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    SULFATED DERIVATIVE OF GASTRODIA ELATA POLYSACCHARIDE, PREPARATION METHOD AND USE THEREOF
    2.
    发明公开
    SULFATED DERIVATIVE OF GASTRODIA ELATA POLYSACCHARIDE, PREPARATION METHOD AND USE THEREOF 有权
    一天麻多糖的生产和使用硫酸酯化修饰和方法

    公开(公告)号：EP2338917A1

    公开(公告)日：2011-06-29

    申请号：EP09817166.3

    申请日：2009-09-21

    申请人： Shanghai Institute Of Materia Medica Chinese Academy of Sciences

    发明人： DING, Kan ,  QIU, Hong

    IPC分类号： C08B37/00 ,  A61K31/737 ,  A61P35/04

    CPC分类号： A61K31/737 ,  A61K36/8988 ,  C08B37/0003 ,  C08B37/0009

    摘要： The present invention discloses a sulfated derivative of polysaccharide extracted from gastrodia elata BL., the preparation method thereof and the use thereof in preparing antineoplastic medicaments, wherein, the gastrodia elata polysaccharide has the following structure: α - D - GLc ⁢ p - 1 [ → 4 - α - D - Glc ⁢ p - ( 1 ] x ↓ 6 - { [ → 4 ) - α - D - Glc ⁢ p - ( 1 ] y → 4 - α - D - Glc ⁢ p - ( 1 → } n -
    wherein, x and y are each an integer, and x + y = 16,
    "n" is and integer, and
    the mean molecular weight of the polysaccharide from gastrodia elata is estimated as 2.8 x 10 5 , the specific rotation of the polysaccharide is +95° in a 0.5 mg/mL aqueous solution thereof;
    the sulfated position is mainly at 6-hydroxy of the gastrodia elata polysaccharide, with mean molecular weight of 6.5 × 10 4 and a specific rotation of +150.0° in a 0.5 mg/mL aqueous solution thereof. In vivo and in vitro experiments indicate that the sulfated derivative of gastrodia elata polysaccharide can inhibit the tumor growth by suppressing the expression ofi Id1 to inhibit angiogenesis, and therefore has an obvious antitumor activity, and shows almost nontoxicity to endothelial cells, thereby having a good prospect of being developed into antineoplastic medicaments.

    摘要翻译： 。本发明盘松动从天麻，及其制备方法和在制备抗肿瘤药物，worin其使用提取的多糖的硫酸化衍生物，天麻多糖具有以下结构：± - D - GLC¢p - 1 [† '4 - ± - D - GLC¢对 - （1]׆“6 - {[†' 4） - ± - D - GLC¢对 - （1 - ] Y†'4 - ± - D - GLC¢对 - （1†“} -N - worin，x和y各自为整数，并且x + y = 16，‘n’是与整数，并且从天麻多糖的平均分子量被估计为 2.8×10 5，该多糖的比旋光为+ 95℃在0.5毫克/毫升wässrige其溶液;硫酸化的位置是主要在天麻多糖的6-羟基，具有6.5×10 4，平均分子量 +的在0.5mg / mL的溶液的特定旋转wässrige其体内。和体外实验表明DASS死克150.0°的硫酸化衍生物 astrodia天麻多糖可以通过抑制表达OFI Id1的抑制血管生成抑制肿瘤的生长，并因此具有明显的抗肿瘤活性，并显示出几乎无毒到内皮细胞，从而具有被开发成抗肿瘤药物的良好的应用前景。