has only methods such as former excision, chemotherapy, radiotherapy, immunization therapy.Chang Yong chemotherapeutics is a lot of clinically, as Taxol (paclitaxel), camptothecin (camptothecine), Doxorubicin (amycin), Ellipticine (ellipticine), Homoharringtonine (homoharringtonine), mithramycin A (plicamycin), Podophyllotoxin (podophyllotoxone), Vinblastine (vinblastine), Vincrstine (vincristine) or the like.These medicines also have very big toxic and side effects to normal cell in killing tumor cell.
Summary of the invention
The object of the present invention is to provide a kind of the have Semen Ziziphi Spinosae extract of selectivity anti-tumor activity and the pharmaceutical formulations of its selectivity anti-tumor activity.
Preparation method of extract of the present invention: with the Semen Ziziphi Spinosae raw material pulverizing to greater than 20 purpose coarse powder, the 60-90 ℃ of petroleum ether equal solvent defat of doubly measuring with the 2.0-4.0 of raw material weight 5～10 hours, use the 2.0-3.0 dichloromethane solvent reflux, extract, doubly 10～15 hours of raw material weight then, extracting solution reclaims dichloromethane to doing, obtain light brown viscosity thick paste, be required extract, mix with the adjuvant of using always again, make granule.Described solvent comprises dichloromethane, methanol, ethanol, ethyl acetate, ether, petroleum ether or hexane.
Semen Ziziphi Spinosae extract active ingredient of the present invention mainly is the mixture of triterpenoid compound, and the pharmaceutical formulations with selectivity anti-tumor activity can be provided, and it makes the dosage form that comprises tablet, capsule, suspension, syrup with the adjuvant that pharmaceutically allows.
Described adjuvant comprises: diluent (calcium gluconate, calcium sulfate, lactose, cellulose, Kaolin, mannitol, sodium chloride, starch, Icing Sugar or hydroxypropyl emthylcellulose); Binding agent (starch, gel); Filler (sucrose, glucose or lactose); Stabilizing agent (polysaccharose substance such as acacia, agar, alginic acid, synthetic resin such as carbomer or cellulose ether); Solvent (water, diformazan sulfoxide-water (50: 50), propylene glycol or phosphate buffer).
Sample antitumor cell toxicity ED among the present invention
50The mensuration of value adopts mtt assay, and concrete operations are as follows:
1. inoculating cell:, make single cell suspension with the RPMI RPMI-1640 that contains 10% hyclone, with every hole 10 with the cultured cell of 0.25% trypsinization
3～10
4Individual cell inoculation is in 96 orifice plates, and every hole 200 μ l, and add the sample be dissolved in DMSO in advance carry out positive control simultaneously;
2. cultured cell: 37 ℃, 5%CO
2And cultivate under the saturated humidity condition, incubation time is decided according to cell;
3. colour generation: every hole adds MTT (5mg/ml) 20 μ l, and 37 ℃, continue to hatch 4h, stop cultivating, absorb supernatant in the hole.For suspension cell, need are centrifugal, and (1000rpm 5min), discards culture fluid in the hole then.Every hole adds 150 μ l DMSO, and vibration 10min fully dissolves crystal;
4. colorimetric: the 490nm place, microplate reader is measured the absorbance value in each hole, is transverse axis with the drug level, and absorbance value is that the longitudinal axis is drawn cell growth curve, calculates the ED to various tumors
50Value.
Advantage of the present invention and effect:
Extract of the present invention to the toxicity of tumor cell be Normocellular 2-10 doubly, can suppress melanoma cell effectively, promptly to the strong (ED of cytotoxicity of melanin tumor cell
50＜20 μ g/ml: 〉.Table 1 provides extract of the present invention and amycin is selected active measurement result to tumor cell; The cytoactive that table 2 provides extract of the present invention and antitumor drug commonly used compares, and data find out that Semen Ziziphi Spinosae extract is expected to obtain specificity melanoma medicine from table.
The specific embodiment
Further set forth characteristics of the present invention below by specific embodiment.
Example 1
This example is the preparation Semen Ziziphi Spinosae extract.
With Semen Ziziphi Spinosae 1.0kg was raw material, and pulverizing is the coarse powder about 10～20 orders, places continuous extractor, with 2500ml petroleum ether (boiling range 60-90 ℃) defat 5 hours.After medicinal residues dry, use 2000ml dichloromethane continuous backflow to extract 11 hours, concentrate dichloromethane extract, get light brown viscosity thick paste to doing.
Example 2
This example is the pharmaceutical formulations that preparation contains Semen Ziziphi Spinosae extract.Extract of the present invention is as follows with ratio of adjuvant commonly used:
| Semen Ziziphi Spinosae extract (light brown viscosity thick paste) | ????50g | |
| Adjuvant | Calcium gluconate | ????50g |
| Starch | ????20g | |
| Carboxymethyl starch sodium | ????5g | |
| Magnesium stearate (adding) | ????1g | |
Concrete preparation method: with extract of the present invention and auxiliary materials and mixing, cross 20 mesh sieves and granulate, add the magnesium stearate granulate after the drying, or encapsulated or tabletting, obtain testing with medicament.
Example 3
This example is the measurement results of example 2 Semen Ziziphi Spinosae extracts to different cytotoxicities.Measure with aforementioned mtt assay.Concrete outcome sees Table 1.
Table 1 Semen Ziziphi Spinosae extract antitumor cell is selected active (ED
50: μ g/ml)
| Cell?Line | Cell strain | Semen Ziziphi Spinosae extract | Amycin) |
| Tumor cells (tumor cell) | |||
| A2780 | Ovarian cancer | 1.8 | ?0.024 |
| A431 | Uterus carcinoma | 1.8 | ?0.037 |
| Me665/2/21 | Malignant melanoma | 1.5 | ?0.21 |
| Me665/2/60 | Malignant melanoma | 1.6 | ?0.27 |
| Normal cells (normal cell) | |||
| HIDFC | Hypodermal cell | 10.2 | ?0.38 |
| PBL | Blood lymphocyte | ＞50 | ?0.02 |
Example 4
This example be clinical medicine commonly used to melanoma cell toxicity test result and with the active comparison of Semen Ziziphi Spinosae extract, measure with aforementioned mtt assay, concrete outcome sees Table 2.
The melanoma cell specific activity of table 2 Semen Ziziphi Spinosae extract and dirty tumour medicine commonly used is (ED
50: μ g/ml)
| Chemical compound | ????MEL-2 |
| Semen Ziziphi Spinosae extract | ????3.7 |
| Betulic acid | ????2.00 |
| Paclitaxel | ????0.06 |
| Camptothecine | ????0.02 |
| Vinblastine | ????0.02 |
| Interleukin-2 | ????0.04 |
Can prove that from embodiment 3,4 Semen Ziziphi Spinosae extract has significant selection activity to tumor cell.Although Semen Ziziphi Spinosae extract is compared with clinical medicine, its anti-tumor activity is high not enough, can expect, by being lead compound to the separation and purification of effective ingredient or with the structure of effective ingredient, carry out structure of modification, can obtain the melanoma medicine that safety is good, effect is single-minded.
Claims (2)
1. Semen Ziziphi Spinosae extract, it is characterized in that this extract can be prepared by following method: be raw material with the Semen Ziziphi Spinosae, it be crushed to be not less than 20 order coarse powder, use 2.0-4.0 60-90 ℃ the petroleum ether solvent doubly of raw material weight to remove degrease, reclaim petroleum ether, obtain Semen Ziziphi Spinosae oil; The 2.0-3.0 of medicinal residues reuse raw material weight dichloromethane equal solvent reflux, extract, doubly 10-15 hour reclaims solvent, gets light brown viscosity thick paste, mixes with adjuvant commonly used, makes the granule with selectivity anti-tumor activity.Described solvent comprises dichloromethane, methanol, ethanol, ethyl acetate, ether, petroleum ether or hexane.
2. the purposes of the described Semen Ziziphi Spinosae extract of claim 1, it is characterized in that providing the pharmaceutical formulations with selectivity anti-tumor activity, described preparation is that the Semen Ziziphi Spinosae extract of the pharmacy active ingredient of pharmaceutically acceptable substrate is made the preparation that comprises tablet, capsule, suspensoid, syrup with the adjuvant that pharmaceutically allows.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031310605A CN1548132A (en) | 2003-05-15 | 2003-05-15 | Common jujube seed extract and its use |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031310605A CN1548132A (en) | 2003-05-15 | 2003-05-15 | Common jujube seed extract and its use |
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| CN1548132A true CN1548132A (en) | 2004-11-24 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7906459B2 (en) | 2004-05-24 | 2011-03-15 | Valent Biosciences Corporation | Stable and water-soluble plant growth regulator liquid compositions and methods for use of same |
| CN103623079A (en) * | 2012-08-21 | 2014-03-12 | 天津瑞贝特科技发展有限公司 | Preparation method and use of spine date seed extract having effects of protecting liver and bladder and improving immunity |
| CN105477100A (en) * | 2015-12-23 | 2016-04-13 | 无锡瑞盈生命科学有限公司 | Lucid ganoderma spore oil compound health care spray and preparation method |
| CN106174560A (en) * | 2016-07-11 | 2016-12-07 | 周晗生 | The extracting method of Radix Ginseng extract |
-
2003
- 2003-05-15 CN CNA031310605A patent/CN1548132A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7906459B2 (en) | 2004-05-24 | 2011-03-15 | Valent Biosciences Corporation | Stable and water-soluble plant growth regulator liquid compositions and methods for use of same |
| CN103623079A (en) * | 2012-08-21 | 2014-03-12 | 天津瑞贝特科技发展有限公司 | Preparation method and use of spine date seed extract having effects of protecting liver and bladder and improving immunity |
| CN105477100A (en) * | 2015-12-23 | 2016-04-13 | 无锡瑞盈生命科学有限公司 | Lucid ganoderma spore oil compound health care spray and preparation method |
| CN106174560A (en) * | 2016-07-11 | 2016-12-07 | 周晗生 | The extracting method of Radix Ginseng extract |
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