CN1951394A - Application of Antitumor Saponins OSW-1 in preparation of anti-cancer medicament - Google Patents
Application of Antitumor Saponins OSW-1 in preparation of anti-cancer medicament Download PDFInfo
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- CN1951394A CN1951394A CN 200610116980 CN200610116980A CN1951394A CN 1951394 A CN1951394 A CN 1951394A CN 200610116980 CN200610116980 CN 200610116980 CN 200610116980 A CN200610116980 A CN 200610116980A CN 1951394 A CN1951394 A CN 1951394A
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Abstract
The invention relates to a method for using rhodea sapogenin OSW-1 to prepare anti-cancer drug. Wherein, the rhodea sapogenin OSW-1 can significantly restrain the growths of MCF-7 breast cancer cell, Hela uterine neck cancer cell, A431 skin cancer cell, HL-60 leukemia cell and A549 lung carcinoma cell, and some restrain the growths of 786-0 kidney cancer cell, CNE nasopharyngeal carcinoma cell, SGC-7901 gastric cancer cell.
Description
Technical field
The present invention relates to field of medicaments, specifically, relate to the application of tiger eye omoto nippoulily saponin OSW-1-1 in the anticancer disease drug of preparation.
Background technology
Malignant tumor is a kind of disease of serious threat human health, chemotherapy of tumors and surgical operation, radiotherapy constitute combined therapy of tumour three big important component parts.Although the research of antitumor drug makes great progress with application, present therapeutic effect to most tumors still is difficult to satisfactory, therefore, finds and develop key subjects and the task that new type antineoplastic medicine remains biomedicine field.
1992, Tokyo pharmacy and life sciences university chemistry man Yutaka professor Sashida are from a kind of South Africa Swaziland (Swaziland) that originates in, Transvaal (Transvaal), separation and Extraction goes out a series of Saponins with cholesterol skeleton in the evergreen ornamental plant Herba Phyllanthi Urinariae's (OrnithogalumSaundersiae) of Natal provinces such as (Natal) the underground bulb, its main constituent is an omoto nippoulily saponin OSW-1-1, and its structural formula is as follows:
The present invention has carried out long term studies to omoto nippoulily saponin OSW-1-1, has found that omoto nippoulily saponin OSW-1-1 has powerful anti-tumor activity.
Summary of the invention
The purpose of this invention is to provide the application of a kind of omoto nippoulily saponin OSW-1-1 in the anticancer disease drug of preparation.
Wherein said cancer first-selection is breast carcinoma, cervical cancer, skin carcinoma, leukemia, pulmonary carcinoma, renal carcinoma, nasopharyngeal carcinoma or gastric cancer.
Omoto nippoulily saponin OSW-1-1 can with receivable carrier pharmaceutically, for example: filler such as starch, microcrystalline Cellulose etc.; Binding agent such as vitamin derivative, starch etc.; Disintegrating agent such as sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose etc. are taken by the mode of oral administrations such as tablet, capsule, granule.
The pharmacological results shows, the growth of omoto nippoulily saponin OSW-1-1 pair MCF-7 human breast cancer cell strain, the strain of Hela human cervical carcinoma cell, A431 application on human skin JEG-3, HL-60 human leukemia cell line, A549 human lung carcinoma cell line shows stronger inhibition effect, and the growth of the strain of 786-0 human renal carcinoma cell, CNE human nasopharyngeal carcinoma cell line, SGC-7901 human stomach cancer cell line is also had certain inhibitory action.
The specific embodiment
Following examples are used to illustrate the present invention, but are not used for limiting the scope of the invention.
Embodiment 1 Herba Phyllanthi Urinariae's preparation
According to the preparation method of document " " J.Org.Chem " 1999,64,202-208 ", preparation omoto nippoulily saponin OSW-1-1.
The physicochemical data of this chemical compound is as follows:
Proton nmr spectra
1H?NMR(600MHz,C
5D
5N)8.31(2H,d),7.07(2H,d),5.67(1H,dd,J=8.0,9.2),5.55(1H,t,J=6.3,7.5),5.37(1H,d,J=3.6),5.11(1H,d,J=8.0),4.79(1H,s),4.57(1H,d,J=6.0),4.39(1H,brs),4.31(1H,dd,J=5.2,11.1),4.26-4.20(2H,m),4.20-4.12(3H,m),3.81(1H,brs),3.73(3H,s),3.18(1H,q,J=7.4),1.96(3H,s),1.27(3H,d,J=7.5),1.06(3H,s),0.98(3H,s),0.87(3H,d,J=6.4),0.84(3H,d,J=6.4)。
Carbon-13 nmr spectra
13C?NMR(75MHz,C5D5N)218.96,169.27,165.47,163.91,141.95,132.45,121.13,114.15,103.68,100.86,88.36,85.72,80.99,76.35,75.15,72.05,71.31,70.75,67.85,67.06,65.59,55.52,50.20,48.58,46.57,46.33,43.55,39.29,37.80,36.90,34.64,32.73,32.28,32.08,27.76,22.85,22.51,20.93,19.64,13.64,11.91。
Ir data
IR(KBr)3467,2957,2934,1726,1695,1607,1513,1465,1373,1258,1232,1170,1044,988,972。
Mass spectrometric data
FABMS?m/z:896(M+1+Na)。
Embodiment 2
The chemical compound that obtains among the embodiment 1 is an amount of with sucrose, and mixing is an adhesive with 70% ethanol, granulates, and drying promptly gets granule.
Embodiment 3
The chemical compound that obtains among the embodiment 1 is added Celluloasun Microcrystallisatum, an amount of mix homogeneously of amylum pregelatinisatum, 95% ethanol wet granulation, drying adds low-substituted hydroxypropyl cellulose, an amount of Pulvis Talci, and tabletting promptly gets tablet.
Embodiment 4
With the chemical compound that obtains among the embodiment 1 add melt in the Cera Flava, mix with colloid mill, mixture rolls capsule in automatic rotation and makes soft capsule, drying is 24 hours under the condition of 20 ℃ of temperature, relative humidity 52%, take out, use washing with alcohol, dry 48 hours under these conditions, promptly get soft capsule.
Embodiment 5
The chemical compound that obtains among the embodiment 1 is an amount of with sucrose, and mixing is an adhesive with 70% ethanol, granulates, and the softgel shell of packing into promptly gets capsule.
Experimental example
Experiment purpose: measure omoto nippoulily saponin OSW-1-1 pair A549 human lung carcinoma cell line, the strain of MCF-7 human breast cancer cell, SMMC-7721 human hepatoma cell strain, the strain of Hela human cervical carcinoma cell, SGC-7901 human stomach cancer cell line, CNE human nasopharyngeal carcinoma cell line, the strain of 786-0 human renal carcinoma cell, A431 application on human skin JEG-3, HL-60 human leukemia cell line, the effect of WI38 human normal cell line strain inhibition of proliferation.
Material:
1. instrument: clean bench (Microcystins in The Dianshan Lake cleaning equipment factory), constant temperature CO
2Incubator (U.S. Forma), enzyme-linked immunosorbent assay instrument (U.S. BIO-RAD), inverted biological microscope (optical instrument factory, Chongqing)
2. reagent: RPMI1640 culture medium (the Lot NO.1304895 of GIBCO company).
MEM culture medium (the Lot NO.1201167 of GIBCO company).
DMEM culture medium (the Lot NO.1201167 of GIBCO company).
F12 culture medium (the Lot NO.1279320 of GIBCO company).
The Lot NO.1106338 of trypsin GIBCO company).
Calf serum (the Lot NO.56546750 of GIBCO company).
Hyclone (the Lot NO.A01005-0983 of PAA company).
MTT (tetrazolium bromide) (the Lot NO.0731 of Genebase company).
The inferior maple (DMSO, the Chinese Medicine Shanghai LotNO.T200411020 of chemical reagents corporation) of diformazan.
3. cell strain: cell strain is provided by Chinese Academy of Sciences's cell.
A549 human lung carcinoma cell line, the strain of Hela human cervical carcinoma cell, SGC-7901 human stomach cancer cell line, CNE human nasopharyngeal carcinoma cell line, the strain of 786-0 human renal carcinoma cell, HL-60 human leukemia cell line are incubated at respectively in the RPMI1640 culture medium, contain 10% calf serum, 37 ℃, 5%CO
2Cultivate under the concentration.
The strain of MCF-7 human breast cancer cell is incubated in the MEM culture medium, contains 10% hyclone, and 37 ℃, 5%CO
2Cultivate under the concentration.
A431 application on human skin JEG-3 is incubated in the F12 culture medium, contains 10% hyclone, and 37 ℃, 5%CO
2Cultivate under the concentration.
The strain of WI38 human normal cell line is incubated in the DMEM culture medium, contains 15% hyclone, and 37 ℃, 5%CO
2Cultivate under the concentration.
Method:
1. get and be in one bottle in cell in good condition exponential phase of growth, make cell suspension.
2. cell counting, and cell density is diluted to 3.5 * 10
4Individual/ml.
3. obtained cell suspension is inoculated on 96 orifice plates, and constant temperature CO is put in 90 μ l/ holes
2Cultivated 24 hours in the incubator.
Remove culture fluid 4.24 inhale after hour, adding is subjected to reagent thing (omoto nippoulily saponin OSW-1-1), and the medicine final concentration is respectively 10ug/ml, 1ug/ml, 1 * 10
-1Ug/ml, 1 * 10
-2Ug/ml, 1 * 10
-3Ug/ml, 1 * 10
-4Ug/ml, 1 * 10
-5Ug/ml, 1 * 10
-6Ug/ml, every hole 100 μ l cultivated 90 hours.
5.A431 application on human skin JEG-3, HL-60 human leukemia cell line, the strain of WI38 human normal cell line and the strain of Hela human cervical carcinoma cell taking-up in 68 hours after dosing adds MTT, all the other cell strains all took out dull and stereotyped after 90 hours, and MTT is made into 5mg/ml solution with PBS solution.MTT is added in 96 orifice plates, 10 μ l/ holes, reaction is inhaled after 4 hours and is removed supernatant in the incubator, add DMSO, rocked 15 minutes in 150 μ l/ holes, precipitation is dissolved fully, is the absorbance that the 570nm place measures every hole with enzyme-linked immunosorbent assay instrument at wavelength, and calculates cell inhibitory rate.
Experimental result: omoto nippoulily saponin OSW-1-1 in-vitro screening the results are shown in Table 1,2,3.
Susceptibility group OD average during each concentration of table 1
Cell inhibitory rate under table 2 variable concentrations (%)
Cell inhibitory rate under table 3 variable concentrations (%)
Conclusion: above experimental result shows, the growth of omoto nippoulily saponin OSW-1-1 pair MCF-7 human breast cancer cell strain, the strain of Hela human cervical carcinoma cell, A431 application on human skin JEG-3, HL-60 human leukemia cell line, A549 human lung carcinoma cell line shows stronger inhibition effect, and the growth of the strain of 786-0 human renal carcinoma cell, CNE human nasopharyngeal carcinoma cell line, SGC-7901 human stomach cancer cell line is also had certain inhibitory action.
Claims (3)
1, the application of omoto nippoulily saponin OSW-1-1 in the anticancer disease drug of preparation.
2, application as claimed in claim 1, wherein said cancer are breast carcinoma, cervical cancer, skin carcinoma, leukemia, pulmonary carcinoma, renal carcinoma, nasopharyngeal carcinoma or gastric cancer.
3, application as claimed in claim 1 or 2, wherein said anticancer disease drug is tablet, capsule, granule or soft capsule.
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102580065A (en) * | 2012-02-13 | 2012-07-18 | 林树芳 | Ornithogalum caudatum saponin OSW-1 oral anticancer preparation and preparation method thereof |
US8552161B2 (en) | 2009-02-09 | 2013-10-08 | Uniwersytet W Bialymstoku | Saponin compounds, methods of preparation thereof, use thereof and pharmaceutical compositions |
-
2006
- 2006-10-10 CN CN 200610116980 patent/CN1951394A/en active Pending
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8552161B2 (en) | 2009-02-09 | 2013-10-08 | Uniwersytet W Bialymstoku | Saponin compounds, methods of preparation thereof, use thereof and pharmaceutical compositions |
CN102580065A (en) * | 2012-02-13 | 2012-07-18 | 林树芳 | Ornithogalum caudatum saponin OSW-1 oral anticancer preparation and preparation method thereof |
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