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Application of 1,3,3-trimethyl-2-benzo-imidazo-pyridine-vinyl-indolium iodide in preparing anticancer drug

A technology of trimethyl, methylbenzene, applied in 1

Active Publication Date: 2019-07-26
SHANDONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] After searching and searching by authoritative organizations, the above compound (E)-1,3,3-trimethyl-2-(2-(4-methylbenzo[4,5]imidazo[1,2-a] Pyridin-3-yl)vinyl)-3H-indol-1-ium iodide is used as a drug for inhibiting the growth of A549 lung cancer cells and promoting the apoptosis and autophagy of A549 cells for pharmacological research and application. to report

Method used

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  • Application of 1,3,3-trimethyl-2-benzo-imidazo-pyridine-vinyl-indolium iodide in preparing anticancer drug
  • Application of 1,3,3-trimethyl-2-benzo-imidazo-pyridine-vinyl-indolium iodide in preparing anticancer drug
  • Application of 1,3,3-trimethyl-2-benzo-imidazo-pyridine-vinyl-indolium iodide in preparing anticancer drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1: Detection of survival rate by SRB method after ZBM-H treatment of A549 cells.

[0050] (1) Compound ZBM-H was added to treat cells pre-seeded in a 96-well plate. (2) After 24 hours of compound treatment, the old culture medium was discarded, 100 μL of trichloroacetic acid was added, and the cells were fixed at 4° C. for 1 hour. (3) Discard the fixative. Wash five times with double-distilled water in gentle motions, and dry at room temperature. (4) Add 50 μL of SRB to each well, shake at room temperature for 10 minutes. (5) Wash 5 times with 1% acetic acid and dry at room temperature. (6) Add 100 μL Tris base in non-buffer solution with a concentration of 10 mM / L to each well and place on a shaker for 10 minutes. (7) Select 540nm excitation light to measure OD value.

[0051] The results show that: 1, 2, 5, 10 μ M ZBM-H can significantly inhibit the survival of A549 cells after 24 hours of treatment, see figure 1 .

Embodiment 2

[0052] Example 2: After A549 cells were treated with ZBM-H, the changes in cell morphology were detected under an inverted microscope.

[0053] A549 lung cancer cells were seeded in 6-well cell culture plates at 37°C in CO 2 After culturing in the incubator for 12 hours, a control group and an experimental group were set up for the following experiments. Control group: cultured with DMSO (0.1%, v / v). Experimental group: treated with ZBM-H at concentrations of 1, 2, 5, and 10 μM, respectively, at 37°C, CO 2 After culturing in the incubator for 3h, 6h, 12h, 24h and 48h, the cell morphology was photographed under an inverted microscope.

[0054] The results showed that: under the above conditions, ZBM-H could reduce the number of A549 cells and promote the release of apoptotic bodies. See figure 2 .

experiment example 3

[0055] Experimental Example 3: After ZBM-H treatment of A549 cells for 48 hours, the apoptosis was detected by Western Blot.

[0056] A549 lung cancer cells were inoculated in a 6 cm-diameter petri dish at 37°C, CO 2 After culturing in the incubator for 12 hours, a control group and an experimental group were set up for the following experiments. Control group: cultured with DMSO (0.1%, v / v). Experimental group: A549 cells were treated with ZBM-H at a concentration of 1, 2, 5, and 10 μM for 48 hours, the cells were lysed, the cell lysate was collected, centrifuged at 12,000 g for 15 minutes at 4°C, the supernatant was taken, and Western Blot was used to detect the concentration of different cells. Caspase12 and PARP protein cleavage and BAX protein levels.

[0057] The results showed that after treating A549 cells with 1, 2, 5, and 10 μM ZBM-H for 48 hours, they could significantly promote the cleavage of Caspase12 and PARP proteins, and at the same time increase the level o...

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Abstract

The invention discloses a compound (E)-1,3,3-trimethyl-2-(2-(4-methylbenzo[4,5]imidazo[1,2-a]pyridine-3-yl)vinyl)-3H-indolium-1- iodide in preparing a drug for inhibiting A549 lung cancer cell growthand promoting the apoptosis of A549 cells and autophagy, wherein the drug dose capable of effectively promoting A549 cell apoptosis and autophagy is 1-10 [mu]M, preferably 5-10 [mu]M. The compound isexpected to serve as an effective tool for inhibiting tumor growth and lay a foundation for developing therapeutic drugs for non-small cell lung cancer.

Description

technical field [0001] The present invention relates to the application of a kind of benzimidazole derivatives, especially to compound (E)-1,3,3-trimethyl-2-(2-(4-methylbenzo[4,5]imidazo[ 1,2-a]pyridin-3-yl)vinyl)-3H-indol-1-ium iodide (ZBM-H for short) in the preparation of drugs that inhibit the growth of A549 lung cancer cells and promote the apoptosis and autophagy of A549 cells Applications. Background technique [0002] Benzimidazole derivatives are a very important class of intermediates and final products, which have good biological activity and can be widely used in the field of organic synthesis. Among them, benzimidazole is an important pharmacophore in many synthetic drugs. At present, most of the research on benzimidazole derivatives is to conduct biological activity experiments on the compounds that have been synthesized by benzimidazole derivatives. It has been clearly reported that there are such Derivatives have anti-tumor, anti-virus, anti-inflammatory an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/437A61P35/00
CPCA61K31/437A61P35/00
Inventor 苗俊英赵宝祥张尚立宁俊娅
Owner SHANDONG UNIV
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