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

A technology of radiosensitizers and anthraquinones, applied in medical preparations containing active ingredients, wave energy or particle radiation treatment materials, pharmaceutical formulations, etc., to achieve the effect of improving the effect, increasing the sensitivity, and reducing the transmembrane potential

Inactive Publication Date: 2012-02-29
侯华新 +1
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  • 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. The inhibitory effect of three anthraquinone compounds on the growth of nasopharyngeal carcinoma cells:

[0021] Nasopharyngeal carcinoma cells CNE-1 in the logarithmic growth phase were collected, digested with trypsin and suspended evenly, and the cell concentration was adjusted to 1×10 5 / ml, add to 96-well plate, 100μl per well, 37℃5%CO 2 Cultivate overnight in an incubator, add different concentrations of anthraquinone compounds to the experimental groups, set 3 parallel wells in each group, and add an equal volume of PBS to the blank control. After continuing to culture for 24h, add 20μl of 5mg / ml MTT to each well, 37℃, 5%CO 2 After incubating in the incubator for 4 hours, discard the supernatant, add 200 μl dimethyl sulfoxide, and measure the absorbance A value at 490 nm. Calculate the growth inhibition rate (IR) according to the following formula, plot the IR against the concentration, and calculate the half inhibitory concentration IC 50 . The results ar...

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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 celland 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 kinds of anthraquinone compounds and the new application of these compounds as radiation sensitizers of nasopharyngeal carcinoma mediated by mitochondria. Background technique [0002] Nasopharyngeal carcinoma is one of the high-incidence tumors in southern my country. About 70% of nasopharyngeal carcinoma patients need radiotherapy during treatment, and about 40% of patients can be cured with radiotherapy. The role and status of radiotherapy in the treatment of nasopharyngeal carcinoma has become increasingly prominent. However, due to factors such as the biological characteristics of tumor cells and the local microenvironment, the curative effect of radiotherapy is often unsatisfactory, and 100% of patients receiving radiotherapy need adjuvant radiosensitization therapy. In recent years, despite the continuous improvement of radiotherapy techniques, the best 5-year survival rate of nasopharyngeal carcinoma pati...

Claims

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Application Information

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