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1. 发明申请

US20070042970A1 Folate-modified cholesterol-bearing pullulan as a drug carrier 审中-公开
标题翻译：叶酸修饰的含胆固醇的支链淀粉作为药物载体
公开(公告)号：US20070042970A1
公开(公告)日：2007-02-22
申请号：US11207888
申请日：2005-08-22
申请人： Junzo Sunamoto , Kazutoshi Ushio , Masaaki Hidaka
发明人： Junzo Sunamoto , Kazutoshi Ushio , Masaaki Hidaka
IPC分类号： A61K31/704 , A61K31/7076
CPC分类号： A61K31/704 , A61K9/5161 , A61K31/7076 , A61K47/551 , A61K47/554 , A61K47/61
摘要： Folate modified cholesterol-bearing pullulan (FA-CHP) was synthesized by the reaction of folic acid γ-2-aminoethylamide and 4-nitorophenyl chloroformate-activated cholesterol-bearing pullulan, wherein folate and pullulan are connected through a NH—CH2—CH2—NH group. Approximately 0.5-1 folates are connected per about 100 glycoside units of pullulan. Then, several combinations of FA-CHP, cholesterol-bearing pullulan (CHP) and doxorubicin (DOX) mixture were tested for cancer selective cytotoxicity. A mixture of FA-CHP, CHP and DOX of 1:4:0.02 (weight ratio) gave sharp and selective damage to cells of a human epidermoid cancer KB known as expressing a high level of folate receptor. The same mixture inhibited the growth of HuH7 cells, which is a human hepatocellular carcinoma and is unknown as a folate receptor.
摘要翻译：叶酸修饰的含胆固醇的支链淀粉（FA-CHP）通过叶酸γ-2-氨基乙酰胺和4-硝苯基氯甲酸酯活化的含胆固醇的支链淀粉的反应合成，其中叶酸和支链淀粉通过NH-CH 2个-CH 2 -NH基。每个约100个糖基单位的支链淀粉连接约0.5-1个叶酸盐。然后，测试FA-CHP，含胆固醇的支链淀粉（CHP）和多柔比星（DOX）混合物的几种组合的癌症选择性细胞毒性。 1：4：0.02（重量比）的FA-CHP，CHP和DOX的混合物对称为表达高水平叶酸受体的人表皮样癌细胞的细胞产生明显和选择性的损伤。相同的混合物抑制HuH7细胞的生长，HuH7细胞是人类肝细胞癌，并且作为叶酸受体是未知的。

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