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Application of compound NZ001 to preparation of preparation used for resisting metastasis of hepatocellular carcinoma

An anti-liver cancer and compound technology, applied in the field of preparation of anti-liver cancer metastasis preparations, can solve the problem of prolonging less than 3 months, and achieve the goal of inhibiting lung metastasis and intrahepatic spread, inhibiting intrahepatic spread, and inhibiting tumor formation and growth. Effect

Inactive Publication Date: 2018-03-06
AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sorafenib is currently the only small-molecule targeted therapy drug for the treatment of liver cancer on the market, with anti-angiogenic therapy as the main mechanism. The extension of the value is less than 3 months, and studies have shown that such molecular targeted drugs have side effects such as promoting tumor metastasis while inhibiting tumor growth. Drugs have important scientific significance and practical application value to further prolong the survival of patients, especially the survival of advanced patients, and improve the prognosis of patients

Method used

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  • Application of compound NZ001 to preparation of preparation used for resisting metastasis of hepatocellular carcinoma
  • Application of compound NZ001 to preparation of preparation used for resisting metastasis of hepatocellular carcinoma
  • Application of compound NZ001 to preparation of preparation used for resisting metastasis of hepatocellular carcinoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 in vitro cell experiment

[0038] 1) Cell proliferation experiment:

[0039] ① Digest liver cancer cells in the logarithmic growth phase with trypsin, resuspend the cells in fresh DMEM culture medium and count them to adjust to 10 4 cells / ml;

[0040] ② Inoculate the cell suspension in a 96-well cell culture plate, 100 μl / well, and culture in a cell incubator;

[0041] ③ Add different concentrations of NZ001 12 hours after cell inoculation;

[0042] ④Take out the 96-well plate at 72 hours, add CCK-8 solution, 100 μl / well, and place in an incubator at 37°C in the dark for 1.5 hours;

[0043] ⑤Measure the OD value with the excitation wavelength of 450nm, and conduct statistical analysis on the results.

[0044] 2) Apoptosis assay:

[0045] ①The adherent cells were digested and collected with EDTA-free trypsin (Note: Trypsinization time should not be too long, otherwise it is easy to cause false positive);

[0046] ② Wash the cells twice with PBS (centri...

Embodiment 2

[0064] Embodiment 2 animal experiments

[0065] 1) Establish animal intervention models and methods

[0066] Mouse feeding: 4-6 weeks C57BL / 6 and BALB / c nu / nu mice were raised at SPF level in an animal room with a room temperature of 22°C and a relative humidity of 55%. They were fed with common rodent diet and free to eat and drink ;

[0067] Subcutaneous tumor: After 1 week of adaptive feeding, the MHCC97H and Huh7 cells in the logarithmic growth phase were taken respectively, digested with 0.25% trypsin / 0.25% EDTA, and made into a single cell suspension, press 10 8 cells / ml, according to the injection of 100ul cell suspension per mouse, subcutaneously inject on the back side of the abdominal wall of nude mice, and the tumor grows to about 50mm after 2 weeks of tumor formation 2 , the mice were randomly grouped and drug intervention was performed for 2 weeks. After 2 weeks, the nude mice were killed by neck dislocation, and the tumors were excised and fixed in 10% neutral...

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PUM

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Abstract

The invention belongs to the field of compounds and relates to the use of compound NZ001 in liver cancer metastasis. The present invention proves through in vitro and in vivo experiments that the compound NZ001 (C34H30F2N4O6S) can inhibit the proliferation of highly metastatic liver cancer cells, promote apoptosis and inhibit cycle, inhibit tumor angiogenesis, and inhibit intrapulmonary metastasis and intrahepatic dissemination of tumors. The present invention has been tested, and the results have confirmed the important role of simultaneous inhibition of MET and VEGFR2 signaling pathways in the treatment of liver cancer metastasis, and provide new targets and ideas for clinical treatment of liver cancer metastasis.

Description

technical field [0001] The invention belongs to the field of compounds and relates to compound NZ001(C 34 h 30 f 2 N 4 o 6 S) New medicinal use, specifically related to compound NZ001 (C 34 h 30 f 2 N 4 o 6 S) Use in the preparation of anti-hepatoma metastasis preparations. Background technique [0002] Data show that hepatocellular carcinoma (hepatocellular carcinoma, HCC) is one of the most common and most malignant tumors in the world, and its mortality rate ranks second and sixth among male and female cancer patients in the world, respectively. Relevant statistics show that the number of HCC deaths in China accounts for 50% of the global total each year, and HCC has become one of the major malignant tumors that seriously threaten the lives and health of our people. [0003] Clinical practice shows that the majority of HCC patients fail to detect, diagnose and treat early, and the high rate of metastasis and recurrence after HCC surgery leads to poor overall pro...

Claims

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Application Information

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IPC IPC(8): A61K31/00A61P35/00A61P35/04
CPCA61K31/00
Inventor 钦伦秀朱克近张钰
Owner AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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