Radiation sensitivity enhancing composition containing aripiprazole as active ingredient

An aripiprazole and active ingredient technology, applied in the directions of organic active ingredients, medical preparations containing active ingredients, and radiosensitizing materials, can solve the problem of unclear radiosensitization effect of aripiprazole, research, and pharmacological effects. Issues such as limited research

Active Publication Date: 2020-12-11
KOREA INST OF RADIOLOGICAL & MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the research on the pharmacological effects of aripiprazole on the central nervous system and nervous system diseases is limited, and its technical research only focuses on improving the solubility and absorption rate of the drug. Clearly, there is no research on this

Method used

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  • Radiation sensitivity enhancing composition containing aripiprazole as active ingredient
  • Radiation sensitivity enhancing composition containing aripiprazole as active ingredient
  • Radiation sensitivity enhancing composition containing aripiprazole as active ingredient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Detection of radiosensitive reagents in breast cancer cells

[0044] No cytotoxicity was observed in a single treatment in radiation-resistant breast cancer cells, but a radiosensitizer drug candidate in combination with radiation therapy to enhance radiation sensitivity was identified in Enzo's drug library.

[0045] MCF-7 cells (human breast cancer cell line) were adjusted to a concentration of 5000 cells / well, then seeded into 96-well plates, and pre-cultured for 24 hours. Subsequently, the medium was removed and the drugs in Enzo's drug library were treated alone or in combination with radiation at a concentration of 5 mM each. After 96 hours, the cell viability was measured with Dogen's EZ-Cytox Cell Viability Assay Kit.

[0046] Such as figure 1 As shown, aripiprazole was identified as a radiosensitizer, and although drug treatment alone had no effect on cell viability, when combined with radiation, aripiprazole reduced the viability of radioresistant cells.

Embodiment 2

[0047] Effect of Aripiprazole on the Radiation Sensitivity of Cancer Cells

[0048] In order to confirm the effect of aripiprazole on the radiosensitivity of cancer cells, a cell viability assay experiment was carried out on radioresistant breast cancer cells using MTT colorimetry as follows.

[0049] After the MCF-7 cells were adjusted to a concentration of 5000 cells / well, they were inoculated into 96-well plates and pre-cultured for 24 hours. Then, the medium was removed and aripiprazole (5 μM, 10 μM, 20 μM) was treated alone or in combination with radiation. After 96 hours, the cell viability was measured with Dogen's EZ-Cytox Cell Viability Assay Kit.

[0050] Such as figure 2 As shown, it was found that when combined with radiation, the survival rate reduction effect was superior to that of aripiprazole alone. Aripiprazole was found to have an excellent radiosensitizing effect in a concentration-dependent manner.

Embodiment 3

[0051] Effect of Aripiprazole on Radiation-Induced Apoptosis in Cancer Cells

[0052] It has recently been reported that aripiprazole can induce apoptosis in cancer cells. In order to confirm the effect of aripiprazole on radiation-induced apoptosis in cancer cells, PARP cleavage and DNA fragmentation assays were performed on cancer cells as follows .

[0053] MCF-7 cells were treated with aripiprazole (1 μM, 5 μM, 10 μM, 20 μM) alone or in combination with radiation. After 24 hr, after washing with PBS, proteins were extracted from the cells, and the extent of PARP cleavage was confirmed by western blotting.

[0054] Such as image 3 As shown, it was found that when combined with radiation, the PARP cleavage-inducing effect was superior to that of aripiprazole alone. Aripiprazole was found to induce apoptosis in irradiated cancer cells in a concentration-dependent manner.

[0055] After adjusting the concentration of MCF-7 cells or U251 cells to 5000 cells / well, they wer...

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Abstract

The present invention pertains to a radiation sensitivity enhancing composition containing aripiprazole as an active ingredient, and more particularly, to a radiation sensitivity enhancing compositionthat can treat cancer with aripiprazole acting as a radiation sensitizer when used in combination with radiation therapy. Administrating an effective amount of aripiprazole according to the present invention in combination with radiation therapy has excellent radiation sensitivity enhancing effects, such as reducing cancer cell viability and inducing cancer cell death, and the present invention can therefore be usefully used as a radiation sensitivity enhancer.

Description

technical field [0001] The present invention relates to a composition for enhancing radiation sensitivity comprising aripiprazole as an active ingredient, and more particularly, to a composition capable of treating cancer as a radiosensitizer when aripiprazole is combined with radiation Compositions for enhancing radiation sensitivity. Background technique [0002] Cancer therapy can be broadly divided into surgery, radiation therapy, and chemotherapy. The importance of radiation therapy in cancer treatment is increasing as the number of cancer patients receiving radiation therapy is increasing year by year worldwide, but the therapy is accompanied by side effects that reduce the efficiency of treatment, such as acquiring cancer cells during high-dose radiation therapy radiation resistance and damage to normal tissues. In order to reduce the side effects of radiation and overcome resistance therein, radiosensitizers that increase the anticancer effect of radiation when adm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/546A61K31/4515A61K31/496A61P43/00A23L33/10A61K31/5415A61P35/00
CPCA61K31/5415A61P43/00A61K31/4515A61P35/00A23L33/10A61K31/496A61K45/06A61K2300/00A23L33/40A23V2002/00A61K9/0056A61K41/0038
Inventor 任荣彬朴明眞李炫知
Owner KOREA INST OF RADIOLOGICAL & MEDICAL SCI
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