Meadowsweet (Filipendula ulmaria) and Inflammation (general): evidence and sources

Ethnopharmacological relevance Meadowsweet (Filipendula ulmaria (L.) Maxim, Rosaceae) has been traditionally used in most European countries for the treatment of inflammatory diseases due to its antipyretic, analgesic, astringent, and anti-rheumatic properties. However, there is little scientific evidence on F. ulmaria anti-inflammatory effects regarding its impact on cyclooxygenases enzymatic activity and in vivo assessment of anti-inflammatory potential. This study aims to reveal the anti-inflammatory activity of methanolic extracts from the aerial parts (FUA) and roots (FUR) of F. ulmaria, both in in vitro and in vivo conditions. Materials and methods The characteristic phenolic compounds in F. ulmaria extracts were monitored via high performance thin layer chromatography (HPTLC). The in vitro anti-inflammatory activity of F. ulmaria extracts was evaluated using cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme assays, and an assay for determining COX-2 gene expression. The in vivo anti-inflammatory effect of F. ulmaria extracts was determined in two doses (100 and 200 mg/kg b.w.) with hot plate test and carrageenan-induced paw edema test in rats. Inflammation was also evaluated by histopathological and immunohistochemical analysis. Results FUA extract showed the presence of rutoside, spiraeoside, and isoquercitrin. Both F. ulmaria extracts at a concentration of 50μg/mL were able to inhibit COX-1 and -2 enzyme activities, whereby FUA extract (62.84% and 46.43% inhibition, respectively) was double as effective as the root extract (32.11% and 20.20%, respectively). Extracts hardly inhibited the level of COX-2 gene expression in THP-1 cells at a concentration of 25μg/mL (10.19% inhibition by FUA and 8.54% by FUR). In the hot plate test, both extracts in two doses (100 and 200mg/kg b.w.), exhibited an increase in latency time when compared with the control group (p Conclusions The observed results of in vitro and, for the first time, in vivo anti-inflammatory activity of meadowsweet extracts, provide support of the traditional use of this plant in the treatment of different inflammatory conditions. Further investigation of the anti-inflammatory compounds could reveal the mechanism of anti-inflammatory action of these extracts.

Ethnopharmacological relevance Meadowsweet (Filipendula ulmaria (L.) Maxim.), and dropwort (Filipendula vulgaris Moench) flowers are traditionally used to treat various ailments, including inflammatory conditions. The aim of the present study was to validate the aforementioned ethnomedicinal claim by assessing antihyperalgesic and antiedematous activities and toxicity of orally administered lyophilized flower infusions (LFIs) of F. ulmaria and F. vulgaris in experimental animals. Materials and methods The phytochemical analysis of LFIs was performed by HPLC-DAD. Antihyperalgesic and antiedematous activities were estimated in a rat model of inflammation induced by intraplantar injection of carrageenan using Von Frey anesthesiometer and plethysmometer, respectively. Moreover, acute oral toxicity of LFIs in mice was evaluated by observing changes in animal behavior and mortality for a period of 14 days following the treatment. Results HPLC-DAD analysis revealed the presence of phenolic acids and flavonoids in LFIs, among which spiraeoside was identified as the principal component (56.27±1.03 and 55.67±1.82mg/g of LFI in F. ulmaria and F. vulgaris, respectively). The LFIs of F. ulmaria and F. vulgaris (100-300mg/kg; p.o.) produced significant and dose-dependent antihyperalgesic effects: ED 50 ±SEM values were 164.8±15.4mg/kg (110.3-246.3mg/kg) and 172.2±6.2mg/kg (147.4-201.3mg/kg) for F. ulmaria and F. vulgaris, respectively. On the other hand, LFIs of both species (100-300mg/kg; p.o.) did not significantly reduce edema. Good safety profiles were evidenced in the toxicological study. The median lethal dose (LD 50 ) of the tested extracts is likely to be greater than 2000mg/kg. Conclusion The results of the present study support the use of F. ulmaria and F. vulgaris flowers in folk medicine for relieving pain in diseases with an inflammatory component.

Ethnopharmacological relevance Meadowsweet (Filipendula ulmaria (L.) Maxim.) and dropwort (Filipendula vulgaris Moench) are herbaceous perennials employed in folk medicine for their antirheumatic, antipyretic and anti-ulcer properties. Aim of the study To assess ethnomedicinal claims through investigation of antioxidant, anti-inflammatory and gastroprotective effects of F. ulmaria and F. vulgaris lyophilized flower infusions (LFIs) as well as the F. vulgaris isolated flavonoids spiraeoside, kaempferol 4'-O-glucoside, astragalin 2'-O-gallate, mixture of hyperoside 2'-O-gallate and isoquercitrin 2'-O-gallate, and a tannin tellimagrandin II. Materials and methods Free radical scavenging activity of the tested samples was determined by examining their ability to neutralize DPPH and OH radicals in vitro, whereas reducing properties were assessed in Ferric Reducing Antioxidant Power (FRAP) assay. Anti-inflammatory activity was studied ex vivo in human platelets by monitoring the effect on eicosanoid biosynthesis. Gastroprotective action was estimated in animal model of acute gastric injury induced by ethanol. Results LFIs and spiraeoside exerted activities comparable to those of positive control in DPPH-radical scavenging and FRAP antioxidant assays, whereas notable hydroxyl radical scavenging ability was demonstrated only for spiraeoside (IC 50 = 5.1μg/mL). Among tested samples, astragalin 2″-O-gallate (IC 50 = 141.1μg/mL) and spiraeoside (IC 50 = 4.69μg/mL) the most markedly inhibited production of pro-inflammatory prostaglandin E 2 and 12(S)-hydroxy-(5Z,8Z,10E,14Z)-eicosatetraenoic acid in human platelets, respectively. Examination of LFIs (100-300mg/kg, p.o.) gastroprotective action in rats revealed their capacity to preserve mucosal integrity. In addition, spiraeoside (50mg/kg, p.o.) and tellimagrandin II (40mg/kg, p.o.) showed ulcer preventive ability. Conclusion Current study supports documented traditional use of investigated herbs and indicates that flavonoid and tannin components are partially responsible for the demonstrated pharmacological activities.

(1) Background: Filipendula ulmaria (L.) Maxim. (Rosaceae) (meadowsweet) is widely used in phytotherapy against inflammatory diseases. However, its active constituents are not exactly known. Moreover, it contains many constituents, such as flavonoid glycosides, which are not absorbed, but metabolized in the colon by gut microbiota, producing potentially active metabolites that can be absorbed. The aim of this study was to characterize the active constituents or metabolites. (2) Methods: A F. ulmaria extract was processed in an in vitro gastrointestinal biotransformation model, and the metabolites were characterized using UHPLC-ESI-QTOF-MS analysis. In vitro anti-inflammatory activity was evaluated by testing the inhibition of NF-κB activation, COX-1 and COX-2 enzyme inhibition. (3) Results: The simulation of gastrointestinal biotransformation showed a decrease in the relative abundance of glycosylated flavonoids such as rutin, spiraeoside and isoquercitrin in the colon compartment, and an increase in aglycons such as quercetin, apigenin, naringenin and kaempferol. The genuine as well as the metabolized extract showed a better inhibition of the COX-1 enzyme as compared to COX-2. A mix of aglycons present after biotransformation showed a significant inhibition of COX-1. (4) Conclusions: The anti-inflammatory activity of F. ulmaria may be explained by an additive or synergistic effect of genuine constituents and metabolites.