Screening of Wood/Forest and Vine By-Products as Sources of New Drugs for Sustainable Strategies to Control Fusarium graminearum and the Production of Mycotoxins.

Fusarium graminearum is a fungal pathogen that can colonize small-grain cereals and maize and secrete type B trichothecene (TCTB) mycotoxins. The development of environmental-friendly strategies guaranteeing the safety of food and feed is a key challenge facing agriculture today. One of these strategies lies on the promising capacity of products issued from natural sources to counteract crop pests. In this work, the in vitro efficiency of sixteen extracts obtained from eight natural sources using subcritical water extraction at two temperatures was assessed against fungal growth and TCTB production by F. graminearum. Maritime pine sawdust extract was shown to be extremely efficient, leading to a significant inhibition of up to 89% of the fungal growth and up to 65% reduction of the mycotoxin production by F. graminearum. Liquid chromatography/mass spectrometry analysis of this active extract revealed the presence of three families of phenolics with a predominance of methylated compounds and suggested that the abundance of methylated structures, and therefore of hydrophobic compounds, could be a primary factor underpinning the activity of the maritime pine sawdust extract. Altogether, our data support that wood/forest by-products could be promising sources of bioactive compounds for controlling F. graminearum and its production of mycotoxins.

The phenolic acids of Agen prunes (dried plums) or Agen prune juice concentrates do not account for the protective action on bone in a rat model of postmenopausal osteoporosis.

Dietary supplementation with dried plum (DP) has been shown to protect against and reverse established osteopenia in ovariectomized rodents. Based on in vitro studies, we hypothesized that DP polyphenols may be responsible for that bone-sparing effect. This study was designed to (1) analyze whether the main phenolic acids of DP control preosteoblast proliferation and activity in vitro; (2) determine if the polyphenolic content of DP or DP juice concentrate is the main component improving bone health in vivo; and (3) analyze whether DP metabolites directly modulate preosteoblast physiology ex vivo. In vitro, we found that neochlorogenic, chlorogenic, and caffeic acids induce the proliferation and repress the alkaline phosphatase activity of primary preosteoblasts in a dose-dependent manner. In vivo, low-chlorogenic acid Agen prunes (AP) enriched with a high-fiber diet and low-chlorogenic acid AP juice concentrate prevented the decrease of total femoral bone mineral density induced by estrogen deficiency in 5-month-old female rats and positively restored the variations of the bone markers osteocalcin and deoxypyridinoline. Ex vivo, we demonstrated that serum from rats fed with low-chlorogenic acid AP enriched with a high-fiber diet showed repressed proliferation and stimulated alkaline phosphatase activity of primary preosteoblasts. Overall, the beneficial action of AP on bone health was not dependent on its polyphenolic content.

Phenolic composition and antioxidant properties of poplar bud (Populus nigra) extract: individual antioxidant contribution of phenolics and transcriptional effect on skin aging.

The Populus species possess great potential for therapeutical applications, especially for their known anti-inflammatory properties. The antioxidant properties of propolis, a hive product collected by honey bees mainly from poplar bud exudates, suggest that poplar buds also possess antioxidant properties. Here is reported the characterization of the antioxidant properties of an aqueous poplar bud (Populus nigra) extract. It presented a high total phenolic content, and moderate antioxidant properties as determined by ORAC assay. The main phenolic compounds identified were phenolic acids and flavonoid aglycons. These phenolic compounds were analyzed by ORAC assay for their individual antioxidant activity, in order to determine the major contributors to the total antioxidant activity of the extract. Thanks to their high antioxidant activity, caffeic and p-coumaric acids were identified as the major antioxidant components. Representing only 3.5% of its dry weight, these compounds represented together about 50% of the total antioxidant activity of the extract. The antioxidant properties of poplar bud extract and the phenolic compounds identified were also analyzed by cellular antioxidant activity assay (CAA), which was weakly correlated with ORAC assay. The transcriptional effect of poplar bud extract on skin aging was evaluated in vitro on a replicative senescence model of normal human dermal fibroblasts, using a customized DNA macroarray specifically designed to investigate skin aging markers. Among the detected genes, poplar bud extract significantly regulated genes involved in antioxidant defenses, inflammatory response and cell renewal. The collective antioxidant properties and transcriptional effect of this extract suggest potential antiaging properties which could be utilized in cosmetic and nutraceutical formulations.

DNA macroarray study of skin aging-related genes expression modulation by antioxidant plant extracts on a replicative senescence model of human dermal fibroblasts.

The formation of reactive oxygen species (ROS) is a widely accepted pivotal mechanism leading to skin aging. It increases with age, while the endogenous defense mechanisms that counter them decrease. This imbalance, called oxidative stress, leads to the progressive damage of cellular structures and results in accelerated aging. Antioxidant compounds can provide protection from endogenous and exogenous oxidative stress by scavenging free radicals. The main phenolic compounds of oak wood, mate leaf and benjoin resin antioxidant extracts were identified and the effects of these extracts on skin aging markers were evaluated using DNA macroarray technology. The transcriptional effect of the three antioxidant extracts was evaluated in vitro on a replicative senescence model of normal human dermal fibroblasts (NHDF), using a customized DNA macroarray specifically designed to investigate aging markers such as dermal structure, cell renewal, inflammatory response and oxidative stress mechanisms. Among the 149 genes detected, the three antioxidant extracts presented a significant regulation of five genes involved in inflammatory response, cell renewal and antioxidant defenses. The collective transcriptional effects of these extracts suggest interesting antiaging properties which could be utilized in nutraceutical antiaging formulations.

Contribution of chlorogenic acids to the inhibition of human hepatic glucose-6-phosphatase activity in vitro by Svetol, a standardized decaffeinated green coffee extract.

Glucose-6-phosphatase (Glc-6-Pase) is a multicomponent system that exists primarily in the liver and catalyzes the terminal step in gluconeogenesis and glycogenolysis. Several studies have attempted to identify synthetic or natural compounds that inhibit this enzyme complex for therapeutic use in regulating blood glucose and type 2 diabetes. For this paper an in vitro structure-activity relationship study of several natural chlorogenic acids was conducted, and the active components of the natural decaffeinated green coffee extract Svetol were identified. Glucose-6-phosphate (Glc-6-P) hydrolysis was measured in the presence of Svetol or chlorogenic acids in intact human liver microsomes. Svetol significantly inhibited Glc-6-P hydrolysis in intact human liver microsomes in a competitive manner, and it was determined that chlorogenic acids (caffeoylquinic acids and dicaffeoylquinic acids) were the chief compounds mediating this activity. In addition, the structure-activity analysis showed that variation in the position of the caffeoyl residue is an important determinant of inhibition of Glc-6-P hydrolysis. This inhibition by Svetol contributes to its antidiabetic, glucose-lowering effects by reducing hepatic glucose production.

Comparative study of antioxidant properties and total phenolic content of 30 plant extracts of industrial interest using DPPH, ABTS, FRAP, SOD, and ORAC assays.

Aqueous extracts of 30 plants were investigated for their antioxidant properties using DPPH and ABTS radical scavenging capacity assay, oxygen radical absorbance capacity (ORAC) assay, superoxide dismutase (SOD) assay, and ferric reducing antioxidant potential (FRAP) assay. Total phenolic content was also determined by the Folin-Ciocalteu method. Antioxidant properties and total phenolic content differed significantly among selected plants. It was found that oak (Quercus robur), pine (Pinus maritima), and cinnamon (Cinnamomum zeylanicum) aqueous extracts possessed the highest antioxidant capacities in most of the methods used, and thus could be potential rich sources of natural antioxidants. These extracts presented the highest phenolic content (300-400 mg GAE/g). Mate (Ilex paraguariensis) and clove (Eugenia caryophyllus clovis) aqueous extracts also showed strong antioxidant properties and a high phenolic content (about 200 mg GAE/g). A significant relationship between antioxidant capacity and total phenolic content was found, indicating that phenolic compounds are the major contributors to the antioxidant properties of these plants.

Grape-seed procyanidins act as antiinflammatory agents in endotoxin-stimulated RAW 264.7 macrophages by inhibiting NFkB signaling pathway.

Procyanindin extract (PE) is a mixture of polyphenols, mainly procyanidins, obtained from grape seed with putative antiinflammatory activity. We evaluated the PE effect on RAW 264.7 macrophages stimulated with lipopolysaccharide plus interferon-gamma that show a rapid enhanced production of prostaglandin E2 (PGE2) and nitric oxide (NO). Our results demonstrated that PE significantly inhibited the overproduction of NO, dose and time dependently. PE caused a marked inhibition of PGE2 synthesis when administered during activation. Moreover, PE pretreatment diminished iNOS mRNA and protein amount dose dependently (10-65 microg/mL). PE (65 microg/mL) pretreatment inhibited NFkappaB (p65) translocation to nucleus by nearly 40%. Trimeric and longer oligomeric-rich procyanidin fractions from PE (5-30 microg/mL) inhibited iNOS expression but not the monomeric forms catechin and epicatechin. Thus, we show that the degree of polymerization is important in determining procyanidin effects. PE was considerably a more effective inhibitor of NO biosynthesis (IC50 = 50 microg/mL) in comparison to other antiinflammatories, such as aspirin (3 mM), indomethacin (20 microM), and dexamethasone (9 nM). In conclusion, PE modulates inflammatory response in activated macrophages by the inhibition of NO and PGE2 production, suppression of iNOS expression, and NFkB translocation. These results demonstrate an immunomodulatory role of grape seed procyanidins and thus a potential health-benefit in inflammatory conditions that exert an overproduction of NO and PGE2.