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Application of cyclopamine or derivatives thereof

A technology of derivatives and uses, applied in the field of new uses of cyclotamine or its derivatives, can solve the problems of unsustainable insecticidal effect, failure to eliminate schistosomiasis, and no public reports of cyclotamine anti-schistosomiasis drugs, etc. Achieve the effect of strong killing of schistosomiasis juveniles and broad application prospects

Inactive Publication Date: 2020-03-03
SHANGHAI VETERINARY RES INST CHINESE ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Large-scale treatment can achieve 60-90% reduction in worm load, but not complete elimination of schistosomiasis
(2) Praziquantel is a racemate, and half of the dose used is pharmacologically ineffective
(3) The praziquantel absorbed into the body can be rapidly metabolized into ineffective metabolites through hydroxylation. Only a limited amount of drugs can enter the blood circulation and directly contact with schistosomiasis. The action time of the drugs is short and the insecticidal effect is not durable
[0006] Previous studies on cyclotamine focused on the drug's tumor suppressive effect, and so far there is no public report on the use of cyclotamine as an anti-schistosomal drug

Method used

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  • Application of cyclopamine or derivatives thereof
  • Application of cyclopamine or derivatives thereof
  • Application of cyclopamine or derivatives thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The anti-schistosome experiment of embodiment 1 cyclotamine

[0025] 1. Material method

[0026] 1.1 Collection of schistosome material

[0027] The cercariae of Anhui strain infected healthy New Zealand white rabbits by patching on the abdomen. The patching lasted for 20 minutes. The number of infected rabbits is about 5000. Necropsy was performed 14 days after infection. The cercariae parasitize in the hepatic portal vein and mesenteric vein. The worms are flushed out by perfusion of the hepatic portal vein, and the worms are washed lightly with PBS with high pressure sterilization and anticoagulant to remove the impurities and blood cells mixed in the worms.

[0028] 1.2 Determination of the range of effective concentration of cyclotamine

[0029] Dissolve 1.23 mg of cyclotamine powder in 150 μl of ethanol to a final concentration of 20 mM, and store at -20°C. An appropriate amount of 14-day-old Schistosoma japonicum larvae was placed in a 12-well culture plate,...

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Abstract

The invention discloses application of cyclopamine or its derivatives in preparing a medicine for preventing or treating schistosomiasis. The invention also discloses a pharmaceutical composition containing cyclopamine or its derivatives. The cyclopamine or its derivatives of the invention can kill 14-day-old schistosomulum japonicum when the concentration is more than 1uM, has a strong killing effect on schistosomulum japonicum, is expected to become a new antischistosomal drug, and has a very broad application prospect.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a new application of cyclotamine or its derivatives. Background technique [0002] Schistosomiasis is a zoonotic parasitic disease caused by schistosomiasis infection. The disease causes severe pathological damage to multiple organs of the host, resulting in anemia, malnutrition, growth retardation, reduced labor capacity and even death. It is recognized that the disease is harmful to human and animal health and The social and economic impact is huge, and it is listed by the World Health Organization as one of the six major tropical diseases for key prevention and control. At present, 78 countries and regions in the world have reported schistosomiasis, about 200,000 people die from the disease every year, and 800 million people are at risk of schistosomiasis infection, mainly school-age children. According to the data updated by the World Health Organization in October 2017,...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61K31/4985A61P33/12
CPCA61K31/58A61K31/4985A61P33/12Y02A50/30
Inventor 苑纯秀许静秀冯新港张佳男贾英英
Owner SHANGHAI VETERINARY RES INST CHINESE ACAD OF AGRI SCI
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