Bufadienolide compound and application thereof to preparation of medicine for resisting gastric cancer

A technology of bufadienolide and compound is applied in the field of anti-gastric cancer drugs, which can solve the problems of unreported anti-gastric cancer activity of bufadienolide compounds.

Inactive Publication Date: 2016-11-23
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The anti-gastric cancer activity of the bufadienolactone com

Method used

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  • Bufadienolide compound and application thereof to preparation of medicine for resisting gastric cancer
  • Bufadienolide compound and application thereof to preparation of medicine for resisting gastric cancer
  • Bufadienolide compound and application thereof to preparation of medicine for resisting gastric cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1: Establishment of a 3D cell spheroid screening model for gastric cancer

[0015] Sand toad toxin, sand toad toxin-3-pimeloyl arginine ester, far cinobufin toxin-3-adipyl arginine ester, far cinobufin toxin, deacetylated cinobufin toxin, Chinese Bufafen-3-suberoyl arginine ester, bufafen-3-suberoyl arginine ester, 3-dehydrobufafolin and sea bufo toxin were sourced from Shanghai Yuanye Biotechnology Co., Ltd. .

[0016] Docetaxel and epirubicin hydrochloride were purchased from Dalian Meilun Biotechnology Co., Ltd.; gastric cancer cell line HGC-27 was purchased from Shanghai Cell Bank, Chinese Academy of Sciences; ULA-96-well plates were purchased from Corning; inverted microscopes were purchased from OLYMPUS.

[0017] The HGC-27 cells in the logarithmic growth phase were seeded in ULA-96 well plates at a density of 20000 cells / well (20K cells / well), 10000 cells / well, 5000 cells / well, 2500 cells / well, and 1250 cells / well. Cells / well, 625 cells / well, 313 cells / ...

Embodiment 2

[0018] Example 2: Inhibitory effect of coarsely screened bufadienolactone compounds on the growth of 3D cell spheres

[0019] Docetaxel and epirubicin hydrochloride, typical drugs for the clinical treatment of gastric cancer, were selected as positive control drugs, and the inhibitory effect of 9 typical bufadiene lactone compounds on the growth of HGC-27 3D cell spheres was roughly screened. Among them, 9 typical bufadiene lactone compounds (as a coarse screening drug) are bufabufagin, bufabufalin-3-pimeloyl arginate, and bufabufalin-3-adipyl Arginine Esters, Cinobufagin, Deacetylated Cinobufagin, Cinobufagin-3-Suberoyl Arginate, Cinobufagin-3-Suberoyl Arginate, 3 - Dehydrobufalin and sea bufotoxin. Cells at the optimal density (313 cells / well) were inoculated on ULA-96 well plates, and the inoculation volume of the medium (RPMI-1640 containing 20% ​​fetal bovine serum) was 200 μL / well. After culturing for 4 days and growing to 3D cell spheres with optimal particle size, 10...

Embodiment 3

[0020] Example 3: The dose relationship of deacetylated cinobufagin inhibiting the growth of 3D cell spheres

[0021] Different doses of the compound with the strongest inhibitory ability, 5-deacetylcinobufagin, were applied to the 3D cell spheres. Inoculate the cells with optimal density (313 cells / well) in ULA-96 well plate, culture medium (RPMI-1640 containing 20% ​​fetal calf serum) with an inoculation volume of 200 μL / well for 4 days, and grow to the optimal particle size After 3D cell spheres, replace 100 μL of fresh medium in each well, add compound 5 to 16 wells with a volume of 10 μL, and the concentration gradient of the compound is 40 μM, 20 μM, 10 μM, 5 μM, 2.5 μM, 1.25 μM, 0.625 μM and 0.3125 μM, each concentration was replicated twice. The blank control group was cell spheres treated with medium containing 0.2% DMSO (RPMI-1640 containing 20% ​​fetal bovine serum), and two wells were used as the blank control group. Use an inverted microscope to record the size ...

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Abstract

The present invention relates to anti-gastric cancer drugs, in particular to the application of bufadienolactone compounds in anti-gastric cancer drugs. Diacyl arginine ester, cinobufagin-3-adipyl arginine ester, cinobufagin, deacetylated cinobufagin, cinobufagin-3-suberoyl arginine Esters, bufafolin-3-suberoyl arginine ester, 3-dehydrobufafolin and sea bufotoxin and their pharmaceutically acceptable salt-forming compounds. In vitro cell experiments show that the compound of the present invention can significantly inhibit the growth of gastric cancer cell spheres, and therefore can be used to prepare tumor drugs for treating gastric cancer.

Description

technical field [0001] The present invention relates to anti-gastric cancer drugs, in particular to the application of bufadienolactone compounds in anti-gastric cancer drugs. Diacyl arginine ester, cinobufagin-3-adipyl arginine ester, cinobufagin, deacetylated cinobufagin, cinobufagin-3-suberoyl arginine Esters, bufafolin-3-suberoyl arginine ester, 3-dehydrobufafolin and sea bufotoxin and their pharmaceutically acceptable salt-forming compounds. Background technique [0002] Toad is a commonly used medicinal protozoan in traditional Chinese medicine. Its toad skin and its preparations have definite curative effects in the treatment of liver cancer, gastric cancer, lung cancer, breast cancer, esophageal cancer and colon cancer. At present, cinobufacin injection and cinobufacin capsules are widely used in clinical anti-tumor therapy, among which bufadiene lactone compounds and polar nitrogen-containing compounds are considered to be the main active ingredients in toad skin. ...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61P35/00A61P1/00
Inventor 梁鑫淼王纪霞张秀莉刘艳芳张云黄润祺
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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