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.

Vegetal Polyphenol Extracts as Antioxidants for the Stabilization of PLA: Toward Fully Biobased Polymer Formulation.

The use of natural antioxidants as substitutes for traditional synthetic stabilizers has been investigated for the stabilization of biobased and biodegradable polymers, with the aim of designing fully biobased plastic formulations. This study focused on the thermo- and photostabilization of poly(lactic acid) (PLA) using vegetal polyphenol extracts as biosourced antioxidants. The polyphenols were extracted by microwave-assisted extraction from the valorization of vegetal waste, and their potential as antioxidant additives was evaluated (e.g., polyphenol content, composition, and antioxidant activity). PLA was then formulated with 2 wt % of the extracts exhibiting the highest antioxidant activities: green tea residues, pomegranate peels, grape marc, bramble leaves, and yellow onion peel extracts. The efficiency of the natural additives as thermal stabilizers was evaluated and compared with a synthetic antioxidant using rheological and thermal analyses. The results demonstrated the capacity of grape marc extract and pomegranate peel extract to significantly improve PLA thermal stability during processing and thermo-oxidation. Finally, photorheology was conducted to evaluate the influence of the bioadditives on the biopolyester photodegradation. The different polyphenol extracts seemed to significantly hinder the photo-oxidation of PLA and constitute very promising natural UV stabilizers, combining UV absorbers and antioxidant functions.

Chemical Profile, Antioxidant and Anti-Inflammatory Potency of Extracts of Vitex madiensis Oliv. and Crossopteryx febrifuga (Afzel ex G. Don).

Vitex madiensis Oliv. (Lamiaceae) and Crossopteryx febrifuga (Rubiaceae), two plants commonly used in traditional African medicines to treat malaria and pain, were studied either to determine their chemical profiles or to evaluate their antioxidant and anti-inflammatory activities. In this study, we investigated leaves, trunk bark, root bark and fruits methanolic extracts of both plants in order to find out which part of the plant is responsible for the activity. The analyses of the chemical profiles allowed us to confirm the presence of several ecdysteroids, especially 20-hydroxyecdysone in some parts of V. madiensis and to highlight the presence of organic acids and phenol derivatives in C. febrifuga. Among the four parts of the plants studied, only the fruits extract of C. febrifuga could present anti-inflammatory activity by decreasing ROS production. The leaves and trunk bark extracts of V. madiensis showed significant free radical scavenging activity compared to ascorbic acid, and the same extracts decrease ROS production significantly. The activity of these two extracts could be explained by the presence of ecdysteroids and flavonoids. The ROS production inhibition of V. madiensis is particularly interesting to investigate with further analyses.

In Vitro Anti-Inflammatory and Immunomodulatory Activities of an Extract from the Roots of Bupleurum rotundifolium.

BACKGROUND: Some Bupleurum species, such as the Bupleurum chinense DC. or the Bupleurum scorzonerifolium Willd have been extensively studied (especially their roots) for the treatment of inflammation. In contrast, only compounds extracted from the aerial parts of Bupleurum rotundifolium have been studied and showed anti-inflammatory or antiproliferative activities. This study was conducted to investigate the antioxidant, anti-inflammatory, and immunomodulatory effects of Bupleurum rotundifolium roots. METHODS: To tackle the various aspects of inflammation, we studied in vitro a methanolic extract from the roots of Bupleurum rotundifolium on peripheral blood mononuclear cells (PBMCs), polymorphonuclear neutrophils (PMNs), and the monocytic cells THP-1. Its antioxidant capacities and iron-chelating activity were assessed. The extract was tested on THP-1 differentiation, reactive oxygen species (ROS) production by leukocytes, neutrophils chemotaxis, cytokines, PGE2 production, and NF-κB activation in PBMCs. RESULTS: The extract showed a decreased ROS production in stimulated cells. It increased PBMC chemokine secretion and up-regulated the differentiation of THP-1 monocytes into macrophage-like cells, indicating a potential interest of the extract in the resolution of acute inflammation. In addition, the analysis of cytokine production suggests that Bupleurum rotundifolium has immunomodulatory properties. CONCLUSIONS: Cytokines secretion, especially IL-1ß and IL-12p70, provided us with a set of indicators suggesting that the extract might be able to drive the polarization of macrophages and lymphocytes toward a Th2 anti-inflammatory profile in excessive inflammation.