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Application of three anthraquinone substances of targeted mitochondria as nasopharyngeal darcinoma radiosensitizers

A radiation sensitizer and anthraquinone technology, applied to medical preparations containing active ingredients, wave energy or particle radiation treatment materials, pharmaceutical formulations, etc., to reduce transmembrane potential, improve efficacy, and increase sensitivity

Inactive Publication Date: 2013-03-20
侯华新 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these three compounds have not been reported as radiosensitizers of nasopharyngeal carcinoma mediated by mitochondria

Method used

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  • Application of three anthraquinone substances of targeted mitochondria as nasopharyngeal darcinoma radiosensitizers
  • Application of three anthraquinone substances of targeted mitochondria as nasopharyngeal darcinoma radiosensitizers
  • Application of three anthraquinone substances of targeted mitochondria as nasopharyngeal darcinoma radiosensitizers

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Experimental program
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Effect test

Embodiment Construction

[0020] 1. Three anthraquinone compounds inhibit the growth of nasopharyngeal carcinoma cells:

[0021] Take the nasopharyngeal carcinoma cells CNE-1 in logarithmic growth phase, trypsinize and suspend them evenly, adjust the cell concentration to 1×10 5 / ml, add to 96-well plate, 100μl per well, 37℃5% CO 2 After culturing overnight in the incubator, the experimental groups were added with different concentrations of anthraquinone compounds, each group had 3 parallel holes, and the blank control was added with equal volume of PBS. After culturing for 24 hours, add 20μl of 5mg / ml MTT to each well, 37℃, 5% CO 2 After 4h incubation in the incubator, discard the supernatant, add 200μl dimethyl sulfoxide, and measure the absorbance A value at 490nm. Calculate the growth inhibition rate (IR) according to the following formula, plot the IR vs. concentration, and find the half inhibitory concentration IC 50 . The results are shown in Table 1.

[0022]

[0023] Table 1 Anthraquinone compoun...

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Abstract

The invention provides three compounds which have structural characteristics of anthraquinone substances and exert the radiosensitization by taking mitochondria as a target point, namely 1,8-dihydroxy-3-acetyl-6-methyl-9,10 anthraquinone, 1,8-dihydroxy-3-methoxy-6-methyl-9,10 anthraquinone and 1,3,8-trimethoxy-6-methyl-9,10 anthraquinon. The compounds can be gathered on the mitochondria of a cell and have a certain function of growth inhibition for nasopharyngeal darcinoma CNE-1. When the compounds without cytotoxic concentration are combined with a low-dose ray, the sensitiveness of a nasopharyngeal darcinoma cell to the ray can be improved, the transmembrane potential of the cell mitochondria is reduced and mitochondrial cristae is promoted to swell, generate vacuolation and appear oncosis characteristics, thereby the effect of radiation therapy is improved.

Description

Technical field [0001] The present invention relates to three anthraquinone compounds and the new use of these compounds as mitochondrial-mediated radiosensitizers for nasopharyngeal carcinoma. Background technique [0002] Nasopharyngeal cancer is one of the high-incidence tumors in southern my country. About 70% of nasopharyngeal cancer patients need radiotherapy during treatment, and about 40% of patients can be treated with radiotherapy. The role and status of radiotherapy in the treatment of nasopharyngeal carcinoma have become increasingly prominent. However, due to the biological characteristics of tumor cells and local microenvironment and other factors, the efficacy of radiotherapy is often unsatisfactory. 100% of patients receiving radiotherapy require adjuvant radiosensitization therapy. In recent years, despite the continuous improvement of radiotherapy technology, the best 5-year survival rate of nasopharyngeal carcinoma patients still stays at 30%-50%, and the loca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K41/00
Inventor 侯华新黎丹戎
Owner 侯华新