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Pharmaceutical composition containing PI3K inhibitor and PERK inhibitor, and applications thereof

A composition and inhibitor technology, applied in the field of medicine, to achieve the effects of inhibiting growth, inducing apoptosis, and low toxicity

Active Publication Date: 2017-07-21
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no relevant research report on the combined use of PI3K inhibitors and PERK inhibitors for anti-tumor

Method used

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  • Pharmaceutical composition containing PI3K inhibitor and PERK inhibitor, and applications thereof
  • Pharmaceutical composition containing PI3K inhibitor and PERK inhibitor, and applications thereof
  • Pharmaceutical composition containing PI3K inhibitor and PERK inhibitor, and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 The effect of LY294002 and GSK2656157 alone on the growth of tumor cells and normal cells

[0031] Firstly, the drug sensitivity of esophageal cancer cells Eca-109, EC9706, lung cancer cells A549, liver cancer cells HepG2 and normal vascular endothelial cells HUVEC to LY294002 and GSK2656157 alone was tested.

[0032] 1. Experimental method

[0033] The cells were inoculated into 96-well plate with the number of 3000-6000 cells per well. After the cells adhered to the wall (24h), the LY294002 and GSK2656157 drugs were diluted to a certain gradient concentration, and each concentration was set to 5 replicate wells, divided into experimental groups and Dosing in the zeroing group. After 48 hours, use the MTT method to detect cell viability. Add 10 μl of MTT solution to each well and continue to incubate for 4 hours. Carefully suck out the liquid in the wells to avoid contact with crystals in the wells. Add 100 μl of DMSO to each well and shake on a constant speed...

Embodiment 2

[0035] Example 2 Effect of LY294002 on downstream target protein S6 of PI3K pathway

[0036] Eca-109 cells were divided into 4 × 10 per well 5 cells at a density of 6 wells. After the cells adhered to the wall, the cells were treated with LY294002 for 0, 1, 3, and 6 h, and the expression of the downstream target protein S6 of the PI3K pathway was detected by Western blot. The implementation method of Western blot is as follows: collect the whole protein of each group of cells separately. After SDS electrophoresis, the protein was transferred to a PVDF membrane, blocked with 5% skimmed milk powder at room temperature for 1 hour, incubated with the primary antibody corresponding to the protein to be detected, and incubated overnight at 4°C. After 24 hours, the primary antibody was recovered, washed three times with TBST for 5 minutes each time, and then incubated with the secondary antibody for 1 hour at room temperature. Afterwards, wash with TBST for 3 times, each time for ...

Embodiment 3

[0038] Example 3 Effects of combined action of LY294002 and GSK2656157 on tumor cells and normal cells

[0039] The tumor Eca-109, EC9706, A549 and HepG2 cells and HUVEC normal vascular endothelial cells were inoculated into 96-well plates at the number of 3000-6000 cells per well. In addition, the Eca-109 cell line was placed in a 96-well plate and grouped as follows: control group, 0.5 μg / ml cisplatin group (GDDP), 5 μM GSK2656157 group and 0.5 μg / ml cisplatin (GDDP) Combined with 5μM GSK2656157 group, 2μg / ml 5-fluorouracil group (5-FU) and 2μg / ml 5-fluorouracil group (5-FU) combined with 5μM GSK2656157 group; after 48 hours of culture, add 10μl concentration of 5mg to each well / ml of MTT solution, continue to culture for 4h, then discard the culture medium, add 100μl of DMSO to each well, and shake on a constant speed shaker in the dark. After the crystals are fully dissolved, read the OD value (wavelength 570nm, reference wavelength 630nm) on a microplate reader, read th...

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PUM

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Abstract

The invention relates to a pharmaceutical composition containing a PI3K inhibitor and a PERK inhibitor, and applications thereof in preparing anti-tumor drugs. Independent application of the PI3K inhibitor and independent application of the PERK inhibitor both possesses certain inhibition effect on growth of tumor cells; after drug combination of the PI3K inhibitor and the PERK inhibitor, the pharmaceutical composition is capable of inhibiting growth of tumor cells, inducing apoptosis, and inhibiting formation of cell colonies obviously, the effect is much better than that of independent application, and excellent synergistic effect is achieved. The toxicity of the pharmaceutical composition on human normal vascular endothelial cells is relatively low; the pharmaceutical composition possesses excellent inhibition effect on tumor cells; cancer treatment effect is promising to be improved; and the pharmaceutical composition can be used for preparing anti-tumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition containing a PI3K inhibitor and a PERK inhibitor and application thereof. Background technique [0002] Cancer is a disease with a high mortality rate second only to cardiovascular diseases, and the number of cancer patients and deaths worldwide is increasing. Nearly half of the new cancer cases occurred in Asia, most of which were in China, which ranked first in the world in terms of new cancer cases. Especially in the four types of malignant tumors including liver cancer, esophageal cancer, gastric cancer and lung cancer, China ranks first in the number of new cases and deaths in the world. Although the treatment of these cancers is mainly based on surgery, since early patients generally have no obvious symptoms, many of the cancer patients diagnosed for the first time are already in the middle and advanced stages and have lost the cha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/519A61P35/00
Inventor 王绍祥王绍其王晓王艳王熙昊常港陈家杰
Owner SHENZHEN UNIV
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