A kind of basic acid derivative with the function of preventing and treating tumor metastasis
A technology for anticancer drugs and tumor metastasis, which can be applied in the fields of antineoplastic drugs, medical preparations containing active ingredients, organic chemistry, etc., and can solve the problem of preparing drugs for the prevention and treatment of tumor metastasis from derivatives of anticancer drugs that have not been found. However, there are no reports in the literature on the prevention and treatment of tumor metastasis by the derivatives of basic acid, which can inhibit the ability of movement and migration, improve solubility and good selectivity.
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Embodiment 1
[0033] Example 1 Study on Inhibitory Proliferation of Hepatic Cancer Cell HepG2 and LO2 Toxicity of Hepatic Acid and Its Derivatives to Normal Liver Cells
[0034] 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 medium, add the test drug (basic acid and its derivatives) to dilute the stock solution of the test drug with the medium, set different concentrations, 100 μL per well, and set a blank For the control group, 5 replicate wells were set up for 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 plate For the su...
Embodiment 2
[0038] Example 2 Bispinic acid and its derivatives inhibit the adhesion of liver cancer cell HepG2 to extracellular matrix
[0039] 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-linked detector t...
Embodiment 3
[0044] Example 3 Experiment of Inhibiting the Adhesion of Hepatic Cancer Cells HepG2 and HUVEC Cells by Respiratory Acid and Its Derivatives
[0045] 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,...
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