CN103784470A - Drug for treating tumor - Google Patents
Drug for treating tumor Download PDFInfo
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- CN103784470A CN103784470A CN201210428754.8A CN201210428754A CN103784470A CN 103784470 A CN103784470 A CN 103784470A CN 201210428754 A CN201210428754 A CN 201210428754A CN 103784470 A CN103784470 A CN 103784470A
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- ethoxy
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- fluorouracil
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Abstract
The invention discloses a drug for treating tumor. The drug contains an effective amount of poly[2-2(2-ethoxy ethoxy ethyl)guanidine hydrochloride and an effective amount of 5-fluorouracil, wherein the average molecular weight of poly[2-2(2-ethoxy ethoxy ethyl)guanidine hydrochloride is 1200 D, and the mass ratio of poly[2-2(2-ethoxy ethoxy ethyl)guanidine hydrochloride to 5-fluorouracil is 5:1 to 10:1. Compared with a cell inhibitory activity of the prior art, a cell inhibitory activity of the drug is greatly improved, and the drug can effectively treat malignant tumor.
Description
Technical field
The present invention relates to a kind of medicine, be specifically related to a kind of medicine for the treatment of tumor.
Background technology
Tumor (Tumor) be body under various carcinogenic factor effects, some cells of local organization lose the normal regulation to its growth on gene level, cause its clonal abnormality hypertrophy and the abnormality that forms.Educational circles is generally divided into tumor optimum and pernicious two large classes.Malignant tumor has another name called cancer.
Tumor is genopathy in itself.All-environment and hereditary carcinogenic factor is to work in coordination with or sequential mode causes DNA infringement, thereby activate proto-oncogene and (or) deactivation tumor suppressor gene, add the change of apoptosis regulator gene and (or) DNA-repair gene, then cause the abnormal of expression, target cell is transformed.The cell being converted is first the hypertrophy of clone's property more, through a very long multistage evolution process, one of them clones relatively unconfined amplification, pass through addition mutation, optionally form the sub-clone (heterogeneousization) with different characteristics, thereby obtain the ability (vicious transformation) that infiltrates and shift, form malignant tumor.
At present, the method for the treatment tumor of international mainstream is chemotherapy, but for the chemotherapeutic subject matter of these diseases is, cancerous cell only has certain percentage rate to react to used cytostatic medicament.In addition,, even if tumor reacts to treatment, usually can not expect the alleviation completely of symptom.
In order to increase chemotherapeutical curative effect, current trend is number of chemical treatment, adopts various kinds of cell to suppress medicine.More and more frequently, by combined to improve treatment of cancer the multiple cytostatic medicament with different application points.Obtain better curative effect on the one hand thus, and run on the other hand the progressively drug-fast problem of development.
Other probability is that the cell that carrys out selective protection health by while dosed cells protective agent is not subject to the impact of cytostatic medicament, thus can the higher dosage of administration, produce lower side effect simultaneously.
Although there are these measures, chemotherapeutical side effect rate is still very high.Just because of this reason, research had not only had good effect but also had had good toleration that the active component foot of wide as far as possible treatment window is extremely important.
Summary of the invention
The object of the present invention is to provide a kind of medicine for the treatment of tumor, it is characterized in that, poly-[the 5-fluorouracil of 2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and effective dose that described medicine contains effective dose, it is described that poly-[2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate mean molecule quantity is 1200D, and described poly-[mass ratio of 2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and 5-fluorouracil is 5:1 ~ 10:1.
It is poly-that [2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate is known compound, and it can obtain in market purchase, also can prepare voluntarily.Its typical but non-limiting example of preparing is: at 50 ℃, 4.43mol guanidine hydrochlorate is dissolved in 4.03mol triethylene glycol diamine.Be heated to subsequently 120 ℃ and stir 2 hours in described temperature.Then keep this temperature 2 hours, then apply vacuum and continue again in a vacuum to stir 2 hours at 170 ℃.Be inflated to subsequently normal pressure, be cooled to 120 ℃ and be diluted to approximately 50% with deionized water.Neutralize pH value approximately 6 with phosphoric acid, make it cooling and be diluted to desired concn.Molecular weight records as 1200D.
5-fluorouracil is converted into after effective fluorodeoxyuridine acid in cell, is subject to thymidylate synthetase in cell to be converted into thymidylic acid, and disturbs synthesizing of DNA by blocking-up deoxyribose uridylic acid.Fluorouracil equally can RNA interfering synthetic. after intravenous administration, fluorouracil is distributed widely in body fluid, and from blood, disappears in 4 hours.It is being converted into after nucleotide.Tissue and tumor by active division are preferentially absorbed, and fluorouracil easily enters in cerebrospinal fluid.Approximately 20% with prototype from homaluria, all the other major parts in liver by the general machine-processed institute metabolism to uracil metabolism.Described 5-fluorouracil is known substance, and it is also the medicine that is used for the treatment of the earliest malignant tumor.
For measuring the cell inhibitory activity of material, cancerous cell is used from culture bottle suspension through RPMI washing with 200 μ l in the concentration of 20000 cells transfer in microtitration plate.Under the existence of the test substances of variable concentrations, cancerous cell is subsequently at the temperature of 37 ℃ and 5% CO
2under atmosphere, cultivate three days.For medicine of the present invention, and all comparative examples, the concentration adopting in all tests is that 0.12-500 μ g/m is to dilute 2 times.After three days incubation times, evaluate by non-radioactive cell proliferation and cell toxicity test EZ4U.After three hours, be that 49/630nm among Dias-Photometers (delustring of test sample divided by the blank extinction value of control sample) by photometer method with percentage ratio evaluate at wavelength with EZ4U cultivation.
Lymphocytic vigor is 1.2 × 10
7variable concentrations with test substances in the suspension of/ml is measured.Under the existence of test substances, cell suspending liquid is at 37 ℃ and 5% CO
2in atmosphere, cultivate 24 hours, then use trypan blue staining.After dyeing, lymphocyte is applied in counting chamber and with percentage ratio metering vigor.
Described measuring, medicine of the present invention is 60% to the cell inhibitory activity of cancerous cell, and independent poly-[2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate is 46% to the cell inhibitory activity of cancerous cell, and independent 5-fluorouracil is 35% to the cell inhibitory activity of cancerous cell.Hence one can see that, in medicine of the present invention, poly-[2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and 5-fluorouracil combine use, compared to the cell inhibitory activity of prior art, obtained significantly and improved, it can effectively treat malignant tumor.
The specific embodiment
For ease of understanding the present invention, it is as follows that the present invention enumerates embodiment.Those skilled in the art should understand, described embodiment only, for helping to understand the present invention, should not be considered as concrete restriction of the present invention.
Embodiment 1
A kind of medicine for the treatment of tumor, it is characterized in that, poly-[the 5-fluorouracil of 2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and effective dose that described medicine contains effective dose, it is described that poly-[2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate mean molecule quantity is 1200D, and described poly-[mass ratio of 2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and 5-fluorouracil is 6:1.
For measuring the cell inhibitory activity of material, cancerous cell is used from culture bottle suspension through RPMI washing with 200 μ l in the concentration of 20000 cells transfer in microtitration plate.Under the existence of the test substances of variable concentrations, cancerous cell is subsequently at the temperature of 37 ℃ and 5% CO
2under atmosphere, cultivate three days.For medicine of the present invention, and all comparative examples, the concentration adopting in all tests is that 0.12-500 μ g/m is to dilute 2 times.After three days incubation times, evaluate by non-radioactive cell proliferation and cell toxicity test EZ4U.After three hours, be that 49/630nm among Dias-Photometers (delustring of test sample divided by the blank extinction value of control sample) by photometer method with percentage ratio evaluate at wavelength with EZ4U cultivation.
Lymphocytic vigor is 1.2 × 10
7variable concentrations with test substances in the suspension of/ml is measured.Under the existence of test substances, cell suspending liquid is at 37 ℃ and 5% CO
2in atmosphere, cultivate 24 hours, then use trypan blue staining.After dyeing, lymphocyte is applied in counting chamber and with percentage ratio metering vigor.
Described measuring, medicine of the present invention is 60% to the cell inhibitory activity of cancerous cell, and independent poly-[2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate is 46% to the cell inhibitory activity of cancerous cell, and independent 5-fluorouracil is 35% to the cell inhibitory activity of cancerous cell.
Hence one can see that, in medicine of the present invention, poly-[2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and 5-fluorouracil combine use, compared to the cell inhibitory activity of prior art, obtained significantly and improved, it can effectively treat malignant tumor.
Applicant's statement, the present invention illustrates detailed process composition and engineering flow process of the present invention by above-described embodiment, but the present invention is not limited to above-mentioned detailed process composition and engineering flow process, do not mean that the present invention must rely on above-mentioned detailed process composition and engineering flow process and could implement.Person of ordinary skill in the field should understand, any improvement in the present invention, and the selections of the equivalence replacement to the each raw material of product of the present invention and the interpolation of auxiliary element, concrete mode etc., within all dropping on protection scope of the present invention and open scope.
Claims (1)
1. treat the medicine of tumor for one kind, it is characterized in that, poly-[the 5-fluorouracil of 2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and effective dose that described medicine contains effective dose, it is described that poly-[2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate mean molecule quantity is 1200D, and described poly-[mass ratio of 2-2 (2-ethoxy ethoxy ethyl) guanidine hydrochlorate and 5-fluorouracil is 5:1 ~ 10:1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210428754.8A CN103784470A (en) | 2012-10-31 | 2012-10-31 | Drug for treating tumor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210428754.8A CN103784470A (en) | 2012-10-31 | 2012-10-31 | Drug for treating tumor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103784470A true CN103784470A (en) | 2014-05-14 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210428754.8A Pending CN103784470A (en) | 2012-10-31 | 2012-10-31 | Drug for treating tumor |
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| Country | Link |
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| CN (1) | CN103784470A (en) |
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2012
- 2012-10-31 CN CN201210428754.8A patent/CN103784470A/en active Pending
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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Application publication date: 20140514 |