Applications of artemisine derivatives and pharmaceutically acceptable salts thereof in preparing drugs for treating leukemia
A technology of artemisinin derivatives and medicinal salts, applied in the medical field, can solve the problems of diseases affecting the survival rate of patients and poor prognosis of patients.
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Embodiment 1
[0015] Embodiment 1 Preparation of artemisinin derivative biarteether amine maleate
[0016] In this embodiment, starting from the known compound hydroxyarteether (references: Li Ying et al., Acta Pharmaceutica Sinica, 1981, 16: 429-439), its p-toluenesulfonate was first prepared, and then in the solvent dimethylformamide React with ammonia water to obtain biarteether amine, the reaction route is:
[0017]
[0018] The obtained biarteetheramine is then re-formed into the maleate salt.
[0019] The specific operation is as follows:
[0020] Dissolve p-toluenesulfonate of hydroxyarteether (1.54g) in dimethylformamide (10mL), add ammonia (0.5mL) and stir to heat to 40-50°C, and react for about 20h. After TLC detected that the raw material spots basically disappeared, the reaction solution was poured into ice water, extracted repeatedly with ethyl acetate, the organic phases were combined, washed with saturated brine, and dried over anhydrous sodium sulfate. The solvent was ...
Embodiment 2
[0023] Example 2 SM1044 Inhibitory Test on Leukemia Cells
[0024] Firstly, SM1044 was dissolved in triple distilled water at a concentration of 1 mg / ml, and then the typical acute myeloid leukemia M3 retinoic acid-resistant cell line NB4-R1 was selected for the experiment. We will 5×10 4 The cells were suspended in 200 μl medium and seeded in 96-well plates. A blank group, a control group without drug addition, and a drug group with different concentrations (0.0025 μM, 0.005 μM, 0.01 μM, 0.04 μM, 0.4 μM, 0.8 μM, 1.6 μM SM1044) were set up, and three parallel wells were set up for each concentration. After culturing for 24h, 48h and 72h respectively, MTT (5mg / ml) was added to continue culturing for 4h. After centrifugation, 180 μl supernatant was sucked off, 180 μl DMSO was added to each well, and placed on a shaker for 15 minutes. Detect the absorbance value (A) at 570nm with a microplate reader, and calculate the half inhibitory concentration IC 50 . The result is as f...
Embodiment 3
[0025] Example 3 SM1044 induces NB4-R1 cell apoptosis test
[0026] will be 5×10 5 NB4-R1 cells were suspended in 1ml medium and seeded in 24-well plates. Set up the control group (0μM), different concentrations (0.1μM, 0.5μM, 1μM SM1044) dosing groups respectively, culture for 24h and 48h respectively, collect the cells to be tested, wash with pre-cooled phosphate buffered saline (PBS) twice and use Resuspend in 200 μl binding buffer, add 5 μl Annexin V-FITC and 5 μl propidium iodide (PI), mix gently, incubate at room temperature in the dark for 15 minutes, and detect by flow cytometry within 1 hour, the results are as follows figure 2 As shown, the concentration of SM1044 is 0.1 μM-1 μM, and it can induce apoptosis in NB4-R1 cells within 24-48 hours. It indicated that SM1044 could induce apoptosis of NB4-R1 cells, and the proportion of apoptotic cells increased with the increase of drug concentration and treatment time.
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