CN102028685A - Application of Gimeracil - Google Patents
Application of Gimeracil Download PDFInfo
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- CN102028685A CN102028685A CN2009100933953A CN200910093395A CN102028685A CN 102028685 A CN102028685 A CN 102028685A CN 2009100933953 A CN2009100933953 A CN 2009100933953A CN 200910093395 A CN200910093395 A CN 200910093395A CN 102028685 A CN102028685 A CN 102028685A
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- gimeracil
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Abstract
The invention discloses a new application of Gimeracil, which is characterized by an application of the Gimeracil in preparing antitumor drugs, wherein the drugs in unit dose form are prepared from the Gimeracil, and the unit dose is 1-500 mg. Pharmacological experiments indicate good antitumor activity of the Gimeracil.
Description
Technical field
The present invention relates to medical technical field, be specifically related to a kind of new purposes of Gimeracil.
Gimeracil antitumor action of the present invention is meant that Gimeracil directly acts on the antitumor action that tumor cell plays, do not comprise that Gimeracil is as biochemical regulator, be that Gimeracil is a liver dihydropyrimidine dehydrogenase inhibitor, can suppress the decomposition of 5-FU competitively, make 5-FU in blood plasma and tumor tissues, keep stable blood drug level to make it keep anti-tumor activity for more time.
Background technology
Gimeracil has another name called gimeracil, CDHP, chemical name: 5-chloro-2,4-dihydroxy-pyridine, English name: Gimeracil, molecular formula: C5H4C1N02, molecular weight: 145.55 CAS:103766-25-2; Gimeracil is a kind of composition in the compound recipe ftorafur capsule, and this medicine is developed by Japanese Taiho Pharmaceutical Co. Ltd, becomes to be grouped into this medicine gets permission to be used for gastric cancer and incidence cancer in Japan treatment for 3 kinds by ftorafur, Gimeracil and oxygen throat acid potassium.Ftorafur is the prodrug of 5-fluorouracil (5-FU), is converted into 5 one FU in vivo after taking and brings into play antitumor action.5 one FU are the choice drug of kinds of tumors such as gastrointestinal tract, clinical practice more than 40 year, but have the defective that the half-life is short, toxicity is big in the body; Add the people in this this product Gimeracil be biochemical regulator, Gimeracil is a liver dihydropyrimidine dehydrogenase inhibitor, can suppress the decomposition of 5-FU competitively, makes 5-FU keep stable blood drug level for more time in blood plasma and tumor tissues.In sum, traditional medicine thinks that Gimeracil itself does not have anti-tumor activity, just as the auxiliary element in the antitumor drug.
Summary of the invention
We find that unexpectedly Gimeracil has anti-tumor activity in clinical research, this activity could embody when using separately, and the Gimeracil antitumor action is very outstanding, can be used as antitumor drug and develops.
The present invention realizes by following proposal.
The application of Gimeracil in preparation antitumor action medicine.
Gimeracil antitumor action of the present invention is meant that Gimeracil directly acts on the antitumor action that tumor cell plays, do not comprise that Gimeracil is as biochemical regulator, be that Gimeracil is a liver dihydropyrimidine dehydrogenase inhibitor, can suppress the decomposition of 5-FU competitively, make 5-FU in blood plasma and tumor tissues, keep stable blood drug level to make it keep anti-tumor activity for more time.
Wherein Gimeracil is prepared into the medicine of unit dose.
Wherein unit dose is 1-500mg.
Wherein unit dose is 10-200mg.
Its Chinese medicine is oral formulations or ejection preparation.
The MTT reducing process detects the preparation anti-tumor activity test
Experiment material:
MTT: with phosphate buffer (PBS) the dissolving MTT final concentration 2.5mg/ml of 0.02mol/L, filtration sterilization, 5 ℃ keep in Dark Place after the packing.
The preparation of MTT lysate: the 80g dodecyl sodium sulfate is dissolved in the N-N-dimethyl methyl phthalein amine of 200ml, and the heating in water bath hydrotropy adds the 200ml distilled water, mixes with 1N hydrochloric acid (1: 1) with 80% acetic acid and transfers pH to 4.7.
Cell strain is selected for use: human normal cell line strain, human hepatoma cell strain, National People's Congress's sclc cell line, human pancreas cancer cell strain, human renal carcinoma cell strain, the strain of people's colon-cancer cell.
Experimental technique: single cell suspension is inoculated in 96 orifice plates (with the RPM-1640 basal medium with cell dilution to 30000/ml, every hole adds 200 μ l and dilutes good cell), cultivates 24 hours under 37 ℃, 5% carbon dioxide saturated humidity; Every group of four parallel samples; Remove culture medium, get new preparation culture medium and prepare cancer therapy drug (the application's preparation) solution by series concentration, every hole 20 μ l cultivated 48 hours; Every hole adds the MTT20 μ l of 2mg/ml, hatches 4 hours; Culture fluid in the sucking-off hole (as far as possible fully) adds DMSO liquid (150 μ l/ hole), vibrates 10 minutes, and crystal is fully dissolved; Microplate reader detects each hole OD value, (detecting wavelength 560nm); Draw the cell viability curve chart, obtain the IC50 value.Experimental result is as shown in table 1:
Table 1 cytotoxicity experiment result
Brief summary: Gimeracil of the present invention has stronger cell toxicant, and its toxicity has certain selectivity to normal cell and cancerous cell, and Gimeracil of the present invention can be used for making each antitumor drug.
Comparison to the rats'liver tumor suppression
Laboratory animal: rat, 150g-180g, male and female are regardless of.
Experiment medicine: normal saline; Gimeracil of the present invention; Sodium cantharidinate.
Experimental technique: get rat and be divided into normal saline group, sodium cantharidinate group, this Gimeracil group, make W
256Liver in inoculation, inoculate after 7 days, press the dosage intraperitoneal injection of anesthesia of 35mg/kg with pentobarbital sodium, fixing, cutting open the belly exposes liver, tumor surface maximum diameter (a) and path (b) are pressed (a*b on the measurement liver
2)/2=V (gross tumor volume).Separate stomach, arteria duodenalis, common hepatic artery and proper hepatic artery, ligation stomach, arteria duodenalis far-end, with silver brain clip blocking-up common hepatic artery, in sending into proper hepatic artery again at the gastroduodenal artery upper cut and after inserting external diameter 0.3mm conduit under the operating loupe, inject respectively by the experiment grouping then and be subjected to reagent thing (dosage is identical), postoperative tube drawing ligation gastroduodenal artery, decontrol the common hepatic artery silver brain clip, sew up the incision again, place animal housing to wait to revive rat, continue breeding observing, performed the operation back 8 days, detect gross tumor volume by last method, experimental result sees Table 2:
The rejection ratio of table 2 pair tumor
Annotate: compare * * P＜0.01 with the normal saline group; Compare #P＜0.05 with positive sodium cantharidinate group
Method according to existing document realizes that to pancreas tumor, intestinal canal tumour, lung tumor we find that Gimeracil all has favorable anti-tumor effect.
Above-mentioned experiment shows that Gimeracil has good antitumor activity.
Embodiment
Embodiment 1
The application of Gimeracil in preparation antitumor action medicine.
Embodiment 2
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 1mg.
Embodiment 3
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 500mg.
Embodiment 4
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 250mg.
Embodiment 5
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 10mg.
Embodiment 6
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 200mg.
Embodiment 7
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 100mg.
Embodiment 8
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 5mg.
Embodiment 9
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 15mg.
Embodiment 10
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 40mg.
Embodiment 11
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 95mg.
Embodiment 12
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 145mg.
Embodiment 13
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 295mg.
Embodiment 14
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 375mg.
Embodiment 15
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 425mg.
Embodiment 16
The application of Gimeracil in preparation antitumor action medicine, wherein Gimeracil is prepared into the pharmaceutical preparation of unit dose, and wherein the Gimeracil of unit dose is 495mg.
Claims (5)
1. the application of Gimeracil in preparation antitumor action medicine.
2. application according to claim 1, wherein Gimeracil is prepared into the medicine of unit dose.
3. application according to claim 2, wherein unit dose is 1-500mg.
4. application according to claim 2, wherein unit dose is 10-200mg.
5. application according to claim 2, its Chinese medicine are oral formulations or ejection preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100933953A CN102028685A (en) | 2009-09-29 | 2009-09-29 | Application of Gimeracil |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100933953A CN102028685A (en) | 2009-09-29 | 2009-09-29 | Application of Gimeracil |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102028685A true CN102028685A (en) | 2011-04-27 |
Family
ID=43882495
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009100933953A Pending CN102028685A (en) | 2009-09-29 | 2009-09-29 | Application of Gimeracil |
Country Status (1)
| Country | Link |
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| CN (1) | CN102028685A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106692173A (en) * | 2015-11-18 | 2017-05-24 | 北京诺普德医药科技有限公司 | Anti-tumor compound composition and applications thereof |
| WO2018121669A1 (en) * | 2016-12-30 | 2018-07-05 | 陈晓华 | Pharmaceutical composition for treating cancer and use thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660105A (en) * | 2004-12-23 | 2005-08-31 | 鲁南制药股份有限公司 | Disintegration piece taken through oral cavity containing Gimeracil and Oteracil Potassium with fluorine being added |
-
2009
- 2009-09-29 CN CN2009100933953A patent/CN102028685A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660105A (en) * | 2004-12-23 | 2005-08-31 | 鲁南制药股份有限公司 | Disintegration piece taken through oral cavity containing Gimeracil and Oteracil Potassium with fluorine being added |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106692173A (en) * | 2015-11-18 | 2017-05-24 | 北京诺普德医药科技有限公司 | Anti-tumor compound composition and applications thereof |
| WO2018121669A1 (en) * | 2016-12-30 | 2018-07-05 | 陈晓华 | Pharmaceutical composition for treating cancer and use thereof |
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| PB01 | Publication | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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Application publication date: 20110427 |