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

磷酸化和硫酸化多糖和多酚的制备及其生理活性

• 批准号: 09556036
• 负责人: NAKATSUBO Fumiaki
• 金额: $ 8.83万
• 依托单位: KYOTO UNIVERSITY
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (B)
• 财政年份: 1997
• 资助国家: 日本
• 起止时间: 1997 至 1998
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-09556036/
• 关键词: Sulfation; Polysaccharides; Polyphenols; Physiological activities; Heparin binding assay; Anticoagulant activity; Lung metastases

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.

对天然和化学合成的多糖进行硫酸酯化，研究其生物活性。首先，研究了乙酰肝素酶抑制活性。[5]-β-D-呋喃葡聚糖硫酸盐，（10）SY. [5）-β-D-半乳呋喃硫酸酯、木聚糖硫酸酯和凝胶多糖硫酸酯具有乙酰肝素酶抑制活性。然后，通过APTT（活化部分凝血活酶时间）测量抗凝活性。在所测试的化合物中，（1（）SY.三取代左。[5]-β-D-呋喃葡聚糖硫酸盐，（1）SY.三取代的左。β-D-呋喃半乳聚糖硫酸酯、木聚糖硫酸酯和可得兰硫酸酯具有低的抗凝活性。此外，还观察了4种多糖对B 16 BL 6肺转移瘤的抑制作用.例如，（1）SY.三取代的左。[)5)-β-D-呋喃葡聚糖硫酸盐，（10）SY.三取代的左。（5）-β-D-半乳呋喃硫酸酯、木聚糖硫酸酯和凝胶多糖硫酸酯的顺序为：（1）SY.三取代的左。[5]-β-D-半乳呋喃硫酸酯>[1]-三取代的左半乳呋喃硫酸酯。（5）-β-D-呋喃葡聚糖硫酸酯>木聚糖硫酸酯、可得兰硫酸酯。发现（1（）SY. [5]-β-D-呋喃葡聚糖硫酸盐，（1）SY.三取代的左。β-D-半乳呋喃硫酸酯和木聚糖硫酸酯不仅具有低的抗凝活性，而且具有高的抑制Bi 6 BL 6肺转移的活性。

项目成果

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Michiko Hori 等人：“1,4-anhyfto-α-D-吡喃木糖衍生物的两种新合成方法”CarboHydr.Res.309 (1998)。

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Fumiaki Nakatsubo：“纤维素的首次化学合成及其未来前景”第 10 届 ISWPC 会议记录（1999 年）。

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上高原 浩ら: "Syntheses,Characterization,and Biological Activities of Sulfated Polysacoharides" 10th ISWPC Proceedings. (1999)

Hiroshi Kamikohara 等人：“硫酸化多糖的合成、表征和生物活性”第 10 届 ISWPC 会议记录（1999 年）。

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Yuji Mikawa：“苯基 4-O-甲基-β-D-葡萄糖苷的硫酸化”J.Wood Science。