Anti-Inflammatory Activities of Arnica montana Planta Tota versus Flower Extracts: Analytical, In Vitro and In Vivo Mouse Paw Oedema Model Studies

Zugehörigkeit
Preclinical Development, Weleda AG, 4144 Arlesheim, Switzerland
Röhrl, Johann;
Zugehörigkeit
Preclinical Development, Weleda AG, 4144 Arlesheim, Switzerland
Piqué-Borràs, Maria-Riera;
Zugehörigkeit
Preclinical Development, Weleda AG, 4144 Arlesheim, Switzerland
Jaklin, Manuela;
GND
1219876291
ORCID
0000-0002-0298-5136
Zugehörigkeit
Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany
Werner, Markus;
ORCID
0000-0002-5064-4379
Zugehörigkeit
Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, 07743 Jena, Germany
Werz, Oliver;
Zugehörigkeit
Quality Control, Weleda AG, 73525 Schwäbisch Gmünd, Germany
Josef, Heinke;
Zugehörigkeit
Quality Control, Weleda AG, 73525 Schwäbisch Gmünd, Germany
Hölz, Hubert;
Zugehörigkeit
Research and Development, Weleda AG, 4144 Arlesheim, Switzerland
Ammendola, Aldo;
Zugehörigkeit
Preclinical Development, Weleda AG, 4144 Arlesheim, Switzerland
Künstle, Gerald

Arnica montana is well known for its anti-inflammatory properties. While the anti-inflammatory activity of Arnica flowers (Arnicae flos) has been extensively studied, that of the whole plant (Arnicae planta tota) is less characterized. We compared the ability of Arnicae planta tota and Arnicae flos extracts to inhibit the pro-inflammatory NF-κB—eicosanoid pathway, using several in vitro and in vivo assays. We showed that Arnicae planta tota inhibited NF-κB reporter activation, with an IC 50 of 15.4 μg/mL (vs. 52.5 μg/mL for Arnicae flos). Arnicae planta tota also inhibited LPS-induced expression of ALOX5 and PTGS2 genes in human differentiated macrophages. ALOX5 and PTGS2 encode the 5-lipoxygenase (5-LO) and cyclooxygenase-2 (COX-2) enzymes that initialize the conversion of arachidonic acid into leukotrienes and prostaglandins, respectively. Arnicae planta tota inhibited 5-LO and COX-2 enzymatic activity in vitro and in human primary peripheral blood cells, with lower IC 50 compared to Arnicae flos. Finally, Arnicae planta tota applied topically reduced carrageenan-induced mouse paw oedema more efficiently than Arnicae flos. Altogether, Arnicae planta tota displayed a superior anti-inflammatory activity compared to Arnicae flos, suggesting that Arnicae-planta-tota-containing products might be more effective in alleviating the manifestations of acute inflammation than those based on Arnicae flos alone.

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