CN113893250A - Application of GSK126 in preparation of anti-osteosarcoma drugs - Google Patents
Application of GSK126 in preparation of anti-osteosarcoma drugs Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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Abstract
The invention discloses application of GSK126 in preparing an anti-osteosarcoma medicament, and relates to the technical field of new application of medicaments. The invention discovers that GSK126 can obviously inhibit the proliferation of osteosarcoma cells, increase the expression of autophagosomes and induce autophagy of the osteosarcoma cells to achieve the effect of inhibiting the growth of osteosarcoma. The GSK126 can be used for developing novel medicaments for treating osteosarcoma, and has wide medical prospect and economic value.
Description
Technical Field
The invention relates to the technical field of new application of medicaments, in particular to application of GSK126 in preparing an anti-osteosarcoma medicament.
Background
Osteosarcoma is a primary mesenchymal tissue malignant tumor, is better developed at the metaphysis of young and old bones, especially at the far end of the femur and the near end of the tibia, and has the characteristics of early lung metastasis, high disability rate, high recurrence rate and the like. Surgery and drug chemotherapy are the standard treatment for the disease, and the new progress of osteosarcoma treatment has led to significant improvement of the prognosis of patients, but the 5-year overall survival rate of patients with metastatic or recurrent osteosarcoma is still lower than 30%. Osteosarcoma is a differentiation defect disease, is related to osteogenic differentiation related genes and/or epigenetic changes, and is manifested by the differentiation resistance of mesenchymal stem cells or osteoblasts.
Studies have shown that epigenetic changes play an important role in the development of tumors and are regulated by epigenetic proteins. The drosophila Zeste gene enhancer human homolog 2(enhancer of Zeste homolog2, EZH2) is one of epigenetic protein families, and can catalyze the trimethylation of histone H3 lysine 27(H3K27) and silence downstream related genes, so that the occurrence of tumors and the multi-directional differentiation disorder of stem cells are caused. The epigenetic protein EZH2 was found to be abnormally expressed in a variety of tumors, but the role of EZH2 in osteosarcoma is not clear. In recent years, small molecule inhibitors developed against EZH2 have gained popularity as the role of EZH2 in a variety of tumors has gained increasing importance. Potential inhibitors of EZH2 are mainly divided into two classes, one class is cysteine hydrolase inhibitors, which belong to indirect inhibitors, such as 3-deazaneplanocina (dznep); the other is a methionine competitive inhibitor, belonging to the direct inhibitor, such as GSK 126. Research shows that the indirect EZH2 inhibitor plays an inhibiting role in various tumors, but the effect of the direct EZH2 inhibitor GSK126 in osteosarcoma is not reported at present.
Disclosure of Invention
The invention aims to overcome the defects of the prior art and provides application of GSK126 in preparing anti-osteosarcoma medicaments.
In order to achieve the purpose, the invention adopts the technical scheme that: application of GSK126 in preparing anti-osteosarcoma medicine is provided.
The EZH2 gene encodes a histone lysine N-methyltransferase that participates in DNA methylation to inhibit transcription of other genes, and EZH2 also methylates histone H3 lysine 27. Mutations or overexpression of EZH2 are associated with various types of cancer, such as breast, prostate, melanoma, and bladder cancer. GSK126 is a novel small molecule compound which directly inhibits EZH2, and no report on the efficacy of the GSK in treating osteosarcoma exists at present.
The inventor unexpectedly finds that GSK126 can obviously inhibit the proliferation of osteosarcoma cells, increase the expression of autophagosomes and induce autophagy of the osteosarcoma cells to achieve the effect of inhibiting the growth of osteosarcoma. Therefore, GSK126 can be used for developing novel anti-osteosarcoma drugs and has wide medical prospect and economic value.
As a preferred embodiment of the application of the invention, the molecular formula of the GSK126 is C31H38N6O2And the molecular weight is 526.27.
As a preferred embodiment of the use according to the invention, the anti-osteosarcoma is an agent inhibiting the proliferation of osteosarcoma cells.
As a preferred embodiment of the use according to the invention, the anti-osteosarcoma is an increase in the expression of autophagosomes.
As a preferred embodiment of the use of the invention, the anti-osteosarcoma is induced by autophagy in osteosarcoma cells.
As a preferable embodiment of the application of the invention, the concentration of the GSK126 in the medicine is 5-15 mu M.
The invention also provides a pharmaceutical composition comprising GSK126 and a pharmaceutically acceptable carrier.
As a preferable embodiment of the pharmaceutical composition, the concentration of GSK126 in the pharmaceutical composition is 5-15 μ M.
The invention also provides application of the pharmaceutical composition in preparing an anti-osteosarcoma drug.
The invention has the beneficial effects that: the invention provides application of GSK126 in preparing anti-osteosarcoma drugs, and GSK126 is applied to treating osteosarcoma, so that a new source is provided for preparing anti-osteosarcoma drugs, and a new medicinal value of GSK126 is developed.
Drawings
FIG. 1: a: proliferation experiment result graphs of human osteosarcoma Saos-2 cells after treatment of GSK126 with different concentrations; b: proliferation experiment result chart of human osteosarcoma U2OS cells after GSK126 treatment of different concentrations.
FIG. 2A: immunofluorescence experimental plots of human osteosarcoma Saos2 cells after treatment with GSK126 at different concentrations; b: immunofluorescence experimental plots of human osteosarcoma U2OS cells after treatment with GSK126 at different concentrations.
FIG. 3 is a graph showing the expression levels of autophagy-related proteins p62 and LC3 in cells after GSK126 is acted on human osteosarcoma Saos-2 cells and human osteosarcoma Saos2 cells at different concentrations.
Detailed Description
The present invention will be described in further detail with reference to the following examples. This should not be understood as limiting the scope of the above-described subject matter of the present invention to the following examples. All the technologies realized based on the above contents of the present invention belong to the scope of the present invention.
Example 1 cell proliferation assay
(1) Experimental materials: human osteosarcoma Saos-2 cell line and human osteosarcoma U2OS cell line, purchased from Shanghai cell bank of Chinese academy of sciences; high glucose DMEM from Gibco, usa; fetal bovine serum was purchased from Gibco, usa; MTS cell proliferation kit was purchased from Promega (Promega, usa); GSK126 was purchased from seleck (china, shanghai blue wood chemical limited); 96-well plates were purchased from Thermo (Sammerfei, USA).
(2) The experimental method comprises the following steps: inoculating Saos2 cells and U2OS cells into 96-well plate (about 2000 cells per well), adding GSK126 drugs (5 μ M, 10 μ M, and 15 μ M) to 100 μ l culture medium, and culturing at 37 deg.C with 5% CO2Culturing for 48h, adding 20 μ l MTS, incubating at 37 deg.C for 2h, and detecting absorbance at OD 490 nm.
(3) The results of the experiment are shown in FIG. 1. As shown in FIG. 1, GSK126 can significantly inhibit the proliferation of osteosarcoma cells, and the inhibitory effect is enhanced with the increase of the concentration of GSK 126.
Example 2 immunofluorescence assay
(1) Experimental materials: human osteosarcoma Saos-2 cell line and human osteosarcoma U2OS cell line, purchased from Shanghai cell bank of Chinese academy of sciences; GSK126 was purchased from seleck (china, shanghai blue wood chemical limited); rabbit anti-human LC3 polyclonal antibody was purchased from CST (Cell signaling technology, usa); FITC fluorescent secondary antibody, DAPI staining solution from Sigma (Sigma, USA); goat serum and paraformaldehyde solution were purchased from doctor warrior, wuhan.
(2) The experimental method comprises the following steps: after treating human osteosarcoma Saos2 cells and human osteosarcoma U2OS cells with GSK126 with the concentration of 5 mu M, 10 mu M and 15 mu M for 48 hours, fixing the cells with 4% paraformaldehyde solution for 15 minutes, washing the cells with PBS for 3 times, blocking the cells with 10% goat serum, adding rabbit anti-human LC3 primary antibody diluted by 1:100, incubating the cells at 4 ℃ overnight, adding FITC-IgG secondary antibody diluted by 1:200 the next day, incubating the cells at room temperature for 1 hour, finally adding DAPI to counterstain the cells, blocking the cells, and observing the result by a fluorescence microscope.
(3) The results of the experiment are shown in FIG. 2. As can be seen from fig. 2, GSK126 was able to increase expression of autophagosomes, and as the concentration of GSK126 increased, expression of autophagosomes increased.
Example 3 immunoblotting experiments
(1) Experimental materials: human osteosarcoma Saos-2 cell line and human osteosarcoma U2OS cell line, purchased from Shanghai cell bank of Chinese academy of sciences; GSK126 was purchased from seleck (china, shanghai blue wood chemical limited); rabbit anti-human LC3 polyclonal antibody, rabbit anti-human p62 polyclonal antibody were purchased from CST (Cell signaling technology, USA); BCA kit.
(2) The experimental method comprises the following steps: inoculating Saos2 cells and U2OS cells into 96-well plate (about 2000 cells per well), adding GSK126 drugs (5 μ M, 10 μ M, and 15 μ M) to 100 μ l culture medium, and culturing at 37 deg.C with 5% CO2Culturing for 48h, collecting human osteosarcoma Saos2 cells and human osteosarcoma U2OS cells respectivelyAn appropriate amount of cell lysate RIPA (containing 1mmol/L PMSF) was added to each tube of cells, the cells were covered sufficiently, and the tube was lysed on ice for 30 minutes. The cell debris was scraped off and the whole volume was transferred to a clean EP tube and centrifuged at 13000 Xg for 10 min at 4 ℃. The BCA kit is used for detecting the concentration of cell protein, about 40 mu g of protein sample per well is loaded in 12% SDS-PAGE, transferred to a PVDF membrane, then 5% skimmed milk powder is sealed for 1 hour, and corresponding rabbit anti-human GAPDH, p62 and LC3 polyclonal antibody are incubated overnight at 4 ℃. The following day the PVDF membrane was removed and washed 3 times with TBST at room temperature. Adding a proper amount of secondary antibody, and incubating for 1 hour at normal temperature in a dark place. The PVDF membrane was removed, washed 3 times with TBST at room temperature, and the expression of p62 and LC3 proteins was detected using ECL luminescence.
(3) The results of the experiment are shown in FIG. 3. As shown in FIG. 3, GSK126 can reduce the expression level of p62 protein and increase the expression level of LC 3-II/LC 3-I, indicating that GSK126 can induce autophagy of osteosarcoma cells, and that the autophagy of osteosarcoma cells is enhanced with the increase of the concentration of GSK 126.
Finally, it should be noted that the above embodiments are only used for illustrating the technical solutions of the present invention and not for limiting the protection scope of the present invention, and although the present invention is described in detail with reference to the preferred embodiments, it should be understood by those skilled in the art that modifications or equivalent substitutions can be made on the technical solutions of the present invention without departing from the spirit and scope of the technical solutions of the present invention.
Claims (9)
- Application of GSK126 in preparing anti-osteosarcoma drugs.
- 2. The use of claim 1, wherein GSK126 has the formula C31H38N6O2And the molecular weight is 526.27.
- 3. The use of claim 1, wherein the anti-osteosarcoma is an agent that inhibits cell proliferation of osteosarcoma.
- 4. The use of claim 1, wherein the anti-osteosarcoma is an anti-osteosarcoma that increases expression from autophagosomes.
- 5. The use of claim 1, wherein the anti-osteosarcoma is induced by autophagy in osteosarcoma cells.
- 6. The use according to claim 1, wherein the concentration of GSK126 in the medicament is 5-15 μ Μ.
- 7. A pharmaceutical composition comprising GSK126 and a pharmaceutically acceptable carrier.
- 8. The pharmaceutical composition of claim 7, wherein the concentration of GSK126 in the pharmaceutical composition is 5-15 μ M.
- 9. The use of the pharmaceutical composition of claim 7 in the preparation of an anti-osteosarcoma medicament.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116350755A (en) * | 2022-12-22 | 2023-06-30 | 唐颢 | Application of m5C methylation regulatory factors DNMT1 and NSun2 in tumor |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105541801A (en) * | 2016-01-18 | 2016-05-04 | 常州大学 | Method for synthesizing EZH2 methyltransferase inhibitor GSK126 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105541801A (en) * | 2016-01-18 | 2016-05-04 | 常州大学 | Method for synthesizing EZH2 methyltransferase inhibitor GSK126 |
Non-Patent Citations (1)
| Title |
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| 袁晓峰等: "组蛋白甲基转移酶在骨肉瘤中的研究进展", 《中国细胞生物学学报》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116350755A (en) * | 2022-12-22 | 2023-06-30 | 唐颢 | Application of m5C methylation regulatory factors DNMT1 and NSun2 in tumor |
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