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Novel medical application of ethane-1,2-double ovate leaf holly bark acid ester

A technology of biscubic acid ester and ethane, applied in the field of medicine, can solve the problems such as the role of derivatives of cubing acid in preventing and treating tumor metastasis that have not been found or reported in the literature, and achieves good selectivity.

Active Publication Date: 2017-09-22
JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Before the completion of the present invention, except for the research of the present inventor, there was no literature report that derivatives of basic acid had the effect of preventing and treating tumor metastasis, nor did it find that ethane-1,2-bisbine Preparation of reports on the application of drugs for the prevention and treatment of tumor metastasis

Method used

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  • Novel medical application of ethane-1,2-double ovate leaf holly bark acid ester

Examples

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Embodiment 1

[0029] Inhibition of Proliferation of Hepatic Cancer Cell HepG2 and LO2 Toxicity of Hepatic Cells by Hepatic Acid and Ethane-1,2-Bisic acid

[0030] After digesting hepatoma cells HepG2 in the logarithmic growth phase and human normal liver cells LO2, the cell density was adjusted to 1×10 5 cells / mL, seeded in a 96-well plate, 100 μL per well, placed at 37°C, 5% CO 2 Cultivate in the incubator for 24 hours; remove the old culture medium, add the test drug (hebine acid and ethane-1,2-bisbine acid ester) and dilute the test drug stock solution with the culture medium, set Different concentrations, 100 μL per well, and a blank control group were set up, and 5 replicate wells were set up in each group. After 24 hours of drug action, discard the drug-containing medium, add 100 μL of serum-free phenol red-free medium to each well, and then add 100 μL of 0.5 mg / mL MTT solution, and continue to incubate for 4 hours before terminating the culture; aspirate and discard the 96-well plat...

Embodiment 2

[0036] Binding acid and ethane-1,2-bisbining acid inhibit the adhesion of hepatocellular carcinoma cells HepG2 to extracellular matrix

[0037] The fibronectin FN (fibronectin) stored at -20°C was placed in a 37°C water bath until it was completely melted, and then prepared into a FN working solution with a concentration of 10 μg / ml in serum-free culture medium. Use 100 μL / well FN working solution to completely cover the 96-well plate, leave it at room temperature overnight, and gently suck off the liquid. Take HepG2 cells in the logarithmic growth phase and make a single cell suspension with a cell concentration of 5×10 5 / ml, mixed with different concentrations of drugs (0, 0.25, 0.5, 1.0, 2.5, 5.0 μM), and inoculated in FN-coated 96-well plates. After incubating at 37°C and 5% CO2 for 2 hours, lightly wash with PBS for 3 times, add 10 μl of MTT culture solution after drying, continue to incubate for 4 hours, discard the supernatant, add 100 μl DMSO, and use an enzyme-linke...

Embodiment 3

[0043] Experiment of Inhibition of Adhesion between HepG2 and HUVEC Cells by Hepatic Acid and Ethane-1,2-Bisic Acid

[0044] Human umbilical vein endothelial cells were isolated from umbilical cord veins delivered in normal pregnancy and cultured. Digest the HUVEC cells in the logarithmic phase and inoculate them in a 24-well plate. When the endothelial cells in the 24-well plate are full of the plate, wash it two or three times with PBS, and then add the endothelial stimulating factor IL-1β at a concentration of 1 ng / L culture medium, incubated at 37°C, 5% CO2 for 4h. After 4 hours, take out the well plate, wash it two or three times with PBS, take HepG2 cells in the logarithmic growth phase, and make 4×10 cells after fluorescent labeling. 5 / ml -1 Single cell suspension, and RPM-1640 culture solution with different concentrations of derivatives of the present invention were added, the final drug concentrations were: 0, 0.25, 0.2, 1.0, 2.5, 5.0 μM, 500 μl per well. After ...

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Abstract

The invention provides application of an ovate leaf holly bark acid derivative to preparation of a medicine for preventing and treating tumor metastasis, and concretely relates to application of an ethane-1,2-double ovate leaf holly bark acid ester to preparation of the medicine for preventing and treating tumor metastasis. In vitro experiments show that the ethane-1,2-double ovate leaf holly bark acid ester has remarkable inhibiting effects on proliferation, adhesion, migration and the like of tumor cells, and is safe and low-toxic for human body normal cells. In vivo animal experiments show that the experimental lung metastasis of mice B16-F10 melanoma can be effectively reduced, and the ethane-1,2-double ovate leaf holly bark acid ester has a better anti-tumor metastasis effect. The ethane-1,2-double ovate leaf holly bark acid ester can be applied to the medicine for preventing tumor metastasis, and the new application of the ovate leaf holly bark acid derivative to prevention and treatment of tumors is exploited. The ethane-1,2-double ovate leaf holly bark acid ester has more remarkable pharmacological activity compared with ovate leaf holly bark acid.

Description

technical field [0001] The present invention relates to a kind of ethane-1,2-dibasic acid ester and its application, in particular to a kind of ethane-1,2-basic acid ester and its use in the preparation of medicines for preventing and treating tumor metastasis The application in medicine belongs to the field of medicine. Background technique [0002] Malignant tumors are one of the major diseases that seriously endanger human health. Most of the deaths of cancer patients are caused by late metastasis of malignant tumors. Tumor metastasis refers to the whole process in which malignant tumor cells separate from the primary tumor, reach secondary tissues or organs through various transfer methods, and continue to proliferate and grow, forming secondary tumors with the same properties as the primary tumor. The process of tumor metastasis is very complicated, that is, tumor cells will break away from the primary mother tumor at random; some enzymes secreted will degrade the base...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61P35/00A61P35/04
CPCC07J63/008
Inventor 赫玉芳南敏伦王雪何忠梅赵昱玮赵全成
Owner JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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