葛根素-稀土配合物抗痛风性关节炎活性研究

Synthesis of puerarin rare earth complex and its anti-inflammatory activity in rats with gouty arthritis

以葛根素为配体,以稀土金属为中心,控制反应条件,设计合成了一系列葛根素-稀土(Gd,Nd,Pr,Sm,Eu)配合物,并对其结构进行红外(IR)表征.其中采用正交试验对葛根素-钕配合物的合成工艺进行考察.采用尿酸钠诱导的急性痛风性关节炎大鼠模型,检测葛根素-钕配合物对造模后2~48 h大鼠踝关节肿胀率的影响.结果表明,反应得到葛根素-稀土(Gd,Nd,Pr,Sm,Eu)配合物.其中葛根素与氯化钕配合反应的最佳合成工艺条件为p H=7,葛根素∶氯化钕物质量的比为3∶1,温度为80℃,此时产率为67.78%;IR结果表明,葛根素与稀土金属发生配位的是分子中的酚羟和羰基氧原子.葛根素-钕配合物对大鼠痛风性关节炎肿胀具有显著的抑制作用,且作用优于葛根素.

Puerarin rare earth complexes （ Gd, Nd, Pr, Sm, Eu） were synthesized with puer-arin as ligands and rare earth metal as the center by controlling the reaction conditions. The structures of these complexes including PUE - Gd、PUE - Nd、PUE - Pr、PUE - Sm and PUE -Eu were characterized through IR method respectively. The synthesis process of PUE - Nd was investigated by the orthogonal test. The effect of PUE - Nd on ankle swelling rate of rats induced by sodium urate detection during 2 -48 h was studied to detect its activity of acute gouty arthritis. The results showed that puerarin rare earth complexes（ Gd, Nd, Pr, Sm, Eu） were synthesized. The optimum reaction conditions of PUE - Nd were pH = 7,puerarin＊ sa-marium chloride by 3： 1, the temperature by 80 ℃. Under these conditions, the yield was 67. 78%. The result of IR showed that puerarin was coordinated with rare earth metal through the phenolic oxygen atoms and carbonyl oxygen atoms. The anti - inflammatory ac-tivity of PUE - Nd in Rats with gouty arthritis was better than that of puerarin.