首页|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

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

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

rheintaurinexanthine oxidasehyperuricemiacombination principle

邢志华、高明宇、徐志远、申光焕、韩维娜、张文君、刘颖杰

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哈尔滨商业大学 药学院,黑龙江 哈尔滨 150076

哈尔滨医科大学 药学院,黑龙江 哈尔滨 150081

大黄酸 牛磺酸 黄嘌呤氧化酶 高尿酸血症 拼合原理

黑龙江省教育厅基础科研业务费项目黑龙江省博士后面上资助项目黑龙江省自然科学基金联合引导项目黑龙江省横向合作项目

18XN082LBH-Z21066LH2022H013HL0092

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
年,卷(期):2024.32(10)
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