合成化学2024,Vol.32Issue(10) :853-859.DOI:10.15952/j.cnki.cjsc.1005-1511.23132

新型大黄酸-牛磺酸化合物的合成、表征及其抑制黄嘌呤氧化酶的活性研究

Synthesis,Characterization of Novel Rhein-taurine Compound and Its Inhibitory Activity Research on Xanthine Oxidase

邢志华 高明宇 徐志远 申光焕 韩维娜 张文君 刘颖杰
合成化学2024,Vol.32Issue(10) :853-859.DOI:10.15952/j.cnki.cjsc.1005-1511.23132

新型大黄酸-牛磺酸化合物的合成、表征及其抑制黄嘌呤氧化酶的活性研究

Synthesis,Characterization of Novel Rhein-taurine Compound and Its Inhibitory Activity Research on Xanthine Oxidase

邢志华 1高明宇 1徐志远 1申光焕 1韩维娜 2张文君 1刘颖杰1
扫码查看

作者信息

  • 1. 哈尔滨商业大学 药学院,黑龙江 哈尔滨 150076
  • 2. 哈尔滨医科大学 药学院,黑龙江 哈尔滨 150081
  • 折叠

摘要

大黄酸(Rhein,RH)可以促进尿酸肠道排泄,改善肾脏损伤,降低血清尿酸水平.牛磺酸(Taurine,T)可以修复肾脏损伤,降低黄嘌呤氧化酶(Xanthine oxidase,XOD)活力,还可降低血清尿酸水平.因此两种化合物在降尿酸、改善肾损伤方面具有相似的药理活性.通过拼合原理,将RH和T通过酰胺键连接,合成大黄酸-牛磺酸化合物(T-RH),以期发挥协同增效作用.采用1H NMR、13C NMR、IR和MS(ESI)对T-RH化学结构进行表征,并考察了T-RH对体外XOD的抑制作用.结果表明:T-RH被成功合成,产率为 65.73%.T-RH对体外XOD的抑制作用均显著优于大黄酸(**P<0.01)和牛磺酸(##P<0.01),且抑制活性与T-RH的浓度呈正相关.

Abstract

Rhein(RH)can promote intestinal excretion of uric acid,improve kidney injury and reduce serum uric acid level.Taurine(T)can repair kidney damage,reduce xanthine oxidase(XOD)activi-ty,and also lower serum uric acid levels.Therefore,the two compounds have similar pharmacological activities in reducing uric acid and improving renal injury.The compound of rhein-taurine(T-RH)was synthesized by the combination of RH and T by amide bond to play a synergistic role.The chemical structure of T-RH was characterized by 1H NMR,13C NMR,IR,and MS(ESI).The inhibitory effect of T-RH on XOD in vitro was investigated.The results showed that T-RH was successfully synthesized and the yield was 65.73%.The inhibitory effect of T-RH on XOD in vitro was significantly better than RH(**P<0.01)and T(##P<0.01),and the inhibitory activity was positively correlated with the concentration of T-RH.

关键词

大黄酸/牛磺酸/黄嘌呤氧化酶/高尿酸血症/拼合原理

Key words

rhein/taurine/xanthine oxidase/hyperuricemia/combination principle

引用本文复制引用

基金项目

黑龙江省教育厅基础科研业务费项目(18XN082)

黑龙江省博士后面上资助项目(LBH-Z21066)

黑龙江省自然科学基金联合引导项目(LH2022H013)

黑龙江省横向合作项目(HL0092)

出版年

2024
合成化学
四川省化学化工学会 中国科学院成都有机化学研究所

合成化学

CSTPCD
影响因子:0.42
ISSN:1005-1511
参考文献量6
段落导航相关论文