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Synthesis and anticoagulant activity of pectin sulfates

机译:果胶硫酸盐的合成及抗凝活性

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In this article, we describe the first use of trisulfonated sodium amine as a sulfating reagent for preparing pectin sulfate in aqueous solution. The main reaction parameters that were expected to affect the degree of substitution (DS) were studied. The optimal reaction conditions for the synthesis of pectin sulfate were found to be as follows: the pH of the reaction medium, the reaction temperature, the reaction time, and the ratio of the mole of sodium nitrite (n _(NaNO2)) to the mass of pectin (m _(pectin)) were 6, 60°C, 12 h, and 2.5/190 mol/g, respectively. Pectin and pectin sulfate were characterized by Fourier transform infrared (FTIR) spectroscopy and ~(13)C-NMR. The FTIR spectra showed the characteristic absorptions of sulfate ester bonds at 1264 and 830 cm ~(-1). Furthermore, the anticoagulant activity of pectin sulfates with different DSs, concentrations, and molecular weights were investigated with respect to the activated partial thromboplastin time (APTT), thrombin time (TT) and prothombin time. The clotting assay indicated that the pectin sulfate prolonged APTT and TT through inhibition of the activity of antithrombin. These results suggest that the introduction of sulfate groups into the pectin structure improved its anticoagulant activity.
机译:在本文中,我们描述了三磺化钠胺作为硫酸化试剂在水溶液中制备果胶硫酸盐的首次用途。研究了预期会影响取代度(DS)的主要反应参数。发现用于合成果胶硫酸盐的最佳反应条件如下:反应介质的pH,反应温度,反应时间以及亚硝酸钠(n_(NaNO2))与亚硝酸钠的摩尔比。果胶的质量(m_(果胶))分别为6、60℃,12h和2.5 / 190mol / g。果胶和果胶硫酸盐通过傅里叶变换红外(FTIR)光谱和〜(13)C-NMR进行表征。 FTIR光谱表明在1264和830 cm〜(-1)处有硫酸酯键的特征吸收。此外,针对活化的部分凝血活酶时间(APTT),凝血酶时间(TT)和凝血酶原时间,研究了具有不同DS,浓度和分子量的果胶硫酸盐的抗凝活性。凝血试验表明,果胶硫酸盐通过抑制抗凝血酶的活性而延长了APTT和TT的时间。这些结果表明在果胶结构中引入硫酸根基团改善了其抗凝活性。

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