Iron ion chelating agent and application of medicinal salt of chelating agent
A chelating agent, iron ion technology, applied in the field of medicine, can solve the problems of increasing patient pressure, only 20%-40%, and high cost of medication for patients
Inactive Publication Date: 2019-04-19
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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Problems solved by technology
Although PD-1 / PD-L1 immunotherapy has shown efficacy in a variety of cancer treatments, the above drugs are all antibody drugs. Compared with small molecule drugs, their preparation, storage, transportation and technical costs are higher, which lead to The cost of medication for patients is too high; in addition, the effective rate of this therapy for most cancers is only 20%-40%, and some patients will relapse after remission, which invisibly increases the pressure on patients, and some patients have to consider The “to use or not to use” question
Method used
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Embodiment
[0033] Example Deerasirox (4-[3,5-bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl]benzoic acid) in a melanoma trial
[0034] 1. In vitro cytotoxicity test
[0035] After digesting B16F10 cells with trypsin, make 10 5 cells / mL cell suspension, 100 μL per well was inoculated into a 96-well plate, and after culturing for 18-24 hours, different final concentrations (120 / 60 / 30 / 15 / 0 μM) of deferasirox were added, and the culture was continued for 6 hours. The cell viability was detected by thiazolium blue (MTT) colorimetry (survival rate (%)=(OD value of test well / OD value of control well)×100%), repeated three times.
[0036] 2. Western Blot detection of the effect of deferasirox on the expression of PD-L1 on B16F10 cells
[0037] Digest B16F10 cells with trypsin, inoculate 2 mL per well into a 6-well plate, add 30 μM final concentration of deferasirox after 18-24 hours and continue culturing for 6 hours, wash with PBS 2-3 times, add 100 μL of cells to each well Lysis solution, gently s...
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The invention relates to the field of medicine, in particular to an iron ion chelating agent and application of medicinal salt of the chelating agent. According to the iron ion chelating agent and themedicinal salt thereof, the expression level of PD-L1 of the surfaces of multiple kinds of tumor cells can be effectively lowered, application of immunosuppression of multiple kinds of tumor cells, such as melanoma, bladder cancer, non-small cell lung cancer, bladder cancer, head and neck cancer, Hodgkin lymphoma, renal cell carcinoma and Merkel cell carcinoma, mediated by the PD-1 / PD-L1 passageis removed, and the application is different from novel application for treating diseases or symptoms caused by accumulation of excessive in-vivo iron ions.
Description
technical field [0001] The invention relates to the field of medicine, in particular to the application of an iron ion chelating agent and a pharmaceutically acceptable salt thereof. For example, Deferasirox, Desferrioxamine, Deferiprone, L1NA11, Deferitrin or pharmaceutically acceptable salts thereof. Background technique [0002] Iron ion chelators include any pharmaceutically useful therapeutic agent for sequestering iron in patients in need of iron chelation, including 3,5-diphenyl-1,2,4-tri An azole derivative or a salt thereof, [0003] [0004] where R 1 and R 5 Simultaneously or independently of each other, hydrogen, halogen, hydroxyl, lower alkyl, halogen-lower alkyl, lower alkoxy, halogen-lower alkoxy, carboxyl, carboxyl, carbamoyl, N-lower alkylcarbamoyl , N,N-di-lower alkylcarbamoyl or nitrile; R 2 and R 4 Simultaneously or independently of each other is hydrogen, unsubstituted or substituted lower alkanoyl or aroyl or a group that can be removed under p...
Claims
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Login to View More IPC IPC(8): A61K45/00A61K31/4196A61K31/16A61K31/185A61K31/426A61K31/4412A61P37/06A61P35/00
CPCA61K31/16A61K31/185A61K31/4196A61K31/426A61K31/4412A61K45/00A61P35/00A61P37/06
Inventor 张海元菅慧
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI