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Application of antagonist SR140333 of neurokinin receptor in hepatoma treatment

A technology of neurokinin and antagonist, applied in the field of treatment of liver cancer with neurokinin receptor antagonist SR140333, which can solve the problems of fast metabolism, low selectivity and weak effect

Inactive Publication Date: 2013-04-17
ZHEJIANG SCI-TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The first generation of antagonists starts with changing tachykinin amino acids, and substitutes D-amino acids to obtain some antagonistic polypeptides, but their effects are weak, their selectivity is low, and they have neurotoxicity and release histamine.
The second-generation antagonists are short peptide and cyclic peptide antagonists with high affinity and high selectivity obtained on the basis of shortening the peptide chain and chemical modification, but their oral bioavailability is low and metabolism is fast
However, the company has not carried out research on the anti-tumor effect of the organic small molecule, and there is no literature report that it has an anti-tumor effect

Method used

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  • Application of antagonist SR140333 of neurokinin receptor in hepatoma treatment
  • Application of antagonist SR140333 of neurokinin receptor in hepatoma treatment
  • Application of antagonist SR140333 of neurokinin receptor in hepatoma treatment

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Experimental program
Comparison scheme
Effect test

Embodiment

[0030] 1. Materials and methods

[0031] 1.1 Materials, instruments and reagents

[0032] 1.1.1 Cell lines and peptides

[0033] Human liver cancer Bel-7404 cells were purchased from the Tumor Cell Bank of the Chinese Academy of Medical Sciences. SR140333 was synthesized by WuXi AppTec.

[0034] 1.1.2 Main reagents

[0035]

[0036]

[0037] 1.1.3 Reagent preparation

[0038] Phosphate buffer saline (PBS): 8g sodium chloride, 0.2g potassium chloride, 2.9g disodium hydrogen phosphate, 0.2g potassium dihydrogen phosphate, 1L deionized water, store at 4°C.

[0039] SR140333 was first dissolved in DMSO, then added to PBS to make 9×10 -3 Mother liquor of M. The concentration of DMSO in the working solution is less than 1%. The prepared mother liquor was sterilized by filtration with a 0.22 μm filter membrane, then dispensed into 1.5 mL EP tubes, and stored separately at -20°C.

[0040] 1.2 Experimental method

[0041] 1.2.1 Cell culture

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Abstract

The invention relates to an anti-hepatoma effect of an antagonist SR140333 of a neurokinin receptor 1, in particular to a method for treating hepatoma of a subject, relieving a hepatoma symptom of the subject or inhibiting hepatoma cell proliferation, an application of the antagonist of the neurokinin receptor 1 in preparing medicine, an reagent or a medicine composition for treating the hepatoma, relieving the hepatoma symptom or inhibiting the hepatoma cell proliferation, and a pharmaceutical product. The pharmaceutical product comprises the antagonist SR140333 of the neurokinin receptor 1 as an active ingredient and a specification of the pharmaceutical product.

Description

technical field [0001] The present invention relates to the use of neurokinin receptor antagonist SR140333 in the treatment of liver cancer. Specifically, the present invention relates to: a method for treating liver cancer in a subject, relieving the symptoms of liver cancer in a subject, or inhibiting the proliferation of liver cancer cells; the neurokinin receptor antagonist SR140333 is used in the preparation for treating liver cancer, relieving symptoms of liver cancer or inhibiting Use in a drug, medicament or pharmaceutical composition for the proliferation of liver cancer cells; and a pharmaceutical product comprising neurokinin receptor antagonist SR140333 as an active ingredient and instructions related to the pharmaceutical product. Background technique [0002] Cancer is a kind of disease that seriously endangers human health. At present, the global cancer death toll is higher than the sum of the death toll from AIDS, tuberculosis and malaria, and it has become t...

Claims

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Application Information

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IPC IPC(8): A61K31/4545A61P35/00
Inventor 夏瑞龙付彩云张世馥赵辅昆朱晓翠陈麒
Owner ZHEJIANG SCI-TECH UNIV
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