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了硫酸盐化处理，以考察其生物活性。首先对乙酰肝素酶抑制活性进行了研究，发现(L三取代左旋)-β-D-葡糖呋喃硫酸酯、(L三取代左旋)-β-D-呋喃半乳糖硫酸酯、木聚糖硫酸酯和可得兰硫酸盐对乙酰肝素酶具有抑制活性。然后用活化部分凝血活酶时间(APTT)测定抗凝活性。在被试化合物中，(1)三取代左.[)5)-β-D-葡糖呋喃硫酸盐、(1)三取代左.[)5)-β-D-半乳呋喃硫酸盐、木聚糖硫酸酯和可得兰硫酸盐具有较低的抗凝血活性。此外，(1()三取代左.[)5)-β-D-葡聚呋喃硫酸酯、()5)-β-D-半乳呋喃硫酸酯、()5)-β-D-半乳呋喃硫酸盐、木聚糖硫酸盐和可得聚糖硫酸盐对B16BL6肺转移的抑制活性顺序为：(1)三取代左.[)5)-β-D-呋喃半乳糖硫酸酯&GT；(L()三取代左.[)5)-β-D-呋喃葡聚糖硫酸盐&GT；木聚糖硫酸酯、可德聚糖硫酸酯。研究发现，(L三取代左旋)-β-D-葡糖呋喃硫酸酯、(1三取代左旋)-β-D-半乳呋喃硫酸酯和木聚糖硫酸酯不仅具有较低的抗凝活性，而且对BI6BL6肺转移有较高的抑制活性。

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.