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Applications of phosphodiesterase 4 inhibitor ZL-n-91 in preparation of medicines preventing lung cancer proliferation and metastasis

A phosphodiesterase, anti-metastasis technology of lung cancer, applied in the field of tumor biology, can solve the problems of poor prognosis and survival rate of less than 15%, achieve the effects of inhibiting proliferation and metastasis, high selectivity, and good development and application prospects

Active Publication Date: 2017-08-15
GUANGZHOU HUAZHEN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although modern medical research has made great progress, lung cancer has made some progress in radiotherapy, chemotherapy, and surgical treatment, but the overall prognosis is poor, and the 5-year survival rate is less than 15%.
In fact, with most PDE4 inhibitors, the side effect of vomiting is common at high doses

Method used

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  • Applications of phosphodiesterase 4 inhibitor ZL-n-91 in preparation of medicines preventing lung cancer proliferation and metastasis
  • Applications of phosphodiesterase 4 inhibitor ZL-n-91 in preparation of medicines preventing lung cancer proliferation and metastasis
  • Applications of phosphodiesterase 4 inhibitor ZL-n-91 in preparation of medicines preventing lung cancer proliferation and metastasis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: The effect of ZL-n-91 on the proliferation of lung cancer cells was detected by CCK8 method.

[0026] 1) Take the cells in the logarithmic growth phase (A549 and LLC respectively) and prepare a single cell suspension. 100ul cell suspension per well (containing 1×10 4 cells) were inoculated in a 96-well plate, and were divided into 5 groups, blank control group, DMSO group, 10uM, 50uM, 100uM, and 200uM groups, with 6 replicate wells in each group, and the cells were pre-cultured for 24 hours (at 37°C, 5%CO 2 Under conditions);

[0027] 2) Replace the fresh medium, add different concentrations of ZL-n-91 to each group, and continue to culture the cells for 24 hours and 48 hours respectively (at 37 ° C, 5% CO 2 Under conditions);

[0028] 3) Add 100ul of 10% CCK-8 solution to each well to avoid bubbles;

[0029] 4) Continue to incubate the cells for 1-2 hours, take out the culture plate at 30 min, 60 min, and 90 min respectively, and measure the absorbance ...

Embodiment 2

[0031] Example 2: Effect of ZL-n-91 on LLC migration ability of mouse lung cancer cells.

[0032] 1) Take the cells in the logarithmic growth phase and make a suspension with serum-free DMEM medium. 100ul cell suspension (containing 5×10 4 cells) were seeded in transwell chambers. Divided into 3 groups: blank control group, 50uM, 100uM groups, each group set up 3 duplicate holes, and given different concentrations of drug treatment;

[0033]2) Add 10% FBS complete DMEM medium to the lower chamber of the 12-well plate, and then put it into the small chamber;

[0034] 3) After 24 hours, take out the small chamber, place it in ice methanol for 30 minutes, and let it dry naturally at room temperature;

[0035] 4) Add 600 ul of 0.1% crystal violet solution to the 12-well plate and soak the lower surface of the chamber for 15 minutes to stain the cells in purple;

[0036] 5) Add PBS, suck out the PBS after 5 minutes, and gently wipe off the cells in the small chamber with a clea...

Embodiment 3

[0041] Example 3: The curative effect of ZL-n-91 on mice with lung cancer.

[0042] 1) Take LLC lung cancer cells and place them in 5% CO 2 , 37°C, cultivated in an incubator with saturated humidity, collected well-growing cells in logarithmic phase, diluted with 1×PBS, and adjusted the concentration to 1.67×10 6 / ml;

[0043] 2) Use a 1ml sterile syringe to inoculate 0.3ml of the prepared cell suspension into the tail vein of wild-type C57BL6 mice;

[0044] 3) The mice were given drug treatment 3 days after inoculation.

[0045] 4) Solvent preparation: 40% hydroxypropyl-β-cyclodextrin and 6% polyethyl alcohol stearate 15 were dissolved in normal saline;

[0046] 5) Dissolve 10mg, 20mg, and 40mg of ZL-n-91 in 10ml of the above solvent, vortex and mix well, and prepare three doses of 5mg / kg, 10mg / kg, and 20mg / kg;

[0047] 6) Take 100ul of the solvent and the above-mentioned three concentrations of drugs and give each group of mice a daily gavage, observe and record the surv...

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Abstract

The invention discloses applications of a novel phosphodiesterase 4 (PDE4) inhibitor ZL-n-91 in preparation of medicines preventing lung cancer proliferation and metastasis. A survivorship curve and in-vitro cell experiments of mice prove that the phosphodiesterase 4 inhibitor ZL-n-91 can significantly inhibit lung cancer cell proliferation and metastasis, indicating that the phosphodiesterase 4 inhibitor ZL-n-91 is expected to be an important target in lung cancer proliferation and metastasis preventing researches, and providing bases for preparing medicines preventing lung cancer proliferation and metastasis. The phosphodiesterase 4 inhibitor ZL-n-91 has a good application prospect.

Description

technical field [0001] The invention relates to the application of a phosphodiesterase 4 inhibitor, in particular to the application of a phosphodiesterase 4 inhibitor ZL-n-91, which belongs to the field of tumor biology. Background technique [0002] Cancer has become an important cause of human death, among which lung cancer is one of the malignant tumors with the fastest-growing morbidity and mortality and the greatest threat to human health and life. Lung cancer is the second most common cancer among men in the world. In 2012 alone, almost 1.6 million people died of lung cancer in the world, of which China accounted for more than 1 / 3 of such cases. Lung cancer is the most common cancer in Chinese men, and 80%-85% of them are non-small cell lung cancer (NSCLC). The traditional treatment methods for lung cancer include local treatment (including surgery, radiotherapy, etc.) and systemic treatment (including traditional chemotherapy, molecular targeted drug therapy, etc.)....

Claims

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Application Information

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IPC IPC(8): A61K31/341A61P35/00A61P35/04
CPCA61K31/341A61P35/04A61K9/0019A61K47/10A61K47/40
Inventor 赵子建巩思嘉林艳李芳红李晓曦
Owner GUANGZHOU HUAZHEN PHARM CO LTD
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