Antimalarial drug taking protein degradation pathway as target

A drug, proteasome technology, used in drug combinations, anti-infective drugs, pharmaceutical formulations, etc.

Inactive Publication Date: 2012-07-04
SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, first detected in 2008 on the border of Thailand and Cambodia, Plasmodium falciparum has developed resistance to artemisinin-based drugs

Method used

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  • Antimalarial drug taking protein degradation pathway as target
  • Antimalarial drug taking protein degradation pathway as target
  • Antimalarial drug taking protein degradation pathway as target

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Embodiment 1: Plasmodium proteasome inhibition experiment

[0066] I. The experimental materials used in this embodiment include: RPMI 1640 medium (GibcoBRL company), rabbit serum (from rabbits, self-made), mouse anti-polyubiquitinylated protein monoclonal antibody (Enzo company), PVDF membrane (MILLIPORE company ), NC membrane (BIO-RAD company), SuperSignal chemiluminescence liquid (Thermo company). Plasmodium Hainan strain (FCC1 / HN) came from the Institute of Parasitic Diseases, Chinese Center for Disease Control and Prevention; human red blood cells (type O) came from Shanghai Ruijin Hospital; tripterygium came from aladdin company.

[0067] Other unmentioned experimental materials, instruments, reagents, etc. are various materials, instruments and reagents routinely used in this field.

[0068] II. the experimental method of the present embodiment is as follows:

[0069] (1) Plasmodium culture

[0070]Plasmodium culture conditions are RPMI 1640 medium, add 22mM H...

Embodiment 2

[0135] Embodiment 2: tripterine inhibits the proliferation of Plasmodium

[0136]Commonly used antimalarial drug screening methods include in vitro microtest (WHO microtest, also known as WHO schizont maturation assay) recommended by WHO, isotopic microtest (isotopic microtest), lactate dehydrogenase method (parasite lactate dehydrogenase (pLDH), double-site enzyme-linked lactate dehydrogenase immunodetection assay (DELI), histidine-rich protein II (HRP2) and fluorescence assay method (fluorescence assay, FA) and so on. Among them, in vitro micromethod and isotope microtest method are antimalarial drug screening and sensitivity detection methods recommended by WHO. The present invention uses these two methods respectively to detect the screening platform for the influence of the compound to be tested on the proliferation of Plasmodium falciparum in vitro. In vitro micromethod [see Rieckmann, K.H., etc., Drug Sensitivity of Plasmodium-Falciparum-Invitro Microtechnique.Lancet,...

Embodiment 3

[0139] Embodiment 3: animal experiments

[0140] Plasmodium P.berghei NK65 strain and wild-type mouse BALB / c (from Shanghai Experimental Animal Center) were used in this experiment.

[0141] Inoculate 10 times per week intraperitoneally 6 The way parasites infect blood cells maintain passage of Plasmodium parasites in mice.

[0142] In vivo anti-malarial experimental steps are as follows:

[0143] The mice were randomly divided into 5 groups, and 10 groups were inoculated intraperitoneally 6 Plasmodium infection was carried out in the manner of carrying worms infecting blood cells, and at the same time, group drug treatment was started. The method of administration is tail vein injection. 5 groups of dosages are respectively negative control (the PBS solution of DMSO), positive control (chloroquine of 50mg / kg dosage), experimental group (50mg / kg, 150mg / kg, tripterine of 500mg / kg dosage). Dose every 24 hours. On the 4th, 7th, and 15th days, rat blood was collected, smeare...

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Abstract

The invention relates to an antimalarial drug taking a protein degradation pathway as a target. Particularly, the invention relates to use of tripterine or derivatives of the tripterine in the preparation of drugs for treating malaria and use of the tripterine or the derivatives of the tripterine in the preparation of drugs for the inhibition of proteasome. The invention further relates to a pharmaceutical composition containing the tripterine or the derivatives of the tripterine.

Description

technical field [0001] The present invention relates to antimalarial drugs targeting protein degradation pathways. Specifically, the present invention relates to the use of tripterine or its derivatives in the preparation of medicines for treating malaria. Background technique [0002] Research on protein degradation has initially focused on understanding the process by which animals digest protein foods. This is an energy-free process that takes place outside the cell. Proteolytic enzymes such as pepsin, trypsin, and chymotrypsin involved in these extracellular protein degradation processes have been common tools for studying proteins. For the protein degradation process that occurs in the cell, for a long time people have focused on the protein degradation process that occurs in the lysosome. This is a process of hydrolytic enzymes in an acidic environment that degrades major biomacromolecules including proteins, nucleic acids, sugars, and lipids. For the degradation o...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K31/585A61P33/06
CPCY02A50/30
Inventor 胡荣贵眭飞
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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