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Application of a kind of sulfamethoxine derivative in the preparation of antitumor drugs

A technology of sulfamethoxine and its derivatives, which is applied in the field of medicine and achieves good application prospects and obvious inhibitory effect

Active Publication Date: 2021-05-25
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Its tumor-related effects have not been reported

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  • Application of a kind of sulfamethoxine derivative in the preparation of antitumor drugs
  • Application of a kind of sulfamethoxine derivative in the preparation of antitumor drugs
  • Application of a kind of sulfamethoxine derivative in the preparation of antitumor drugs

Examples

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Effect test

Embodiment 1

[0041] Compound Sulfamono-methoxine (Sulfamono-methoxine), cpd-1, cpd-2, cpd-3, cpd-4 and cpd-5 inhibition of ALDOA activity assay:

[0042] The expressed and purified ALDOA protein was added to the 96-well plate according to different concentration gradients, and the ALDOA activity was determined by the aldolase activity colorimetric assay method. In particular ALDOA activity is determined by a colorimetric product whose absorbance at 450 nm is proportional to ALDOA activity. One unit of ALDOA is defined as the amount of enzyme that produces 1.0uM NADH per minute at a pH of 7.2 at 37°C ( figure 1 ).

Embodiment 2

[0043] Example 2: Compound Sulfamono-methoxine and cpd-5 inhibit ALDOA protein expression assay

[0044] Liver cancer, lung cancer, and pancreatic cancer cells were inoculated into 96-well plates at 1,000 cells per well, and cultured in 100 μl 10% FBS RPMI1640 culture medium. After culturing in an incubator for 24 hours, the cells were divided into groups, with 3 replicates in each group. Add the compounds Sulfamono-methoxine and cpd-5 in a 2-fold gradient, continue culturing until a specific detection time, collect the purified protein from the cells, add it to a 96-well plate that has been pre-bound with ALDOA antibody, add HRP-bound avidin for incubation, and add TMB Color development after the substrate solution, after adding sulfuric acid solution to terminate the enzyme substrate reaction, measure the color change at a wavelength of 450nm, and calculate the protein concentration of ALDOA after compound treatment ( figure 2 with image 3 ).

Embodiment 3

[0045] Example 3: Compound Sulfamono-methoxine and cpd-5 inhibit tumor cell viability assay

[0046] Liver cancer, lung cancer, and pancreatic cancer cells were inoculated into 96-well plates at 1,000 cells per well, and cultured in 100 μl 10% FBS RPMI1640 culture medium. After culturing in an incubator for 24 hours, the cells were divided into groups, with 3 replicates in each group. Add compounds Sulfamono-methoxine and cpd-5 in a 2-fold gradient and continue culturing until a specific detection time, add 10 μl CCK8 to each well, and incubate for 0.5-4 hours depending on the cells, use a microplate reader to detect cell viability at a wavelength of 450 nm, and calculate IC50( Figure 4 with Figure 5 ).

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Abstract

The invention discloses the application of a sulfamethoxine derivative in the preparation of antitumor drugs. The structure of the derivative is shown below. The derivative of the invention can specifically inhibit the activity of fructose diphosphate aldolase A, and expands the new application of sulfa-metamethoxine series compounds. The derivatives of the present invention can be used to prepare antitumor drugs, especially have good inhibitory effects on liver cancer cells, pancreatic cancer cells and lung cancer cells, and also have obvious inhibitory effects on mouse liver cancer PDX tumor growth, and have good applications prospect.

Description

technical field [0001] The present invention relates to the technical field of medicine, more specifically, relates to the application of a sulfamethoxine derivative in the preparation of antitumor drugs, in particular, the sulfamethoxine derivative is used as a fructose diphosphate aldolase A inhibitor exerts an antitumor effect. [0002] technical background [0003] As an important cause of death worldwide, malignant tumors seriously threaten human life and health. According to the analysis report on the prevalence of malignant tumors in China released by the National Cancer Center in 2019, the number of new cases of malignant tumors in the country in 2015 was about 3.929 million, resulting in about 2.338 million deaths, and the annual medical expenses caused by malignant tumors exceeded 2,200. billion yuan. The high incidence of malignant tumors seriously threatens our national health and causes huge economic losses. [0004] Fructose diphosphate aldolase A (ALDOA) ​​i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/635A61P35/00
CPCA61K31/635A61P35/00
Inventor 万国辉牛艺卜宪章
Owner SUN YAT SEN UNIV
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