Enhancer of anti-tumor drug and application of enhancer

An anti-tumor drug and enhancer technology, applied in the field of biomedicine, can solve problems such as unsatisfactory efficacy, unbearable patient suffering, heterogeneous reactions, etc., and achieve the effects of wide application, improved selectivity, and reduced toxicity

Active Publication Date: 2017-11-03
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, on the one hand, due to the complexity of cancer biological characteristics, traditional antineoplastic drugs are prone to drug resistance, and due to poor selectivity, often lead to the failure to achieve the expected curative effect, a...

Method used

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  • Enhancer of anti-tumor drug and application of enhancer
  • Enhancer of anti-tumor drug and application of enhancer
  • Enhancer of anti-tumor drug and application of enhancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Such as figure 2 , image 3 , Figure 5 As shown, the present embodiment 1 is to use the group without any treatment as a control group, 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydro Under the condition that the final concentration of pyrimidin-2-one is 75 μM, the changes of cell survival rate, intracellular calcium ion and total intracellular reactive oxygen species in different administration regimens. The preparation method of 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one is carefully packaged on a 4°C temperature control box Open it, add 1070.81 μL of anhydrous DMSO to the tube with a total mass of 10 mg to dissolve, and prepare a 30 mmol / L stock solution. Before adding the drug, dilute to 75 μM with DMEM culture solution containing 5% fetal bovine serum as needed to ensure DMSO does not exceed 0.5% by volume. The concentration of epirubicin in each culture system was 0.1 μM.

[0032] In terms of cell treatment, the cells i...

Embodiment 2

[0037] Such as Figure 4 As shown, in Example 2, the group without any treatment was used as the control group, and 600 μM of 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6 - Adding tetrahydropyrimidin-2-one into the culture system, the cell treatment, detection method, grouping and legend are the same as in Example 1. The survival rate of the two cell lines was detected by SRB method. Figure 4 In , we found that adding 600 μM 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one alone had an effect on three kinds of cells HepG2, The inhibition rates of SMMC7721 and L-02 were significantly increased. Although the survival rate of L-02 is still higher than that of the other two liver cancer cell lines, its average survival rate has dropped below 50%, even lower than that of epirubicin alone, which shows that 600 μM 1-(2- Hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one had a certain inhibitory effect on the proliferation of the three cell ...

Embodiment 3

[0039] Such as Figure 6 As shown, the cell treatment method of this Example 3 is the same as that of Examples 1 and 2, and the group without any treatment is used as a control group, and 300 μM of 1-(2-hydroxyphenyl)-4-(3-nitro Phenyl)-1,2,3,6-tetrahydropyrimidin-2-one was added to the culture system, and the survival rate of the two cell lines was detected by the SRB method. Such as Figure 6 As shown, in the case of 300 μM 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one alone, the drug The inhibitory effect on HepG2 cell proliferation was significantly higher than that on L02 cell proliferation (p<0.05). In the combined group, with the addition of 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one, human embryonic liver Although the survival rate of cell L-02 was higher than that of 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one alone decreased, but the survival rate was still higher than 50%, and its...

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Abstract

The invention provides an enhancer of a chemotherapeutic drug based on 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-ectoine-2-ketone, and aims to enhance a chemotherapeutic effect of an anti-tumor drug. Under the same anti-tumor action, the use amount of the anti-tumor drug is effectively reduced, or under the same using dosage, the toxic and side effects of pharmorubicin are effectively reduced; furthermore, the pharmorubicin enhancer based on1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-ectoine-2-ketone can selectively enhance the killing effect of pharmorubicin on tumor cells, and reduce the side effect on normal cells.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and more specifically relates to a 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidine-2- A ketone enhancer is used to improve the killing effect of antitumor drugs on cancer cells and its application. Background technique [0002] Chemotherapy of tumors is one of the main methods of current cancer treatment. Antitumor drugs are widely used in tumor chemotherapy because of their broad anticancer spectrum, strong antitumor effect and definite curative effect. However, on the one hand, due to the complexity of the biological characteristics of cancer, traditional antineoplastic drugs are prone to drug resistance, and due to poor selectivity, often lead to less than expected curative effect, and even severe heterogeneous reactions, such as myelosuppression, Cardiotoxicity makes patients miserable and even life-threatening; on the other hand, the adverse reactions of antineoplast...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61P35/00
CPCA61K31/513
Inventor 吴志刚吴文博
Owner HUAZHONG UNIV OF SCI & TECH
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