The Herbal DrugMelampyrum pratenseL. (Koch): Isolation and Identification of Its Bioactive Compounds Targeting Mediators of Inflammation

Abstract

Melampyrum pratense L. (Koch) is used in traditional Austrian medicine for the treatment of different inflammation-related conditions. In this work, we show that the extracts of M. pratense stimulated peroxisome proliferator-activated receptors- (PPARs-)α and -γ that are well recognized for their anti-inflammatory activities. Furthermore, the extract inhibited the activation of the proinflammatory transcription factor NF-κB and induction of its target genes interleukin-8 (IL-8) and E-selectin in vitro. Bioassay-guided fractionation identified several active flavonoids and iridoids including melampyroside and mussaenoside and the phenolic compound lunularin that were identified in this species for the first time. The flavonoids apigenin and luteolin were distinguished as the main components accountable for the anti-inflammatory properties. Apigenin and luteolin effectively inhibited tumor necrosis factor α (TNF-α)-induced NF-κB-mediated transactivation of a luciferase reporter gene. Furthermore, the two compounds dose-dependently reduced IL-8 and E-selectin protein expression after stimulation with lipopolysaccharide (LPS) or TNF-α in endothelial cells (ECs). The iridoids melampyroside and mussaenoside prevented the elevation of E-selectin in LPS-stimulated ECs. Lunularin was found to reduce the protein levels of the proinflammatory mediators E-selectin and IL-8 in ECs in response to LPS. These data validate the ethnomedical use of M. pratense for the treatment of inflammatory conditions and point to the constituents accountable for its anti-inflammatory activity.

Complex effects of aqueous extract of Melampyrum pratense and of its flavonoids on activity of primary cultured hippocampal neurons

“…The following approximate quantitative content of individual main flavonoids was calculated: 12% of hyperoside, 10% of cinaroside, less than 1% of apigenin and of luteolin. The last two components are poorly soluble in water and their concentration is reported to be higher in the ethanol extracts of Melampyrum pratense (Galishevskaya and Petrichenko, 2010;Suchinina et al, 2010;Vogl et al, 2013).…”

“…It was found that the density of the air-dried stock of Mp ranges from 76713 to 240723 kg/ha. Biological stock ranges from 3.2 to 4 t, and the operating stock is about Contents lists available at ScienceDirect journal homepage: www.elsevier.com/locate/jep 2.9 t. According to some studies Mp may affect the nervous system (Galishevskaya and Petrichenko, 2010;Vogl et al, 2013). Due to their unique properties, these plants are widely used in folk medicine as sedatives and anticonvulsants (Sokolov, 1990;Galishevskaya and Petrichenko, 2010;Vogl et al, 2013).…”

“…Biological stock ranges from 3.2 to 4 t, and the operating stock is about Contents lists available at ScienceDirect journal homepage: www.elsevier.com/locate/jep 2.9 t. According to some studies Mp may affect the nervous system (Galishevskaya and Petrichenko, 2010;Vogl et al, 2013). Due to their unique properties, these plants are widely used in folk medicine as sedatives and anticonvulsants (Sokolov, 1990;Galishevskaya and Petrichenko, 2010;Vogl et al, 2013). Above ground plant parts are used for the preparation of aqueous extracts (tinctures, decoctions), which are prescribed in small doses as an effective treatment in antiinflammatory, cardio-vascular and neurological diseases, particularly as sedatives and anxiolytics (Sokolov, 1990;Stajner et al, 2009;Vogl et al, 2013).…”

“…Due to their unique properties, these plants are widely used in folk medicine as sedatives and anticonvulsants (Sokolov, 1990;Galishevskaya and Petrichenko, 2010;Vogl et al, 2013). Above ground plant parts are used for the preparation of aqueous extracts (tinctures, decoctions), which are prescribed in small doses as an effective treatment in antiinflammatory, cardio-vascular and neurological diseases, particularly as sedatives and anxiolytics (Sokolov, 1990;Stajner et al, 2009;Vogl et al, 2013).…”

“…This plant contains a broad range of biologically active compounds, including flavonoids, iridoids and alkaloids (Damtoft et al, 1984;Roeder and Bourauel, 1992;Stajner et al, 2009;Galishevskaya and Petrichenko, 2010;Munteanu and Vlase, 2011;Vogl et al, 2013). Particularly, it has been found that Mp contains hyperoside, luteolin, cinaroside, apigenin and other flavonoids, known to have multiple pronounced effects on the central nervous system.…”