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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

Active Publication Date: 2021-08-24
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a new compound, the basaltine derivative Z23 is obtained by modifying the structure of basaltine. Its anti-gastric cancer activity has not been studied, and its related mechanism has not been studied yet.

Method used

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  • Application of neocryptolepine derivative in preparation of medicine for treating gastric cancer
  • Application of neocryptolepine derivative in preparation of medicine for treating gastric cancer
  • Application of neocryptolepine derivative in preparation of medicine for treating gastric cancer

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The invention belongs to the field of medicines, and particularly relates to application of a neocryptolepine derivative in preparation of a medicine for treating gastric cancer. It is found that the neocryptolepine derivative Z23 can inhibit migration of gastric cancer cells, induce apoptosis of the gastric cancer cells and inhibit proliferation of the gastric cancer cells; and meanwhile, the neocryptolepine derivative Z23 basically has no toxic or side effect on normal gastric mucosa cells. Namely, compared with other neocryptolepine derivatives, cis-platinum and 5-Fu, the neocryptolepine derivative Z23 disclosed by the invention has a more remarkable effect of treating the gastric cancer and has a good application prospect.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of a basalpine derivative in the preparation of a drug for treating gastric cancer. Background technique [0002] In the 2018 global cancer statistics, gastric cancer is a digestive system tumor with a relatively high incidence rate. There are about 1.03 million new cases of gastric cancer worldwide, and the incidence rate ranks fifth among malignant tumors. Although there are different cancer treatment methods, including radiotherapy, chemotherapy, surgical treatment, gene therapy, etc., chemotherapy is still a necessary means for the treatment of solid tumors. However, chemical drugs have large side effects, tumor heterogeneity, and chemical drugs are prone to resistance. Drug resistance is a difficult problem to solve, therefore, it is very necessary to develop new chemical drugs for treating cancer with less toxicity. [0003] Neocryptolepine, which was fi...

Claims

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Application Information

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IPC IPC(8): A61K31/4745A61P35/00C07D471/04
CPCA61K31/4745A61P35/00C07D471/04
Inventor 陈朋刘映前马云浩杨程杰张智军马万通周忠坤杜康嘉张豪江欣荣
Owner LANZHOU UNIVERSITY
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