Zhu Ji Xiao, Wang Ying, Kong Ling Dong, Yang Cheng, Zhang Xin
Institute of Functional Biomolecule, State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, PR China.
J Ethnopharmacol. 2004 Jul;93(1):133-40. doi: 10.1016/j.jep.2004.03.037.
The hypouricemic actions of Biota orientalis (BO) extract and its flavonoid constituents quercetin and rutin, were in vivo examined using oxonate-induced hyperuricemic mice. Quercetin and rutin, when administered three times orally to the oxonate-induced hyperuricemic mice, were able to elicit dose-dependent hypouricemic effects. The effects of quercetin and rutin were more potent than that of Biota orientalis extract at the same dose of 100 mg/kg. At doses of 50 mg/kg of quercetin or above, or at doses of 100 mg/kg of rutin or above, the serum urate levels of the oxonate-pretreated mice were not different from normal mice. In addition, Biota orientalis extract, quercetin and rutin, when tested in vivo on mouse liver homogenates, elicited significant inhibitory actions on the xanthine dehydrogenase/xanthine oxidase (XDH/XO) activities. The effects of quercetin and rutin resulted less potent than that of allopurinol. However, intraperitoneal administration at the same scheme did not produce any observable hypouricemic effect. These hypouricemic effects are partly due to the inhibition of XDH/XO activities in mouse liver. The pharmacological profile of the flavonoids is partly different from that of allopurinol. Such hypouricemic action and inhibition of the enzyme activity of quercetin and rutin may be responsible for a part of the beneficial effects of Biota orientalis extract on hyperuricemia and gout. The effects of quercetin and rutin on serum urate levels in hyperuricemic mice induced by oxonate and the inhibition of enzyme activities in mouse liver are discussed in relation to their absorption and metabolism, and their potential application to treat gout and hyperuricemia.
采用氧嗪酸钾诱导的高尿酸血症小鼠,对侧柏叶提取物及其黄酮类成分槲皮素和芦丁的降尿酸作用进行了体内研究。当对氧嗪酸钾诱导的高尿酸血症小鼠口服给药三次时,槲皮素和芦丁能够产生剂量依赖性的降尿酸作用。在相同剂量100mg/kg时,槲皮素和芦丁的作用比侧柏叶提取物更强。在槲皮素剂量为50mg/kg及以上,或芦丁剂量为100mg/kg及以上时,氧嗪酸钾预处理小鼠的血清尿酸水平与正常小鼠无异。此外,当在小鼠肝脏匀浆中进行体内试验时,侧柏叶提取物、槲皮素和芦丁对黄嘌呤脱氢酶/黄嘌呤氧化酶(XDH/XO)的活性均有显著抑制作用。槲皮素和芦丁的作用效果不如别嘌醇。然而,按照相同方案腹腔给药未产生任何可观察到的降尿酸作用。这些降尿酸作用部分归因于对小鼠肝脏中XDH/XO活性的抑制。黄酮类化合物的药理特性与别嘌醇部分不同。槲皮素和芦丁的这种降尿酸作用以及对酶活性的抑制可能是侧柏叶提取物对高尿酸血症和痛风有益作用的一部分。本文讨论了槲皮素和芦丁对氧嗪酸钾诱导的高尿酸血症小鼠血清尿酸水平的影响以及对小鼠肝脏酶活性的抑制作用,并涉及其吸收、代谢以及在治疗痛风和高尿酸血症方面的潜在应用。