CN101104003A - Xuezhikang purpose-made monascus anti-cancer new use - Google Patents
Xuezhikang purpose-made monascus anti-cancer new use Download PDFInfo
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- CN101104003A CN101104003A CNA2006100986533A CN200610098653A CN101104003A CN 101104003 A CN101104003 A CN 101104003A CN A2006100986533 A CNA2006100986533 A CN A2006100986533A CN 200610098653 A CN200610098653 A CN 200610098653A CN 101104003 A CN101104003 A CN 101104003A
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Abstract
The invention discloses a newly-developed pharmaceutical application of special monascus purpureus of Xuezhikang (medicine for treating hyperlipaemia) incancer resistance. Ten compounds are separated and identified from the chemical compositions of the Xuezhikang by the inventor, namely, 4-methyle-5-(2-methyle propylidene)-1 H-pyrrole-2(5H)-one(P-3), dehydrated monacolin K(C-1), stigmast-5, 22-dien-3Beta-ol(C-2), monocolin K(C-3), 3Beta-hydroxy-5Alpha, 8Beta- epidioxyergost -6, 22-dien(C-5), nitrogen-(1(tetrahydro-5-oxofuryl-2- substituent)-dethyl) acetamide (C-6), daidzein (C-7), glycitein (C-8), genistein (C-9) and erythritol (M-1). Most of the compounds have the anticancer activity, thereby the special monascus purpureus of Xuezhikang is proved to have the anticancer activity.
Description
Technical field
The present invention relates to a kind of new purposes of medicine, particularly the new pharmaceutical use of Xuezhikang purpose-made monascus.
Background technology
Xuezhikang purpose-made monascus is to make according to the method for ZL97103970.4 patent.
XUEZHIKANG JIAONANG is to be the Chinese medicine preparation of raw material with the purpose-made monascus, has clinical efficacies such as blood fat reducing, atherosclerosis, anticancer, osteoporosis.The evidence-based medicine EBM clinical research proves, can obviously reduce the coronary event incidence rate, reduces general mortality rate.Bibliographical information, chemical compound 3 beta-hydroxies-5 α, 8 β-epidioxy Ergota steroid-6, the 22-diene has extremely strong active anticancer to the L-1210 cell strain and can suppress the growth of MCF-7 human breast carcinoma and the strain of Walder256 sarcoma cell, people's hepatocarcinoma PLC/PRF5 and KB cell are also had inhibitory action, can also optionally strengthen linoleic acid (≤10mmol/L) to the inhibitory action of archaeal dna polymerase 'beta ' activity; In addition, also have antiinflammatory, anticomplementary, immunosuppressant and promotion platelet aggregation isoreactivity.That chemical compound daidzein, Glycitein, genistein have is anticancer, blood fat reducing, blood sugar lowering, vasodilator, antioxidation, inhibition smooth muscle proliferation isoreactivity.Chemical compound dehydration Monacolin K, Monacolin K have the blood fat reducing activity.
Summary of the invention
The objective of the invention is to the new pharmaceutical use of open Xuezhikang purpose-made monascus in anticancer.
From Xuezhikang purpose-made monascus, separate and identified 10 chemical compounds, be respectively 4-methyl-5-(2-methyl propylidene)-1 hydrogen-pyrroles-2 (5 hydrogen)-ketone (P-3), dehydration Monacolin K (C-1), bean steroid-5,22-diene-3 β-alcohol (C-2), Monacolin K (C-3), 3 beta-hydroxies-5 α, 8 β-epidioxy Ergota steroid-6,22-diene (C-5), nitrogen-(1-(tetrahydrochysene-5-oxo furan-2)-ethyl) acetazolamide (C-6), daidzein (C-7), Glycitein (C-8), genistein (C-9), erithritol (M-1).Compound C-5 pair L-1210 cell strain has extremely strong active anticancer and can suppress the growth of MCF-7 human breast carcinoma and the strain of Walder256 sarcoma cell, people's hepatocarcinoma PLC/PRF5 and KB cell are also had inhibitory action, can also optionally strengthen linoleic acid (≤10mmol/L) to the inhibitory action of archaeal dna polymerase 'beta ' activity; In addition, also have antiinflammatory, anticomplementary, immunosuppressant and promotion platelet aggregation isoreactivity.That Compound C-7, C-8, C-9 have is anticancer, blood fat reducing, blood sugar lowering, vasodilator, antioxidation, inhibition smooth muscle proliferation isoreactivity.Compound C-1, C-3 have the blood fat reducing activity.
The present invention seeks to realize by following experimental technique:
The separation method experiment of experimental example 1 blood fat recovery purpose-made monascus active ingredient
Get the Xuezhikang crude drug, distinguish supersound extraction 3-5 time with petroleum ether, chloroform, the methanol of 3 times of weight successively, 20min/ time, merge extractive liquid, reclaims solvent, gets petroleum ether part P, chloroform extract C, methanol position M;
Get silica gel column chromatography on the C position,, get chloroform portion C-I, 95: 5 chloroform-methanol portion C-II, 90: 10 chloroform-methanol portion C-III, methanol portion C-IV with the chloroform-methanol gradient elution;
Get C-I and partly continue silica gel column chromatography, with 95: 5-0: 100 petroleum ether-ethyl acetate gradient elutions, petroleum ether-ethyl acetate eluting position discarded in 95: 5; 90: 10 petroleum ether-ethyl acetate eluting positions merge similar stream part through silica gel column chromatography, obtain Compound P-3 by 4-6 stream part, obtain Compound C-2 by 7-10 stream part, flow part by 8-13 and obtain Compound C-1; 80: 20 petroleum ether-ethyl acetate eluting positions merge similar stream part through silica gel column chromatography, obtain Compound C-5 by 6-8 stream part, be further purified through Sephadex LH-20,50: 50 chloroform-methanol eluting obtain purification C-5, obtain Compound C-3 by 11-17 stream part; The C-II part is with 90: 10-0: 100 petroleum ether-ethyl acetate gradient elutions, and the petroleum ether-ethyl acetate part merged with above-mentioned C-I same section in 90: 10; 80: 20 petroleum ether-ethyl acetate eluting positions merge similar stream part through silica gel column chromatography, obtain Compound C-3 by 3-10 stream part; Obtain Compound C-6 by 9-11 stream part, go up Sephadex LH-20 post again,, obtain pure compound C-6 with 50: 50 chloroform-methanol eluting;
C-III part is with 90: 10-50: 50 chloroform-methanol gradient elutions, and wherein 90: 10 chloroform-methanol eluting parts obtain C-7, C-9, C-8 through silica gel column chromatography once more;
The M position is through placing the nature crystallize, and crystal washs with chloroform, obtains chemical compound M-1.
Above-mentioned C-1, C-2, C-3, C-5, C-6, C-7, C-8, C-9, M-1, P-3 chemical formula are as follows:
5，7，4′-trihydroxyisoflavone(C-9)
Following embodiment all can realize the effect of above-mentioned experimental example.
The specific embodiment
Embodiment 1:
Get purpose-made monascus 10kg, make capsule according to a conventional method, be used for the treatment of tumor.
Embodiment 2:
Get purpose-made monascus 8kg, make tablet according to a conventional method, be used for the treatment of tumor.
Embodiment 3:
Get purpose-made monascus 5kg, make granule according to a conventional method, be used for the treatment of tumor.
Claims (1)
1. the application of Xuezhikang purpose-made monascus in the preparation cancer therapy drug.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006100986533A CN101104003A (en) | 2006-07-11 | 2006-07-11 | Xuezhikang purpose-made monascus anti-cancer new use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CNA2006100986533A CN101104003A (en) | 2006-07-11 | 2006-07-11 | Xuezhikang purpose-made monascus anti-cancer new use |
Publications (1)
| Publication Number | Publication Date |
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| CN101104003A true CN101104003A (en) | 2008-01-16 |
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| CNA2006100986533A Pending CN101104003A (en) | 2006-07-11 | 2006-07-11 | Xuezhikang purpose-made monascus anti-cancer new use |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102617533A (en) * | 2011-02-01 | 2012-08-01 | 北京北大维信生物科技有限公司 | Compound separated from red yeast rice, its preparation method and application |
| CN103172693A (en) * | 2011-12-26 | 2013-06-26 | 北京北大维信生物科技有限公司 | Sterol derivative, and preparation method and application thereof |
| WO2013113294A1 (en) * | 2012-02-02 | 2013-08-08 | 北京北大维信生物科技有限公司 | Sterol derivative, preparation method therefor and use thereof |
| CN103239459A (en) * | 2012-02-02 | 2013-08-14 | 北京北大维信生物科技有限公司 | Use of sterol derivative in preparation of medicines for preventing and/or treating and/or adjunctively treating cancers |
| CN104311517A (en) * | 2014-10-17 | 2015-01-28 | 上海应用技术学院 | Polysubstituted phenanthrene ring statin lactone dehydrated compounds and application thereof |
| EP2799444A4 (en) * | 2011-12-26 | 2015-07-01 | Univ Beijing Peking Wbl Biotech Co Ltd | Sterols derivative, and preparation method and purpose thereof |
-
2006
- 2006-07-11 CN CNA2006100986533A patent/CN101104003A/en active Pending
Cited By (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102617533B (en) * | 2011-02-01 | 2014-08-27 | 北京北大维信生物科技有限公司 | Compound separated from red yeast rice, its preparation method and application |
| WO2012103777A1 (en) * | 2011-02-01 | 2012-08-09 | 北京北大维信生物科技有限公司 | Compound isolated from monascus purpureus, preparation method therefor and uses thereof |
| US9371304B2 (en) | 2011-02-01 | 2016-06-21 | Beijing Peking University Wbl Biotech Co. Ltd | Compound separated from monascus-fermented rice,the preparation method and uses thereof |
| CN103339121B (en) * | 2011-02-01 | 2016-04-13 | 北京北大维信生物科技有限公司 | A kind of compound, Preparation Method And The Use be separated from red colouring agent for food, also used as a Chinese medicine |
| CN102617533A (en) * | 2011-02-01 | 2012-08-01 | 北京北大维信生物科技有限公司 | Compound separated from red yeast rice, its preparation method and application |
| CN103339121A (en) * | 2011-02-01 | 2013-10-02 | 北京北大维信生物科技有限公司 | Compound isolated from monascus purpureus, preparation method therefor and uses thereof |
| US11845775B2 (en) | 2011-12-26 | 2023-12-19 | Beijing Peking University Wbl Biotech Co., Ltd. | Sterol derivatives and preparation method and uses thereof |
| US11845774B2 (en) | 2011-12-26 | 2023-12-19 | Beijing Peking University Wbl Biotech Co., Ltd. | Sterol derivatives and preparation method and uses thereof |
| US11634454B2 (en) | 2011-12-26 | 2023-04-25 | Beijing Peking University Wbl Biotech Co., Ltd. | Sterol derivatives and preparation method and uses thereof |
| EP2799444A4 (en) * | 2011-12-26 | 2015-07-01 | Univ Beijing Peking Wbl Biotech Co Ltd | Sterols derivative, and preparation method and purpose thereof |
| CN103172693B (en) * | 2011-12-26 | 2016-01-27 | 北京北大维信生物科技有限公司 | A kind of sterol derivative, Preparation Method And The Use |
| US10889612B2 (en) | 2011-12-26 | 2021-01-12 | Beijing Peking University Wbl Biotech Co., Ltd. | Sterol derivatives and preparation method and uses thereof |
| CN103172693A (en) * | 2011-12-26 | 2013-06-26 | 北京北大维信生物科技有限公司 | Sterol derivative, and preparation method and application thereof |
| CN103239459A (en) * | 2012-02-02 | 2013-08-14 | 北京北大维信生物科技有限公司 | Use of sterol derivative in preparation of medicines for preventing and/or treating and/or adjunctively treating cancers |
| CN103239459B (en) * | 2012-02-02 | 2015-03-11 | 北京北大维信生物科技有限公司 | Use of sterol derivative in preparation of medicines for preventing and/or treating and/or adjunctively treating cancers |
| WO2013113294A1 (en) * | 2012-02-02 | 2013-08-08 | 北京北大维信生物科技有限公司 | Sterol derivative, preparation method therefor and use thereof |
| CN104311517A (en) * | 2014-10-17 | 2015-01-28 | 上海应用技术学院 | Polysubstituted phenanthrene ring statin lactone dehydrated compounds and application thereof |
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