【摘要】 以葛根素为配体,以金属钆为配位中心,通过控制反应条件,设计合成了葛根素-钆(Gd)配合物,并对葛根素-钆的结构进行红外(IR)表征.采用尿酸钠诱导的急性痛风性关节炎大鼠模型,利用敷线法考察造模后2～48 h大鼠踝关节肿胀率的变化,并对大鼠血清、肝脏及滑膜中PGE2、IL-1β、TNF-α的水平进行检测.结果表明,葛根素与稀土金属钆发生配位,得到葛根素-钆(Gd)配合物.葛根素-钆配合物对大鼠痛风性关节炎肿胀抑制作用比葛根素强,葛根素-钆配合物组大鼠血清、肝脏及滑膜中的PGE2、IL-1β和TNF-α水平均低于葛根素组.综上,说明葛根素-钆配合物抗痛风性关节炎活性优于其配体葛根素,其抗炎机制可能与降低体内PGE2、IL-1β和TNF-α的水平有关.更多还原

【Abstract】 Puerarin rare earth complexe( Gd) was synthesized with puerarin as ligands and rare earth metal gadolinium as the center by controlling the reaction conditions. The structure of the PUE-Gd was characterized through IR method. The effect of PUE-Gd on ankle swelling rate of rats induced by sodium urate detection during 2 ～ 48 h was studied by wire method,and the levels of PGE2,IL-1β and TNF-α in the serum,liver and synovium were detected to detect its Anti-inflammatory activity and mechanism in rats with gouty rrthritis. The result of IR showed that puerarin is coordinated with rare earth metal through the phenolic oxygen atoms and carbonyl oxygen atoms. The inhibitory effect of puerarin-gadolinium complexe on rat gouty arthritis swelling with in 48 h was more significant than that of puerarin. The levels of PGE2,IL-1β and TNF-α in the serum,liver and synovium of rats fed with puerarin-gadolinium complexe group were lower than that of rats fed with pueraringroup,respectively. To sum up,the anti-inflammatory activity of puerarin-gadoliniumcomplexe was better than that of puerarin in rats with gouty rrthriti and the mechanism of anti-inflammatory activity might be related to reducing levels of PGE2,IL-1 beta and TNF-alpha.更多还原