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Application of tanshinone IIA as inhibitor for redox function of APE1 and application of tanshinone IIA in preparation of drugs used for treating cancers

A technology of tanshinone and inhibitor, applied in drug combination, antitumor drug, pharmaceutical formulation, etc., to achieve the effect of inhibiting proliferation, improving chemosensitivity, and less toxic and side effects

Inactive Publication Date: 2013-04-24
THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no research report on its selective inhibition of the redox function of APE1

Method used

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  • Application of tanshinone IIA as inhibitor for redox function of APE1 and application of tanshinone IIA in preparation of drugs used for treating cancers
  • Application of tanshinone IIA as inhibitor for redox function of APE1 and application of tanshinone IIA in preparation of drugs used for treating cancers
  • Application of tanshinone IIA as inhibitor for redox function of APE1 and application of tanshinone IIA in preparation of drugs used for treating cancers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The effect of embodiment 1 Tanshinone IIA on Hela cell proliferation

[0048] Inoculate Hela cells in a 96-well plate to make the cell density about 5000-10000 / well, fill the peripheral wells with 100 μL of PBS buffer, and the temperature is 37°C, CO 2 Under the conditions of 5% volume fraction and saturated humidity, cultivate for 24 hours;

[0049]Then take the cultured Hela cells and add tanshinone IIA solution with 5 drug concentration gradients respectively (so that the final concentration is 2nmol / mL, 4nmol / mL, 8nmol / mL, 16nmol / mL, 32nmol / mL in order of molar concentration) , set 5 duplicate wells for each concentration, and take 5 wells containing Hela cells but without adding tanshinone IIA solution as a control. 2 Incubate for 24 hours at a volume fraction of 5% and saturated humidity; take another two cultured Hela cells, do the same treatment, and culture for 48 hours and 72 hours respectively;

[0050] Then, 20 μL of MTT solution with a mass-volume concent...

Embodiment 2W

[0056] Example 2 Western Blot verification of endogenous APE1 protein knockdown and exogenous APE1 protein expression in three groups of Hela cell models

[0057] First, extract Hela cells, APE1 shRNA , APE1 wt and APE1 C65S For total cell protein, the specific operation is as follows: discard the cell culture supernatant, and then wash it twice with ice-cold PBS; add 150 μL of 1× protein loading buffer, and hang the adherent cells with a cell brush until the liquid becomes viscous; Take the viscous sample liquid into a clean 1.5mL centrifuge tube, ultrasonic 30pulse to lyse the nucleic acid until white bubbles are produced; the lysed liquid is placed on a dry thermostat for 5 minutes at a temperature of 100°C; the extracted sample is stored at -80 Store at ℃.

[0058] Then, prepare Western Blot electrophoresis gel, wherein, the lower gel consists of:

[0059]

[0060]

[0061] Prepared, after the lower layer of gel is coagulated, the concentrated gel is prepared, an...

Embodiment 3

[0069] Example 3 MTT experiment to investigate the effect of APE1 stable knockdown and APE1 redox deletion on the tumor killing effect of tanshinone IIA

[0070] APE1 wt , APE1 shRNA and APE1 C65S Cells were inoculated into 96-well plates at a density of 5,000-10,000 / well; the peripheral wells were filled with 100 μL of PBS; at 37°C, CO 2 The volume fraction is 5%, cultivated for 24 hours under saturated humidity;

[0071] in APE1 wt , APE1 shRNA and APE1 C65S Two tanshinone IIA solutions with drug concentration gradients were added to the cells (to make the final concentrations respectively 8 nmol / mL and 16 nmol / mL in terms of molar concentration), and 5 replicate wells were set up for each concentration. At 37°C, CO 2 The volume fraction was 5%, and cultured for 24 hours under saturated humidity.

[0072] Add 20 μL of MTT solution with a mass-volume concentration of 5 mg / mL to each well, and continue culturing for 4 hours; terminate the culture, and carefully suck of...

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Abstract

The invention relates to the technical field of natural drugs, especially to application of tanshinone IIA as an inhibitor for the redox function of APE1 and application of tanshinone IIA in preparation of drugs used for treating cancers. Tanshinone IIA can inhibit the redox function of APE1 and directly kill tumor cells through inhibition of the redox function of APE1; tanshinone IIA can also reverse overactivity of the redox function caused by high expression of APE1 in the tumor cells, inhibit propagation and infiltration of tumor cells, reverse anti-apoptosis of the tumor cells and prevent metastasis of the tumor cells; tanshinone IIA can further reverse drug resistance of the tumor cells to chemotherapeutics caused by high expression of APE1 in the tumor cells; moreover, while having anticancer and chemosensitization performances, tanshinone IIA has a usage and development potential due to small toxic and side effects.

Description

technical field [0001] The invention relates to the technical field of natural medicines, in particular to the application of tanshinone IIA as an inhibitor of APE1 redox function and its application in the preparation of medicines for treating cancer. Background technique [0002] With the improvement of living standards and the aggravation of environmental pollution, the incidence of malignant tumors has been increasing year by year. It has been clinically defined as a common disease and frequently-occurring disease, which seriously threatens human health. Apurinic aprimidinic endonuclease / Redox factor-1 (APE1 / Ref-1) is an example of a functional complex of biological macromolecules. On the one hand, APE1 has DNA repair activity, and it acts as an AP nucleic acid Endonuclease is one of the main rate-limiting enzymes in the DNA base excision repair (BER) pathway; on the other hand, APE1 can also regulate the DNA binding activity of key transcription factors through its uniq...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61P35/00A61P35/04
Inventor 隋江东王东李梦侠钱程远
Owner THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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