CN101690738A - New application of harrisonia perforata and extractive thereof in preparing antitumor medicine - Google Patents
New application of harrisonia perforata and extractive thereof in preparing antitumor medicine Download PDFInfo
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- CN101690738A CN101690738A CN200910151418A CN200910151418A CN101690738A CN 101690738 A CN101690738 A CN 101690738A CN 200910151418 A CN200910151418 A CN 200910151418A CN 200910151418 A CN200910151418 A CN 200910151418A CN 101690738 A CN101690738 A CN 101690738A
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Abstract
The invention discloses a new application of harrisonia perforata and an extractive thereof in preparing antitumor medicine, belonging to the field of traditional Chinese medicine and natural medicine. Harrisonia perforata is collected by alcohol and is extracted by petroleum ether, and left aqueous solution is extracted by acetic ether to obtain petroleum ether extract after concentration. Experiments prove that the obtained petroleum ether position has the action of resisting tumour cells.
Description
Technical field
The present invention relates to a kind of medicinal plants new medical application, especially Harrisonia Perforata (Bl) Merr.(perforatus blanco) and extract thereof the new purposes in the preparation antitumor drug, belong to Chinese medicine, natural medicine field.
Background technology
Harrisonia Perforata (Bl) Merr.(perforatus blanco) [Harrisonia perforata (Blanco) Merrill)] be that Simarubaceae (Simaroubaceae) Harrisonia Perforata (Bl) Merr.(perforatus blanco) belongs to (Harrisonias) plant.Another name: bow thorn, Lian Jiang le.The Harrisonia Perforata (Bl) Merr.(perforatus blanco) platymiscium whole world has 4 kinds, is distributed in Southeast Asia, China.China produces a kind of Harrisonia Perforata (Bl) Merr.(perforatus blanco), is distributed in ground such as south, Guangdong, Hainan, grows in the sparse woods of hillside, hilly ground of low height above sea level or in the bushes.Root of perforatus blanco, stem, leaf, Guo Gebu have antitumor, pulmonary tuberculosis, malaria effect.Harrisonia Perforata (Bl) Merr.(perforatus blanco) is used as medicine and can be used as expectorant, anthelmintic, and is among the people with root, stem decoct treatment malaria and carbuncle sore, also is used for affection due to external wind and heat, coughs, coughs up phlegm and laryngopharynx swelling and pain.
At present, from the Harrisonia Perforata (Bl) Merr.(perforatus blanco) plant, isolated 10 surplus kind of chemical compound, wherein chromone, isopentene group polyketone, hydrogen peroxide polyketides are main chemical constituent.So far bibliographical information mostly is research and the application (" Tetrahedron ", 65 (2009) 1147-1152) at aspects such as antitumor of Harrisonia Perforata (Bl) Merr.(perforatus blanco) isopentene group polyketone and hydrogen peroxide polyketides.
Cancer is one group of common name that can influence more than the 100 kind of disease at any position of health.Other term that uses is malignant tumor and tumor.Cancer is the major causes of death in the whole world.Die ten thousand deaths in the whole world 5800 in 2005 and to die in the sum, cancer accounts for 7,600,000 (or 13%) of all death.Cause the main cancer kind of cancer general mortality rate to be: lung (130 die ten thousand deaths dies/year), stomach (about 100 die ten thousand deaths dies/year), liver (662000 death/year), colon (655000 death/year), mammary gland (502000 death/year).Present treatment means is that clinical application carries out the transition to the multiple medicines combined chemotherapy from the single medicine treatment, but, most treatments only can prolong life and can not eradicate disease, many toxic and side effects such as liver failure and the diabetes etc. of following treatment to produce make patient's immune system suffer damage.From natural drug, seek the heat subject that antitumor drug is research at present.The extract of some Chinese herbal medicine such as enmein (" Yunnan plant research ", 2006,28:95), apigenin-8-C-glucoside (" tropical and subtropical zone Botany Gazette ", 2008,16:51), linoleic acid (" shanghai Medicine ", 1994,17:635) grade has the antineoplastic activity, and its chemical constitution comprises diterpene, flavonoid glycoside, organic acid etc.Bulbus Allii, mushroom, Ganoderma and Radix Ginseng etc. are used for treatment of cancer by many countries.
Harrisonia Perforata (Bl) Merr.(perforatus blanco) of the present invention and extract thereof the new purposes in the preparation antitumor drug is not seen bibliographical information and patent disclosure so far as yet.
Summary of the invention
The purpose of this invention is to provide the new medical application of Harrisonia Perforata (Bl) Merr.(perforatus blanco), i.e. Harrisonia Perforata (Bl) Merr.(perforatus blanco) and extract thereof the purposes in the preparation antitumor drug.
Content of the present invention is Harrisonia Perforata (Bl) Merr.(perforatus blanco) and the purposes of extract in the preparation antitumor drug thereof, described purposes is characterised in that: 1, the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract can obtain by following step: the dry branch of Harrisonia Perforata (Bl) Merr.(perforatus blanco), suitably pulverize the back and doubly measure 95% ethanol soaking at room temperature extraction 3 times with 8-11, also but percolation extracts, with the extracting solution decompression recycling ethanol, decompression recycling ethanol is to there not being the alcohol flavor.Ethanol extraction is scattered in becomes suspension in the water, obtain the petroleum ether extractum A through petroleum ether extraction, remaining water liquid ethyl acetate extraction obtains ethyl acetate extractum B through concentrating.Extractum A, B are drying to obtain Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract A, Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B; 2, Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B and/or Harrisonia Perforata (Bl) Merr.(perforatus blanco) fruit 95% ethanol extraction add suitable pharmaceutic adjuvant, and preparation process routinely promptly can be made into oral drug preparation and injectable drug preparations such as tablet, capsule, granule, drop pill, oral liquid.
The Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B is used chromogenic reagent through thin layer chromatography, shows that the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B contains chromone, limonin, isopentene group polyketides.
Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B of the present invention, through the external activity screening, the statistical disposition result shows better antitumor activity.In order to verify that further Harrisonia Perforata (Bl) Merr.(perforatus blanco) and extract thereof in the effect aspect the treatment tumor, have carried out the preliminary clinical observation on the therapeutic effect of 100 routine patients to the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B, the result shows that the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B is effective.By the external activity screening and the preliminary clinical observation on the therapeutic effect result of patient of Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B, can rationally derive Harrisonia Perforata (Bl) Merr.(perforatus blanco) and extract thereof can be used for preparing antitumor drug, i.e. Harrisonia Perforata (Bl) Merr.(perforatus blanco) and extract thereof the purposes aspect the preparation antitumor drug.
The invention has the beneficial effects as follows provides Harrisonia Perforata (Bl) Merr.(perforatus blanco) at the new medical applications that are generally used for preparing beyond the medicines such as treatment malaria, pulmonary tuberculosis among the people, it is Harrisonia Perforata (Bl) Merr.(perforatus blanco) and extract thereof the purposes aspect the preparation antitumor drug, and adopt different solvent extractions to obtain the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B, the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B is added suitable pharmaceutic adjuvant, preparation process routinely promptly can be made into oral and the injectable drug preparation.
Be external activity screening and the preliminary clinical observation on the therapeutic effect test of patient and the result thereof of Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B below.
One, external activity screening
Test method:
Adopt mtt assay to test the external antitumor activity (the results are shown in subordinate list 1) of Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B to the cell strains such as leukaemia P-388, lung adenocarcinoma cell A-549 of human body.Activity test method is as follows: the testing sample of negative control group (water), DMSO solvent control group, positive controls (ametycin) and 8 variable concentrations (0.8,1.6,3.2,6.3,12.5,25,50,100) is established in experiment, each concentration establish 2 parallel.Collect the exponential phase cell, the blood counting chamber counting is inoculated in the flat Tissue Culture Plate in 96 holes by 4500 the cancerous cell amounts in every hole, places 5%CO
2, humidity more than 90%, cultivate in 37 ℃ of incubators.Take out behind the 24h and add a certain amount of testing sample, taking-up places microscopically to observe every porocyte form after continuing to cultivate 3d, record cellular morphology situation of change, follow MTT solution (being dissolved in balanced salt solution PBS) the 50 μ L that every hole adds 5mg/mL, behind 37 ℃ of reaction 4h, with the cell culture fluid sucking-off, every hole adds 100 μ L DMSO Formazane is fully dissolved, Tissue Culture Plate is placed on the MK3 microplate reader, survey the absorbance (A) in each hole with the 570nm wavelength, by the following formula long suppression ratio of seeking survival.
With the sample concentration is abscissa, is vertical coordinate with the suppression ratio, maps and obtains the concentration (IC that suppression ratio is 50% o'clock sample
50), the active result of sample is promptly with half-inhibition concentration (IC
50) expression.
Experimental result:
Subordinate list 1 sample is to the toxic action of tumor cell lines such as P-388, A-549
Annotate: toxicity value IC
50, promptly the medicine pair cell is killed 50% o'clock concentration value.IC
50It is more little to be worth big more then toxicity.
Two, preliminary clinical observation on the therapeutic effect
Object of study: tumor patient, wherein male 58 examples, women 42 examples, age reckling 32 years old, the maximum 75 years old.
Diagnostic criteria: 1, do not have other any ill symptomses; 2, do not take any other antitumor drug.
Research method: this test is an object of study with 100 tumor patients, is tried thing and takes for patent medicine of the present invention (No. 0 capsule that contains 0.15g Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B approximately), and three times on the one, each two, boiled water is taken after mixing it with water.Per 40 days is a course of treatment, and drug withdrawal is had a rest a week after continuous two courses of treatment, observes change of illness state inspection in detail.Carry out the 3rd course of therapy then, withdraw other medicine at period in a medicine.
Clinical cure: the positive sign of symptom and objective determination disappears, and does not have the recidivist continuously half a year.
Clinical significantly: symptom disappears substantially, and cancer dwindles over half, and other objective determination takes an evident turn for the better, and observes more than half a year no longer development person.
Clinical effective: symptom makes moderate progress, and focus is basicly stable, observes person more than month.
Clinical invalid: symptom and objective determination do not have improvement, or only have short-term to improve, and deterioration person rapidly.
Efficacy result:
Advantage of the present invention is:
1, the natural drug selected for use of the present invention is a raw material, low toxicity, and side effect is little.
2, the present invention need not decoct, and treatment is convenient, and effective percentage reaches 94%.
3, the present invention can the control cancer cell hypertrophy, prevents the cancerous cell diffusion, makes the withered disappearance that comes off of cancerous cell.
4, the invention provides low dosage (0.5～2mg/kg) can produce anti-tumor activity, thus long-term low dose ((5～10mg/kg) antitumor action is stronger than high dose as 0.6～1.25mg/kg).
The specific embodiment
Embodiment 1
Get Harrisonia Perforata (Bl) Merr.(perforatus blanco) dry product 2.0kg, divide 3 (5,3,3 days) lixiviates with 10 times of amount 95% ethanol, decompression recycling ethanol, concentrate drying obtains extract powder, and it is an amount of that extract powder adds starch, is mixed, granulates, dry, granulate, incapsulates, and makes 1000 and get final product.
Embodiment 2
Get Harrisonia Perforata (Bl) Merr.(perforatus blanco) dry product 10.0kg, with 9 times of amount 90% ethanol percolations, the concentrating under reduced pressure percolate to do not have alcohol distinguish the flavor of concentrated solution, concentrated solution is scattered in and becomes suspension in the water, obtain the petroleum ether extractum A through petroleum ether extraction, remaining water liquid ethyl acetate extraction obtains ethyl acetate extractum B through concentrating, and extractum B is drying to obtain the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B.Get Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B 100.0g, add appropriate amount of auxiliary materials such as starch, be mixed, granulate, drying, be pressed into 1000 and get final product.
Embodiment 3
Get Harrisonia Perforata (Bl) Merr.(perforatus blanco) dry product 5.0kg, with 8 times of amount 80% ethanol percolations, the concentrating under reduced pressure percolate to do not have alcohol distinguish the flavor of concentrated solution, concentrated solution is scattered in and becomes suspension in the water, obtain petroleum ether extractum through petroleum ether extraction, remaining water liquid ethyl acetate extraction obtains ethyl acetate extractum through concentrating, and the ethyl acetate extract dry promptly gets the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B; Get Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B 25.0g, add an amount of water for injection dissolving, aqueous injection technology routinely transfers pH value, filtration, embedding, sterilization to make 1000ml and get final product; Perhaps add an amount of additives such as mannitol, dissolving stirs evenly, and filtration, lyophilizing, packing are made 500 bottles and got final product.
Claims (4)
1. the new purposes of Harrisonia Perforata (Bl) Merr.(perforatus blanco) in the preparation antitumor drug is characterized in that described Harrisonia Perforata (Bl) Merr.(perforatus blanco) is that Simarubaceae (Simaroubaceae) Harrisonia Perforata (Bl) Merr.(perforatus blanco) belongs to (Harrisonias) plant Harrisonia Perforata (Bl) Merr.(perforatus blanco) (Harrisonia perforata), medicinal Herb.
2. the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract is in the purposes of preparation in the antitumor drug, it is characterized in that the Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract can be by following step acquisition:
The dry branch of Harrisonia Perforata (Bl) Merr.(perforatus blanco) suitably pulverizes the back and doubly measure 95% ethanol soaking at room temperature extraction 3 times with 8-11, but also percolation extracts, and with the extracting solution decompression recycling ethanol, decompression recycling ethanol is not distinguished the flavor of to there being alcohol.Ethanol extraction is scattered in becomes suspension in the water, obtain the petroleum ether extractum A through petroleum ether extraction, remaining water liquid ethyl acetate extraction obtains ethyl acetate extractum B through concentrating.Extractum A, B are drying to obtain Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract A, Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B.
3. according to the described Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract of claim 2, it is characterized in that described Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B contains chromone, isopentene group polyketone, hydrogen peroxide polyketone and limonoid.
4. according to claim 1,2 described purposes, it is characterized in that: with Harrisonia Perforata (Bl) Merr.(perforatus blanco) extract B and/or Harrisonia Perforata (Bl) Merr.(perforatus blanco) 95% ethanol extraction, add suitable pharmaceutic adjuvant, preparation process routinely promptly can be made into oral drug preparation and injectable drug preparations such as freeze-dried powder, liquid drugs injection such as tablet, capsule, granule, drop pill, oral liquid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN200910151418A CN101690738A (en) | 2009-07-15 | 2009-07-15 | New application of harrisonia perforata and extractive thereof in preparing antitumor medicine |
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| CN200910151418A CN101690738A (en) | 2009-07-15 | 2009-07-15 | New application of harrisonia perforata and extractive thereof in preparing antitumor medicine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112592351A (en) * | 2020-12-07 | 2021-04-02 | 中国科学院昆明植物研究所 | Eleusine indica trilactone A, medicine for treating Alzheimer disease, preparation method and application |
-
2009
- 2009-07-15 CN CN200910151418A patent/CN101690738A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112592351A (en) * | 2020-12-07 | 2021-04-02 | 中国科学院昆明植物研究所 | Eleusine indica trilactone A, medicine for treating Alzheimer disease, preparation method and application |
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Open date: 20100407 |