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    • 9. 发明公开
    • FRUCTOSYLATED PUERARIN, AND PREPARATION METHOD THEREFOR AND USE THEREOF
    • 贝壳葡萄酒(VERWENDUNG,FRERGOYLIERTES PUERARIN,HERSTELLUNGSVERFAHRENDAFÜRUND SEINE VERWENDUNG)
    • EP2615100A1
    • 2013-07-17
    • EP11831919.3
    • 2011-09-23
    • Nanjing University of Technology
    • HE, BingfangWU, XuemingCHU, JianlinWU, BinZHANG, SenOUYANG, Pingkai
    • C07H17/07C12P19/60A61K31/7048A61P9/00A61P35/00
    • C07H15/26A61K31/353A61K31/7048C12N1/20C12P17/162C12P19/58C12P19/605
    • This invention is in the field of bio-pharmaceutical technology, specifically involving the new derivatives of puerarin, the biological conversion methods and their pharmaceutical applications. This invention published a new type fructosylated puerarin with structure as shown in Formula (I) below, its preparation method being converting puerarin into fructosyl and fructose oligosaccharyl puerarin in a aqueous phase or nonaqueous phase system by bioconversion method, and at a puerarin concentration of 107.5g/L, the monofructosyl-β (2,6)-puerarin concentration can reach 111.7g/L, and conversion rate of fructosylated puerarin is 90%. By adsorption with AB-8 macroporous resin and gradient elution, product with purity over 97% and complying drug specification can be obtained, with extraction rate over 80%. Tests have shown that fructosylated puerarin is effective to acute myocardio ischemia, and can markedly suppress in vitro the proliferation of human breast cancer cell strain MDA-MB-23 and human chronmyelogenors leukemia cell strain K562, and such oligosaccharylated puerarin has low toxicity, with good application prospects in making drugs to treat cardio-cerebral vascular diseases and/or tumour diseases.
    • 本发明在生物制药技术领域,具体涉及葛根素的新衍生物,生物转化方法及其制药应用。 本发明公开了一种具有如下式(I)所示结构的新型果糖基葛根素,其制备方法是通过生物转化法将葛根素转化为水相或非水相体系中的果糖基和果糖寡糖基葛根素,葛根素浓度为107.5 g / L,单糖基-2(2,6) - 葛根素浓度可达111.7g / L,果糖基葛根素的转化率为90%。 通过AB-8大孔树脂吸附和梯度洗脱,可以得到纯度超过97%,符合药品规格的产品,提取率超过80%。 测试结果表明,果糖醛酸葛根素对急性心肌缺血有效,体外可显着抑制人乳腺癌细胞株MDA-MB-23和人类慢性白血病细胞株K562的增殖,而这种寡糖基化的葛根素毒性低,具有良好的 制造药物治疗心脑血管疾病和/或肿瘤疾病的应用前景。