芹菜素-钐配合物的合成及其抗小鼠高尿酸血症研究

Synthesis of Apigenin-samarium Complex and Its Anti-hyperuricemia in Mice

秉承中药配位化学理论,以具有一定抗炎、抗痛风活性的芹菜素(AP)为配体,以稀土金属钐(Ⅲ)离子为配位中心,设计合成芹菜素-钐配合物(AP-Sm),以期提高抗高尿酸血症活性。采用紫外(UV)、红外(IR)、氢核磁共振(1H NMR)、电导法、差热-热重分析(TG-DTA)等技术对配合物的化学结构进行表征。考察配合物对酵母浸粉联合氧嗪酸钾诱导的高尿酸血症小鼠模型中尿酸、黄嘌呤氧化酶及超氧阴离子水平的影响。结果表明,芹菜素与钐(Ⅲ)离子配位生成了配合物,配合物组成式为:Sm(C_(15)H_9O_5)_3. 2H_2O。芹菜素A环的5-OH和C环的4位C=O与钐(Ⅲ)离子形成了配合物,且芹菜素与钐(Ⅲ)离子的配位比为3。抗高尿酸血症活性研究发现,芹菜素-钐配合物对高尿酸血症小鼠黄嘌呤氧化酶的抑制作用、清除超氧阴离子能力、降低血清尿酸水平及促进尿酸排泄能力均优于芹菜素。综上说明芹菜素与钐(Ⅲ)离子配位后,所得配合物抗高尿酸血症活性增强。

Based on the theory of traditional Chinese medicine coordination chemistry,an AP-Sm complex was synthesized with anti-inflammatory and anti-gout agent apigenin(AP)as a ligand,and rare earth metal Sm(Ⅲ)ion as coordination center to improve the activity of anti-hyperuricemia.The chemical structure of the AP-Sm complex was characterized by UV,IR,and 1H NMR,conductometry and TG-DTA.Effect of AP-Sm complex on uric acid(UA)level,xanthine oxidase(XOD)activity and superoxide anion(SOA)level in hyperuricemia mice induced by yeast extract combined with potassium oxazinate was investigated respectively.The results showed that AP-Sm complex was coordinated through 5-OH and 4-C=O of apigenin with Sm(Ⅲ)ion.The coordination ratio of AP to Sm(Ⅲ)was 3.The study on the activity of anti-hyperuricemia found that AP-Sm complex was superior to AP in inhibiting XOD,removing SOA,reducing SUA and promoting UA excretion ability.Compared with apigenin,the AP-Sm complex showed increased anti-hyperuricemia activity after the coordination of apigenin to Sm(Ⅲ)ion.