Department of Biochemistry and Molecular Biology, College of Basic Medical Sciences, Second Military Medical University, Shanghai, 200433, P.R. China.
J Enzyme Inhib Med Chem. 2009 Jun;24(3):663-8. doi: 10.1080/14756360802323829.
In this study we investigated the superoxide radicals scavenging effect and xanthine oxidase inhibitory activity by magnesium lithospermate B, which was originally isolated from the roots of Salvia miltiorrhiza (also named Danshen or Dansham), an important herb in Oriental medicine. Superoxide radicals were generated both in beta-NADH/PMS system and xanthine/ xanthine oxidase system. Magnesium lithospermate B significantly inhibited the reduction of NBT induced by superoxide radicals with an IC(50) of 29.8 microg/mL and 4.06 microg/mL respectively in the two systems. Further study suggested that magnesium lithospermate B can directly inhibit xanthine oxidase and exhibits competitive inhibition. Magnesium lithospermate B was also found to have the hypouricemic activity in vivo against potassium oxonate-induced hyperuricaemia in mice. After oral administration of magnesium lithospermate B at doses of 10, 20 and 30 mg/kg, there was a significant decrease in the serum urate level when compared to the hyperuricemia control. In addition, magnesium lithospermate B significantly protected HL-60 cells from superoxide radicals-induced apoptosis in the xanthine/ xanthine oxidase reactions. This study provided evidence that magnesium lithospermate B exhibits direct superoxide radicals scavenging and xanthine oxidase inhibitory activity.
在这项研究中，我们研究了丹参（又称丹参或丹参）根中分离出的镁丹参素 B 的超氧自由基清除作用和黄嘌呤氧化酶抑制活性。超氧自由基在β-NADH/PMS 系统和黄嘌呤/黄嘌呤氧化酶系统中均有生成。镁丹参素 B 对两种系统中 NBT 被超氧自由基还原的抑制作用具有显著的抑制作用，IC50 分别为 29.8μg/mL 和 4.06μg/mL。进一步的研究表明，镁丹参素 B 可以直接抑制黄嘌呤氧化酶，并表现出竞争性抑制。体内研究还发现镁丹参素 B 对氧嗪酸钾诱导的高尿酸血症小鼠具有降尿酸作用。口服 10、20 和 30mg/kg 剂量的镁丹参素 B 后，与高尿酸血症对照组相比，血清尿酸水平显著降低。此外，镁丹参素 B 还可显著保护 HL-60 细胞免受黄嘌呤/黄嘌呤氧化酶反应中超氧自由基诱导的凋亡。这项研究提供了证据表明，镁丹参素 B 具有直接清除超氧自由基和抑制黄嘌呤氧化酶的活性。
