CN101732306B - New application of natural product amentoflavone in treating cancers - Google Patents
New application of natural product amentoflavone in treating cancers Download PDFInfo
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- CN101732306B CN101732306B CN 200910220374 CN200910220374A CN101732306B CN 101732306 B CN101732306 B CN 101732306B CN 200910220374 CN200910220374 CN 200910220374 CN 200910220374 A CN200910220374 A CN 200910220374A CN 101732306 B CN101732306 B CN 101732306B
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Abstract
The invention discloses new application of a natural product amentoflavone in treating cancers. The natural product amentoflavone is extracted from plants, Chinese medicinal materials or Chinese medicaments prepared in ready-to-use forms containing the amentoflavone. The compound serves as a pharmacodynamic component to prepare medicament preparations for treating the cancers, and can be independently or combined with an excipient acceptable in the pharmaceutical technology to be prepared into the medicament preparations such as tablets, capsules, granules, sustained release preparations and pills for oral administration, gels and suppositories administrating through orifices such as vagina, anus and nasal cavity, and intramuscular or intravenous injections. The content of the amentoflavone in the medicament preparations is over 90 percent. The invention discloses the pharmacodynamic component of a Chinese medicament tamariskoid spikemoss herb for treating the cancers, and provides a scientific basis for clinical application, so the amentoflavone can serve as a natural anticancer agent and has the characteristics of no addiction and low dosage.
Description
Technical field:
The present invention relates to medical technical field, relate to amentoflavone (amentoflavone) in the new purposes of pharmaceutical field, be specifically related to the new purposes of amentoflavone aspect the treatment cancer.
Background technology:
According to World Health Organization (WHO) (WHO) statistics, the whole world has 6,000,000 people to die from cancer every year, and annual new cases approximately have 1,000 ten thousand people.China relevant department statistics has 1,300,000 people to die from cancer every year, and new cases are about 1,600,000 people, and annual economy damage reaches hundred billion yuan.
Studying office according to national treatment and prevention of tumour provides " the up-to-date seniority among brothers and sisters table of the Chinese population cause of the death " to show, mortality of malignant tumors occupies various cause of the death seconds, due to the severe contamination of earth environment and the variation of dietetic life form, malignant tumor has the trend of further rising.2000, Chinese Urban Residents pathogenesis of cancer number was 180-200 ten thousand, and death toll is 1,500,000, occupied city cause of the death first place, and rank is followed successively by: pulmonary carcinoma, hepatocarcinoma, gastric cancer, colon cancer, the esophageal carcinoma.
Amentoflavone is a kind of chemical composition with remarkable antitumaous effect by extracting in natural plants, Chinese crude drug or the prepared slices of Chinese crude drugs.The English of this natural product is by name: amentoflavone; Molecular formula is C
30H
18O
10Molecular weight is 538.47, chemical structure names is the 4H-1-benzopyran-4-one, 8-[5-(5,7-dihydroxy-4-oxo-4H-1-.alpha.-5:6-benzopyran)-2-hydroxyphenyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)-, English chemical constitution name (4H-1-Benzopyran-4-one, 8-[5-(5,7-dihydroxy-4-oxo-4H-1-benzopyran-2-yl)-2-hydroxyphenyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)-), structural formula is as follows:
In Chinese Pharmacopoeia version in 2005, the regulation Herba Selaginellae is the dry herb of Spikemoss plant Herba Selaginellae Selaginellatamariscina (Beauv.) Spring or cushion Herba Selaginellae Selaginella pulvinata (Hook.et Grev.) Maxim..All can gather the whole year, removes fibrous root and silt, dries.Suffering, flat.Return liver, heart channel.Has promoting blood circulation to restore menstrual flow.Be used for amenorrhea dysmenorrhea ， mass in the abdomen mass in the abdomen, injury from falling down.The hemostasis of the Herba Selaginellae carbonization stasis of blood.Be used for spitting blood, metrorrhagia is had blood in stool, proctoptosis.Contain the number of chemical composition in Herba Selaginellae, as flavonoid, have now found that and contain apigenin (apigenin), amentoflavone (amentoflavone), hinokiflavone (hinokiflavone), isocryptomerin (isocryptomerin) and Oman's holder yellow (amentoflavone) etc. in Herba Selaginellae; The compounds such as Phenylpropanoid Glycosides class, alkaloids, phenols, organic acid.Pharmacological action shows to have: the effects such as immunity and antitumor action, the effect to blood system, antiviral, antibacterial and antiinflammatory action, antalgic and sedative.And being used for the treatment of the effect of cancer, amentoflavone has no relevant report.
Summary of the invention:
Technical problem to be solved by this invention is to provide the new purposes that a kind of native compound amentoflavone (amentoflavone) is used for the treatment of cancer.Can be prepared into the pharmaceutical preparation that is used for the treatment of cancer clinically.Described native compound amentoflavone (amentoflavone) is to extract from the plant, Chinese crude drug or the prepared slices of Chinese crude drugs that contain this composition.Come pharmaceutical preparation for the preparation of the treatment cancer with this compound as active ingredient, can be separately or in pharmaceutical technology acceptable excipient be combined, make the pharmaceutical dosage form of oral administration, cavity/canal drug administration, muscle or intravenously administrable according to conventional method.The content of described amentoflavone (amentoflavone) is more than 90%.The present invention has found the active ingredient of Chinese medicine Herba Selaginellae treatment cancer, for its clinical practice provides scientific basis, makes the amentoflavone (amentoflavone) can be as a natural anticarcinogen, has without addiction, characteristics that consumption is little.
Amentoflavone (amentoflavone) adopts the extracorporeal culture-ing screening experiment, result shows: amentoflavone (amentoflavone) is to A2780 (ovarian cancer cell line, its IC50 is 8ug), HCT-8 (colon-cancer cell strain, its IC50 is 8ug), BGC823 (gastric adenocarcinoma cells, its IC50 is 14ug), BEL-7402 (hepatoma cell strain, its IC50 are 14ug) cell has certain lethal effect.Therefore, amentoflavone (amentoflavone) is a kind of anticancer active constituent that obtains that separates from natural plants, and component content more than 90%, is a kind of anti-tumor Chinese medicine new drug preparation with DEVELOPMENT PROSPECT.
According to World Health Organization (WHO) (WHO) statistics, the whole world has 6,000,000 people to die from cancer every year, and annual new cases approximately have 1,000 ten thousand people.China relevant department statistics has 1,300,000 people to die from cancer every year, and new cases are about 1,600,000 people, and annual economy damage reaches hundred billion yuan.
Very harmful in view of cancer to health, the market prospect of antineoplastic agent is boundless.Therefore, the cancer therapy drug so that amentoflavone (amentoflavone) is made enters the sales platform after date, and a year wound output value should be in RMB more than 500,000,000 yuan, approximately 10～15 years product life cycle, have huge economic benefit and social benefit.Therefore, this product has wide market prospect.
The specific embodiment:
Come more detailed description the present invention below in conjunction with embodiment, but the present invention is not subjected to the restriction of these embodiment.
Embodiment 1: the right inhibitory action of amentoflavone (amentoflavone).
Method: adopt the MMT method, operating procedure: take the logarithm respectively trophophase HCT-8, Bel-7402, A549, A2780 cell strain, each is inoculated on 96 orifice plates with 2 * 104/ porocytes, the DMTCCI that adds respectively variable concentrations, if the 0.1%DMSO matched group is cultivated 72h, before finishing, the every hole of 4h adds 5mg/mlMTT10ul, when cultivating end, off-line also carefully sucks supernatant, add 200ulDMSO and slight concussion, after making the first Save of generation dissolve colour developing fully, survey the OD value with Bio-RadModel 550Microplate Reader with the 570nm wavelength.And calculating IC50.
Result:
The MTT the selection result
Embodiment 2:
Get amentoflavone (amentoflavone) 50g, add starch dust 150g, with equivalent incremental method mixing, add Pulvis Talci 5g, magnesium stearate 2g, mixing is used 85% alcohol granulation, drying, granulate is pressed into 1000, every day 3 times, each 2.
Embodiment 3:
Get amentoflavone (amentoflavone) 50g, add starch dust 200g, Pulvis Talci 10g, magnesium stearate 5g, mixing is granulated, and drying incapsulates, and makes 1000, every day 3 times, each 2.
Embodiment 4:
Get amentoflavone (amentoflavone) 100g, add microcrystalline Cellulose 250g, crospolyvinylpyrrolidone 50g, mixing, add 90 alcohol granulations, drying, granulate, add carboxymethyl starch sodium 10g, magnesium stearate 5g, mixing is pressed into 1000, take each 1 every day 3 times.
Embodiment 5:
Get amentoflavone (amentoflavone) 50g, mannitol 150g injects water 2000ml, is stirred to dissolve, transfer pH to 9.60～10.0 with 1M NaOH solution, be stirred to dissolve, filter, filtrate adds active carbon by 1% solution body accumulated amount, and heating is 30 minutes under 70～80 ℃, the coarse filtration mistake, pipeline and container add water to 2500ml with the washing of 400mL water for injection, and medicinal liquid filters through 0.22 μ m sterilizing filter, fill, lyophilizing, tamponade, roll lid, make 1000 bottles, and get final product.
Claims (7)
1. the application of amentoflavone in preparation treatment ovarian cancer, liver-cancer medicine.
2. application according to claim 1 is characterized in that: the purity of described amentoflavone is: amentoflavone content is greater than 90%.
3. application according to claim 1 is characterized in that: described amentoflavone can be with pharmaceutically acceptable carrier or mixed with excipients prepare acceptable pharmaceutical preparation clinically.
4. application according to claim 3 is characterized in that: described pharmaceutical preparation is oral Preparation; Vagina, anus, nasal cavity administrated preparation; Muscle or intravenous administration formulation.
5. application according to claim 4 is characterized in that: described oral formulations is tablet, capsule, granule, slow releasing preparation, drop pill.
6. any one described application according to claim 1-5, it is characterized in that: described amentoflavone is to extract from the plant, Chinese crude drug and the prepared slices of Chinese crude drugs that contain this composition.
7. application according to claim 6 is characterized in that described Chinese crude drug is: the dry herb of Spikemoss plant Herba Selaginellae Selaginella tamariscina (Beauv.) Spring or cushion Herba Selaginellae Selaginella pulvinata (Hook.et Grev.) Maxim..
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200910220374 CN101732306B (en) | 2009-12-03 | 2009-12-03 | New application of natural product amentoflavone in treating cancers |
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| CN 200910220374 CN101732306B (en) | 2009-12-03 | 2009-12-03 | New application of natural product amentoflavone in treating cancers |
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| CN101732306A CN101732306A (en) | 2010-06-16 |
| CN101732306B true CN101732306B (en) | 2013-11-06 |
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Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103181934A (en) * | 2011-12-31 | 2013-07-03 | 柏丁臣 | Application of herba selaginellae in preparing anti-cancer drugs |
| CN104523724A (en) * | 2014-11-11 | 2015-04-22 | 济南星懿医药技术有限公司 | Pharmaceutical composition for treating stomach cancer |
| CN104510750A (en) * | 2014-11-11 | 2015-04-15 | 济南星懿医药技术有限公司 | Pharmaceutical composition for treating gastric cancer |
| CN104510743A (en) * | 2014-11-11 | 2015-04-15 | 济南星懿医药技术有限公司 | Pharmaceutical composition for treating gastric cancer |
| CN104473925A (en) * | 2014-11-11 | 2015-04-01 | 济南星懿医药技术有限公司 | Pharmaceutical composition used for treating stomach cancer |
| CN104473950A (en) * | 2014-11-11 | 2015-04-01 | 济南星懿医药技术有限公司 | Pharmaceutical composition used for treating stomach cancer |
| CN104873530A (en) * | 2015-06-05 | 2015-09-02 | 泰山医学院 | Anti-cancer drug composition containing amentoflavone |
| CN106588853B (en) * | 2017-01-22 | 2018-08-14 | 广西师范大学 | One kind phenolic compound containing pyranoid ring and its preparation method and application |
| CN108586410B (en) * | 2018-06-22 | 2020-06-23 | 中国药科大学 | Biflavonoid compound and application thereof |
| CN112263573A (en) * | 2020-10-23 | 2021-01-26 | 宁夏医科大学 | Application of amentoflavone in preparation of medicine for treating glioma |
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| KR960009183B1 (en) * | 1993-01-29 | 1996-07-16 | 강삼식 | Anticancer agents of biflavonoids from ginkgo biloba and lonicera japonican |
| CN101361733B (en) * | 2008-09-17 | 2012-02-22 | 暨南大学 | Use of flavone derivates and preparation method thereof |
| CN101361765B (en) * | 2008-09-19 | 2012-07-18 | 湖北中医学院 | Anti-coxsackie and anti-herpesvirus extract of selaginella tamariscina and extraction technique and formulation thereof |
| CN101585825B (en) * | 2009-06-17 | 2013-11-27 | 沈阳药科大学 | Method for preparing amentoflavone |
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