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Screening and application method of small-molecule inhibitor capable of inhibiting proliferation of toxoplasma gondii

A technology of small molecule inhibitor and Toxoplasma gondii, applied in the field of biomedicine, can solve the problems of limited source of small molecule drugs, high cost, no independent intellectual property rights, etc.

Inactive Publication Date: 2018-04-06
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, due to defects such as limited sources of small molecule drugs, high cost, and no independent intellectual property rights, it is not suitable for follow-up research and drug development.

Method used

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  • Screening and application method of small-molecule inhibitor capable of inhibiting proliferation of toxoplasma gondii
  • Screening and application method of small-molecule inhibitor capable of inhibiting proliferation of toxoplasma gondii
  • Screening and application method of small-molecule inhibitor capable of inhibiting proliferation of toxoplasma gondii

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Embodiment Construction

[0077] The scope of protection of the present invention is not limited to the following specific embodiments. Those skilled in the art can adopt other various specific embodiments to implement the present invention according to the disclosed content of the present invention, or use the design structure and ideas of the present invention to make Simple changes or modifications all fall within the protection scope of the present invention.

[0078] A specific embodiment of the present invention is a screening method for small molecule inhibitors capable of inhibiting the proliferation of Toxoplasma gondii, the process of which is as follows Image 6 As shown, the specific steps are as follows:

[0079] (1) Purification of HIS-TgAtg3 protein

[0080] Select the correct strain (Chen Di, Lin Jiaxin, Liu Yangyang, Li Xiangzhi, Chen Gaozhi, Nie Qinqin, Hua Qianqian, Hu Xin and Tan Feng; 2016; Identification of Toxoplasma TgAtg8-TgAtg3 Interaction; Journal of Tropical Medicine v.153,...

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Abstract

The invention discloses a screening method of small-molecule inhibitor capable of inhibiting proliferation of toxoplasma gondii. The method utilizes an Alphascreen experiment to primarily select 11 small-molecule inhibitors and one small-molecule accelerant, and the 12 drugs are used for clinical treatment. The 12 drugs are further screened at the cellular level, a plaque experiment proves that GSK J4HCL apparently inhibits the proliferation of toxoplasma gondii, and the value EC50 of the GSK J4HCL to toxoplasmagondii is determined to be about 4.5 muM by virtue of intracellular proliferation experiment. The AlphaScreen competitive inhibition experiment evaluates that the value IC50 of the GSK J4HCL for inhibiting the interaction of TgAtg8 to TgAtg3 is 11.01 muM. The CCK8 experiment is usedfor proving that the value IC50 of the drug for inhibiting the growth of a host cell is 34.359 muM which is far greater than the value EC50 of the drug for the insect, which illustrates that the GSKJ4HCL is a low-toxicity and high-efficiency drug for resisting the toxoplasma gondii.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, in particular to a screening and application method of a small molecule inhibitor capable of inhibiting the proliferation of toxoplasma gondii. Background technique [0002] Currently, Toxoplasma gondii is an important zoonotic pathogen that obligately parasitizes almost all nucleated cells. When the immunity of the infected population is low, the parasite can induce an inflammatory response, which can cause death in severe cases. Women who are infected for the first time during pregnancy may experience miscarriage, stillbirth or deformities. Livestock animals infected with Toxoplasma gondii are prone to miscarriages and reduced quality of meat / milk products, which bring huge economic losses to the livestock industry. In addition, animal food / products infected by Toxoplasma gondii is an important transmission route of the disease. With the changes in the eating habits of the Chinese popula...

Claims

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Application Information

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IPC IPC(8): G01N33/68
CPCG01N33/68
Inventor 刘淑贤谭峰张芳菲华倩倩曹佳欣王炎胡昕
Owner WENZHOU MEDICAL UNIV
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