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Long-acting artesunate drug for preventing schistosome infection and preparation method thereof

A technology of artesunate and schistosomiasis, which is applied in the direction of anti-infective drugs, drug combinations, and pharmaceutical formulations, can solve the problems of not being suitable for schistosomiasis infection, unable to maintain effective drug concentration for a long time, and short half-life, so as to prevent schistosomiasis infection, Good application prospects and the effect of prolonging the half-life

Active Publication Date: 2013-11-27
JIANGSU INST OF PARASITIC DISEASES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the disadvantage of artesunate is that its half-life is relatively short. The half-life in rats is about 10 minutes, and the average plasma elimination half-life in healthy humans is 34.2 minutes. It cannot maintain the effective drug concentration in the body for a long time, so it is not suitable for those people. Prevention of schistosomiasis infection in people and domestic animals repeatedly exposed to infested water for a long time

Method used

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  • Long-acting artesunate drug for preventing schistosome infection and preparation method thereof
  • Long-acting artesunate drug for preventing schistosome infection and preparation method thereof
  • Long-acting artesunate drug for preventing schistosome infection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: (AS) n - Preparation of GST-NSP conjugates

[0040] (a) Construction of GST-NSP recombinant expression plasmid: pET41a(+) was used as the expression vector plasmid, and the expression vector plasmid pET41a(+) was first cut with BamH1 and Sal1, the specific conditions were as follows, the expression vector plasmid pET41a(+ ), 10 μL; BamH11 μL, Sal11 μL, digestion buffer 5 μL; double distilled water 33 μL, the total volume is 50 μL, reacted in a constant temperature water bath at 37 °C for 3 hours, and recovered the linearized pET41a(+) plasmid DNA by agarose gel electrophoresis The NSP / pET43.1a plasmid DNA containing the NSP gene fragment was subjected to the same double digestion, and the NSP gene fragment with a molecular weight of about 1368bp was recovered by agarose gel electrophoresis, such as figure 1 shown.

[0041] The recovered NSP gene fragment was ligated with the expression plasmid pET41a(+) which was digested with the above double restriction e...

Embodiment 2

[0051] Embodiment 2: the mensuration of coupling rate

[0052] Determination of AS, (AS) by ultraviolet scanning method n - GST-NSP and the highest absorption peak of GST-NSP. And use the highest absorption wavelength to measure AS, (AS) n - GST-NSP and absorbance value of GST-NSP.

[0053] According to the formula:

[0054]

[0055] (Note: ε represents the molar absorptivity; A represents the absorbance value; Ca represents the mole percentage of AS in the conjugate; Cb represents the mole percentage of the carrier protein NSP in the conjugate)

[0056] The results show that AS, (AS) n - GST-NSP and the highest absorption wavelengths of GST-NSP are: 260nm, 270nm and 280nm. Such as Figure 4 shown. This result indicates that the conjugate has its own unique light wave absorption peak (270nm), indicating that the conjugate is successfully prepared. The coupling ratio of AS was calculated to be 506:1, that is, 506 AS molecules were coupled to one GST-NSP protein.

Embodiment 3

[0057] Embodiment 3: (AS) n -GST-NSP conjugate in vitro killing effect and half-lethal dose

[0058] As determined (AS) n -Whether the GST-NSP conjugate retains the insecticidal activity of AS, AS, (AS) were determined by in vitro culture method n -Activity of the GST-NSP conjugate, the specific method is as follows:

[0059]1) Take 30 positive snails of Schistosoma japonicum and put them in a 100mL beaker, wash them several times with clean water, put a nylon mesh on the cup mask, add dechlorinated water and cover the nylon mesh, put it in an environment of 25-28℃, light it for about 2 hours, and escape cercariae.

[0060] 2) After soaking the 25×25mm coverslip in alcohol, wash it with tap water and wipe it clean.

[0061] 3) Fill the ice-bathed RPMI1640 basal medium into a 15mL conical glass centrifuge tube, and refrigerate on ice. Break off a 25×25mm cover glass, use tweezers to pick up a thin piece of glass with a suitable length and width (can enter the tube but not ...

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Abstract

The invention discloses a long-acting artesunate drug for preventing schistosome infection and a preparation method thereof. According to the method, a low immunogenicity GST-NSP protein is adopted, a chemical coupling method is employed to couple artesunate (AS) having an effect with the GST-NSP protein so as to prepare an (AS) n-GST-NSP conjugate. While maintaining the adolescent schistosome killing activity of the AS, the conjugate prolongs the half-life period of the AS in a host, not only has an early treatment effect on schistosome infection, and also has a function of preventing schistosome infection, thus providing a new means for preventing schistosome infection of human and a variety of reservoir animal hosts, and controlling the epidemics of schistosomiasis. The drug provided in the invention has good application prospects the pharmacy field, including treatment and prevention of schistosomiasis.

Description

technical field [0001] The invention belongs to the technical field of preparation of long-acting drugs, and in particular relates to a long-acting artesunate drug for preventing schistosome infection and a preparation method thereof. Background technique [0002] Schistosomiasis is a zoonotic parasitic disease that seriously endangers human health. Worldwide, this disease is mainly distributed in Africa, Asia and Latin America. About 600 million people in 74 countries and regions are threatened by schistosomiasis infection, and nearly 200 million people are infected with schistosomiasis. Schistosomiasis is prevalent in China. According to the national schistosomiasis epidemic report in 2011, there are still 454 counties in my country where schistosomiasis is endemic, with more than 280,000 patients and more than 510,000 sick cattle. The prevalence and harm of schistosomiasis It still exists in our country, and will even last for quite a long time. [0003] The "concomitant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/357A61P33/12C12N15/62C12N15/70C07K19/00A61K47/64
CPCY02A50/30
Inventor 余传信金一宋丽君王玠殷旭仁沈双
Owner JIANGSU INST OF PARASITIC DISEASES
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