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Rotundic acid derivant having effect of preventing and treating tumour 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.

Active Publication Date: 2017-09-26
JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Before the completion of the present invention, except for the research of the inventor, there was no literature report that the derivatives of basic acid had the effect of preventing and treating tumor metastasis, nor had it been found that the derivatives of basic acid were used in the preparation of prevention and treatment of tumor metastasis. reports on drug use

Method used

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  • Rotundic acid derivant having effect of preventing and treating tumour metastasis
  • Rotundic acid derivant having effect of preventing and treating tumour metastasis
  • Rotundic acid derivant having effect of preventing and treating tumour metastasis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Study on the inhibition of the proliferation of hepatocarcinoma cells HepG2 and the toxicity of salvage acid and its derivatives to normal liver cells LO2

[0034] After digesting HepG2 liver cancer cells in logarithmic growth phase and human normal liver cells LO2, the cell density is adjusted to 1×10 5 Pcs / mL, seeded in 96-well plate, 100μL per well, placed at 37℃, 5% CO 2 Incubate in an incubator for 24 hours; remove the old medium, add the test drug (slavic acid and derivatives) to dilute the test drug storage solution with the medium, set different concentrations, 100μL per well, and set a blank For the control group, each group has 5 multiple holes. After the drug has been used for 24 hours, aspirate and discard the drug-containing medium, add 100μL of serum-free and phenol red medium to each well, and then add 100μL of 0.5mg / mL MTT solution, continue to incubate for 4h, stop the culture; aspirate the 96-well plate Add 100μL DSMO to each well, shake for 10m...

Embodiment 2

[0038] Example 2 Salvage acid and its derivatives inhibit the adhesion of hepatoma cell HepG2 to extracellular matrix

[0039] The fibronectin FN (fibronectin) stored at -20°C was placed in a 37°C water bath until completely dissolved, and a serum-free culture medium was used to prepare an FN working solution with a concentration of 10 μg / ml. Use 100μL / well of FN working solution to completely cover the 96-well plate, leave it at room temperature overnight, and gently aspirate the liquid. Take HepG2 cells in logarithmic growth phase to 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 a 96-well plate coated with FN. After incubating for 2 hours at 37°C with 5% CO2, wash gently with PBS 3 times, add 10μl of MTT culture solution after drying, continue incubating for 4h, discard the supernatant, add 100μl DMSO, dissolve, use an enzyme-linked detector to detect OD at ...

Embodiment 3

[0044] Example 3 Experiments of inhibiting the adhesion of hepatocarcinoma cell HepG2 and HUVEC cells by salvage acid and its derivatives

[0045] Human umbilical vein endothelial cells were isolated from the umbilical cord vein during normal pregnancy and cultured. The HUVEC cells in the logarithmic phase were digested and seeded on a 24-well plate. When the endothelial cells of the above-mentioned 24-well plate were overgrown, they were washed two or three times with PBS, and then IL-1β containing endothelial stimulating factor was added at a concentration of 1ng / Incubate L medium at 37°C and 5% CO2 for 4h. After 4h, take out the well plate, wash two or three times with PBS, take the HepG2 cells in logarithmic growth phase, and make 4×10 cells after fluorescent labeling. 5 / ml -1 Single cell suspension, and adding RPM-1640 culture solution of the derivative of the present invention with different concentrations, the final drug concentration is: 0, 0.25, 0.2, 1.0, 2.5, 5.0 μM, ...

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Abstract

The invention provides application of a rotundic acid derivant in preparation of a medicine for preventing and treating tumour metastasis. An in vitro experiment proves that the rotundic acid derivant disclosed by the invention has significant inhibition effects on proliferation, adhesion, migration and the like of tumor cells, and is safe and low-toxicity to normal cells of a human body. An in vivo animal experiment proves that experimental lung metastasis of B16-F10 melanoma of mice can be effectively reduced, and a preferable tumour metastasis prevention effect is prompted. The rotundic acid derivant disclosed by the invention can be applied to a medicine for preventing the tumour metastasis, so that new application of the rotundic acid derivant to prevention and treatment of tumors is developed, and a new choice is provided for developing a new drug for treating the tumour metastasis and preventing postoperative re-metastasis of malignant tumour; moreover, the rotundic acid derivant has more obvious pharmacological activity.

Description

Technical field [0001] The invention relates to a medicine for preventing postoperative metastasis of malignant tumors, in particular to the application of salvage acid derivatives in medicines for preventing and treating tumor metastasis, and 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 tumor patients are caused by late metastasis of malignant tumors. Tumor metastasis refers to the process of tumor cells dissociating from the primary tumor, infiltrating into the surrounding tissues, invading into the circulatory system, and then transferring in the body, and adhering to endothelial cells to form metastases. Tumor metastasis is one of the main reasons why tumors are difficult to cure and relapse, and it is also a key factor leading to the death of tumor patients. Clinical diagnosis results show that more than 60% of newly diagnosed tumor patients have met...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/58A61P35/04
CPCC07J63/008
Inventor 南敏伦赫玉芳王雪赵昱玮何忠梅赵全成
Owner JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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