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Application of bufadienolide compounds having amino acid chains in preparing anti-tumor drugs

A technology of bufadienolide and anticancer drug, which is applied in the application field of bufadienolide compound with amino acid chain in the preparation of anticancer drug, and can solve the problems of unreported anti-colon cancer and gastric cancer activity and the like

Inactive Publication Date: 2017-01-04
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

[0005] The anti-colon and gastric cancer activity of the bufadienolactone fractions with amino acid chains mentioned in the present invention has not yet been reported

Method used

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  • Application of bufadienolide compounds having amino acid chains in preparing anti-tumor drugs
  • Application of bufadienolide compounds having amino acid chains in preparing anti-tumor drugs
  • Application of bufadienolide compounds having amino acid chains in preparing anti-tumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: preparation process of toad skin fraction

[0034] The skin of the giant toad is collected from Linyi, Shandong, and it has been identified as authentic by Yang Xiaoping, Xiyuan Chinese Medicine Research Office, China Academy of Chinese Medical Sciences.

[0035] Weigh 200g of shredded toad skin, add 1.4L of pure methanol according to the material-liquid ratio of 1:7, soak for two days, reflux at 80°C for 4 hours, filter to obtain the filtrate, add 1.4L of pure methanol to the filter residue, and boil slightly at 80°C Reflux for 4 hours, filter to obtain the filtrate, and extract twice in total. The two extracts were combined to obtain 2730 mL, concentrated under reduced pressure at 60° C. and evaporated to dryness to obtain 7 g of the total extract. Dissolve the total extract with 160mL 65-75% methanol-water (V / V), extract with 160mL n-heptane, extract the methanol part with 160mL n-heptane again, extract twice, and then depressurize the methanol part at ...

Embodiment 2

[0037] Example 2: Establishment of 3D cell spheroid screening model

[0038] Human colon cancer cells HT-29 and human gastric cancer cells HGC-27 were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences; ULA-96 well plates were purchased from Corning; toad skin fractions were fractions 1-11 obtained in Example 1; inverted microscopes were purchased from OLYMPUS.

[0039] HT-29 cells and HGC-27 cells in the logarithmic growth phase were seeded in ULA-96 well plates, so that the number of cells in each well plate were 20K, 10K, 5K, 2.5K, 1.25K and 0.625K, The inoculation volume is 200 μL / well, the medium used for HT-29 cells is McCOY's 5A containing 10% fetal bovine serum, the medium used for HGC-27 cells is RPMI-1640 containing 20% ​​fetal bovine serum, and each cell density is repeated three times , using an inverted microscope to record micrographs of 3D cell spheroid morphology every 24 hours for 4 consecutive days. The result is as Figure 5 and Im...

Embodiment 3

[0040] Example 3: Research on the Effect of Amino Acid Chains on the Anticancer Activity of Toad Skin Compounds

[0041] Inoculate HT-29 and HGC-27 cells at the optimal density (1.25K / well) on ULA-96 well plates and culture them for 4 days. The medium used by HT-29 cells is McCOY's 5A containing 10% fetal calf serum, HGC The medium used for -27 cells is RPMI-1640 containing 20% ​​fetal bovine serum. After growing to 3D cell spheres with optimal particle size, 100 μL of fresh medium was replaced in each well, and the cells eluted by Click XIon column were added respectively. Bufadienolactone fractions with amino acid chains and bufadienolactone fractions without amino acid chains, the final concentration of each fraction is 10 μM and 1 μM (the average molecular weight of the compound in the fraction is calculated as 500Da), each Fraction samples were repeated three times. The size of the 3D cell spheroids was recorded using an inverted microscope every 24 hours for 6 consecuti...

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Abstract

The invention discloses the influence of an amino acid chain on the anti-tumor activity of toad skin compounds as well as the inhibitory effect of fractions of bufadienolide compounds having the amino acid chains on the growth of colon cancer HT-29 cells and gastric cancer HGC-27 cells. The bufadienolide compounds include a mixture of bufadienolide fractions having and having no amino acid chains as well as a bufadienolide No.1-11 fraction having the amino acid chain, wherein the bufadienolide No.1-11 fraction is separated by virtue of high performance liquid chromatography. In vitro cell experiments indicate that the bufadienolide compounds having the amino acid chains are more significant in inhibitory effect on the growth of colon cancer and gastric cancer than bufadienolide compounds having no the amino acid chains, and meanwhile, some bufadienolide fractions having the amino acid chains take an obvious inhibitory effect on colon cancer cell globules and gastric cancer cell globules; therefore, the bufadienolide fractions having the amino acid chains can be used for preparing medicines for treating the colon cancer and the gastric cancer.

Description

technical field [0001] This paper introduces the effect of the presence or absence of amino acid chains on the anticancer activity of toad skin compounds and the growth inhibitory effect of bufadienolactone fractions on colon cancer HT-29 cells and gastric cancer HGC-27 cells. The bufadiene lactone fractions with amino acid chains described herein include a mixture of bufadienolide fractions with amino acid chains and bufadienolides with amino acid chains separated by high performance liquid chromatography 1 - Fraction No. 11. Background technique [0002] Toad skin is an important traditional Chinese medicine resource in my country. In recent years, reports on the anticancer activity of toad skin have attracted widespread attention. Toad skin has definite curative effect in the treatment of liver cancer, stomach cancer, esophageal cancer and colon cancer, and bufadienolide compounds and polar nitrogen-containing compounds are considered to be the most effective pharmacolog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/585A61K35/65A61P35/00A61P1/00
Inventor 梁鑫淼黄润祺张秀莉王纪霞钟正升
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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