Application of phosphodiesterase4 inhibitor ZL-n-91 in preparing medicine for treating prostate cancer proliferation and transfer

A phosphodiesterase, prostate cancer technology, applied in the field of tumor biology, to achieve the effect of inhibiting proliferation and migration, high selectivity, and good development and application prospects

Active Publication Date: 2018-02-23
SHENZHEN HANHUI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In fact, with most PDE4 inhibitors, the side effect of vomiting is common at high doses

Method used

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  • Application of phosphodiesterase4 inhibitor ZL-n-91 in preparing medicine for treating prostate cancer proliferation and transfer
  • Application of phosphodiesterase4 inhibitor ZL-n-91 in preparing medicine for treating prostate cancer proliferation and transfer
  • Application of phosphodiesterase4 inhibitor ZL-n-91 in preparing medicine for treating prostate cancer proliferation and transfer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: The effect of ZL-n-91 on the proliferation of prostate cancer cells was detected by CCK8 method.

[0027] 1) Take PC-3 cells in logarithmic growth phase and prepare 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, 10uM, 50uM, 100uM, and 200uM groups, with 6 duplicate holes in each group, and the cells were pre-cultured for 24 hours (at 37 ° C, 5% CO 2 Under conditions);

[0028] 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);

[0029] 3) Add 100ul of 10% CCK-8 solution to each well to avoid bubbles;

[0030] 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 at 450 nm with a microplate reader.

...

Embodiment 2

[0032] Example 2: Treatment of nude mice with subcutaneous PC-3 tumors.

[0033] 1) Take the PC-3 cells in the logarithmic growth phase, prepare a single cell suspension with serum-free F-12K medium, and use 120ul cell suspension per tube (containing 2×10 6 cells) in 1.5ml EP tubes;

[0034] 2) Draw 0.1ml of the prepared cell suspension with a 1ml sterile syringe and inoculate it subcutaneously in nude mice;

[0035] 3) The mice were given drug treatment 3 days after inoculation.

[0036] 4) Divide nude mice into two groups: solvent control group and administration group (10mg / kg), intragastric administration of drug treatment every day, and measure subcutaneous tumor volume and mouse body weight of nude mice twice a week;

[0037] 5) When the mouse tumor volume reaches 1500mm 3 , the mouse tumors were taken out, the tumor sizes were compared, and the tumor weights were recorded.

[0038] The result is as figure 2 showed that the administration of drug treatment had no eff...

experiment example 3

[0039] Experimental Example 3: ZL-n-91 inhibits the expression of Ki-67 in transplanted tumor tissues.

[0040] The tumor tissues mentioned above were taken, fixed overnight with 4% formalin, embedded in paraffin and sectioned for tumor proliferation antigen Ki67 staining.

[0041] The result is as Figure 5 As shown, the positive rate of Ki67 staining of the tumor tissue in the administration group was significantly lower than that in the blank group, indicating that the proliferation of tumor cells in the administration group was reduced.

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PUM

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Abstract

The invention discloses application of a phosphodiesterase4 (PDE4) inhibitor ZL-n-91 in preparing medicine for treating prostate cancer proliferation and transfer. Animal experiments and cytology experiments of mice are utilized to show that the phosphodiesterase4 inhibitor ZL-n-91 disclosed by the invention can obviously inhibit prostate cancer cell proliferation and transfer, so that the phosphodiesterase4 inhibitor ZL-n-91 is indicated to hopefully become an important target of prostate cancer proliferation and transfer researches, a foundation is provided for preparing medicine for resisting prostate cancer proliferation and transfer, and the phosphodiesterase4 inhibitor ZL-n-91 has a good development and 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] Prostate cancer is the most common malignant tumor in men in European and American countries. Its incidence rate ranks first in male malignant tumors in the United States, and its mortality rate is second only to lung cancer. In recent years, the incidence of prostate cancer in my country has also shown an increasing trend year by year, and the histological malignancy of prostate cancer is higher than that of American patients. According to the survey on the relative survival rate of patients with malignant urological tumors in Shanghai, China, 80.0% to 90.0% of patients in China have advanced prostate cancer when they see a doctor, and the 5-year survival rate is less than 30%. Due to the large population base in our country ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/341A61P35/00A61P35/04
CPCA61K31/341A61P35/04A61P35/00A61K9/0019A61K9/0053A61K9/0073
Inventor 赵子建巩思嘉林艳李芳红李晓曦周素谨赵正刚
Owner SHENZHEN HANHUI PHARM TECH CO LTD
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