Investigation of EPs^®7630 in co-culture assays to predict possible drug effects

EPs^®7630 is an herbal drug preparation from the roots of Pelargonium sidoides (1:8-10; extraction solvent: ethanol 11% [w/w]) and is used for the treatment of respiratory tract infections. Numerous pharmacological test models have shown that EPs^®7630 exerts antibacterial and antiviral activity [1]. To investigate further pharmacological effects of EPs^®7630, it was analyzed in the BioMAP^® Diversity PLUS Panel assay (provided by Eurofins DiscoverX Corporation) which includes 12 individual human primary cell-based systems predicting potential drug effects in multiple tissues and disease states. With this assay an identification and biological interpretation of relevant biomarker activities and a search for a phenotypically similar compound from a database (> 4,500 reference compounds) is possible. For EPs^®7630 (3.3, 10, 30 µg/ml) anti-proliferative activities on endothelial cells and T-cells as well a as inflammation-related, tissue remodeling, hemostasis-related and immunomodulatory activities were found. At a concentration of 30 µg/ml, a strong correlation was found with respect to the activity profile of methimazole, an antithyroid drug, and troglitazone, a ligand of peroxisome proliferator-activated receptors (PPARα and PPARµ). PPARα agonists have been proposed to play a role in inflammatory lung diseases [2]. At 10 µg/ml, a close EPs^®7630 activity resembled that of myricetin, a flavonoid with antioxidant properties. In addition, effects similar to those of LPS, a Toll-like-receptor-4 agonist, and fucoidan, an L-selectin antagonist, were obtained. In summary, EPs^®7630 showed amongst other an immunomodulatory potential in the BioMAP^® Assay and gives new interesting approaches for further investigations, such as PPAR, TLR-4 and L-selection signaling experiments.

• References

• 1 Kolodziej Herbert. “Antimicrobial, antiviral and immunomodulatory activity studies of Pelargonium sidoides (EPs® 7630) in the context of health promotion”. Pharmaceuticals 2011; 4 (10) : 1295-1314.
• 2 Belvisi MG, and Mitchell JA. “Targeting PPAR receptors in the airway for the treatment of inflammatory lung disease”. Br J pharmacol 158 (04) ; 2009; 994-1003.