高等学校化学学报2016，Vol.37Issue(8)：1451-1459,9.DOI:10.7503/cjcu20160222
间接糖基化马蹄金素衍生物的合成及抗乙肝病毒活性研究
Synthesis and Anti-HBV Activities of the Indirect Galactopyranosyl Derivatives of Matijin-Su†
摘要
Abstract
To explore the effect of the length of the linker on the activities of the derivatives of Matijin-Su ( MTS) with potential for hepatic targeting, six galactosyl derivatives of MTS with potential for hepatic targe-ting were synthesized by binding galactosyl to derivatives of MTS using triethylene glycol or tetraethylene glycol as a linking arm, and their structures were confirmed by means of 1 H NMR, 13 C NMR, 1 H-1 H COSY, HMQC and ESI-MS. The anti-HBV activities of those compounds were evaluated using HepG2 2. 2. 15 cells. The screening results showed that all the target compounds had inhibitory effect on HBV DNA replication in HepG2 2. 2. 15 cells in a dose-response manner. The inhibition rates of compounds 15b ( 72. 24%), 15c(56. 49%), 15f(65. 24%) on the replication of HBV DNA were better than other tested compounds, when the in concentration of the drug was 50 μg/mL. The results can provide reference for further research of hepatic targeting MTS derivatives. For the evaluation of the hepatic target distribution of galactopyranosyl derivatives of MTS, compound 15b with best anti HBV activity will be selected to do tissue distribution experi-ments in vivo and comparative study with derivative of MTS(13b) and Y101.关键词
肝靶向/半乳糖/马蹄金素衍生物/抗HBV活性Key words
Hepatic targeting/Glacatose/Derivatives of Matijin-Su( MTS)/Anti-hepatitis B virus activity分类
化学化工引用本文复制引用
徐广灿,袁洁,刘青川,黄正明,梁光义,徐必学..间接糖基化马蹄金素衍生物的合成及抗乙肝病毒活性研究[J].高等学校化学学报,2016,37(8):1451-1459,9.基金项目
国家自然科学基金(批准号:81360472)资助.? Supported by the National Natural Science Foundation of China(No.81360472) （批准号:81360472）
