Chien Shih-Chang, Yang Chen-Wei, Tseng Yen-Hsueh, Tsay Hsin-Sheng, Kuo Yueh-Hsiung, Wang Sheng-Yang
School of Chinese Medicine Resources, China Medical University, Taichung, Taiwan.
Planta Med. 2009 Mar;75(4):302-6. doi: 10.1055/s-0029-1185300. Epub 2009 Jan 30.
Xanthine oxidase (XOD) catalyzes the oxidation of hypoxanthine to xanthine and then to uric acid, and is a key enzyme in the pathogenesis of hyperuricemia. The ability of extracts of Lonicera hypoglauca (Caprifoliaceae) to inhibit XOD was investigated in this study. An ethanol extract (LH-crude) of the leaves of L. hypoglauca and its derived EtOAc soluble sub-fractions (LH-EA) significantly inhibited XOD activity, with IC50 values for LH-crude and LH-EA of 48.8 and 35.2 microg/mL. Moreover, LH-EA reduced serum urate levels IN VIVO in a potassium oxonate-induced hyperuricemic mouse model, by 70.1% and 93.7% of the hyperuricemic untreated group at doses of 300 and 500 mg/kg of LH-EA, respectively. Finally, we used bioactivity-guided fractionation to isolate a new bisflavonoid, loniceraflavone, which showed significant inhibition of XOD (IC50=0.85 microg/mL). These results suggest that L. hypoglauca and its extracts may have a considerable potential for development as an anti-hyperuricemia agent for clinical application.
黄嘌呤氧化酶(XOD)催化次黄嘌呤氧化为黄嘌呤,进而氧化为尿酸,是高尿酸血症发病机制中的关键酶。本研究考察了淡红忍冬(忍冬科)提取物抑制XOD的能力。淡红忍冬叶的乙醇提取物(LH-粗提物)及其衍生的乙酸乙酯可溶亚组分(LH-EA)显著抑制XOD活性,LH-粗提物和LH-EA的IC50值分别为48.8和35.2μg/mL。此外,在氧嗪酸钾诱导的高尿酸血症小鼠模型中,LH-EA在体内降低了血清尿酸水平,在LH-EA剂量为300和500mg/kg时,分别为高尿酸血症未治疗组的70.1%和93.7%。最后,我们采用生物活性导向分离法分离出一种新的双黄酮类化合物,忍冬黄酮,其对XOD表现出显著抑制作用(IC50=0.85μg/mL)。这些结果表明,淡红忍冬及其提取物作为抗高尿酸血症药物用于临床应用可能具有相当大的开发潜力。