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A long-acting artesunate drug for preventing schistosomiasis infection and its preparation method

A technology of artesunate and schistosomiasis, applied in the directions of anti-infective drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of short half-life, inapplicable to schistosomiasis infection, unable to maintain effective drug concentration for a long time, etc., to prolong half-life, prevent Schistosomiasis infection, the effect of good application prospects

Active Publication Date: 2015-09-30
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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  • A long-acting artesunate drug for preventing schistosomiasis infection and its preparation method
  • A long-acting artesunate drug for preventing schistosomiasis infection and its preparation method
  • A long-acting artesunate drug for preventing schistosomiasis infection and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0040] (a) Construction of GST-NSP recombinant expression plasmid: Using pET41a(+) as the expression vector plasmid, firstly digest the expression vector plasmid pET41a(+) with BamH1 and Sal1. The specific conditions are as follows, the expression vector plasmid pET41a(+ ), 10μL; BamH11μL, Sal11μL, enzyme digestion buffer 5μL; double-distilled water 33μL, total volume 50μL, react in a constant temperature water bath at 37°C for 3 hours, and recover 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] Connect the recovered NSP gene fragment with the above-mentioned double-enzyme-cut expression plasmid pET41a(+) to construct a recombinant expression plasmid GST-NSP...

Embodiment 2

[0051] Example 2: Determination of coupling rate

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

[0053] According to the formula:

[0054]

[0055] 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 -The highest absorption wavelengths of GST-NSP and GST-NSP are: 260nm, 270nm and 280nm. Such as Figure 4 Shown. This result indicates that the conjugate has its own unique light absorption peak (270nm), indicating that the conjugate was successfully prepared. After calculating the coupling ratio of AS is 506:1, that is, 506 AS molecules are coupled to a GST-NSP protein.

Embodiment 3

[0057] Example 3: (AS) n -GST-NSP coupling in vitro killing children's insects and its half-lethal dose

[0058] For Assay (AS) n -Whether the GST-NSP conjugate retains the insecticidal activity of AS, use the in vitro culture method to determine AS and (AS) respectively n -GST-NSP conjugate activity, the specific method is as follows:

[0059] 1) Take 30 positive Oncomelania snails of Schistosoma japonicum into a 100mL beaker, wash several times with clean water, put a nylon net on the cup mask, add dechlorinated water and cover the nylon net, place it at 25-28℃, light for about 2h, and escape Cercariae.

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

[0061] 3) Load the ice-bathed RPMI1640 basal medium in a 15mL conical glass centrifuge tube, and place it on ice for refrigeration. Break off the 25×25mm cover glass, use tweezers to grab the glass flakes of appropriate length and width (can enter the tube but not reach the bott...

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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 long-acting medicine preparation, and specifically relates to a long-acting artesunate medicine for preventing schistosomiasis infection and a preparation method thereof. Background technique [0002] Schistosomiasis is a zoonotic parasitic disease that seriously endangers human health. At present, the 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 japonica 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 a long time. [0003] The characteri...

Claims

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Application Information

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Patent Type & Authority Patents(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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