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Sulfated Derivatives of Arabinogalactan and Their Anticoagulant Activity
Russian Journal of Bioorganic Chemistry ( IF 1.1 ) Pub Date : 2021-01-13 , DOI: 10.1134/s1068162020070079
S. A. Kuznetsova , N. Yu. Vasilyeva , N. N. Drozd , M. A. Mikhailenko , T. P. Shakhtshneider , Yu. N. Malyar , B. N. Kuznetsov , N. V. Chesnokov

Abstract

A comparison of IR spectra and molecular weight distribution of arabinogalactan sulfates as sodium and ammonium salts obtained using various sulfating reagents was performed. According to the data, sulfated derivatives of arabinogalactan differ from each other in the nature of hydrogen bonds and molecular weight distribution. Using coagulological tests during activation of coagulation of platelet-poor human plasma in vitro, the anticoagulant properties of sulfated arabinogalactan derivatives in various salt forms differing in the preparation method, sulfation degree, and molecular weight were studied. It was found that the sample in the form of the sodium salt of sulfated arabinogalactan (SAG 1) with a sulfur content of 13.2 wt % and a polydispersity degree of 1.52 exhibited twofold greater anticoagulant activity than the sample in the form of the ammonium salt of sulfated arabinogalactan (SAG 2) with a sulfur content of 6.6 wt % and a polydispersity degree of 1.30. The antithrombin (aIIa) activity of the samples obtained by sulfation with a complex of pyridine and sulfuric anhydride (SAG 1) and a complex of sulfamic acid (SAG 2) was 23.42 ± 1.86 and 10.20 ± 1.50 U/mg, respectively; the value of the antifactor Xa activity of SAG 1 and SAG 2 was 2.13 ± 0.42 and 0.37 ± 0.08 U/mg; the aIIa/aXa ratio for SAG 1 and SAG 2 was 11 and 28, respectively. The antifactor Xa (aXa) activity of SAG, which is lower than that of unfractionated heparin (UFH), and a high aIIa/aXa activity ratio may contribute to less provocation of bleeding by SAG samples compared to UFH.



中文翻译:

阿拉伯半乳聚糖的硫酸盐衍生物及其抗凝活性

摘要

比较了使用各种硫酸化试剂获得的阿拉伯半乳糖硫酸盐钠盐和铵盐的红外光谱和分子量分布。根据数据,阿拉伯半乳聚糖的硫酸化衍生物在氢键的性质和分子量分布上彼此不同。通过体外贫血人血浆凝血活化过程中的凝血学测试,研究了各种盐形式的硫酸化阿拉伯半乳聚糖衍生物的抗凝血特性,其制备方法,硫酸化度和分子量均不同。发现该样品为硫酸化阿拉伯半乳聚糖(SAG 1)的钠盐形式,硫含量为13.2 wt%,多分散度为1。52以硫含量为6.6 wt%,多分散度为1.30的硫酸​​化阿拉伯半乳聚糖(SAG 2)铵盐形式,具有比样品高两倍的抗凝血活性。用吡啶和硫酸酐的复合物(SAG 1)和氨基磺酸的复合物(SAG 2)进行硫酸化制得的样品的抗凝血酶(aIIa)活性分别为23.42±1.86和10.20±1.50 U / mg;SAG 1和SAG 2的抗Xa活性值为2.13±0.42和0.37±0.08 U / mg。SAG 1和SAG 2的aIIa / aXa比分别为11和28。SAG的抗凝血因子Xa(aXa)活性低于普通肝素(UFH),并且较高的aIIa / aXa活性比与UFH相比,可能会减少SAG样品引起的出血。

更新日期:2021-01-13
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