Preparation of phosphated and sulfated polysaccharides and polyphenols and their physiological activities

对天然和化学合成的多糖进行硫酸酸化，研究其生物活性。首先，对肝素酶抑制活性进行了研究，发现(1 []SY。tri-substituted离开了。[)5)- β - d -葡聚糖硫酸酯，(1)；tri-substituted离开了。[)5)- β - d -半乳糖呋喃硫酸酯、硫酸木聚糖和硫酸凝血素具有抑制肝素酶的活性。然后，用APTT（活化部分凝血活素时间）测定抗凝活性。在被测化合物中，(1 []SY。tri-substituted离开了。[)5)- β - d -葡聚糖硫酸盐，(1)；tri-substituted离开了。[)5)- β - d -半乳糖呋喃硫酸酯、硫酸木聚糖和硫酸凝血素的抗凝活性较低。此外，4种多糖对b16bl6肺转移的抑制作用，即[1(]SY。tri-substituted离开了。[] 5)- β - d -葡聚糖硫酸酯，(1)；tri-substituted离开了。[)5)- β - d -半乳糖呋喃硫酸酯、硫酸木聚糖、硫酸凝乳素依次为：(1 []SY。tri-substituted离开了。[)5)- β - d -半乳糖呋喃硫酸酯> (l)；tri-substituted离开了。[)5)- β - d -硫酸葡聚糖>硫酸木聚糖；结果发现(1)(1)。tri-substituted离开了。[)5)- β - d -葡聚糖硫酸盐，(1)；tri-substituted离开了。[)5)- β - d -半乳糖呋喃硫酸酯和硫酸木聚糖的抗凝血活性低，但对Bi 6BL6肺转移的抑制活性高。

Natural and chemically synthesized polysaccharides were sulfated to investigate its biological activities. First, heparanase inhibition activities were investigated, It was found that (l(]SY.tri-substituted left.[)5)-beta-D-glucofuranan sulfate, (l(]SY.tri-substituted left.[)5)-beta-D-galactofuranan sulfate, xylan sulfate, and curdlan sulfate have heparanase inhibition activities. Then, anticoagulant activities were measured by an APTT (activated partial thromboplastin time). Among the tested compounds, (1(]SY.tri-substituted left.[)5)-beta-D-glucofuranan sulfate, (1(]SY.tri-substituted left.[)5)-beta-D-galactofuranan sulfate, xylan sulfate, and curdlan sulfate have low anticoagulant activities. Furthermore, inhibition activities of B 16BL6 lung metastasis by the four polysaccharides, i. e., (1(]SY.tri-substituted left.[)5)- beta-D-glucofuranan sulfate, (1(]SY.tri-substituted left.[)5)-beta-D-galactofuranan sulfate, xylan sulfate, and curdlan sulfate is in the order : (1(]SY.tri-substituted left.[)5)-beta-D-galactofuranan sulfate> (l(]SY.tri-substituted left.[)5)-beta-D-Glucofuranan sulfate> xylan sulfate, curdlan sulfate. It was found that (l(]SY.tri-substituted left.[)5)-beta-D-glucofuranan sulfate, (1(]SY.tri-substituted left.[)5)-beta-D-galactofuranan sulfate, and xylan sulfate have not only low anticoagulant activities but also high inhibition actibities of Bi 6BL6 lung metastasis.