Potential Anti-Inflammatory and Chondroprotective Effect of Luzula sylvatica.

(1) Interest in the Juncaceae family has risen as some members have shown anti-inflammatory properties and interesting compounds. In this regard, we decided to investigate the antioxidant and anti-inflammatory properties of Luzula sylvatica, a Juncaceae not yet extensively studied, in the context of osteoarthritis. (2) The Luzula sylvatica Ethanol extract (LS-E) was used to test the production of reactive oxygen species (ROS) by leucocytes, the IL1ß and PGE2 production by peripheral blood mononuclear cells (PBMCs), the production of EP4, and the activation of NFκB in THP-1, as well as the IL1ß-activated normal human knee articular chondrocytes (NHAC-Kn) gene expression, grown in monolayers or maintained in alginate beads. (3) Organic acids, caffeoylquinic acids, quercetin and luteolin, compounds frequently found in this family were identified. The LS-E exhibited inhibited ROS formation. The LS-E did not affect NFκB activation and IL1ß secretion but dampened the secretion of PGE2 by PBMCs and the presence of EP4 in THP-1. It also modulated the expression of NHAC-Kn in both models and inhibited the expression of several proteases and inflammatory mediators. (4) Luzula sylvatica might supply interesting antioxidant protection against cartilage damages and lessen joint inflammation, notably by decreasing PGE2 secretion in the synovial fluid. Moreover, it could act directly on chondrocytes by decreasing the expression of proteases and, thus, preventing the degradation of the extracellular matrix.

Xanthine Oxidase Inhibitors from Filipendula ulmaria (L.) Maxim. and Their Efficient Detections by HPTLC and HPLC Analyses.

Filipendula ulmaria is a plant commonly used for the treatment of several pathologies, such as diarrhoea, ulcers, pain, stomach aches, fevers, and gout. Our study focused on the use of F. ulmaria for the treatment of gout disease. We first studied the chemical composition of a methanolic extract of the aerial parts and demonstrated its xanthine oxidase (XO) inhibitory activity. Then, we performed a fractionation and evaluated the most XO inhibitory active fractions by UV measurement. Purification of some fractions allowed the determination of the inhibitory activity of pure compounds. We demonstrated that spiraeoside, a glycosylated flavonoid, possesses an activity around 25 times higher than allopurinol, used as a reference in the treatment of gout disease. In order to easily and quickly identify potent inhibitors in complex matrix, we developed a complementary strategy based on an HPLC method and an Effect Directed Assay (EDA) method combining HPTLC and biochemical assays. The HPLC method, capable of determining compounds exhibiting interactions with the enzyme, could be an efficient strategy for evaluating potent enzyme inhibitors in a complex mixture. This strategy could be applied for quantitative assays using LC/MS experiments.

Anti-Inflammatory and Cytotoxic Potential of New Phenanthrenoids from Luzula Sylvatica.

Phenanthrenoids have been widely described, in the Juncaceae family, for theirbiological properties such as antitumor, anxiolytic, anti-microbial, spasmolytic, and antiinflammatoryactivities. The Juncaceae family is known to contain a large variety ofphenanthrenoids possessing especially anti-inflammatory and cytotoxic properties. Luzulasylvatica, a Juncaceae species, is widely present in the Auvergne region of France, but has neverbeen studied neither for its phytochemical profile nor for its biological properties. We investigatedthe phytochemical profile and evaluated the potential anti-inflammatory activities of L. sylvaticaaerial parts extracts. A bioassay-guided fractionation was carried out to identify the most activefractions. Nine compounds were isolated, one coumarin 1 and eight phenanthrene derivatives (2-9), including four new compounds (4, 5, 8 and 9), from n-hexane and CH2Cl2, fractions. Theirstructures were established by HRESIMS, 1D and 2D NMR experiments. The biological properties,especially the anti-inflammatory/antioxidant activities (ROS production) and antiproliferativeactivity on THP-1, a monocytic leukemia cell line, of each compound, were evaluated. Threephenanthrene derivatives 4, 6, and 7 showed very promising antiproliferative activities.Phenanthrene derivatives.

Benefits of the ipowder® extraction process applied to Melissa officinalis L.: improvement of antioxidant activity and in vitro gastro-intestinal release profile of rosmarinic acid.

The objective of this study was to evaluate the benefits of a new extraction process, the ipowder® technology, applied to Melissa officinalis L. Compared to M. officinalis ground dry leaves, the ipowder® had a similar phytochemical fingerprint but contained twice the concentration of rosmarinic acid (by HPTLC and HPLC) and had a two-fold greater antioxidant activity (DPPH* method). In vitro digestion experiments (TIM-1 model) showed better availability of rosmarinic acid for intestinal absorption with the ipowder® than with ground dry leaves, manifested by a three-fold reduction in the quantity of ingested product needed for delivery of the same amount of rosmarinic acid into the upper gastro-intestinal tract. This study shows that the ipowder® technology preserves all the original plant compounds intact while making some active ingredients more accessible and available to exert their effects. To obtain a given effect, the amount of ipowder® extract to ingest will therefore be lower; a reduction in the daily dosage will be more convenient for the patient and will improve patient compliance with supplementation.

Basal and Spasmolytic Effects of a Hydroethanolic Leaf Extract of Melissa officinalis L. on Intestinal Motility: An Ex Vivo Study.

Melissa officinalis L. (lemon balm) has been used for decades with symptomatic benefits in patients with digestive disorders. However, very little is known on the effects of M. officinalis on the gastrointestinal (GI) tract. In this study, the basal and spasmolytic properties of a hydroethanolic leaf extract (HLE) of M. officinalis were assessed ex vivo on different segments of the GI tract of mice after phytochemical characterization of the extract. M. officinalis HLE had site- and dose-dependent effects on the contractile activity of the GI tract, the motility response being impacted in the jejunum and ileum but not in the antrum and colon. The observed effects could be caused by the phenolic compounds (mainly rosmarinic acid) detected in the extract.

Skeletal muscle relaxant effect of a standardized extract of Valeriana officinalis L. after acute administration in mice.

Valeriana officinalis L. root extracts are traditionally taken for their sedative and anxiolytic properties and are also used for muscle relaxation. Relaxant effects were clearly observed on smooth muscle whereas data on effects on skeletal muscle are scarce and inconsistent. The aim of this study was to assess whether a standardized extract (SE) of V. officinalis had myorelaxant effects by decreasing skeletal muscle strength and/or neuromuscular tone in mice. Mice received an acute dose of V. officinalis SE (2 or 5 g/kg per os) or tetrazepam (10 mg/kg ip), a standard myorelaxant drug. Thirty minutes later, the maximal muscle strength was measured using a grip test, while global skeletal muscle function (endurance and neuromuscular tone) was assessed in a wire hanging test. Compared to tetrazepam, both doses of V. officinalis SE induced a pronounced decrease in skeletal muscle strength without any significant effects on endurance and neuromuscular tone. This study provides clear evidence that the extract of V. officinalis tested has a relaxant effect on skeletal muscle. By decreasing skeletal muscle strength without impacting endurance and neuromuscular tone, V. officinalis SE could induce less undesirable side effects than standard myorelaxant agents, and be particularly useful for avoiding falls in the elderly.