Institute of Pharmacy/Pharmacognosy, University of Innsbruck, Josef-Moeller-Haus, Innrain 52c, A-6020 Innsbruck, Austria.
J Ethnopharmacol. 2011 Jan 27;133(2):704-9. doi: 10.1016/j.jep.2010.10.049. Epub 2010 Oct 30.
The performed investigations aimed on the identification of the anti-inflammatory principal of extracts of leaves of Sambucus ebulus L. (dwarf elder) in order to rationalize the traditional use of this plant for the treatment of chronically inflammatory diseases.
Dwarf elder leaf extract was subjected to activity guided fractionation using inhibition of TNFα induced expression of vascular cell adhesion molecule 1 (VCAM-1) on the surface of human umbilical vein endothelial cells (HUVECs) as monitoring tool (positive control: parthenolide 10μM, VCAM-1 expression (% of control): 5.35±0.38%).
Bio-guided isolation resulted in identification of ursolic acid as anti-inflammatory principal. Besides its inhibitory effects against TNFα induced expression of VCAM-1 (IC(50) 6.25 μM), ursolic acid inhibits also TNFα induced expression of ICAM-1 (IC(50) value between 3.13 and 6.25 μM) (positive control: parthenolide 10 μM, ICAM-1 expression (% of control): 38.89±16.6%). Toxic effects of ursolic acid on HUVECs can be drastically reduced using an enriched extract instead of the pure compound.
Our findings suggest an additional mechanism of the anti-inflammatory activity of ursolic acid by demonstrating its ability to inhibit TNFα-stimulated expression of VCAM-1 and ICAM-1 and support the traditional use of extracts and preparations of Sambucus ebulus L., rich in ursolic acid, for the treatment of chronically inflammatory processes.
本研究旨在鉴定接骨木(矮接骨木)叶提取物的抗炎成分,以合理化该植物用于治疗慢性炎症性疾病的传统用途。
使用 TNFα 诱导的人脐静脉内皮细胞(HUVEC)表面血管细胞黏附分子 1(VCAM-1)表达抑制作为监测工具(阳性对照:小白菊内酯 10μM,VCAM-1 表达(%对照):5.35±0.38%),对矮接骨木叶提取物进行活性导向分离。
生物导向分离鉴定出熊果酸为抗炎成分。除了抑制 TNFα 诱导的 VCAM-1 表达(IC50 为 6.25μM)外,熊果酸还抑制 TNFα 诱导的 ICAM-1 表达(IC50 值在 3.13 至 6.25μM 之间)(阳性对照:小白菊内酯 10μM,ICAM-1 表达(%对照):38.89±16.6%)。使用富含熊果酸的提取物代替纯化合物可以大大降低熊果酸对 HUVECs 的毒性作用。
我们的发现表明熊果酸通过抑制 TNFα 刺激的 VCAM-1 和 ICAM-1 表达来证明其抗炎活性的另一种机制,并支持接骨木(矮接骨木)提取物和制剂的传统用途,这些制剂富含熊果酸,用于治疗慢性炎症过程。