National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herb Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
Molecules. 2019 Sep 6;24(18):3248. doi: 10.3390/molecules24183248.
Erding granule (EDG) is a traditional Chinese medicine that has recently been identified as having anti-hypouricemic effects. However, the active components and underlying mechanism for this new indication have not been elucidated. Therefore, we compared the effects of different EDG extracts (water, 50% ethanol and 95% ethanol) on serum uric acid concentrations in the hyperuricemia model mouse. We also analyzed the constituents of different extracts by ultra-high performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS) to observe the variation between the active and inactive products. Extract activity and target site were evaluated by assessing uric acid- and inflammation-suppressing effects along with evaluating ability to regulate the uric acid transporter. The results showed that the 50% ethanol extract (EDG-50) had an obvious serum uric acid concentration lowering effect compared with water (EDG-S) and the 95% ethanol extract (EDG-95). UHPLC-Q-TOF-MS/MS analysis showed that EDG-50 was compositionally different to EDG-S and EDG-95. EDG-50 showed dose-dependent effects on reducing uric acid, suppressing inflammation and regulating uric acid transporters. Moreover, western blot analysis showed that EDG-50 down-regulated GLUT9 and URAT1 expression, and up-regulated OAT1 expression. Therefore, our findings enable the preliminarily conclusion that EDG-50 lowers serum uric acid concentrations, mainly by down-regulating the expression of GLUT9 and URAT1 proteins and up-regulating the expression of OAT1 proteins. This provides a research basis for clinical use of EDG as an anti-hyperuricemic agent.
二地颗粒（EDG）是一种中药，最近被发现具有降血尿酸作用。然而，其新适应证的活性成分和作用机制尚未阐明。因此，我们比较了不同 EDG 提取物（水、50%乙醇和 95%乙醇）对高尿酸血症模型小鼠血清尿酸浓度的影响。我们还通过超高效液相色谱-电喷雾电离四极杆飞行时间质谱联用（UHPLC-Q-TOF-MS/MS）分析了不同提取物的成分，观察活性产物和非活性产物的变化。通过评估尿酸和炎症抑制作用以及评估调节尿酸转运体的能力，评价提取物的活性和作用部位。结果表明，与水（EDG-S）和 95%乙醇提取物（EDG-95）相比，50%乙醇提取物（EDG-50）具有明显降低血清尿酸浓度的作用。UHPLC-Q-TOF-MS/MS 分析表明，EDG-50 与 EDG-S 和 EDG-95 在成分上有所不同。EDG-50 对降低尿酸、抑制炎症和调节尿酸转运体具有剂量依赖性作用。此外，Western blot 分析表明，EDG-50 下调 GLUT9 和 URAT1 的表达，上调 OAT1 的表达。因此，我们的研究结果初步得出结论，EDG-50 通过下调 GLUT9 和 URAT1 蛋白的表达，上调 OAT1 蛋白的表达来降低血清尿酸浓度。这为 EDG 作为抗高尿酸血症药物的临床应用提供了研究基础。
