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目的黄嘌呤氧化酶(XOD)抑制剂对痛风或其他XOD诱导的疾病有潜在的治疗作用,因此探讨了从丹参(Salvia miltiorrhiza Bge.)中分离的丹参二萜醌---隐丹参酮(CT)和次甲丹参酮(MT)对XOD的抑制作用。方法在分子氧存在的条件下,XOD催化黄嘌呤产生尿酸和超氧阴离子。在黄嘌呤/XOD的反应媒介中加入CT或MT,通过测量波长290nm处吸光度的增加测定尿酸形成速率。结果CT和MT对XOD有抑制作用,酶动力学曲线Dixon图显示抑制方式是竞争型。CT和MT的Ki值分别为17.8和25.9μmol.L-1,抑制活性与浓度正相关。CT和MT的IC50值分别为70和67μmol.L-1,阳性对照别黄嘌呤醇的IC50值为60μmol.L-1。结论CT和MT对XOD活性有抑制作用,对痛风或其他XOD诱导的疾病可能有一定的治疗作用。
The purpose of xanthine oxidase (XOD) inhibitors has a potential therapeutic effect on gout or other XOD-induced diseases, and therefore the study of Salvia miltiorrhiza Bunge, isolated from Salvia miltiorrhiza Bge., as a cryptotanshinone (CT) Inhibition of XOD by Hexatanshinone (MT). Methods XOD catalyzes the production of uric acid and superoxide anions in the presence of molecular oxygen. CT or MT was added to the xanthine/XOD reaction medium, and the uric acid formation rate was measured by measuring the increase in absorbance at a wavelength of 290 nm. RESULTS: CT and MT had inhibitory effects on XOD. Dixon plot of enzyme kinetics showed that the inhibition mode was competitive. The Ki values of CT and MT were 17.8 and 25.9 μmol.L-1, respectively, and the inhibitory activity was positively correlated with the concentration. The IC50 values of CT and MT were 70 and 67 μmol.L-1, respectively. The IC50 value of the positive control allopurinol was 60 μmol.L-1. Conclusion CT and MT have inhibitory effects on XOD activity and may have certain therapeutic effects on gout or other XOD-induced diseases.