Pharmaceutical application of 2-(4-piperidinylstyrene)-1,3,3-trimethyl-3h-indolium iodide

A technology based on styrene and trimethyl, applied in the field of fluorescent compound-2--1,3,3-trimethyl-3H-indolium iodide

Active Publication Date: 2021-06-15
THE SECOND HOSPITAL OF SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After retrieval, the relevant fluorescent compound (E)-2-(4-piperidinylstyrene)-1,3,3-trimethyl-3H-indolium iodide inhibits the growth of A549 cells and promotes the apoptosis of A549 cells. Patents for the application of death and autophagy drugs have not been reported

Method used

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  • Pharmaceutical application of 2-(4-piperidinylstyrene)-1,3,3-trimethyl-3h-indolium iodide
  • Pharmaceutical application of 2-(4-piperidinylstyrene)-1,3,3-trimethyl-3h-indolium iodide
  • Pharmaceutical application of 2-(4-piperidinylstyrene)-1,3,3-trimethyl-3h-indolium iodide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: Detection of survival rate by SRB method after PSI treatment of A549 cells.

[0054] (1) Compound PSI was added to treat the cells pre-planted in 96-well plate. (2) After compound treatment for 24 hours and 48 hours, 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.

[0055] The results show that: PSI can reduce the survival rate of A549 cells in a concentration-dependent manner after 24h and 48h of cells, see figure 1 .

Embodiment 2

[0056] Example 2: After PSI treatment of A549 cells, detection of morphological changes and apoptosis levels.

[0057] A549 cells were seeded in a 6 cm-diameter petri dish at 37°C in CO 2 After being cultured in the incubator for 12 hours, PSI was added for 3 hours, 6 hours, 12 hours and 24 hours, and the cell morphology was photographed under an inverted microscope.

[0058] A549 cells were seeded in a 6 cm-diameter petri dish at 37°C in CO 2 After culturing in the incubator for 12 hours, add PSI to treat for 24 hours, lyse the cells, collect the cell lysate, centrifuge at 12000g for 15 minutes at 4°C, take the supernatant, and use western blot to detect the level of PARP protein cleavage in different cells.

[0059] The results showed that after treating A549 cells with different concentrations of PSI for different times, the density of cells could be significantly reduced and the release of apoptotic bodies could be promoted; after treatment of A549 cells with different co...

Embodiment 3

[0060] Example 3: Western blot detection of autophagy level after PSI treatment of A549 cells.

[0061] A549 cells were seeded in a 6 cm-diameter petri dish at 37°C in CO 2 After culturing in the incubator for 12 hours, add PSI to treat for 24 hours, lyse the cells, collect the cell lysate, centrifuge at 12,000g for 15 minutes at 4°C, take the supernatant, and use western blot to detect LC3-Ⅰ, LC3-Ⅱ and P62 proteins in differently treated cells Level.

[0062] The results show that: A549 cells treated with different concentrations of PSI can significantly increase the protein level of LC3-II and reduce the protein level of P62, see Figure 4 .

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Abstract

The invention discloses a compound (E)-2-(4-piperidinylstyrene)-1,3,3-trimethyl-3H-indolium iodide, which inhibits the growth of A549 cells and promotes the growth of A549 cells. The application of apoptosis and autophagy drugs, wherein the dose of the drug that can effectively promote the apoptosis and autophagy of A549 cells is 1-10 μM. The present invention is (E)-2-(4-piperidinylstyrene)-1,3,3-trimethyl-3H-indolium iodide as an effective tool for studying the inhibition of mTOR activity, The foundation has been laid for the development of non-small cell lung cancer treatment drugs.

Description

technical field [0001] The present invention relates to the pharmaceutical use of fluorescent compound (E)-2-(4-piperidinylstyrene)-1,3,3-trimethyl-3H-indolium iodide (abbreviated as PSI), especially Its application in the preparation of drugs for inhibiting A549 cell growth and promoting A549 cell apoptosis and autophagy. Background technique [0002] Cancer is one of the leading causes of death. Lung cancer is the leading cause of cancer-related death in the world. About 85% of lung cancers are non-small cell lung cancers. There are several conventional methods of cancer treatment, namely surgery, radiation therapy, hormone therapy, chemotherapy (alone or in combination) and targeted therapy. Chemotherapy is an effective method against cancer. It can interfere with the process of cell division, affect tumor angiogenesis or induce cancer cell death through various signaling pathways, but it has potential harm to normal cells. Autophagy is an important intracellular cata...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/454A61P35/00C07D209/14
CPCA61K31/454A61P35/00C07D209/14
Inventor 林兆民赵宝祥李娜闫业浩
Owner THE SECOND HOSPITAL OF SHANDONG UNIV
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