CN103830293A - Medicine with hederagenin as active ingredient, and applications of medicine in medicine preparation - Google Patents
Medicine with hederagenin as active ingredient, and applications of medicine in medicine preparation Download PDFInfo
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- CN103830293A CN103830293A CN201210474897.2A CN201210474897A CN103830293A CN 103830293 A CN103830293 A CN 103830293A CN 201210474897 A CN201210474897 A CN 201210474897A CN 103830293 A CN103830293 A CN 103830293A
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Abstract
The invention provides a medicine with hederagenin as an active ingredient, and applications of the medicine in aspect of medicine preparation, and specifically provides applications of the medicine in preparation of antitumor medicines. The medicine can be used for preparing medicines independently with pharmaceutic adjuvants or with other medicines.
Description
Technical field
The present invention relates to the medicine taking helexin as effective ingredient, and application aspect medicine, its application aspect antitumor drug is more specifically provided.
Background technology
helexin, for adding section's Hedera plant Caulis Hederae Sinensis
hederanepalensisK.Kochvar.sinensis(Tobl.) the contained main component of Rehd., there is the effect of hygroscopicity, bitter in the mouth, irritates nucous membrane, general water soluble, is soluble in hot water, hot methanol and hot ethanol, is insoluble to the organic solvent that ether isopolarity is little.The inventor, through research, finds that helexin has antitumor action.
Summary of the invention
The invention provides the medicine taking helexin as effective ingredient.
The invention provides the pharmaceutical composition that comprises helexin, said composition can be that helexin is combined and is prepared from pharmaceutically acceptable adjuvant or other medicines.
The invention provides the application of helexin aspect medicine.
The invention provides helexin in the application of preparing aspect antitumor drug.
The preparation method of compound provided by the invention can be prepared according to preparation method described in ZL200710146725.1.The medicine that contains helexin compound provided by the invention, can by compound is added pharmaceutically acceptable adjuvant or optionally other composition make the pharmaceutical composition that is suitable for clinical use.
Compound of the present invention, in the application of preparing in medicine for treating tumor thing, is to be confirmed by following effect experiment.
Detailed description of the invention
Experimental example 1: the inhibitory action of helexin to tumor cell in vitro
material and reagent
Medicine and reagent: helexin, prepare according to preparation method described in ZL200710146725.1.Injection vincristine sulfate, Hualian Pharmaceutical Co., Ltd., Shanghai, 1mg/ props up.RPMI1640 culture medium: GIBCO company produces; New-born calf serum (super), Hangzhou Sijiqing Biological Engineering Material Co., Ltd..Trypsin, Sigma company produces; Sulfo group rhodamine B (sulforhadamine B, SRB), Sigma company; Injection streptomycin, Shangdong Ruiyang Pharmaceutical Co., Ltd, 1g(,100 ten thousand units)/; Benzylpenicillin sodium for injection, Lukang Medical Co., Ltd., Shandong, 800,000 units/.Other conventional chemical reagent is domestic analytical pure.
Cell strain: human hepatoma cell strain SMMC-7721, Bel-7402, human oophoroma cell line HO8910, human prostata cancer born of the same parents PC-3M, human lung adenocarcinoma cell line A549, human colon cancer cell strain HCT-8, human esophagus cancer cell strain CaEs-17, human glioma cell line U251, Human gastric carcinoma cell line BGC-823, people's gastric adenocarcinoma cells strain SGC-7901, all purchased from pharmacological room of Beijing institute of oncology of the Chinese Academy of Medical Sciences.
Instrument: CO2 incubator, superclean bench, microplate reader, inverted microscope, Tissue Culture Flask (Costar, USA), 96 porocyte culture plates (Costar, USA).
Software: Microsoft Excel 7.0 statistical analysis softwares; Microcal Origin 6.0 data processing softwares.
experimental technique
Medicine and reagent preparation:
One bag of RPMI1640 culture medium adds water one liter, adds 2 grams of sodium bicarbonate, and 100,000 unit penicillins and 100mg streptomycin regulate pH value to 7.4, with 0.22 μ m degerming membrane filtration degerming.90ml culture medium adds deactivation new-born calf serum 10ml and is complete culture solution.Trypsin is made into filtration sterilization after 0.25% solution with D-hanks buffer.
Accurately take helexin 20.0 mg in sterilizing centrifuge tube, add DMSO 1ml, be made into 20 mg/ml stock solutions.Get 10 μ l stock solutions and be added in the complete culture solution of 10ml, become 20 μ g/ml application liquid, then be the application liquid of 10,5,2.5 and 1.25 μ g/ml with complete culture solution dilution respectively.
Cell culture and going down to posterity:
The equal adhere-wall culture of all cells is in containing 10ml complete culture solution Tissue Culture Flask, in 37 DEG C, 5%CO
2, full closing under humidity cultivate.After at the bottom of cell covers with bottle, wash twice with sterilizing D-hanks liquid, add 0.25% trypsin digestion and cell 2 minutes, outwell trypsin, after jog cell can come off completely, add after complete culture solution 30ml, dispel cell with pipet, be sub-packed in 3 new Tissue Culture Flasks, continue to cultivate.
Drug treating: get one bottle, the cell that just covered with, after trypsinization, add 10ml complete culture solution suspension cell, with pipet piping and druming evenly, get two cell suspension counting cells number under microscope, adjust cell number to 10 with complete culture solution
5individual cells/ml.Get one of 96 orifice plate, draw 100ul cell suspension be added in 96 orifice plates with liquid-transfering gun, every strain cell adds 4 row, and a culture plate can add the different cells of 3 strains.Separately do background contrast with each four holes of the same cell suspension of a culture plate.Add the culture plate of cell in CO
2in incubator, cultivate after 12 hours and outwell original fluid, in 96 orifice plates, A is capable adds fresh complete culture solution 200 μ l, B is capable, and the 200 μ l that add make solvent control containing the complete culture solution of 0.02% dimethyl sulfoxide (DMSO), C is capable, and the 200 μ l that add make positive control containing the complete culture solution of 25 μ g/ml vincristine, D is capable of the capable complete culture solution 200ul adding containing variable concentrations helexin of H, maximum concentration is 20 μ g/ml, by 0.5 times of doubling dilution, be respectively 10,5,2.5,1.25 μ g/ml.After adding medicine, culture plate is placed in CO
2in incubator, cultivate.
Above-mentioned experiment is all carried out under strict aseptic condition.
Result is measured: contrast is taken out and in containing cell hole, added gently the trichloroacetic acid solution of 25ul 50% pre-cooling in cultivating on liquid level with culture plate, leave standstill after 5 minutes, place 1 hour at 4 DEG C of refrigerators, discard supernatant liquid, wash 5 times with deionized water, wait until and dosing culture plate in the lump staining analysis after putting air drying.
Cell dosing was cultivated after 48 hours, take out culture plate, add 50% trichloroacetic acid of 50ul pre-cooling in every hole, standing immigration after 5 minutes in 4 DEG C of refrigerators leaves standstill 1 hour, and taking-up is washed 5 times with deionized water, air drying, after bone dry, every hole adds 0.4% SRB 100ul of 1% acetic acid preparation, dye and outwell dye liquor after 20 minutes, wash 5 times with 1% acetic acid, remove unconjugated dyestuff.After air drying, use the non-buffering Tris alkali liquor 150ul of the 10mmol/L of pH 10.5 to dissolve, on oscillator plate, vibrate 5 minutes, in BioRad microplate reader, measure the light absorption of each hole at 490nm.The cell of background control board is processed equally and is measured OD490.
Calculate the suppression ratio of medicine on cell proliferation according to each hole OD490:
According to drug level logarithm and suppression ratio, make rectilinear regression with Microcal Origin software, obtain linear equation, calculate suppression ratio corresponding drug level 50% time and be the 503nhibiting concentration (IC of helexin to tumor cell
50).
Under above-mentioned similarity condition, measure the IC of every strain cell
50.
experimental result:
Proliferation inhibition rate and the 503nhibiting concentration (IC of table 1. variable concentrations medicine to cell
50)
Experimental result shows, helexin, to various human source tumor cell line, comprising: hepatocarcinoma, pulmonary carcinoma, carcinoma of prostate, gastric cancer, ovarian cancer cell, carcinoma of prostate, colon cancer, the esophageal carcinoma, glioma etc. all have its proliferation function of stronger inhibition, IC
50all be less than 10 μ g/ml.
Claims (6)
1. the medicine taking helexin as effective ingredient.
2. medicine according to claim 1, itself and pharmaceutically acceptable adjuvant are made pharmaceutical composition, or combine and be prepared into pharmaceutical composition with other medicines.
3. medicine according to claim 1 and 2, is characterized in that the helexin that contains l% to 99% in this medicine.
4. medicine according to claim 1 and 2, is characterized by by oral route, injection or external administration.
5. helexin is in the application of preparing aspect medicine.
6. application according to claim 5, is characterized in that helexin is in the application of preparing aspect antitumor drug.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210474897.2A CN103830293A (en) | 2012-11-21 | 2012-11-21 | Medicine with hederagenin as active ingredient, and applications of medicine in medicine preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210474897.2A CN103830293A (en) | 2012-11-21 | 2012-11-21 | Medicine with hederagenin as active ingredient, and applications of medicine in medicine preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103830293A true CN103830293A (en) | 2014-06-04 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210474897.2A Pending CN103830293A (en) | 2012-11-21 | 2012-11-21 | Medicine with hederagenin as active ingredient, and applications of medicine in medicine preparation |
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| CN (1) | CN103830293A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523699A (en) * | 2013-09-28 | 2015-04-22 | 杨小林 | Application of hederagenin to preparation of drug for resisting to HO-8910PM tumors of ovarian cancer |
| CN104523700A (en) * | 2013-09-28 | 2015-04-22 | 杨小林 | Application of hederagenin to preparation of drug for resisting to MGC-803 tumors of gastric cancer |
| CN104546864A (en) * | 2013-09-28 | 2015-04-29 | 杨小林 | Application of hederagenin in preparation of medicine for resisting liver cancer Hep3B tumors |
| CN104546866A (en) * | 2013-09-28 | 2015-04-29 | 杨小林 | Application of hederagenin in preparation of medicine for resisting tumors of esophageal squamous carcinoma cell Eca-109 |
-
2012
- 2012-11-21 CN CN201210474897.2A patent/CN103830293A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523699A (en) * | 2013-09-28 | 2015-04-22 | 杨小林 | Application of hederagenin to preparation of drug for resisting to HO-8910PM tumors of ovarian cancer |
| CN104523700A (en) * | 2013-09-28 | 2015-04-22 | 杨小林 | Application of hederagenin to preparation of drug for resisting to MGC-803 tumors of gastric cancer |
| CN104546864A (en) * | 2013-09-28 | 2015-04-29 | 杨小林 | Application of hederagenin in preparation of medicine for resisting liver cancer Hep3B tumors |
| CN104546866A (en) * | 2013-09-28 | 2015-04-29 | 杨小林 | Application of hederagenin in preparation of medicine for resisting tumors of esophageal squamous carcinoma cell Eca-109 |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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Application publication date: 20140604 |