公开(公告)号：US08440238B2

公开(公告)日：2013-05-14

申请号：US12998169

申请日：2009-09-21

申请人： Kan Ding ,  Hong Qiu

发明人： Kan Ding ,  Hong Qiu

IPC分类号： A61K36/00

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: 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 2.8×105, 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 6.5×104 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 of 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： 本发明公开了一种从天麻BL提取的多糖的硫酸化衍生物及其制备方法及其在制备抗肿瘤药物中的应用，其中天竺葵多糖具有以下结构：其中x和y各自为整数， 和x + y = 16，“n”为整数，来自天麻的多糖的平均分子量估计为2.8×10 5，在0.5mg / mL水溶液中多糖的比旋光度为+ 95° 的; 硫酸化位置主要是天麻多糖的6-羟基，其0.5mg / mL水溶液中的平均分子量为6.5×10 4，比旋光度为+ 150.0°。 体内和体外实验表明，天竺葵多糖的硫酸化衍生物可抑制Id1的表达抑制血管生成，从而具有明显的抗肿瘤活性，对内皮细胞几乎无毒性，从而具有良好的抑制作用 被发展成抗肿瘤药物的前景。