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 PDF

Info

Publication number
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
Authority
CN
China
Prior art keywords
human
cell
osw
application
preparation
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN 200610116980
Other languages
Chinese (zh)
Inventor
惠永正
杨志奇
俞春莺
葛强
包丽华
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
CHUANGXIN CHINESE MEDICINE RESEARCH CENTER SHANGHAI
Original Assignee
CHUANGXIN CHINESE MEDICINE RESEARCH CENTER SHANGHAI
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by CHUANGXIN CHINESE MEDICINE RESEARCH CENTER SHANGHAI filed Critical CHUANGXIN CHINESE MEDICINE RESEARCH CENTER SHANGHAI
Priority to CN 200610116980 priority Critical patent/CN1951394A/en
Publication of CN1951394A publication Critical patent/CN1951394A/en
Pending legal-status Critical Current

Links

Landscapes

  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

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

The application of omoto nippoulily saponin OSW-1-1 in the anticancer disease drug of preparation
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:
Figure A20061011698000031
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.
Figure A20061011698000071
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
Figure A20061011698000072
Cell inhibitory rate under table 2 variable concentrations (%)
Figure A20061011698000082
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.
CN 200610116980 2006-10-10 2006-10-10 Application of Antitumor Saponins OSW-1 in preparation of anti-cancer medicament Pending CN1951394A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN 200610116980 CN1951394A (en) 2006-10-10 2006-10-10 Application of Antitumor Saponins OSW-1 in preparation of anti-cancer medicament

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN 200610116980 CN1951394A (en) 2006-10-10 2006-10-10 Application of Antitumor Saponins OSW-1 in preparation of anti-cancer medicament

Publications (1)

Publication Number Publication Date
CN1951394A true CN1951394A (en) 2007-04-25

Family

ID=38058078

Family Applications (1)

Application Number Title Priority Date Filing Date
CN 200610116980 Pending CN1951394A (en) 2006-10-10 2006-10-10 Application of Antitumor Saponins OSW-1 in preparation of anti-cancer medicament

Country Status (1)

Country Link
CN (1) CN1951394A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
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

Cited By (2)

* Cited by examiner, † Cited by third party
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

Similar Documents

Publication Publication Date Title
CN108358973B (en) Naphthalimide tetravalent platinum compound, preparation method and application thereof in preparation of antitumor drugs
Li et al. Design, synthesis and biological evaluation of glucose-containing scutellarein derivatives as neuroprotective agents based on metabolic mechanism of scutellarin in vivo
CN105037474A (en) 4'-amino-4'-dehydroxyl-oleandrin and 4'-amino-4'-dehydroxyl-odoroside A and use thereof
Fang et al. Nitric oxide-donating derivatives of hederacolchiside A1: Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents
CN104086617B (en) Close dimethylamine derivative, the preparation method and its usage of flowers and trees ketone Cleistanone
CN104151391A (en) Oleanolic acid derivative having antineoplastic effect, preparation method and purpose thereof
CN1951394A (en) Application of Antitumor Saponins OSW-1 in preparation of anti-cancer medicament
CN103288911A (en) Bufalin glycosylation derivative and preparation method and application thereof in preparation of anti-tumour medicaments
CN110857295B (en) Flavone-ligustrazine compound CH-X with selective anti-liver cancer effect and preparation method and application thereof
CN101519423B (en) Betulinic acid analogue and preparation method and application thereof
CN102030800B (en) Abies holophylla triterpenoid compound, extraction separation thereof and application thereof
CN102382164A (en) Toad lactam compound as well as preparation method and application thereof
CN101624387B (en) Method for purifying and preparing isoalantolactone and application thereof in preparing antineoplastic medicaments
CN105061533B (en) Hexa methoxy flavanone rhamnopyranosyl rhamnoside and its application
CN104926804B (en) One kind has compound, the preparation method and use of antitumor action
CN101590072B (en) Application of calycosin-7-O-beta-D-glucopyranoside or salt thereof in resisting AIDS
CN104098594B (en) Biotin-podophyllotoxin esterification derivative and pharmaceutical composition thereof and its preparation method and application
CN103172555B (en) Indole alkaloid compound separated from rhizoma cimicifugae as well as preparation method and application thereof
Hernandez-Moreno et al. The isoflavonoid brazilin inhibits viability and cell migration in breast cancer cells
CN102267952A (en) Quinazoline compound and preparation method and application thereof
CN103204896B (en) 12-oxo soladulcine amino acid conjugate, its preparation method, preparation and medicinal use thereof
CN106188019B (en) The Preparation method and use of a kind of baicalein -7- methyl ether derivative
CN113181164A (en) Application of loganin aglycone in preparation of medicine for preventing and treating brain glioma
CN107011307B (en) A kind of flavonoids and preparation method thereof, preparation and application
TR201514635A2 (en) N-acetylpyrazole derivatives having anti-cancerogenic efficiency

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C12 Rejection of a patent application after its publication
RJ01 Rejection of invention patent application after publication

Open date: 20070425