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Application of chidamide and derivatives thereof

A technology of chidamide and derivatives, applied in the field of chidamide and its derivatives, can solve the problems of reducing the sensitivity of radiotherapy, increasing tumors, reducing the continuous efficacy of radiotherapy, etc. The effect of tumor activity and excellent sustained curative effect

Pending Publication Date: 2021-05-04
SHENZHEN CHIPSCREEN BIOSCIENCES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, tumors can also evade radiotherapy-induced apoptosis through different mechanisms, resulting in treatment resistance, thereby reducing the sustained efficacy of radiotherapy.
Increasing the dose of radiotherapy can improve the curative effect, but it will bring more side effects. Therefore, it is very important to better realize the efficacy and safety of radiotherapy in clinical practice. Sensitivity or reducing its resistance are also potential development directions

Method used

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  • Application of chidamide and derivatives thereof
  • Application of chidamide and derivatives thereof
  • Application of chidamide and derivatives thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021]Example 1: Effects of comparative Sidaimide combined radiotherapy compared to two individual treatment of proliferation and apoptosis of tumor cell line cultured in vitro

[0022]Test Design: Sida-Dimin monohydrate, different dose radiation therapy, and both joint treatment were used in different in vitro cultured tumor cell lines, and the effects of different treatment methods on cell proliferation and apoptosis were investigated.

[0023]Test process: human lung cancer cell line NCI-H2170 and NCI-H226 were cultured in vitro in vitro according to the recommended culture conditions, and the control solvent dimethyl sulfoxide (1 / 1000), Sida-Dimin 300 nanomola, radiotherapy 1 Gori, 2 Gori, 4 Gori, or Sidim amine and different dose radiotherapy. After 24 hours, the amount of survivinal cells was detected using a conventional CCK-8 kit (Shanghai macro leaf), compared with the control solvent treatment, calculated the relative cell proliferation ratio of each treatment group. Such asfigu...

Embodiment 2

[0028]Example 2: Effect of Sidaimide combined radiotherapy compared to two individual treatment on tumor stem cell characteristics

[0029]Test Design: Tumor Production Resistance (including radiation therapy, chemotherapy, targeted treatment or immunotherapy, etc.) or recurrence is one of the stem cell characteristics, minority or even single tumor cells having stem cell characteristics, tumor cells with stem cell characteristics can be self-renewal. Proliferation and re-forming new tumors. Tumor stem cell characteristics can be evaluated by a single tumor cell in vitro to form clone-like (cell group) growth. In this experiment, under in vitro culture conditions, the effects of different treatment on the formation of tumor cell clones (cells) were investigated.

[0030]Test Process: Tumor cell line NCI-H2170 and NCI-H226 use low adsorption medium for suspension culture, using different treatment conditions, including solvent control (dimethyl sulfoxide 1 / 1000), and Sidaimide 300 nano, Ra...

Embodiment 3

[0032]Example 3: Comparison of the effects of Sidaimide combined radiotherapy relative two separate treatment on tumor growth of transplanted tumors

[0033]Test Design: Human source tumor cells are inoculated in nude mice to form tumor-type growth, and different experimental treatment is used to evaluate its effect on growth in tumors.

[0034]Test process: human tumor cell line NCI-H2170 is inoculated on both sides of Balb / C nude mice, 14 days after visible tumor formation and random packets, respectively gave Sidamine (20 mg / per kilogram of body weight, once daily, suspend Liquid sprouts), radiation therapy (2 Gori dose, once a week), Sida medide combined radiotherapy, or gastric solvent control. Continuous measurement of model mice weight and tumor volume, after six weeks of test, separating tumor weighed. The experiment mainly examines the effects of different experimental treatment on tumor size and weight. Such asFigure 7-8Indicated.

[0035]Test results:Figure 7 ,8As shown, Si Da...

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Abstract

The invention relates to the technical field of medicines, and discloses application of chidamide and derivatives thereof. The invention discloses that chidamide has an anti-tumor radiotherapy sensitization effect, chidamide is combined with radiotherapy to better inhibit tumor cell proliferation and induce cell apoptosis, stem cell characteristics of tumor cells are inhibited at the same time, and the combination of chidamide and radiotherapy shows a better tumor inhibition effect in animal bodies compared with independent treatment. Chidamide not only can enhance the tumor suppression activity of radiotherapy, but also can reduce the risk of generation of treatment resistance and relapse of tumors, and chidamide combined radiotherapy can provide a better continuous curative effect than single treatment.

Description

[0001]The present application claims the Chinese Patent Office on October 29, 2019, the application number is 201911039341.9, the invention is priority for Chinese patent applications in the present invention, and the entire contents are combined by reference This application is in this application.Technical field[0002]The present invention relates to the field of drug technology, and more particularly to the use of Sinaim amine and its derivatives.Background technique[0003]Radiation therapy is a common method of clinical tumor treatment, mainly for topical treatment using radiation (such as α, β, gamma rays, etc. produced by radioisotope). The basic principle of radiation therapy is to cause DNA damage by rays. For proliferating active tumor cells, DNA damage repair can not be effectively completed, resulting in cell apoptosis, achieving anti-tumor effect. The efficacy of radiotherapy depends on the sensitivity of tumor on radiation and the damage thereof. Different tumor types and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4406A61P35/00A61P35/02A61N5/06
CPCA61K31/4406A61P35/00A61P35/02A61N5/06
Inventor 黄旭鲁先平潘德思王绿化
Owner SHENZHEN CHIPSCREEN BIOSCIENCES CO LTD
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