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Antitumor drug prepared through combination of purine deoxynucleoside and other nucleosides or basic groups as well as preparation method and applications thereof

A technology of deoxypurine nucleoside and anti-tumor drug, which is applied in the field of new tumor drug development to achieve the effect of obvious anti-tumor effect, remarkable therapeutic effect and delaying tumor resistance

Inactive Publication Date: 2015-05-20
张始状
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the combination of normal deoxypurine nucleosides with other nucleosides or bases to prepare anti-tumor drugs has not been reported at home and abroad.

Method used

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  • Antitumor drug prepared through combination of purine deoxynucleoside and other nucleosides or basic groups as well as preparation method and applications thereof
  • Antitumor drug prepared through combination of purine deoxynucleoside and other nucleosides or basic groups as well as preparation method and applications thereof
  • Antitumor drug prepared through combination of purine deoxynucleoside and other nucleosides or basic groups as well as preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] 245 combination, 25 combination, 2145 combination tumor inhibition experiment, the specific experimental method is as follows:

[0095] 1. Inoculation of cells

[0096] Take Hela cells and 7402 cells in the logarithmic growth phase, digest with trypsin and dilute to (2.0-3.0)×104 / mL live cell suspension, inoculate 2-10 columns in a 96-well culture plate, each column Set up 6 duplicate wells, 100 μL per well, add 100 μL RPMI-1640 culture solution containing 10% fetal bovine serum to the 11th column, fill with 100 μL PBS around, and place at 37°C, 5% CO 2 Cultivate in the incubator for 24h.

[0097] 2. Dosing intervention

[0098] After the cells adhered to the wall, the culture medium in the well was discarded, and the 245 combination was added in order from large to small, the molar ratio of 2, 4, and 5 was 2:1:2, and the seven concentration gradients of the combined drug (C1~C7 ), the total concentrations are 2.0 mmol / L, 1.0 mmol / L, 0.5 mmol / L, 0.25 mmol / L, 0.125 mm...

Embodiment 2

[0119] The factorial design experiment of any three kinds of nucleoside combination antitumor in vitro, the specific experimental method is as follows:

[0120] 1. Inoculation of cells

[0121] See the "inoculation of cells" step in Example 1

[0122] 2. Dosing intervention

[0123] After the cells adhered to the wall, the culture medium in the well was discarded, and 1 (adenosine), 2 (deoxyadenosine), 3 (adenine), 4 (guanosine), and 5 (deoxyguanosine), 6 (guanine) six drugs and the combination of these six drugs with a molar ratio of 1:1:1 (123, 124, 125, 126, 134, 135, 136, 145, 146, 156 , 234, 235, 236, 245, 246, 256, 345, 346, 356, 456);

[0124] Use RPMI-1640 culture solution containing 10% fetal bovine serum to prepare the drug to the desired concentration, and add 200 μL to each well;

[0125] Add 200 μL of RPMI-1640 culture solution containing 10% fetal bovine serum to the blank control group and the negative control group, and place them at 37°C and 5% CO 2 cultu...

Embodiment 3

[0143] Orthogonal experimental design of the combination concentration ratio of deoxyadenosine-guanosine-deoxyguanosine (245), the specific experimental steps are as follows:

[0144] 1. Inoculation of cells

[0145] Take Hela cells and 7402 cells in the logarithmic growth phase, digest with trypsin and dilute to (2.0-3.0)×104 / mL live cell suspension, inoculate 2-10 columns in a 96-well culture plate, each column Set up 6 duplicate wells, 100 μL per well, add 100 μL RPMI-1640 culture solution containing 10% fetal bovine serum to the 11th column, fill with 100 μL PBS around, and place at 37°C, 5% CO 2 Cultivate in the incubator for 24h.

[0146] 2. Dosing intervention

[0147] After the cells adhered to the wall, the culture medium in the well was discarded, and the dosing scheme was as follows: the concentrations of 2 (deoxyadenosine), 4 (guanosine), and 5 (deoxyguanosine) were all 3 mmol / L, and the nine groups designed were respectively : The molar ratios of 2 (deoxyadenos...

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Abstract

The invention discloses an antitumor drug prepared through the combination of purine deoxynucleoside and other nucleosides or basic groups as well as a preparation method and applications thereof. The purine deoxynucleoside comprises deoxyadenosine and deoxyguanosine; and the other nucleosides or basic groups include deoxycytidine, thymidine, adenosine, guanosine, cytidine, uridine, adenine, guanine, cytosine, uracil, and thymine. The antitumor drug disclosed by the invention has the advantages that the purine deoxynucleoside and the other nucleosides or basic groups are all normal nucleosides of human bodies, the combination of purine deoxynucleoside as a main drug and other nucleosides or basic groups as an adjuvant is used for preparing a drug for treating various common malignant tumors such as gastric carcinoma, lung carcinoma, hepatic carcinoma, colorectal carcinoma, esophageal carcinoma, pancreatic carcinoma, breast carcinoma, genital system tumor, and the like, and the antitumor drug disclosed by the invention has the characteristics of broad-spectrum antitumor effect, low toxicity and new mechanism and the like; toxic and side effects caused by combined medication are reduced in comparison with single medication; the multiplicity of the antitumor effect is increased; and the occurrence of tumor drug-resistance can be delayed.

Description

technical field [0001] The present invention relates to the application of the combination of human normal deoxyadenosine and nucleoside or base in the preparation of tumor medicine, specifically combining one or both of deoxyadenosine and deoxyguanosine with nucleoside or base One or more combinations of these drugs are used to treat tumors, and the most classic is the combination of two deoxypurine nucleosides and one other nucleoside or base to prepare tumor drugs. It belongs to the field of tumor new drug development. Background technique [0002] Nucleosides are connected by bases and five-carbon sugars (ribose or deoxyribose), that is, N-9 of purine or N-1 of pyrimidine and C-1 of ribose or deoxyribose are connected by β-glycosidic bonds The compounds include ribonucleosides and deoxyribonucleosides. Ribonucleosides constitute RNA, mainly adenosine, guanosine, cytidine and uridine; deoxyribonucleosides (referred to as deoxynucleosides) constitute DNA, mainly Deoxyade...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/708A61K31/7076A61P35/00A61K31/52A61K31/522
CPCA61K9/0019A61K9/107A61K9/2059A61K31/7076A61K31/708A61K47/44A61K2300/00
Inventor 张始状韩明高志琴程鑫赵荣荣
Owner 张始状
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