Use of sulphonated calyx [5] arene in aspect of preparing medicament for treating toxicity of Paraguat

A technology of sulfonated cup and paraquat, which is applied in the field of biochemistry, can solve the problems of paraquat poisoning without specific antidote and effective treatment measures, and achieve good therapeutic effect, reduce toxicity and reduce the chance of exposure

Inactive Publication Date: 2010-09-29
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to solve the problem that there is no specific antidote and effective treatment measures for paraquat poisoning so far, and to provide a new application of sulfonated calix[5]arene in the preparation of medicines for treating paraquat poisoning

Method used

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  • Use of sulphonated calyx [5] arene in aspect of preparing medicament for treating toxicity of Paraguat
  • Use of sulphonated calyx [5] arene in aspect of preparing medicament for treating toxicity of Paraguat
  • Use of sulphonated calyx [5] arene in aspect of preparing medicament for treating toxicity of Paraguat

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Effect test

Embodiment 1

[0023] The first group of 10 18-20g healthy male Kunming mice were fed with 100 μL of normal saline as a control group, and observed continuously for 13 days. We found that the mice did not die (see figure 2 mouse survival curve). On the fourteenth day, the surviving mice were killed, weighed and dissected. The average body weight was 32.8 g (calculated from 4 randomly selected mice). The liver and lungs were in good condition, and no pathological changes occurred in the naked eye.

Embodiment 2

[0025] The second group of 10 18-20g healthy male Kunming mice were fed with paraquat at a dose of 106.99 mg / kg, and observed continuously for 13 days. We found that the mortality rate of the mice was as high as 90%, and the deaths all occurred after the administration. the first three days (see image 3 mouse survival curve). On the fourteenth day, the only surviving mouse was sacrificed, weighed and dissected. Its body weight was 14.0 g. The liver was dark red, the lungs were congested severely, and the lesions in the liver and lungs were obvious with the naked eye.

Embodiment 3

[0027] The third group of 10 18-20g healthy male Kunming mice were fed with sulfonated calix[5]arene at an equimolar dose to the second group, and observed continuously for 13 days. We found that the mice did not die (see Figure 4 mouse survival curve). On the fourteenth day, the surviving mice were killed, weighed and dissected. The average body weight was 33.4 g (calculated from 4 randomly selected mice). The liver and lungs were in good condition, and no lesions occurred in the naked eye. This indicates that the compound is non-toxic or of low toxicity.

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Abstract

The invention provides a new use of sulfonatocarlix(5)arene in preparing a medicine for treating paraquat poisoning. The sulfonatocarlix(5)arene reduces probability of contacts between paraguat and NAD(P)H in vivo by inclusion coordination of the sulfonatocarlix(5)arene and the paraguat, and reduces oxidizing ability of the paraguat, thus inhibiting generation of a free radical (HO<.>) which is poisonous to cells in vivo. Additionally, the lower edge of the sulfonatocarlix(5)arene is rich in phenolic hydroxyl structures which can provide active hydrogen to inactivate the HO<.> free radical. Experiments on mice prove that the sulfonatocarlix(5)arene is nontoxic or low toxic and greatly reduces toxicity of the paraguat. After a mouse is poisoned by orally taking the paraguat (dose: 106.99mg / kg), good curative effect can be achieved by orally taking two-fold sulfonatocarlix(5)arene for once, the total lethality is decreased from 90% to 30%, and the lowest lethality is even decreased to 0%. After a mouse is poisoned, good effect can be achieved by orally taking the sulfonatocarlix(5)arene in two hours after poisoning.

Description

【Technical field】 [0001] The invention belongs to the technical field of biochemistry, and relates to the treatment of water-soluble sulfonated calix[5]arene for the toxicity of paraquat in vivo. The invention finds that sulfonated calix[5]arene can significantly reduce the toxicity of paraquat in vivo. Therefore, sulfonated calix[5]arene can be used as a drug for clinical treatment of paraquat poisoning. 【Background technique】 [0002] Paraquat was first synthesized in the nineteenth century as a chemical indicator (redox indicator) and in 1962 as a herbicide in agriculture. It works on millions of growing species and more than a hundred crops, and is still widely used in more than 120 countries around the world. As an important class of non-selective contact herbicides, paraquat has the following characteristics: a) It is non-selective, that is to say, it can kill most annual grasses and broad-leaved weeds, as well as grown perennial weeds The top leaves of weeds; b) th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/05A61K31/185A61P39/02
Inventor 刘育王魁郭东升张弘青
Owner NANKAI UNIV
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