Identification and pharmacological characterization of the anti-inflammatory principal of the leaves of dwarf elder (Sambucus ebulus L.)

• Published in: Journal of ethnopharmacology 2011-01, Vol.133 (2), p.704-709
• Main Authors: Schwaiger, Stefan, Zeller, Iris, Pölzelbauer, Petra, Frotschnig, Sandra, Laufer, Günther, Messner, Barbara, Pieri, Valerio, Stuppner, Hermann, Bernhard, David
• Format: Article
• Language: English
• Subjects: Adoxacea; animal proteins; Anti-inflammatory activity; Anti-Inflammatory Agents - isolation & purification; Anti-Inflammatory Agents - pharmacology; Biological and medical sciences; Cells, Cultured; chronic diseases; cytotoxicity; endothelial cells; Endothelial Cells - drug effects; Endothelial Cells - metabolism; Ethnopharmacology; General pharmacology; human cell lines; Humans; HUVEC; ICAM-1; in vitro studies; inhibitory concentration 50; intercelluar adhesion molecule-1; Intercellular Adhesion Molecule-1 - metabolism; leaves; mechanism of action; Medical sciences; medicinal plants; medicinal properties; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; plant extracts; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Leaves - chemistry; Plants, Medicinal - chemistry; Sambucus - chemistry; Sambucus ebulus; Sambucus ebulus L; TNF-α; Triterpenes - isolation & purification; Triterpenes - pharmacology; Tumor Necrosis Factor-alpha - pharmacology; umbilical veins; Ursolic Acid; vascular cell adhesion molecule-1; Vascular Cell Adhesion Molecule-1 - metabolism; VCAM-1
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2010.10.049

Anti-inflammatory activity of a dwarf elder leaf extract (Sambucus ebulus L.) was assessed by activity guided fractionation using inhibition of TNFα induced expression of VCAM-1 on the surface of HUVECs as monitoring tool. The active principal was identified as ursolic acid (IC50 6.25μM). 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 (IC50 6.25μM), ursolic acid inhibits also TNFα induced expression of ICAM-1 (IC50 value between 3.13 and 6.25μM) (positive control: parthenolide 10μM, 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.