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A Physicochemical and Pharmacological Study of the Newly Synthesized Complex of Albendazole and the Polysaccharide Arabinogalactan from Larch Wood

机译:落叶松木材新合成阿苯达唑与多糖阿拉伯半乳聚糖复合物的理化药理研究

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摘要

Inclusion complexes of albendazole (ABZ) with the polysaccharide arabinogalactan from larch wood Larix sibirica and Larix gmelinii were synthesized using a solid-state mechanochemical technology. We investigated physicochemical properties of the synthesized complexes in the solid state and in aqueous solutions as well as their anthelmintic activity against Trichinella spiralis, Hymenolepis nana, Fasciola hepatica, Opisthorchis felineus, and mixed nematodoses of sheep. Formation of the complexes was demonstrated by means of intrinsic solubility and the NMR relaxation method. The mechanochemically synthesized complexes were more stable in comparison with the complex produced by mixing solutions of the components. The complexes of ABZ showed anthelmintic activity at 10-fold lower doses than did free ABZ. The complexes also showed lower acute toxicity and hepatotoxicity. These results suggest that it is possible to design new drugs on the basis of the ABZ: arabinogalactan complex that are safer and more effective than albendazole.
机译:利用固态机械化学技术,合成了阿苯达唑(ABZ)与落叶松木落叶松和落叶松多糖阿拉伯糖半乳聚糖的包合物。我们研究了在固态和水溶液中合成的复合物的理化性质,以及它们对旋毛虫,膜翅果膜虫,Fasciola hepatica,Opishorchis felineus和绵羊混合线虫的驱虫活性。通过固有溶解度和NMR弛豫方法证明了络合物的形成。机械化学合成的配合物与通过混合组分溶液产生的配合物相比更稳定。与游离ABZ相比,ABZ复合物的驱虫活性低10倍。该复合物还显示出较低的急性毒性和肝毒性。这些结果表明,有可能在ABZ:阿拉伯半乳聚糖复合物的基础上设计比阿苯达唑更安全,更有效的新药。

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