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Inhibitor for tumor cell abnormal lipid metabolism by using plant cyclopeptides as effective component and application thereof

A technology of tumor cells and active ingredients, applied in the field of tumor drugs, to achieve the effect of inhibiting rapid proliferation, broad clinical application prospects, and mature extraction process

Active Publication Date: 2018-05-01
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report in the prior art that Rubiaceae-type cyclic peptides inhibit abnormal lipid metabolism in tumors

Method used

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  • Inhibitor for tumor cell abnormal lipid metabolism by using plant cyclopeptides as effective component and application thereof
  • Inhibitor for tumor cell abnormal lipid metabolism by using plant cyclopeptides as effective component and application thereof
  • Inhibitor for tumor cell abnormal lipid metabolism by using plant cyclopeptides as effective component and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0021] The preparation method of the following Rubiaceae type cyclic peptide RAs is the same as the Chinese invention patent CN 201410445325.0.

[0022] Experimental method: Treat the cultured tumor cells with RAs, and use the SRB method to detect its cell proliferation inhibitory activity, confirming that the compound can inhibit the abnormal proliferation of tumor cells; use a commercial kit to detect intracellular cholesterol, triglyceride, low-density lipoprotein and high-density lipoprotein content, the lipid droplet content in tumor cells was detected by Oil Red O staining, and it was confirmed that the compound inhibited abnormal lipid metabolism of tumor cells. The nude mouse subcutaneous xenograft model was established with liver cancer cells to verify the anti-tumor and anti-tumor abnormal lipid metabolism activities of RAs in vivo.

Embodiment 1

[0024] Growth inhibitory effect of RA-XII on human hepatoma cells:

[0025] Cell viability was measured by SRB method. The human liver cancer HepG2 cell line (purchased from the Cell Bank of the Type Culture Collection Committee of the Chinese Academy of Sciences) cultured overnight in 10% FBS medium was digested with trypsin to form a cell suspension, which was inoculated on a 96-well plate at an appropriate concentration, 100 μl / hole, in CO 2 Cultivate in the incubator for 24 hours until the cells are completely attached to the wall, add different final concentrations of RA-XII, and act for 24 hours, add 50 μl of 4°C pre-cooled TCA solution (30%, w / v) to each well to fix the cells, and the final concentration of TCA solution The concentration is 10%. Let it stand for 5 minutes, move it into a refrigerator at 4°C for 1 hour, take it out, rinse it with deionized water 5 times, and dry it at room temperature. Staining: After the 96-well plate was dried at room temperature, ...

Embodiment 2

[0028] RA-V and RA-XII affect the expression of lipid metabolism-related indicators in human liver cancer cells:

[0029] The human liver cancer HepG2 cell line cultured overnight in 10% FBS medium was digested with trypsin to form a cell suspension, which was inoculated on a 6-well plate at an appropriate concentration. After 24 hours, RA-V or RA-XII was added and treated for 24 hours. Trypsinize, centrifuge at room temperature 2000rpm for 5-10min, collect cells; resuspend cells once in pre-cooled 1×PBS (4°C), centrifuge at 2000rpm for 5-10min, wash cells. Commercial kits were used to detect the contents of total cholesterol and triglyceride in cells by single-reagent GPO-PAP method, and the contents of intracellular low-density lipoprotein and high-density lipoprotein were detected by two-reagent direct method (commercial reagents were included). The boxes were purchased from Nanjing Jiancheng Institute of Bioengineering, the article numbers are A111-1, A110-1, A113-1, and A...

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Abstract

The invention discloses an inhibitor for tumor cell abnormal lipid metabolism by using plant cyclopeptides as an effective component and application thereof in preparation of a medicine for inhibitingthe tumor cell abnormal lipid metabolism, particularly preparation of medicine for treating and preventing related cancers with abnormal lipid metabolism, such as liver cancer, colon cancer, rectum cancer and prostatic cancer. The inhibitor for tumor cell abnormal lipid metabolism has the advantages that the tumor cell abnormal lipid metabolism can be effectively inhibited, the source of the effective component, namely the plant cyclopeptides, is wide, the extracting technology is mature, the preparation type and the medicine usage type are diversified, and the clinical application prospect is broad.

Description

technical field [0001] The invention belongs to the field of tumor drugs, and in particular relates to an inhibitor of abnormal lipid metabolism of tumor cells using plant cyclic peptide as an active ingredient, a preparation method and application thereof. technical background [0002] Lipid is one of the three major nutrients. In addition to being closely related to energy supply and storage, it also has two functions: one is the main building molecule of cells, and lipid molecules include phospholipids (glycerophospholipids and sphingomyelin, etc.) and cholesterol. The main component of cell membrane, lipid metabolism changes directly affect cell membrane synthesis and cell proliferation; the second is an important active molecule in cell life activities, lipid molecules and their metabolic intermediates can participate in various signal transduction of cells, inflammation, blood vessel regulation, etc. , and is closely related to cell proliferation, cell adhesion and mot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61K38/14A61P35/00
CPCA61K38/12A61K38/14A61P35/00C07K7/64C07K9/006
Inventor 谭宁华王玉荣宋立华
Owner CHINA PHARM UNIV
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