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Application of hycanthone in preparation of medicine for treating toxoplasma gondii infection diseases

A technology for infecting diseases and toxoplasma, which is applied in the field of parasitic disease control and toxoplasma control, and can solve problems such as difficult removal and damage to host cells

Inactive Publication Date: 2021-09-17
LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although Toxoplasma gondii and Schistosoma are both parasites that can parasitize the human body, they are quite different in terms of life history, pathogenesis, biological characteristics, and transmission routes. Schistosoma is an extracellular parasite, and intracellular parasites are more severe than extracellular parasites. Difficult to remove and more harmful, because intracellular parasites parasitize in cells and destroy host cells

Method used

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  • Application of hycanthone in preparation of medicine for treating toxoplasma gondii infection diseases
  • Application of hycanthone in preparation of medicine for treating toxoplasma gondii infection diseases
  • Application of hycanthone in preparation of medicine for treating toxoplasma gondii infection diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Determination of the inhibitory effect of hyenone on extracellular RH-2F tachyzoites by biochemiluminescence

[0027] Steps: Toxoplasma gondii type I virulent strain RH-2F expressing β-galactosidase was selected for growth inhibition assay. Harvest fresh and vigorous RH-2F tachyzoites from Vero cells, count on a hemocytometer, and adjust the concentration of RH-2F to 1×10 5 individual / mL. Various concentrations of hyenone were prepared in this way, and added to a white 96-well plate, with 0.25% DMSO as the control group, 10 μg / mL pyrimethamine as the positive control, and the medium only as the blank group. Add Beta- As for the detection reagent, after 30 minutes of action, the luminescence value was detected in a photometer to calculate the survival rate of RH-2F.

[0028] Result: results like figure 1 , IC of Hyenone against Toxoplasma gondii 50 The inhibitory effect on Toxoplasma gondii was dose-dependent, and the higher the concentration, the stronge...

Embodiment 2

[0029] The cytotoxicity of embodiment 2 hyenone to Vero cell

[0030] Steps: CCK-8 method was used to determine the toxicity of hyenone to Vero cells. Vero cells 1 x 10 5 cells / mL, inoculated in 96-well plate, and after culturing for 12 hours, various concentrations of compounds were added. The wells without compound were used as the control group, and the wells containing only the medium were used as the blank group. After culturing for 24 hours, add CCK-8 reagent, measure the OD value of each well in a microplate reader after 1-2 hours of action, calculate the cell survival rate according to the following formula, and repeat the independent experiment 3 times.

[0031] Cell viability (%) = (OD 实验组 -OD 空白组 ) / (OD 对照组 -OD 空白组 )×100%

[0032] Results: IC of Hyenone on African green monkey kidney cells 50 It was 27.66μg / mL, and it was dose-dependent. When the concentration was 100μg / mL, the cell survival rate was 24.53%, and when it was 50μg / mL, it was 33.87%. At 4 μg / mL...

Embodiment 3

[0033] Example 3 Determination of the antiproliferative effect of hyenone on intracellular RH-2F by biochemiluminescence

[0034] Steps: Put 1×10 5 RH-2F tachyzoites / mL were inoculated in a 96-well plate of monolayer Vero cells. After 2 hours of invasion, the non-invading tachyzoites were removed with Duchenne's phosphate buffered saline (DPBS), and seawater at a concentration of 4 μg / mL was added. enone, negative control group (0.25% DMSO) and positive control group (10 μg / mL pyrimethamine) were set at the same time. After 24 hours, add Glo Lysis Buffer to lyse the cells, then add Beta- The detection reagent measures the luminescence value and calculates the survival rate of RH-2F.

[0035]Result: The survival rate of RH-2F tachyzoites in the negative control group was recorded as 100%, and the RH-2F survival rate of hyinone and pyrimethamine was calculated, and the survival rate of positive control pyrimethamine was 15.54%. The survival rate was 14.57%. The results show...

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Abstract

The invention relates to the technical field of parasitic disease prevention and treatment, and provides application of hycanthone in preparation of a medicine for treating toxoplasma gondii infection diseases. It is found that the thioxanthene compound hycanthone has remarkable inhibitory activity on virulent or attenuated toxoplasma gondii of different genotypes and can inhibit proliferation of the toxoplasma gondii, and tests find that after hycanthone acts on the toxoplasma gondii in cells for 24 h, the survival rate of the toxoplasma gondii is only 14.57%, and the hycanthone is superior to that of an existing drug pyrimethamine for treating the toxoplasma gondii. The medication spectrum of the hycanthone is developed, an effective medicine with low side effect is provided for treating acute and chronic toxoplasma gondii infection, and a good application prospect is achieved.

Description

technical field [0001] The invention relates to the technical field of parasitic disease prevention and control, in particular to the field of toxoplasma gondii prevention, and specifically provides the application of hyinone in the preparation of medicines for treating toxoplasma gondii infection. Background technique [0002] Toxoplasmosis is an obligate intracellular parasitic protozoan disease caused by Toxoplasma gondii. Toxoplasma gondii can infect all warm-blooded animals including humans, even some cold-blooded animals, and can parasitize in all nucleated cells of the animal body. Moreover, toxoplasmosis has a wide range of transmission routes, and the host can be infected mainly through diet, vertical transmission, organ transplantation and blood transfusion. In immunocompetent individuals, toxoplasmosis is usually asymptomatic or a mild, self-limited infection. However, toxoplasmosis can be life-threatening in fetuses and newborns with underdeveloped immune syste...

Claims

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Application Information

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IPC IPC(8): A61K31/382A61P33/02
CPCA61K31/382A61P33/02
Inventor 张继瑜邱燕华翟斌涛王玮玮周绪正李冰杨枭荣魏小娟程富胜尚小飞
Owner LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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