Use of carboxytriazole and glutamic acid uptake and metabolism inhibitors in antitumor

A metabolic inhibitor, carboxyaminotriazole technology, applied in the application field of carboxyamidotriazole and glutamic acid uptake and metabolism inhibitors in anti-tumor, can solve the problems of difficult application, high toxicity, etc., and achieve non-toxic Side effects, high safety effects

Active Publication Date: 2021-10-26
GUANGDONG YINZHU PHARMACEUTICAL TECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the energy supply of normal cells in the body is highly dependent on glucose metabolism and fatty acid metabolism, drugs developed for the targets of carbohydrate and fatty acid metabolism in tumor cells are highly toxic to normal cells in the body and are difficult to apply clinically

Method used

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  • Use of carboxytriazole and glutamic acid uptake and metabolism inhibitors in antitumor
  • Use of carboxytriazole and glutamic acid uptake and metabolism inhibitors in antitumor
  • Use of carboxytriazole and glutamic acid uptake and metabolism inhibitors in antitumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Carboxytriazole reduces the sugar utilization rate of tumor cells.

[0053] 1. Experimental method

[0054] After the cells were treated with CAI (10 μM) for 48 hours, the levels of oxidative phosphorylation OCR and glycolytic ECAR of these cells were detected using a seahorse energy metabolism detector.

[0055] 2. Experimental results

[0056] As shown in Figure 1, the results of Seahorse showed that in the case of CAI administration, both OCR and ECAR were reduced, and the reduction of OCR could not be stimulated by the uncoupler FCCP. Similarly, the detection of ECAR in the administration group was added Oligomycin, an inhibitor of oxidative phosphorylation, also did not reverse the drug-induced decrease.

Embodiment 2

[0057] Example 2: Carboxytriazole increases phosphorylated ACC.

[0058] 1. Experimental method

[0059] After the cells were incubated with 5, 10, and 20 μM CAI for 48 hours, protein samples were collected. For protein quantification, the loading amount of 40 μg per well was detected by Western blot electrophoresis to detect the expression level of phosphorylated ACC.

[0060] 2. Experimental results

[0061] Such as figure 2 As shown, the expression of phosphorylated ACC increased with the concentration of CAI.

Embodiment 3

[0062] Example 3. Increased utilization of amino acids in tumor cells after the action of carboxytriazole.

[0063] 1. Experimental method

[0064] After the cells were treated with CAI (10 μM) for 48 hours, the changes in the intake ratios of the three energy sources of glycolipids and amino acids in these cells after administration were detected by using a seahorse energy metabolism detector.

[0065] 2. Experimental results

[0066] Such as image 3 As shown, Seahorse's results showed that in the case of CAI administration, the main source of energy capacitation of cells was more inclined to utilize amino acid production capacity.

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Abstract

The invention relates to the use of carboxyaminotriazole and glutamic acid uptake and metabolism inhibitor in antitumor. Specifically, the present invention relates to the use of carboxytriazole in combination with one or more inhibitors of glutamate uptake and metabolism in the preparation of antitumor drugs for use in mammals. In particular, the combination of carboxytriazole with amino acid transporter inhibitors, glutamate dehydrogenase 1 inhibitors, and glutaminase inhibitors is used in the preparation of antitumor drugs for mammals.

Description

technical field [0001] The present invention relates to the field of medical treatment and medicine, in particular to the treatment of malignant tumors and the anti-cancer drugs through the method of combination drug, in particular to carboxylamine triazole and its derivatives and amino acid transporter inhibitors, GDH1 inhibitors or GLS inhibitors , a method for synergistically controlling the energy utilization of tumor cells, and treating malignant tumors, and a combination of anti-tumor drug preparations. Background technique [0002] Any life activity is inseparable from the corresponding material and energy basis. For tumor cells, they must not only proliferate rapidly, but also find ways to escape immune surveillance, and under certain circumstances, they must also transfer to other parts of the body. While resisting drug attacks, they must also find ways to make a comeback. Metabolic disorder is one of the typical characteristics of malignant tumors and is closely r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4192A61K31/198A61P35/00
CPCA61K31/198A61K31/4192A61P35/00A61K2300/00
Inventor 郭磊张德昌叶菜英石婧
Owner GUANGDONG YINZHU PHARMACEUTICAL TECHNOLOGY CO LTD
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