Application of neocryptolepine derivative in preparation of medicine for treating gastric cancer
A technology of Baiphylline and its derivatives, which is applied in the field of medicine, can solve the problems of unstudied anti-gastric cancer activity and unstudied related mechanisms, and achieve the effects of reducing mitochondrial membrane potential, good application prospects, and no toxic and side effects
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Embodiment 1
[0038] Synthesis of embodiment 1 neo-elephine derivative Z23
[0039] The specific synthetic route of neobasine derivative Z23 is as follows: figure 1 shown.
[0040] Concrete synthesis method comprises the following steps:
[0041] (1) Synthesis of target compound 2:
[0042] Under nitrogen, quinoline (7.7 mmol) and CH 3 A mixture of I (11.6 mmol) in isopropanol (1M) was heated at 90° C. for 3 h and the reaction was cooled to room temperature. The resulting precipitate was isolated by vacuum filtration, washed with a mixture of isopropanol / ethyl acetate (1:1), and dried in vacuo to give a yellow solid which was the target compound 2 (1-methylquinoline iodide).
[0043] (2) Synthesis of target compound 3;
[0044] A mixture of hydrogen peroxide (6.4 mL, 35%) and the target compound 2 (1-methylquinoline iodide, 15 mmol in 15 mL of water) obtained in (1) above was added to a mixture containing 0.148 mol of hydrogen at 0° C. Potassium oxide in water (30 mL) and 1,2-dichloro...
Embodiment 2
[0050] Example 2 Inhibitory effect of eleganine derivatives on gastric cancer cells
[0051] AGS cells treated with different eleganine derivatives Z2-Z49 were added to a 96-well plate, 10 μL of 5 mg / mL MTT solution was added to each well, and the incubation was continued for 4 h in a cell culture incubator.
[0052] After the incubation, carefully suck out the liquid in the 96-well plate, add 100 μL of DMSO solution to each well, and incubate on a shaker at 120 r / min for 20 min. After the solution in the 96-well plate is uniform, measure the absorbance value at 490nm with a microplate reader, and calculate the IC of different elegansine derivatives on AGS cells 50 .
[0053] The results are shown in Table 1 below. Most of the basaltine derivatives have a certain inhibitory effect on AGS cells, and the basaltine derivative Z23 has the most significant inhibitory activity on gastric cancer cells. Its IC 50 It can reach 43.15±3.92nM.
[0054] Table 1 IC of different basaltine...
Embodiment 3
[0061] Example 3 Inhibitory effect of elederine derivative Z23 on gastric cancer cells
[0062] 1. Changes in cell morphology
[0063] (1) AGS cells were placed in RPMI medium (HyClone, USA) containing 10% heat-inactivated fetal bovine serum and 1% penicillin / streptomycin at 37°C, 5% CO 2 When the cell density reaches 80%-90%, take the cells out of the cell culture incubator, wash the cells twice with PBS, 4 mL each time; add 2 mL of trypsin, and put them in the incubator to digest;
[0064] (2) Take the cells out of the incubator, add 3mL of medium to stop digestion, transfer the cell suspension to a 5mL centrifuge tube, take out a new 1.5mL centrifuge tube, add 900μL of fresh medium, and mix the cell suspension evenly , take 100 μL of cell suspension into a 1.5mL centrifuge tube, mix well;
[0065] (3) Take 10 μL of the diluted cell suspension to the cell counting plate prepared in advance, count under the microscope, and count according to the principle of counting up an...
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