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Application of isothiocyanate compound in preparing targeted drug for esophageal cancer

A technology of ester compounds and isothiocyanates, which is applied in the direction of active ingredients of esters, drug combinations, antineoplastic drugs, etc., to achieve the effects of improving survival rate and quality of life, reducing economic burden, and low-cost prevention methods

Pending Publication Date: 2019-12-06
THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the occurrence and development of esophageal cancer is a complex process with multiple carcinogenic mechanisms, so there are still many potential targets that can be blocked or inhibited. The development of a new generation of targets and the development of low-cost targeted drugs are important Important research directions for cancer treatment

Method used

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  • Application of isothiocyanate compound in preparing targeted drug for esophageal cancer
  • Application of isothiocyanate compound in preparing targeted drug for esophageal cancer
  • Application of isothiocyanate compound in preparing targeted drug for esophageal cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1: Screening Research on ITCs Compounds Sensitive to Esophageal Squamous Cell Lines

[0042] (1) Test material

[0043] Esophageal squamous cell carcinoma cell line KYSE150 (p53 R248Q ), esophageal squamous cell carcinoma cells EC109 (p53 + / + ) from the Key Open Laboratory of Esophageal Cancer in Henan Province, the First Affiliated Hospital of Zhengzhou University.

[0044] (2) Test method

[0045] a. Inoculate 100 μL / well of the cell suspension of each cell line in a 96-well plate (5000 cells per well), and place the culture plate at 37°C, 5% CO 2 Cultured under the conditions until the cells adhered to the wall;

[0046] b. Using dimethyl sulfoxide (DMSO) as a control, add 10 μM, 20 μM, 30 μM, 40 μM, 50 μM, 60 μM, 80 μM, 100 μM benzyl isothiocyanate (BITC) or phenylethyl ether Based on isothiocyanate (PEITC), the culture plate was placed in the incubator for 24 h and 48 h;

[0047] c. Add 10 μL of CCK-8 solution to each well (be careful not to generate ai...

Embodiment 2

[0056] Example 2: Validation of the effects of BITC and PEITC on the expression of p53 protein and p21 protein in esophageal squamous cell carcinoma cell lines

[0057] (1) Test groups

[0058] a. Inoculate the cells of each cell line in a 10cm cell culture dish, press 1×10 5 / ml cell concentration, place the culture dish at 37°C, 5% CO 2 Cultured under the conditions until the cells adhered to the wall;

[0059] b. Take dimethyl sulfoxide (DMSO) as the control group, add 10 μM, 50 μM BITC or PEITC as the test group after the cells adhere to the wall, and place the culture dish in the incubator for 24 h.

[0060] (2) Test method

[0061] (I) total protein extraction, protein concentration determination

[0062] a. Take out the cells of the experimental group and the control group from the cell incubator to make a cell suspension, put the counting plate into the automatic cell counter for counting; after counting, extract the cell suspension from the culture bottle into a c...

Embodiment 3

[0082] Example 3: BITC and PEITC on KYSE150 (p53 R248Q ) Study on the Effect of Apoptosis

[0083] (1) Test groups

[0084] a. Inoculate KYSE150 (p53) in a 10cm cell culture dish R248Q ) cells, by 1 x 10 5 / ml cell concentration, place the culture dish at 37°C, 5% CO 2 Cultured under the conditions until the cells adhered to the wall;

[0085] b. Dimethyl sulfoxide (DMSO) was used as the control group, and 5 μM, 10 μM, 15 μM, 20 μM BITC or PEITC were added as the test group after the cells adhered to the wall, and the culture dish was placed in the incubator for 12 h.

[0086] (2) Test method

[0087] a. Collect the cells treated with BITC and PEITC compounds for 12 hours, digest and collect them with EDTA-free trypsin; wash the cells twice with PBS (centrifuge at 2000rmp for 5min), and collect 1-5×10 5 cell;

[0088] b. Add 500 μL of Bingding Buffer to suspend the cells; add 5 μL of Annexin V-FITC and mix well, then add 5 μL of Propidium Iodide and mix well;

[0089] ...

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Abstract

The invention discloses application of an isothiocyanate compound in preparing a targeted drug for esophageal cancer, and aims to solve the technical problem of loss of a wtp53 cancer suppressive function in patients with esophageal squamous cell carcinoma with p53 gene mutation. The application disclosed by the invention applies the isothiocyanate compound in preparing drugs for the p53 mutant esophageal cancer, clarifies the molecular mechanism of the isorhodanate compound in reactivating mutp53, and lays a foundation for targeted therapy for patients with mutp53 esophageal cancer. The application disclosed by the invention can improve the survival rate and quality of life of patients to a certain extent, thereby reducing the pressure on individuals, families and society, and also reducing the economic burden on the families and society.

Description

technical field [0001] The invention relates to the technical field of biomedical engineering, in particular to the application of isothiocyanate compounds (Isothiocyanates, ITCs) in the preparation of targeted drugs for treating esophageal cancer. Background technique [0002] Esophageal cancer is a digestive system tumor that seriously threatens human life and health. In my country, 160,000 to 200,000 people die of esophageal cancer every year, accounting for about 50% of the world's esophageal cancer patients. From the perspective of histopathology, it can be divided into esophageal squamous cell carcinoma and esophageal adenocarcinoma. In China, where the incidence rate is high, more than 90% of esophageal cancer patients belong to esophageal squamous cell carcinoma, and the 5-year overall survival rate is 15% to 34%. [0003] In recent years, my country has made remarkable achievements in the diagnosis, surgery, radiotherapy and chemotherapy of esophageal cancer. Howev...

Claims

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Application Information

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IPC IPC(8): A61K31/26A61P35/00
CPCA61K31/26A61P35/00
Inventor 王峰周悦孟祥瑞陈晓琦关露露周然
Owner THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV
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