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Applications of ursolic acid derivatives in preparation of drug for preventing and treating tumor metastasis

A technology of tumor metastasis and ursolic acid, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of difficult preparation of preparations, low in vivo bioavailability, and no research on normal cytotoxicity and anti-tumor metastasis. selective effect

Inactive Publication Date: 2014-07-23
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, UA is insoluble in water, which leads to difficulties in preparation of its preparations and low bioavailability in vivo. Therefore, by modifying the structure of UA to improve the solubility of insoluble UA, thereby further improving its anticancer activity and effectively improving its bioavailability. Utilization is increasingly becoming a hotspot and difficulty in the research of scientific researchers
[0007] Patents CN101161670B and CN 101830961 B disclose ursolic acid chemical modifiers such as ursolic acid amine and ursolic acid esters with anti-tumor activity. Compared with the UA parent itself, these UA derivatives have a certain improvement on the anti-cancer activity of tumor cells, but they do not involve Toxic to normal cells and its anti-tumor metastasis research; our research group published a UA derivative N-[3β-acetoxy-arbutane-12 with anti-tumor activity in the patent 201110373561.2 previously applied -ene-28-yl]-aminoethylenediamine (abbreviated as US597, see formula I)

Method used

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  • Applications of ursolic acid derivatives in preparation of drug for preventing and treating tumor metastasis
  • Applications of ursolic acid derivatives in preparation of drug for preventing and treating tumor metastasis
  • Applications of ursolic acid derivatives in preparation of drug for preventing and treating tumor metastasis

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Example 1 Study on Inhibition of Proliferation of Hepatoma Cell HepG2 by Ursolic Acid and Its Derivatives and LO2 Toxicity to Normal Liver Cells

[0032] 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, inoculated in 96-well plate, 100 ??l per well, placed at 37°C, 5% CO 2 Cultivate in the incubator for 24 h; remove the old medium, add the test drug (ursolic acid and its derivatives) and dilute the test drug stock solution with the medium, set different concentrations, 100??l per well, A blank control group was also set up, with 5 replicate wells in each group. After 24 hours of drug action, discard the drug-containing medium, add 100??l of serum-free phenol red-free 1640 medium to each well, and then add 100??l of 0.5 mg / ml MTT solution, continue incubation for 4h, and terminate Culture; carefully discard the supernatant in the wells of the 96-well plate, add 100??...

Embodiment 2

[0034] Example 2 Detection of ursolic acid and its derivatives inhibiting the adhesion of liver cancer cell HepG2 to extracellular matrix

[0035] The fibronectin FN (fibronectin) stored at -20°C was placed in a 37°C water bath until it was completely melted, and the serum-free culture medium was used to prepare the FN working solution with a concentration of 10 μg / ml. 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, 0.2, 1, 5μM), inoculated in FN-coated 96-well plates. 37°C, 5% CO 2 After incubation for 2 h, lightly wash with PBS 3 times, add 10 μl of MTT culture solution after drying, continue to incubate for 4 h, discard the supernatant, add 100 μl DMSO, and detect the OD value at 570 nm with an enzyme-li...

Embodiment 3

[0036] Example 3 Ursolic acid and its derivatives inhibit the adhesion of liver cancer cells HepG2 and HUVEC cells

[0037] Human umbilical vein endothelial cells were isolated from umbilical veins of normal gestational deliveries and prepared according to Jaffe, E. A.; Nachman, R. L.; Becker, C. G.; Minick, C. R. Culture of human endothelial cells derived from umbilicalveins: Identification by morphologic and immunological criteria.Clin. In est. 1973, 52, 2745-2756. The cultivation was carried out. 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 medium at 37 °C, 5% CO 2 Incubate for 4 h under conditions. 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 cell...

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Abstract

The invention provides applications of ursolic acid derivatives in preparation of a drug for preventing and treating tumor metastasis. In-vitro experiments show that the ursolic acid derivatives (US597) has an obvious inhibition effect on the proliferation, adhesion, metastasis and the like of cells, can effectively regulate the expression of adherence factors related to the cell surfaces and the tumor metastasis, and is safe and low-toxic to the normal cells of a human body. In-vivo experiments show that the ursolic acid derivatives can effectively reduce experimental pulmonary metastasis of rat B16-F10 melanin tumor, and is prompted to have better tumor metastasis resistance effect. The ursolic acid derivatives can be applied to a drug for preventing the tumor metastasis, the new applications of the ursolic acid derivatives in preventing and treating tumor are developed, thus providing a new choice for developing a new drug for tumor metastasis so as to prevent the postoperative metastasis of malignant tumor.

Description

technical field [0001] The invention relates to a medicine for preventing postoperative metastasis of malignant tumors, in particular to the application of ursolic acid and its derivatives in medicines for preventing and treating tumor metastasis. Background technique [0002] Cancer (also known as malignant tumor) is one of the most serious diseases threatening human health today, and there is no thorough treatment so far. Therefore, seeking effective prevention and treatment of tumor methods and drugs has always been a research hotspot at home and abroad. Metastasis is one of the most important biological characteristics of malignant tumors. Although the level of chemotherapy, radiotherapy and surgical treatment of tumors has been greatly improved compared with the past, tumor recurrence and metastasis after surgery are still the cause of most cancer patients. Leading cause of treatment failure and death. [0003] Liver cancer is one of the most common malignant tumors i...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P35/04
Inventor 邵敬伟向利平杨祥贾力
Owner FUZHOU UNIV
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