浅析利用糖苷化衍生法合成鬼臼毒素类抗肿瘤药物  

Analysis on the Synthesis of Podophyllotoxin Derivative by Glycosylation Methods

作　　者：席芳 Xi Fang(Zhengzhou Health Vocational College,Zhengzhou Henan 450199,China)

机构地区：[1]郑州卫生健康职业学院,河南郑州450199

出　　处：《江西化工》2023年第4期25-31,共7页Jiangxi Chemical Industry

摘　　要：在肿瘤化疗治疗的过程中,发现导致疗效反复甚至失败的重要原因是肿瘤多药耐药性(MDR)问题越来越严重。寻找高效低毒、对多药耐药肿瘤有效的合成类抗肿瘤药物始终是当前抗肿瘤药物研究领域的热点。鬼臼毒素(Podophyllotoxin)是天然木质素中的代表性化合物,源于鬼臼属植物的根茎,具有显著的抗肿瘤活性,但由于其毒性太大,限制了其作为抗肿瘤药物的应用。经由合成以及系统活性测试,将鬼臼毒素进行糖苷化衍生后提高了所需的抗肿瘤活性,而且毒副作用也大大降低。在使用鬼臼毒素糖苷成功开发成临床药物的启发下,对木质素糖苷的研究迅速增多,糖苷化衍生合成思路受到广泛关注。本文主要借助前人对糖苷化的研究报告,浅析鬼臼素类衍生物合成路线及材料方面操作思路,旨在更好地将鬼臼毒素类抗肿瘤药有效地应用到医学临床中,提升医疗临床治疗效果与价值。The aim of this study was to develop a new synthetic method for the synthesis of podophyllotoxin derivative and to investigate the antitumor activity of the synthesized compound.Podophyllotoxin is a representative compound in natural lignin,which originates from the roots of Dysosma plants and has significant anti-tumor activity.Through system activity test,glycosylation derivation of Podophyllotoxin not only improve the anti-tumor activity,but also greatly reduce the side effects.The synthesis of glycosidic derivatives has attracted extensive attention.This paper mainly analyzes the synthetic routes and material operation ideas of podophyllotoxin derivatives with the help of previous research reports on glycosylation,aiming to better apply Podophyllotoxin anti-tumor drugs to clinical medicine and improve the clinical therapeutic effect and value of medicine.

关 键 词：抗肿瘤活性 糖苷化 鬼臼毒素衍生物 结构修饰 

分 类 号：O626[理学—有机化学]