[Neutralization of anticoagulant activity of heparin by N-[(2-hydroxy-3-trimethylammonium) propyl] chloride derivatives of chitosan].

B Ts Shagdarova, N N Drozd, A V Il'ina, Yu S Logviniva, V P Varlamov
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引用次数: 0

Abstract

Alkylated derivatives of low molecular weight chitosan with different substitution degrees of 98, 40, and 9% (I, II, and III respectively) have been synthesized. The structure of the obtained derivatives was defined by spectral assays (IR-spectroscopy and proton magnetic resonance). Chitosan derivatives were characterized with positive zeta-potential (33–51 mV) and solubility from 2 to 100 mg/mL in pH 7.4 and 25°C. It was shown that, at a concentration of 0.0014–0.0029 mg/mL, derivative I, as well as protamine sulfate, could be used to neutralize the anticoagulant activity of unfractionated or low molecular weight heparin. At a concentration of 0.0029–0.58 mg/mL, derivative I enhanced platelet aggregation, which would be necessary when hemostatic compounds or materials were used. Derivatives II and III enhanced platelet aggregation to a lesser extent.

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[壳聚糖N-[(2-羟基-3-三甲基铵)丙基]氯衍生物中和肝素抗凝血活性]。
合成了取代度分别为98、40和9% (I、II和III)的低分子量壳聚糖烷基化衍生物。所得衍生物的结构通过光谱分析(红外光谱和质子磁共振)确定。壳聚糖衍生物在pH 7.4和25°C条件下具有正ζ电位(33-51 mV)和2 ~ 100 mg/mL的溶解度。结果表明,在0.0014-0.0029 mg/mL的浓度下,衍生物I和硫酸鱼精蛋白可以中和未分离或低分子量肝素的抗凝血活性。当浓度为0.0029-0.58 mg/mL时,衍生物I增强血小板聚集,这在使用止血化合物或材料时是必要的。衍生物II和III在较小程度上增强血小板聚集。
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