195 research outputs found

    Interaction of quercetin, cyanidin, and their O-glucosides with planar lipid models: implications for their biological effects

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    Flavonoids are specialized metabolites produced by plants, as free aglycones or as glycosylated derivatives, which are particularly endowed with a variety of beneficial ealth properties. The antioxidant, anti-inflammatory, antimicrobial, anticancer, antifungal, antiviral, anti-Alzheimer’s, anti-obesity, antidiabetic, and antihypertensive effects of flavonoids are now known. These bioactive phytochemicals have been shown to act on different molecular targets in cells including the plasma membrane. Due to their polyhydroxylated structure, lipophilicity, and planar conformation, they can either bind at the bilayer interface or interact with the hydrophobic fatty acid tails of the membrane. The interaction of quercetin, cyanidin, and their O-glucosides with planar lipid membranes (PLMs) similar in composition to those of the intestine was monitored using an electrophysiological approach. The obtained results show that the tested flavonoids interact with PLM and form conductive units. The modality of interaction with the lipids of the bilayer and the alteration of the biophysical parameters of PLMs induced by the tested substances provided information on their location in the membrane, helping to elucidate the mechanism of action which underlies some pharmacological properties of flavonoids. To our knowledge, the interaction of quercetin, cyanidin, and their O-glucosides with PLM surrogates of the intestinal membrane has never been previously monitored

    Nematicidal Potential of Sulla (<i>Hedysarum coronarium</i> L.) against the Root-Knot Nematode <i>Meloidogyne incognita</i>

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    The content of nematicidal metabolites such as saponins, flavonoids and tannins in sulla (Hedysarum coronarium L.) suggests its potential nematicidal activity. In this study, the biocidal activity of 62.5–1000 ÎŒg mL−1 concentrations of flavonoid and tannin fractions from sulla was assessed in in vitro assays on the infective juveniles (J2) of the root-knot nematode (RKN) Meloidogyne incognita, while the suppressive effects of soil amendments with 10–40 g kg−1 soil rates of sulla biomass were investigated on potted tomato infested by M. incognita. The content of total nitrogen, carbon, flavonoids, tannins and saponins of sulla experimental material was also determined. After a 96-h exposure, more than 80% of the M. incognita J2 were killed even by a 125 ”g mL−1 concentration of the flavonoid extract, while mortality peaked at 89% only at the 1000 ”g mL−1 concentration of the tannin solution. Soil incorporation with sulla biomass significantly reduced the M. incognita densities both on tomato roots and in the soil, compared to either the non-treated control and chemical treatment with Fluopyram. The data confirmed the nematicidal potential of sulla, mainly due to its content of flavonoids and tannins, suggesting its suitability as green manure or a soil amendment for sustainable RKN management

    Antioxidant activity and protective effect of the outer scales hydroalcoholic extract of Allium cepa L. var. Tropea on toxicity damage induced by Cadmium in Caco-2 cells

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    The characterization of bioactive metabolites and the protective effects against Cadmium (Cd) of the hydroalcoholic extract from Allium cepa var. Tropea (Tropea red onion) in human Caco-2 colon adenocarcinoma cells and in vitro antioxidant effects were investigated. Tropea red onion extract showed high levels of bioactive compounds and a strong activity as radical scavenger and inhibitor of lipid peroxidation. The most abundant specialized metabolites were quercetin derivatives. In addition, the extract inhibited NO release in a dosedependent manner. Exposure of Cd treated human Caco-2 cells to the Tropea red onion extract resulted in a higher cytoprotection with a significant falloff of cells damage produced by Cd. The effect of Tropea red onion evaluated with the MTT assay and LDH test, was time-dependent and more evident after 24h of treatment. Caco-2 cells treated with the Tropea red onion extract and CdCl2 at 24h showed a significant cytoprotection at concentrations equal to 50 ÎŒg/mL + 25 ÎŒM and 100 ÎŒg/mL + 25 ÎŒM while at 72h at a concentration of 25 ÎŒg/mL + 25 ÎŒM. We observed with MTT and LDH assays that treatment of cells with Tropea red onion extract at 24h was able to significantly prevent Cd-induced cytotoxicity alon

    Chemical Identification of Specialized Metabolites from Sulla (Hedysarum coronarium L.) Collected in Southern Italy

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    Sulla (Hedysarum coronarium L.) is a biennal forage legume originated from the Mediterranean basin and used for animal feeding due to its high forage quality and palatability. Several species of Hedysarum have been considered for their nutritional, pharmaceutical, and biological properties, and different applications have been reported, both for human consumption and animal nutrition. Although a systematic investigation of the chemical constituents of Hedysarum spp. has been performed in order to provide chemotaxonomic evidences for the genus and to support the pharmacological application of several species within the genus, few data are available on the chemical constituents of H. coronarium, and only the content of condensed tannins and flavonoids in leaves has been previously reported. In the present paper, results from a detailed chemical analysis of the extracts from the leaves and flowers of H. coronarium grown wild in southern Italy are presented. Identification of the main specialized metabolites within the chemical classes of flavonoids, proanthocyanidins and saponins, is described, including considerations on their content in the two plant organs. Information acquired from this study expands the knowledge on H. coronarium as a source of valuable phytochemicals for different applications in human and animal health and nutrition

    Relationship between Chemical Composition and Nematicidal Activity of Different Essential Oils

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    In this study, the relationship between nematicidal activity and chemical composition of ten essential oils (EOs) from different plant species was investigated both in in vitro assays on juveniles (J2) and eggs of the root-knot nematode Meloidogyne incognita and in experiments on tomato in soil infested by M. incognita. Nematode J2 were exposed for 4, 8 or 24 h to 0.78–100 ÎŒg mL−1 concentrations of each EO, whereas 24, 48 or 96 h exposures to 250, 500 and 1000 ÎŒg mL−1 solutions were tested on M. incognita egg masses. Treatments with 50, 100 or 200 ÎŒg kg soil rates of each EO were applied in the experiment on potted tomato. The highest nematicidal potential resulted for the C. verum EO, as highly toxic to both M. incognita J2 and eggs and strongly suppressive on nematode multiplication on tomato roots. The infestation of M. incognita on tomato roots was also strongly reduced by the EOs from E. citriodora and S. aromaticum, both highly toxic to M. incognita J2 but less active on nematode eggs. Adversely, R. graveolens EO strongly inhibited the egg hatch but was limitedly toxic to the infective J2. Chemical composition of the EOs was determined by GC-FID and GC-MS. The ten EOs showed a very different chemical composition in terms of major phytochemicals, with one or two dominant components totally amounting up to 85%. The structure–activity relationship based on the main phytochemicals identified in the assayed EOs and their nematicidal effects on M. incognita was also discussed. Results from this study confirmed that the selection of suitable EO raw materials can lead to the formulation on new effective nematicidal products. Keywords: essential oils; bioactive components; nematicidal activity; Meloidogyne incognita

    Plant development and synthesis of essential oils in micropropagated and mycorrhiza inoculated plants of Origanum vulgare L. ssp. hirtum (Link) Ietswaart

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    Abstract Biomass production of micropropagated oregano was induced by inoculation with the fungus Glomus viscosum. The effects of arbuscular mycorrhizal (AM) symbiosis on morphological and metabolic variations of regenerated oregano plants were investigated at different growth stages. AM greatly increased parameters such as plant leaf area, fresh and dry weight, number of spicasters and verticillasters in infected plants. An increase of the gland density, especially on the upper leaf epidermis, was also observed following the physiological ageing of the tissues. The in vitro plants of O. vulgare ssp. hirtum described in this study provided a qualitatively and quantitatively good source of essential oils that have a chemical profile comparable to that of the control mother plants with carvacrol as the main compound

    Lobularia maritima (L.) Desv. Aerial Parts Methanolic Extract: In Vitro Screening of Biological Activity

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    Abstract: Lobularia maritima (L.) Desv. is a perennial herb growing wild in the Mediterranean basin. The aim of this work was to assess the fatty acid, terpene, phytosterol, and phenolic composition of the methanolic extract and its sub‐fractions using Gas Chromatography‐Mass Spectrometry (GCMS), High‐Performance Liquid Chromathography with Dioide‐Array Detector (HPLC‐DAD), High‐Performance Liquid Chromathography‐High Resolution Mass Spectrometry (HPLC‐HRMS), and Electrospray Ionization Tandem Mass Spectrometry (ESI‐MS/MS). The potential health benefits of this plant species have been investigated as well. The antioxidant activity was determined in vitro by means of 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and ÎČ‐carotene bleaching tests. The inhibitory potential towards the production of the pro‐inflammatory mediator nitric oxide was verified on lipopolysaccharide (LPS)‐stimulated murine macrophage RAW 264.7 cell line. A remarkable inhibitory activity was observed for the dichloromethane fraction, with an IC50 value equal to 45.86 ± 1.05 ÎŒg/mL, a significant result if compared to indomethacin and the known nitric oxide synthase inhibitor NG‐nitro‐L‐arginine methyl ester (L‐NAME), used as positive controls. Moreover, the ethyl acetate fraction proved to be effective in inhibiting pancreatic lipase, an enzyme that plays a pivotal role in the gastrointestinal digestion of dietary fat, suggesting that this species could potentially be a promising source of useful compounds for the treatment of obesity

    Natural Products and Drug Discovery

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    Natural products hold a prominent position in the current discovery and development of drugs and have diverse indications for both human and animal health. Plants, in particular, play a leading role as a source of specialized metabolites with medical effects. Other organisms, such as marine and terrestrial animals and microorganisms, produce very important drug candidate molecules. Specialized metabolites from these varied natural sources can be used directly as bioactive compounds or drug precursors. In addition, due to their broad chemical diversity, they can act as drug prototypes and/or be used as pharmacological tools for different targets. Some examples of natural metabolites that have been developed into useful medical drug are cardiotonic digoxin from Digitalis sp., antimalarial artemisinin from Artemisia annua, anti-cancer taxol from Taxus sp., or podophyllotoxin from Podophyllum peltatum, which served as a synthetic model for the anti-cancer etoposide. The study of natural products is still attracting great scientific attention and their current importance, as a valuable lead for drug discovery, is undebatable. I cordially invite authors to contribute original articles, as well as survey articles, that give the readers of Molecules **MOLECULES NEEDS TO BE ITALICIZED** updated and new perspectives on natural products in drug discovery, including but not limited to natural sources, identification and separation of bioactive phytochemicals, standardization, new biological targets, pre-clinical and clinical trials, pharmacological effects/side effects, and bioassays