Hirano S, Tanaka Y, Hasegawa M, Tobetto K, Nishioka A
Carbohydr Res. 1985 Mar 29;137:205-15. doi: 10.1016/0008-6215(85)85161-2.
The effect of some sulfated derivatives of chitosan on several blood-coagulant factors was examined in comparison with those of heparin (174 units/mg). The anticoagulant activity (units/mg) with respect to activated partial thromboplastin time was 331-379 for O-sulfated N-acetylchitosan (2), 190-287 for N, O-sulfated chitosan (1), and 21-31 for sulfated O-carboxymethylchitosan (3). The activity (units/mg) with respect to thrombin time was 70-87 for 2, 44-70 for 1, and 14-22 for 3. The activity (units/mg) with respect to antithrombin activity was 4.9-9.0 for 2, 4.7-8.7 for 1, and 3.3-6.0 for 3. No anti-(factor Xa) activity was observed with 1-3. A 6-sulfate group in the hexosaminyl moiety was a main active site; although a 3-sulfate group was not essential, it promoted the activity of the 6-sulfate group. N-Sulfate was not a prerequisite for activity. The biological activities were also related to molecular weight in the sequence 2 (26,000) greater than heparin (21,000) greater than 1 (12,000) greater than 3 (540,000). For the Methylene Blue complexes, 1, but neither 2 nor 3, exhibited a negative, induced Cotton effect similar to that of heparin.
研究了一些壳聚糖硫酸化衍生物对几种血液凝固因子的影响，并与肝素（174单位/毫克）进行了比较。对于O-硫酸化N-乙酰壳聚糖（2），活化部分凝血活酶时间的抗凝活性（单位/毫克）为331 - 379；对于N，O-硫酸化壳聚糖（1）为190 - 287；对于硫酸化O-羧甲基壳聚糖（3）为21 - 31。对于凝血酶时间的活性（单位/毫克），2为70 - 87，1为44 - 70，3为14 - 22。对于抗凝血酶活性的活性（单位/毫克），2为4.9 - 9.0，1为4.7 - 8.7，3为3.3 - 6.0。1 - 3均未观察到抗（因子Xa）活性。己糖胺部分的6 - 硫酸基团是主要活性位点；虽然3 - 硫酸基团不是必需的，但它促进了6 - 硫酸基团的活性。N - 硫酸化不是活性的先决条件。生物活性也与分子量有关，顺序为2（26,000）大于肝素（21,000）大于1（12,000）大于3（540,000）。对于亚甲蓝复合物，1表现出与肝素类似的负诱导科顿效应，而2和3则没有。
