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Application of 4-hydroxy salicylamide in preparing medicament for preventing and treating hepatitis and resisting tumor

A technology of hydroxysalicylanilide and antineoplastic drugs, applied in the field of application of 4-hydroxysalicylanilide in the preparation of anti-hepatitis and antineoplastic drugs, which can solve problems such as lowering blood cholesterol

Active Publication Date: 2012-03-21
ZHEJIANG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, it has the effect of lowering blood cholesterol

Method used

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  • Application of 4-hydroxy salicylamide in preparing medicament for preventing and treating hepatitis and resisting tumor
  • Application of 4-hydroxy salicylamide in preparing medicament for preventing and treating hepatitis and resisting tumor
  • Application of 4-hydroxy salicylamide in preparing medicament for preventing and treating hepatitis and resisting tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: the recombinant RR enzyme inhibitory activity of medicine

[0037] 1. Experimental materials

[0038] (1) Main reagents: hydroxyurea (Hydroxyurea, HU, Sigma), 4-hydroxysalicylanilide (Shanghai Titan Chemical Co., Ltd.).

[0039] (2) Main instruments: high performance liquid phase analyzer (Shimadzu LC-10ATVP), liquid scintillation counter (Backman LS6500).

[0040] 2. Experimental method

[0041] (1) Sample preparation for recombinant RR enzyme activity assay

[0042] 1) Preparation of reaction samples: Escherichia coli expressed in vitro the purified recombinant human RR enzyme large subunit M1 (see SEQ ID NO.1 for the sequence) and small subunit M2 protein (see SEQ ID NO.2 for the sequence) (the amount of protein used was RR enzyme activity reaches 65-95%), add double-distilled water to adjust the volume to 80 μl, add 10 μl of test compounds of different concentrations; mix well, and incubate at room temperature for 30-60 minutes;

[0043]2) Add reac...

Embodiment 2

[0052] Embodiment 2: the determination of drug test dosage

[0053] 1. Experimental materials

[0054] (1) Cell line: HepG2.2.15 cells (stably transfected with HBV gene, capable of stably replicating and expressing HBV genome) (gifted by Institute of Infectious Diseases, Zhejiang University).

[0055] (2) Main reagents: DMEM medium (Gibco, USA), fetal bovine serum (Gibco, USA), hydroxyurea (Hydroxyurea, HU, Sigma), 4-hydroxy salicylanilide (Shanghai Titan Chemical Co., Ltd.), pull Mivudine (Lamivudine, 3-TC, Tokyo Ninsei Industry Co., Ltd., Japan); Cell Counting Kit-8 kit (CCK8, Dojin Chemical Research Institute, Japan Co., Ltd.).

[0056] (3) Main instruments: carbon dioxide incubator (Thermo Forma, USA), automatic microplate reader (Bio-TEK, Elx800).

[0057] 2. Experimental method

[0058] (1) Cell culture:

[0059] Cells were cultured in DMEM high-glucose medium (DMEM medium supplemented with 10% fetal bovine serum, pH 7.2), added with 400 μg / ml G418, 2 mmol / L glutamin...

Embodiment 3

[0068] Example 3: Drugs inhibit the expression level of HBsAg in the culture supernatant of HepG2.2.15 cells

[0069] 1. Experimental materials

[0070] (1) Main reagents: HBsAg detection ELISA kit (Shanghai Yanji Biotechnology Co., Ltd.).

[0071] (2) Main instrument: automatic microplate reader (Bio-TEK, Elx800).

[0072] 2. Experimental method

[0073] HepG2.2.15 cells (5×10 4 unit / mL) CO 2 After culturing in the incubator for 24 hours, the cells adhered to the wall and grew well, and the culture medium was removed. According to the results of the cytotoxicity test, the cell culture medium containing different concentrations of drugs without G418 was added, and each concentration was set for 3 replicates. Cells in complete medium as normal control, 5% CO 2 , Culture at 37°C. After 48h, 72h, and 96h of continuous culture, the supernatant of each sample was drawn and placed in a 1.5mL sterilized centrifuge tube, centrifuged at 1000rcf for 10min to take the supernatant, ...

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Abstract

The invention provides novel application of 4-hydroxy salicylamide in the field of pharmacy. The compound is an inhibitor of ribonucleotide reductase (RR), and can achieve the aims of inhibiting replication of HBV and treating hepatitis, in particular the hepatitis B by inhibiting activity of RR enzyme to block synthesis of dNTPs (deoxynucleotide triphosphates) required by hepatitis B virus (HBV)replication, achieve the aim of preventing and treating liver cancer by inhibiting the activity of RR of liver cancer cells, including the RR activity activated by HBV to inhibit proliferation of liver cancer cells, and achieve the aim of treating various tumors by inhibiting the RR. The 4-hydroxy salicylamide can be used for preventing and treating hepatitis B, liver cancer, oropharyngeal epithelioma, colorectal cancer, ovarian cancer, non-small cell lung cancer, chronic myeloid leukemia and other tumors, and has important application prospect.

Description

(1) Technical field [0001] The present invention relates to the application of 4-hydroxy salicylanilide in the preparation of drugs targeting ribonucleotide reductase (Ribonucleotide reductase, RR), especially the application of 4-hydroxy salicylanilide in the preparation of drugs targeting RR enzymes Drugs for preventing and treating hepatitis and application in antineoplastic drugs. (2) Background technology [0002] Chronic hepatitis is one of the serious infectious diseases threatening human health worldwide. About more than 2 billion people in the world have been infected with hepatitis B virus (Hepatitis B Virus, HBV), and the number of deaths due to HBV infection reaches 1 million every year. HBV infection is not only an important biological factor causing chronic hepatitis B, but also primary liver cancer. China, Southeast Asia, and Africa are high-incidence areas of HBV infection, and the incidence of primary liver cancer is significantly higher than that in low-i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/609A61P1/16A61P35/00A61P35/02A61P31/20
Inventor 邵吉民朱维良徐志建陈新焕刘霞
Owner ZHEJIANG UNIV
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