Molecules

22 pages, 4683 KB

Open AccessArticle

Surface Properties and Photocatalytic Activity of KTaO₃, CdS, MoS₂ Semiconductors and Their Binary and Ternary Semiconductor Composites

by Beata Bajorowicz, Anna Cybula, Michał J. Winiarski, Tomasz Klimczuk and Adriana Zaleska

Molecules 2014, 19(9), 15339-15360; https://doi.org/10.3390/molecules190915339 - 24 Sep 2014

Cited by 34 | Viewed by 11250

Abstract

Single semiconductors such as KTaO₃, CdS MoS₂ or their precursor solutions were combined to form novel binary and ternary semiconductor nanocomposites by the calcination or by the hydro/solvothermal mixed solutions methods, respectively. The aim of this work was to study [...] Read more.

Single semiconductors such as KTaO₃, CdS MoS₂ or their precursor solutions were combined to form novel binary and ternary semiconductor nanocomposites by the calcination or by the hydro/solvothermal mixed solutions methods, respectively. The aim of this work was to study the influence of preparation method as well as type and amount of the composite components on the surface properties and photocatalytic activity of the new semiconducting photoactive materials. We presented different binary and ternary combinations of the above semiconductors for phenol and toluene photocatalytic degradation and characterized by X-ray powder diffraction (XRD), UV-Vis diffuse reflectance spectroscopy (DRS), scanning electron microscopy (SEM), Brunauer–Emmett–Teller (BET) specific surface area and porosity. The results showed that loading MoS₂ onto CdS as well as loading CdS onto KTaO₃ significantly enhanced absorption properties as compared with single semiconductors. The highest photocatalytic activity in phenol degradation reaction under both UV-Vis and visible light irradiation and very good stability in toluene removal was observed for ternary hybrid obtained by calcination of KTaO₃, CdS, MoS₂ powders at the 10:5:1 molar ratio. Enhanced photoactivity could be related to the two-photon excitation in KTaO₃-CdS-MoS₂ composite under UV-Vis and/or to additional presence of CdMoO₄ working as co-catalyst. Full article

(This article belongs to the Special Issue Photocatalysis)

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15 pages, 825 KB

Open AccessArticle

Hydrogenations without Hydrogen: Titania Photocatalyzed Reductions of Maleimides and Aldehydes

by David W. Manley, Luca Buzzetti, Andrew MacKessack-Leitch and John C. Walton

Molecules 2014, 19(9), 15324-15338; https://doi.org/10.3390/molecules190915324 - 24 Sep 2014

Cited by 16 | Viewed by 9342

Abstract

A mild procedure for the reduction of electron-deficient alkenes and carbonyl compounds is described. UVA irradiations of substituted maleimides with dispersions of titania (Aeroxide P25) in methanol/acetonitrile (1:9) solvent under dry anoxic conditions led to hydrogenation and production of the corresponding succinimides. Aromatic [...] Read more.

A mild procedure for the reduction of electron-deficient alkenes and carbonyl compounds is described. UVA irradiations of substituted maleimides with dispersions of titania (Aeroxide P25) in methanol/acetonitrile (1:9) solvent under dry anoxic conditions led to hydrogenation and production of the corresponding succinimides. Aromatic and heteroaromatic aldehydes were reduced to primary alcohols in similar titania photocatalyzed reactions. A mechanism is proposed which involves two proton-coupled electron transfers to the substrates at the titania surface. Full article

(This article belongs to the Special Issue Free Radicals and Radical Ions)

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10 pages, 923 KB

Open AccessReview

Organic Nitrates: Past, Present and Future

by Maria S. França-Silva, Camille M. Balarini, Josiane C. Cruz, Barkat A. Khan, Pabulo H. Rampelotto and Valdir A. Braga

Molecules 2014, 19(9), 15314-15323; https://doi.org/10.3390/molecules190915314 - 24 Sep 2014

Cited by 32 | Viewed by 12765

Abstract

Nitric oxide (NO) is one of the most important vasodilator molecules produced by the endothelium. It has already been established that NO/cGMP signaling pathway deficiencies are involved in the pathophysiological mechanisms of many cardiovascular diseases. In this context, the development of NO-releasing drugs [...] Read more.

Nitric oxide (NO) is one of the most important vasodilator molecules produced by the endothelium. It has already been established that NO/cGMP signaling pathway deficiencies are involved in the pathophysiological mechanisms of many cardiovascular diseases. In this context, the development of NO-releasing drugs for therapeutic use appears to be an effective alternative to replace the deficient endogenous NO and mimic the role of this molecule in the body. Organic nitrates represent the oldest class of NO donors that have been clinically used. Considering that tolerance can occur when these drugs are applied chronically, the search for new compounds of this class with lower tolerance potential is increasing. Here, we briefly discuss the mechanisms involved in nitrate tolerance and highlight some achievements from our group in the development of new organic nitrates and their preclinical application in cardiovascular disorders. Full article

(This article belongs to the Section Organic Chemistry)

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16 pages, 1165 KB

Open AccessArticle

Electrochemistry of the Self-Assembled Monolayers of Dyads Consisting of Tripod-Shaped Trithiol and Bithiophene on Gold

by Toshikazu Kitagawa, Hiroaki Matsubara, Takao Okazaki and Koichi Komatsu

Molecules 2014, 19(9), 15298-15313; https://doi.org/10.3390/molecules190915298 - 24 Sep 2014

Cited by 15 | Viewed by 9758

Abstract

Self-assembled monolayers (SAMs) of tripod-shaped trithiols, consisting of an adamantane core with three CH₂SH legs and a bithiophene group, were prepared on a Au(111) surface. Adsorption in a tripod-like fashion was supported by polarization modulation-infrared reflection absorption spectroscopy (PM-IRRAS) of the [...] Read more.

Self-assembled monolayers (SAMs) of tripod-shaped trithiols, consisting of an adamantane core with three CH₂SH legs and a bithiophene group, were prepared on a Au(111) surface. Adsorption in a tripod-like fashion was supported by polarization modulation-infrared reflection absorption spectroscopy (PM-IRRAS) of the SAMs, which indicated the absence of free SH groups. Cyclic voltammetry showed an irreversible cathodic wave due to reductive desorption. The SAM also showed an anodic wave due to the single-electron oxidation of the bithiophene moiety without concomitant desorption of the molecules. Although oxidation was irreversible in the absence of a protecting group, it became reversible with the introduction of a terminal phenyl group. The charge of the oxidation was one-third that of the reductive desorption, confirming a three-point adsorption. The surface coverage was ca. 50% of that expected for the anti bithiophene conformation, which suggested that an increase in the surface area per molecule had been caused by the presence of an energetically high-lying syn conformer. In accordance with this, the line shape of the oxidation wave suggested an electrostatic repulsive interaction between neighboring molecules. Full article

(This article belongs to the Section Organic Chemistry)

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40 pages, 3209 KB

Open AccessReview

Current and Potential Applications of Bismuth-Based Drugs

by Donal M. Keogan and Darren M. Griffith

Molecules 2014, 19(9), 15258-15297; https://doi.org/10.3390/molecules190915258 - 23 Sep 2014

Cited by 168 | Viewed by 21665

Abstract

: Bismuth compounds have been used extensively as medicines and in particular for the treatment of gastrointestinal ailments. In addition to bismuth’s well known gastroprotective effects and efficacy in treating H. pylori infection it also has broad anti-microbial, anti-leishmanial and anti-cancer properties. Aspects [...] Read more.

: Bismuth compounds have been used extensively as medicines and in particular for the treatment of gastrointestinal ailments. In addition to bismuth’s well known gastroprotective effects and efficacy in treating H. pylori infection it also has broad anti-microbial, anti-leishmanial and anti-cancer properties. Aspects of the biological chemistry of bismuth are discussed and biomolecular targets associated with bismuth treatment are highlighted. This review strives to provide the reader with an up to date account of bismuth-based drugs currently used to treat patients and discuss potential medicinal applications of bismuth drugs with reference to recent developments in the literature. Ultimately this review aims to encourage original contributions to this exciting and important field. Full article

(This article belongs to the Special Issue Practical Applications of Metal Complexes)

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21 pages, 877 KB

Open AccessArticle

Several Human Cyclin-Dependent Kinase Inhibitors, Structurally Related to Roscovitine, As New Anti-Malarial Agents

by Sandrine Houzé, Nha-Thu Hoang, Olivier Lozach, Jacques Le Bras, Laurent Meijer, Hervé Galons and Luc Demange

Molecules 2014, 19(9), 15237-15257; https://doi.org/10.3390/molecules190915237 - 23 Sep 2014

Cited by 17 | Viewed by 8924

Abstract

In Africa, malaria kills one child each minute. It is also responsible for about one million deaths worldwide each year. Plasmodium falciparum, is the protozoan responsible for the most lethal form of the disease, with resistance developing against the available anti-malarial drugs. [...] Read more.

In Africa, malaria kills one child each minute. It is also responsible for about one million deaths worldwide each year. Plasmodium falciparum, is the protozoan responsible for the most lethal form of the disease, with resistance developing against the available anti-malarial drugs. Among newly proposed anti-malaria targets, are the P. falciparum cyclin-dependent kinases (PfCDKs). There are involved in different stages of the protozoan growth and development but share high sequence homology with human cyclin-dependent kinases (CDKs). We previously reported the synthesis of CDKs inhibitors that are structurally-related to (R)-roscovitine, a 2,6,9-trisubstituted purine, and they showed activity against neuronal diseases and cancers. In this report, we describe the synthesis and the characterization of new CDK inhibitors, active in reducing the in vitro growth of P. falciparum (3D7 and 7G8 strains). Six compounds are more potent inhibitors than roscovitine, and three exhibited IC₅₀ values close to 1 µM for both 3D7 and 7G8 strains. Although, such molecules do inhibit P. falciparum growth, they require further studies to improve their selectivity for PfCDKs. Full article

(This article belongs to the Special Issue Design and Study of Kinase Inhibitors)

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13 pages, 851 KB

Open AccessArticle

Regulatory Effect of Astragalus Polysaccharides on Intestinal Intraepithelial γδT Cells of Tumor Bearing Mice

by Shuyu Sun, Kang Zheng, Hongyan Zhao, Cheng Lu, Biao Liu, Changyuan Yu, Ge Zhang, Zhaoxiang Bian, Aiping Lu and Xiaojuan He

Molecules 2014, 19(9), 15224-15236; https://doi.org/10.3390/molecules190915224 - 23 Sep 2014

Cited by 40 | Viewed by 7877

Abstract

Astragalus polysaccharides (APS) possess multiple immunomodulatory activities. Due to its high molecular weight, orally administration of APS is not easily absorbed into the blood stream, and how APS exerts its capacity in vivo is still not well elucidated. We assume that enteric mucosal [...] Read more.

Astragalus polysaccharides (APS) possess multiple immunomodulatory activities. Due to its high molecular weight, orally administration of APS is not easily absorbed into the blood stream, and how APS exerts its capacity in vivo is still not well elucidated. We assume that enteric mucosal immune response might trigger the immune regulation of APS, and our previous studies demonstrated that APS had regulatory activity on intraepithelial lymphocytes (IELs). Therefore, this study aimed to investigate the functions of APS on intestinal intraepithelial γδT cells, a major subset in IELs and an essential component of maintaining homeostasis and immune regulation in enteric mucosa. Results showed that APS could promote proliferation and function of intestinal intraepithelial γδT cells in vitro, the IFN-γ, FasL and GrB mRNA levels in γδT cells were all significantly increased. Moreover, APS also improved the activity of intestinal intraepithelial γδT cells in vivo, as cytokines production and cytotoxicity of γδT cells were all remarkably improved in tumor-bearing mice treated with APS. In addition, the levels of TNF-α and IFN-γ were significantly increased, whereas the levels of IL-10 and TGF-β were significantly decreased in tumor-bearing mice treated with APS. In conclusion, this study demonstrated that APS could improve proliferation and function of intestinal intraepithelial γδT cells, which might an important pathway for immunomodulation of APS in cancer therapy. Full article

(This article belongs to the Section Medicinal Chemistry)

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11 pages, 712 KB

Open AccessArticle

Antioxidant Effects of Grape Vine Cane Extracts from Different Chinese Grape Varieties on Edible Oils

by Zhuo Min, Zemei Guo, Kai Wang, Ang Zhang, Hua Li and Yulin Fang

Molecules 2014, 19(9), 15213-15223; https://doi.org/10.3390/molecules190915213 - 23 Sep 2014

Cited by 14 | Viewed by 6677

Abstract

This study involved the determination of the peroxide value (POV) as a measure of the resistance of the oxidation of edible oil with grape vine cane additives to assess their antioxidation potential. The study demonstrated that grape extracts of canes could effectively inhibit [...] Read more.

This study involved the determination of the peroxide value (POV) as a measure of the resistance of the oxidation of edible oil with grape vine cane additives to assess their antioxidation potential. The study demonstrated that grape extracts of canes could effectively inhibit the lipid oxidation of edible oils and that this ability varied significantly due to the different extraction solvents employed, as well as to the different varieties of canes used. Lipid oxidation of edible oils was significantly reduced under an accelerated storage condition of 70 ± 1 °C in the presence of Vitamin C (VC), which was chosen as a synergist of grape vine cane extract. A 4:1 ratio of Victoria Blanc-ethyl acetate fraction (EAF) and VC led to a significant lowering of the peroxide value and indicated a better antioxidant effect. Thus, these results indicated that some varieties of grape vine cane extracts could be applied as natural antioxidants for elevation of the quality of edible oils in the food industry. Full article

(This article belongs to the Section Natural Products Chemistry)

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17 pages, 756 KB

Open AccessReview

Small Molecule Tyrosine Kinase Inhibitors of ErbB2/HER2/Neu in the Treatment of Aggressive Breast Cancer

by Richard L. Schroeder, Cheryl L. Stevens and Jayalakshmi Sridhar

Molecules 2014, 19(9), 15196-15212; https://doi.org/10.3390/molecules190915196 - 23 Sep 2014

Cited by 87 | Viewed by 17092

Abstract

The human epidermal growth factor receptor 2 (HER2) is a member of the erbB class of tyrosine kinase receptors. These proteins are normally expressed at the surface of healthy cells and play critical roles in the signal transduction cascade in a myriad of [...] Read more.

The human epidermal growth factor receptor 2 (HER2) is a member of the erbB class of tyrosine kinase receptors. These proteins are normally expressed at the surface of healthy cells and play critical roles in the signal transduction cascade in a myriad of biochemical pathways responsible for cell growth and differentiation. However, it is widely known that amplification and subsequent overexpression of the HER2 encoding oncogene results in unregulated cell proliferation in an aggressive form of breast cancer known as HER2-positive breast cancer. Existing therapies such as trastuzumab (Herceptin^®) and lapatinib (Tyverb/Tykerb^®), a monoclonal antibody inhibitor and a dual EGFR/HER2 kinase inhibitor, respectively, are currently used in the treatment of HER2-positive cancers, although issues with high recurrence and acquired resistance still remain. Small molecule tyrosine kinase inhibitors provide attractive therapeutic targets, as they are able to block cell signaling associated with many of the proposed mechanisms for HER2 resistance. In this regard we aim to present a review on the available HER2 tyrosine kinase inhibitors, as well as those currently in development. The use of tyrosine kinase inhibitors as sequential or combinatorial therapeutic strategies with other HER family inhibitors is also discussed. Full article

(This article belongs to the Special Issue Design and Study of Kinase Inhibitors)

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16 pages, 963 KB

Open AccessArticle

Synthesis, Leishmanicidal Activity and Theoretical Evaluations of a Series of Substituted bis-2-Hydroxy-1,4-Naphthoquinones

by Morgana V. De Araújo, Patricia S. O. De Souza, Aline C. De Queiroz, Carolina B. B. Da Matta, Anderson Brandão Leite, Amanda Evelyn Da Silva, José A. A. De França, Tania M. S. Silva, Celso A. Camara and Magna S. Alexandre-Moreira

Molecules 2014, 19(9), 15180-15195; https://doi.org/10.3390/molecules190915180 - 22 Sep 2014

Cited by 48 | Viewed by 8189

Abstract

A series of eight substituted bis-2-hydroxy-1,4-naphthoquinone derivatives was synthesized through lawsone condensation with various aromatic and aliphatic aldehydes under mild acidic conditions. The title compounds were evaluated for antileishmanial activity in vitro against Leishmania amazonensis and Leishmania braziliensis promastigotes; six compounds showed good [...] Read more.

A series of eight substituted bis-2-hydroxy-1,4-naphthoquinone derivatives was synthesized through lawsone condensation with various aromatic and aliphatic aldehydes under mild acidic conditions. The title compounds were evaluated for antileishmanial activity in vitro against Leishmania amazonensis and Leishmania braziliensis promastigotes; six compounds showed good activity without significant toxic effects. The compound with the highest activity was used for an in vivo assay with Leishmania amazonensis. Full article

(This article belongs to the Section Medicinal Chemistry)

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18 pages, 808 KB

Open AccessArticle

Comparative Studies on Polyphenolic Composition, Antioxidant and Antimicrobial Activities of Schisandra chinensis Leaves and Fruits

by Andrei Mocan, Gianina Crișan, Laurian Vlase, Ovidiu Crișan, Dan Cristian Vodnar, Oana Raita, Ana-Maria Gheldiu, Anca Toiu, Radu Oprean and Ioan Tilea

Molecules 2014, 19(9), 15162-15179; https://doi.org/10.3390/molecules190915162 - 22 Sep 2014

Cited by 112 | Viewed by 13585

Abstract

The aim of this paper was to evaluate the antioxidant and antimicrobial activities and the polyphenolic content of Schisandra chinensis (Turcz.) Baill. leaves and fruits. The leaves are an important source of flavonoids (35.10 ± 1.23 mg RE/g plant material). Qualitative and quantitative [...] Read more.

The aim of this paper was to evaluate the antioxidant and antimicrobial activities and the polyphenolic content of Schisandra chinensis (Turcz.) Baill. leaves and fruits. The leaves are an important source of flavonoids (35.10 ± 1.23 mg RE/g plant material). Qualitative and quantitative analyses of the polyphenolic compounds were achieved using a HPLC-UV-MS method. The main flavonoid from the leaves was isoquercitrin (2486.18 ± 5.72 μg/g plant material), followed by quercitrin (1645.14 ± 2.12 μg/g plant material). Regarding the fruit composition, the dominant compound there was rutin (13.02 ± 0.21 μg/g plant material), but comparing with the leaves, fruits can be considered a poor source of phenolic compounds. The antioxidant activity was evaluated by DPPH, TEAC, hemoglobin ascorbate peroxidase activity inhibition (HAPX), inhibition of lipid peroxidation catalyzed by cytochrome c and EPR spectroscopic assays, revealing a better antioxidant activity for the S. chinensis leaves extract. In the antimicrobial assay, S. chinensis leaves extract showed efficient activities against the targeted bacteria, being more active than the fruits extract. The results suggest the leaves of S. chinensis as a valuable source of antioxidant compounds with significant antioxidant activity. Full article

(This article belongs to the Section Natural Products Chemistry)

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46 pages, 1465 KB

Open AccessReview

Carbonylation of Ethene Catalysed by Pd(II)-Phosphine Complexes

by Gianni Cavinato and Luigi Toniolo

Molecules 2014, 19(9), 15116-15161; https://doi.org/10.3390/molecules190915116 - 22 Sep 2014

Cited by 45 | Viewed by 11424

Abstract

This review deals with olefin carbonylation catalysed by Pd(II)-phosphine complexes in protic solvents. In particular, the results obtained in the carbonylation with ethene are reviewed. After a short description of the basic concepts relevant to this catalysis, the review treats in greater details [...] Read more.

This review deals with olefin carbonylation catalysed by Pd(II)-phosphine complexes in protic solvents. In particular, the results obtained in the carbonylation with ethene are reviewed. After a short description of the basic concepts relevant to this catalysis, the review treats in greater details the influence of the bite angle, skeletal rigidity, electronic and steric bulk properties of the ligand on the formation of the products, which range from high molecular weight perfectly alternating polyketones to methyl propanoate. It is shown that the steric bulk plays a major role in directing the selectivity. Particular emphasis is given to the factors governing the very active and selective catalysis to methyl propanoate, including the mechanism of the catalytic cycles with diphosphine- and monophosphine-catalysts. A brief note on the synthesis of methyl propanoate using a “Lucite” type catalyst in ionic liquids is also illustrated. A chapter is dedicated to the carbonylation of olefins in aqueous reaction media. The nonalternating CO-ethene copolymerization is also treated. Full article

(This article belongs to the Special Issue Carbonylation Chemistry)

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13 pages, 1231 KB

Open AccessArticle

LC-ESI-MS/MS Analysis and Pharmacokinetics of Plantainoside D Isolated from Chirita longgangensis var. hongyao, a Potential Anti-Hypertensive Active Component in Rats

by Manyuan Wang, Shujun Fu, Xinshi Zhang, Jing Li, Muxin Gong and Feng Qiu

Molecules 2014, 19(9), 15103-15115; https://doi.org/10.3390/molecules190915103 - 22 Sep 2014

Cited by 12 | Viewed by 7829

Abstract

Plantainoside D (PD) is a potential anti-hypertensive active ingredient newly isolated from the dried plants of Chirita longgangensis var. hongyao. A sensitive and specific LC-ESI-MS/MS method was first developed and validated for the analysis of PD in rat plasma using genistein as [...] Read more.

Plantainoside D (PD) is a potential anti-hypertensive active ingredient newly isolated from the dried plants of Chirita longgangensis var. hongyao. A sensitive and specific LC-ESI-MS/MS method was first developed and validated for the analysis of PD in rat plasma using genistein as the internal standard (IS). The plasma samples were pretreated with methanol-acetonitrile (50:50, v/v) to precipitate protein, and then chromatographed on a reverse-phase Agilent Zorbax XDB C18 column (50 mm × 2.1 mm, 3.5 μm). Gradient elution was utilized, with a mobile phase consisting of water and acetonitrile both containing 0.1% formic acid, and the flow rate was set at 0.50 mL/min. The analytes were monitored by tandem-mass spectrometry with negative electrospray ionization. The precursor/product transitions (m/z) in the negative ion mode were 639.2 → 160.9 Thomson (Th) and 268.9 → 158.9 Thomson (Th) for PD and IS, respectively. Linearity was achieved in the 0.10–200 ng/mL range, with a lower limit of quantification of 0.10 ng/mL. The precision and accuracy for both intra- and inter-day determination of the analyte were all within ±15%. The present method has been applied for pharmacokinetic study of PD after oral and intravenous administration in rats. The oral absolute bioavailability (F) of PD in rats was estimated to be 1.12% ± 0.46% with an elimination half-life (t_1/2) value of 1.63 ± 0.19 h, suggesting its poor absorption and/or strong metabolism in vivo. Full article

(This article belongs to the Collection Bioactive Compounds)

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15 pages, 1182 KB

Open AccessArticle

The Plant Decapeptide OSIP108 Can Alleviate Mitochondrial Dysfunction Induced by Cisplatin in Human Cells

by Pieter Spincemaille, Hamed Alborzinia, Jeroen Dekervel, Petra Windmolders, Jos Van Pelt, David Cassiman, Olivier Cheneval, David J. Craik, Julia Schur, Ingo Ott, Stefan Wölfl, Bruno P. A. Cammue and Karin Thevissen

Molecules 2014, 19(9), 15088-15102; https://doi.org/10.3390/molecules190915088 - 19 Sep 2014

Cited by 5 | Viewed by 6739

Abstract

We investigated the effect of the Arabidopsis thaliana-derived decapeptide OSIP108 on human cell tolerance to the chemotherapeutic agent cisplatin (Cp), which induces apoptosis and mitochondrial dysfunction. We found that OSIP108 increases the tolerance of HepG2 cells to Cp and prevents Cp-induced changes in [...] Read more.

We investigated the effect of the Arabidopsis thaliana-derived decapeptide OSIP108 on human cell tolerance to the chemotherapeutic agent cisplatin (Cp), which induces apoptosis and mitochondrial dysfunction. We found that OSIP108 increases the tolerance of HepG2 cells to Cp and prevents Cp-induced changes in basic cellular metabolism. More specifically, we demonstrate that OSIP108 reduces Cp-induced inhibition of respiration, decreases glycolysis and prevents Cp-uptake in HepG2 cells. Apart from its protective action against Cp in human cells, OSIP108 also increases the yeast Saccharomyces cerevisiae tolerance to Cp. A limited yeast-based study of OSIP108 analogs showed that cyclization does not severely affect its activity, which was further confirmed in HepG2 cells. Furthermore, the similarity in the activity of the D-stereoisomer (mirror image) form of OSIP108 with the L-stereoisomer suggests that its mode of action does not involve binding to a stereospecific receptor. In addition, as OSIP108 decreases Cp uptake in HepG2 cells and the anti-Cp activity of OSIP108 analogs without free cysteine is reduced, OSIP108 seems to protect against Cp-induced toxicity only partly via complexation. Taken together, our data indicate that OSIP108 and its cyclic derivatives can protect against Cp-induced toxicity and, thus, show potential as treatment options for mitochondrial dysfunction- and apoptosis-related conditions. Full article

(This article belongs to the Special Issue Peptide Chemistry)

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13 pages, 2242 KB

Open AccessReview

Are TiO₂ Nanotubes Worth Using in Photocatalytic Purification of Air and Water?

by Pierre Pichat

Molecules 2014, 19(9), 15075-15087; https://doi.org/10.3390/molecules190915075 - 19 Sep 2014

Cited by 29 | Viewed by 8268

Abstract

Titanium dioxide nanotubes (TNT) have mainly been used in dye sensitized solar cells, essentially because of a higher transport rate of electrons from the adsorbed photo-excited dye to the Ti electrode onto which TNT instead of TiO₂ nanoparticles (TNP) are attached. The [...] Read more.

Titanium dioxide nanotubes (TNT) have mainly been used in dye sensitized solar cells, essentially because of a higher transport rate of electrons from the adsorbed photo-excited dye to the Ti electrode onto which TNT instead of TiO₂ nanoparticles (TNP) are attached. The dimension ranges and the two main synthesis methods of TNT are briefly indicated here. Not surprisingly, the particular and regular texture of TNT was also expected to improve the photocatalytic efficacy for pollutant removal in air and water with respect to TNP. In this short review, the validity of this expectation is checked using the regrettably small number of literature comparisons between TNT and commercialized TNP referring to films of similar thickness and layers or slurries containing an equal TiO₂ mass. Although the irradiated geometrical area differed for each study, it was identical for each comparison considered here. For the removal of toluene (methylbenzene) or acetaldehyde (ethanal) in air, the average ratio of the efficacy of TNT over that of TiO₂ P25 was about 1.5, and for the removal of dyes in water, it was around 1. This lack of major improvement with TNT compared to TNP could partially be due to TNT texture disorders as seems to be suggested by the better average performance of anodic oxidation-prepared TNT. It could also come from the fact that the properties influencing the efficacy are more numerous, their interrelations more complex and their effects more important for pollutant removal than for dye sensitized solar cells and photoelectrocatalysis where the electron transport rate is the crucial parameter. Full article

(This article belongs to the Special Issue Photocatalysis)

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17 pages, 679 KB

Open AccessReview

New Uses for Old Drugs: The Tale of Artemisinin Derivatives in the Elimination of Schistosomiasis Japonica in China

by Yi-Xin Liu, Wei Wu, Yue-Jin Liang, Zu-Liang Jie, Hui Wang, Wei Wang and Yi-Xin Huang

Molecules 2014, 19(9), 15058-15074; https://doi.org/10.3390/molecules190915058 - 19 Sep 2014

Cited by 52 | Viewed by 10488

Abstract

Artemisinin (qinghaosu), extracted from the Chinese herb Artemisia annua L. in 1972, and its three major derivatives—artemether, artesunate and dihydroartemisinin—were firstly identified as antimalarials and found active against all species of the malaria parasite. Since the early 1980s, artemisinin and its derivatives have [...] Read more.

Artemisinin (qinghaosu), extracted from the Chinese herb Artemisia annua L. in 1972, and its three major derivatives—artemether, artesunate and dihydroartemisinin—were firstly identified as antimalarials and found active against all species of the malaria parasite. Since the early 1980s, artemisinin and its derivatives have been found efficacious against Schistosoma spp., notably larval parasites, and artemisinin derivatives have played a critical role in the prevention and treatment of human schistosomiasis in China. Currently, China is moving towards the progress of schistosomiasis elimination. However, the potential development of praziquantel resistance may pose a great threat to the progress of elimination of schistosomiasis japonica in China. Fortunately, these three major artemisinin derivatives also exhibit actions against adult parasites, and reduced sensitivity to artemether, artesunate and dihydroartemisinin has been detected in praziquantel-resistant S. japonicum. In this review, we describe the application of artemisinin derivatives in the prevention and treatment of schistosomiasis japonica in China, so as to provide tools for the global agenda of schistosomiasis elimination. In addition to antimalarial and antischistosomal actions, they also show activities against other parasites and multiple cancers. Artemisinin derivatives, as old drugs identified firstly as antimalarials, continue to create new stories. Full article

(This article belongs to the Collection Natural Products as Leads or Drugs against Neglected Tropical Diseases)

16 pages, 1578 KB

Open AccessArticle

Rapid Identification of Coumarins from Micromelum falcatum by UPLC-HRMS/MS and Targeted Isolation of Three New Derivatives

by Eirini Kouloura, Eirini Danika, Sothea Kim, Mélanie Hoerlé, Muriel Cuendet, Maria Halabalaki and Leandros A. Skaltsounis

Molecules 2014, 19(9), 15042-15057; https://doi.org/10.3390/molecules190915042 - 19 Sep 2014

Cited by 7 | Viewed by 7391

Abstract

Micromelum falcatum, a medicinal plant of the Rutaceae family, has been used in the Traditional Chinese Medicine (TCM) mainly against colds and rheumatoid arthritis. Despite its traditional use the association of its constituents with possible anti-inflammatory activity has not been explored. During [...] Read more.

Micromelum falcatum, a medicinal plant of the Rutaceae family, has been used in the Traditional Chinese Medicine (TCM) mainly against colds and rheumatoid arthritis. Despite its traditional use the association of its constituents with possible anti-inflammatory activity has not been explored. During this study, a rapid UPLC-ESI(+)-HRMS method was developed for the profiling of M. falcatum leave extracts and the targeted isolation of coumarin constituents. Based on chromatographic, spectroscopic and spectrometric features several 7-oxygenated coumarin derivatives were detected. After targeted isolation, eight coumarins, among them three new natural products, namely microfalcrin, microcoumaririn and micromelosidester, were purified using semi-preparative HPLC and unambiguously identified by 1 and 2D NMR. Furthermore, important spectrometric characteristics were revealed based on the HRMS and HRMS/MS spectra of the isolated 7-oxygenated coumarins facilitating their identification in complex mixtures. Finally, the anti-inflammatory properties of the extracts and representative compounds were evaluated by measuring the inhibition of the pro-inflammatory mediator NF-κB induction and nitric oxide (NO) production. Full article

(This article belongs to the Section Natural Products Chemistry)

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16 pages, 1382 KB

Open AccessArticle

Photochemistry and Radical Chemistry under Low Intensity Visible Light Sources: Application to Photopolymerization Reactions

by Jacques Lalevée, Fabrice Morlet-Savary, Céline Dietlin, Bernadette Graff and Jean-Pierre Fouassier

Molecules 2014, 19(9), 15026-15041; https://doi.org/10.3390/molecules190915026 - 18 Sep 2014

Cited by 17 | Viewed by 9415

Abstract

The search for radical initiators able to work under soft conditions is a great challenge, driven by the fact that the use of safe and cheap light sources is very attractive. In the present paper, a review of some recently reported photoinitiating systems [...] Read more.

The search for radical initiators able to work under soft conditions is a great challenge, driven by the fact that the use of safe and cheap light sources is very attractive. In the present paper, a review of some recently reported photoinitiating systems for polymerization under soft conditions is provided. Different approaches based on multi-component systems (e.g., photoredox catalysis) or light harvesting photoinitiators are described and discussed. The chemical mechanisms associated with the production of free radicals usable as initiating species or mediators of cations are reported. Full article

(This article belongs to the Special Issue Free Radicals and Radical Ions)

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21 pages, 785 KB

Open AccessArticle

Synthesis and Biological Evaluation of New 1,3-Thiazolidine-4-one Derivatives of 2-(4-Isobutylphenyl)propionic Acid

by Ioana Mirela Vasincu, Maria Apotrosoaei, Andreea-Teodora Panzariu, Frédéric Buron, Sylvain Routier and Lenuta Profire

Molecules 2014, 19(9), 15005-15025; https://doi.org/10.3390/molecules190915005 - 18 Sep 2014

Cited by 23 | Viewed by 8895

Abstract

New thiazolidine-4-one derivatives of 2-(4-isobutylphenyl)propionic acid (ibuprofen) have been synthesized as potential anti-inflammatory drugs. The structure of the new compounds was proved using spectral methods (FR-IR, ¹H-NMR, ¹³C-NMR, MS). The in vitro antioxidant potential of the synthesized compounds was evaluated according [...] Read more.

New thiazolidine-4-one derivatives of 2-(4-isobutylphenyl)propionic acid (ibuprofen) have been synthesized as potential anti-inflammatory drugs. The structure of the new compounds was proved using spectral methods (FR-IR, ¹H-NMR, ¹³C-NMR, MS). The in vitro antioxidant potential of the synthesized compounds was evaluated according to the total antioxidant activity, the DPPH and ABTS radical scavenging assays. Reactive oxygen species (ROS) and free radicals are considered to be involved in many pathological events like diabetes mellitus, neurodegenerative diseases, cancer, infections and more recently, in inflammation. It is known that overproduction of free radicals may initiate and amplify the inflammatory process via upregulation of genes involved in the production of proinflammatory cytokines and adhesion molecules. The chemical modulation of acyl hydrazones of ibuprofen 3a–l through cyclization to the corresponding thiazolidine-4-ones 4a–n led to increased antioxidant potential, as all thiazolidine-4-ones were more active than their parent acyl hydrazones and also ibuprofen. The most active compounds are the thiazolidine-4-ones 4e, m, which showed the highest DPPH radical scavenging ability, their activity being comparable with vitamin E. Full article

(This article belongs to the Section Medicinal Chemistry)

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6 pages, 672 KB

Open AccessCommunication

A Novel Synthesis of the Oxazolidinone Antithrombotic Agent Rivaroxaban

by Jianyong Yuan, Kai Liu, Lun Li, Yong Yuan, Xuelei Liu and Yanwu Li

Molecules 2014, 19(9), 14999-15004; https://doi.org/10.3390/molecules190914999 - 18 Sep 2014

Cited by 21 | Viewed by 12031

Abstract

A facile synthetic route of rivaroxaban has been developed. Using commercially available (R)-epichlorohydrin and bromobenzene as the starting materials, rivaroxaban was obtained in 39% overall yield using a Goldberg coupling as the key step. The synthetic route represents a convenient procedure [...] Read more.

A facile synthetic route of rivaroxaban has been developed. Using commercially available (R)-epichlorohydrin and bromobenzene as the starting materials, rivaroxaban was obtained in 39% overall yield using a Goldberg coupling as the key step. The synthetic route represents a convenient procedure for the production of rivaroxaban. Full article

(This article belongs to the Section Organic Chemistry)

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12 pages, 815 KB

Open AccessArticle

Synthesis of New Quinoxalines Containing an Oxirane Ring by the TDAE Strategy and in Vitro Evaluation in Neuroblastoma Cell Lines

by Marc Montana, Florian Correard, Omar Khoumeri, Marie-Anne Esteve, Thierry Terme and Patrice Vanelle

Molecules 2014, 19(9), 14987-14998; https://doi.org/10.3390/molecules190914987 - 18 Sep 2014

Cited by 28 | Viewed by 7008

Abstract

Neuroblastoma is an aggressive pediatric malignancy with significant chemotherapeutic resistance. In order to obtain new compounds active on neuroblastoma cell lines, we investigated the reactivity of carbanion formed via TDAE in quinoxaline series. The new synthesized compounds were tested for their anti-proliferative activity [...] Read more.

Neuroblastoma is an aggressive pediatric malignancy with significant chemotherapeutic resistance. In order to obtain new compounds active on neuroblastoma cell lines, we investigated the reactivity of carbanion formed via TDAE in quinoxaline series. The new synthesized compounds were tested for their anti-proliferative activity on two neuroblastoma cell lines, and seven oxirane derivatives obtained interesting activities. Full article

(This article belongs to the Section Medicinal Chemistry)

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8 pages, 705 KB

Open AccessArticle

Pharmacological Effects of “Jutsu” (Atractylodis rhizome and Atractylodis lanceae rhizome) on 1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane (DOI)-Induced Head Twitch Response in Mice (I)

by Chiaki Murayama, Ching-Chiung Wang, Seiwa Michihara and Hisayoshi Norimoto

Molecules 2014, 19(9), 14979-14986; https://doi.org/10.3390/molecules190914979 - 18 Sep 2014

Cited by 11 | Viewed by 6712

Abstract

Hallucinations are a common non-motor symptom of Parkinson’s disease and various forms of dementias. Yokukansan and Yokukansankachimpihange have attracted attention due to their effectiveness in the treatment of hallucinations of dementia. To clarify which component in these formulas contribute to the effects, at [...] Read more.

Hallucinations are a common non-motor symptom of Parkinson’s disease and various forms of dementias. Yokukansan and Yokukansankachimpihange have attracted attention due to their effectiveness in the treatment of hallucinations of dementia. To clarify which component in these formulas contribute to the effects, at first, we focused on their differences in compositions to examine the pharmacological effects on the selective 5-HT_2A/2C agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI)-induced head-twitch response (HTR) in mice that has been used as animal hallucination model. Results indicated that water extract of Byaku-jutsu (Atractylodes japonica) showed a stronger inhibitory effect on DOI-induced HTR than that of So-jutsu (A. lancea) corresponding to their major constituents of atractylenolide III and β-eudesmol, and suggested that the major constituents should be active constituents contributing to the antihallucination effects of Byaku- and So-jutsu. Besides, the part B–C ring (butenolide) in atractylenolide III was found to be similar to the structure of serotonin and suggested that the B–C ring may partially play role in antagonistic activity against serotonin receptors. Thus, a novel, rational design of butenolide-related compounds may as potential lead compounds for new drug development. Analysis of the chemical components of Byaku- and So-jutsu and further study on their structure-activity relationships are currently in progress. Full article

(This article belongs to the Section Natural Products Chemistry)

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18 pages, 4310 KB

Open AccessArticle

A Multi-Scale–Multi-Stable Model for the Rhodopsin Photocycle

by Francesco Tavanti and Valentina Tozzini

Molecules 2014, 19(9), 14961-14978; https://doi.org/10.3390/molecules190914961 - 18 Sep 2014

Cited by 11 | Viewed by 9624

Abstract

We report a multi-scale simulation study of the photocycle of the rhodopsins. The quasi-atomistic representation (“united atoms” UA) of retinal is combined with a minimalist coarse grained (CG, one-bead-per amino acid) representation of the protein, in a hybrid UA/CG approach, which is the [...] Read more.

We report a multi-scale simulation study of the photocycle of the rhodopsins. The quasi-atomistic representation (“united atoms” UA) of retinal is combined with a minimalist coarse grained (CG, one-bead-per amino acid) representation of the protein, in a hybrid UA/CG approach, which is the homolog of QM/MM, but at lower resolution. An accurate multi-stable parameterization of the model allows simulating each state and transition among them, and the combination of different scale representation allows addressing the entire photocycle. We test the model on bacterial rhodopsin, for which more experimental data are available, and then also report results for mammalian rhodopsins. In particular, the analysis of simulations reveals the spontaneous appearance of meta-stable states in quantitative agreement with experimental data. Full article

(This article belongs to the Special Issue Multiscale Chemical Modeling Using Quantum Mechanics/Molecular Mechanics (QM/MM) Methods: Advances and Applications)

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13 pages, 997 KB

Open AccessArticle

Effect of Standardized Cranberry Extract on the Activity and Expression of Selected Biotransformation Enzymes in Rat Liver and Intestine

by Hana Bártíková, Iva Boušová, Pavla Jedličková, Kateřina Lněničková, Lenka Skálová and Barbora Szotáková

Molecules 2014, 19(9), 14948-14960; https://doi.org/10.3390/molecules190914948 - 18 Sep 2014

Cited by 9 | Viewed by 9075

Abstract

The use of dietary supplements containing cranberry extract is a common way to prevent urinary tract infections. As consumption of these supplements containing a mixture of concentrated anthocyanins and proanthocyanidins has increased, interest in their possible interactions with drug-metabolizing enzymes has grown. In [...] Read more.

The use of dietary supplements containing cranberry extract is a common way to prevent urinary tract infections. As consumption of these supplements containing a mixture of concentrated anthocyanins and proanthocyanidins has increased, interest in their possible interactions with drug-metabolizing enzymes has grown. In this in vivo study, rats were treated with a standardized cranberry extract (CystiCran^®) obtained from Vaccinium macrocarpon in two dosage schemes (14 days, 0.5 mg of proanthocyanidins/kg/day; 1 day, 1.5 mg of proanthocyanidins/kg/day). The aim of this study was to evaluate the effect of anthocyanins and proanthocyanidins contained in this extract on the activity and expression of intestinal and hepatic biotransformation enzymes: cytochrome P450 (CYP1A1, CYP1A2, CYP2B and CYP3A), carbonyl reductase 1 (CBR1), glutathione-S-transferase (GST) and UDP-glucuronosyl transferase (UGT). Administration of cranberry extract led to moderate increases in the activities of hepatic CYP3A (by 34%), CYP1A1 (by 38%), UGT (by 40%), CBR1 (by 17%) and GST (by 13%), while activities of these enzymes in the small intestine were unchanged. No changes in the relative amounts of these proteins were found. Taken together, the interactions of cranberry extract with simultaneously administered drugs seem not to be serious. Full article

(This article belongs to the Special Issue Anthocyanins)

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29 pages, 1014 KB

Open AccessReview

Experimental Studies of the Molecular Pathways Regulated by Exercise and Resveratrol in Heart, Skeletal Muscle and the Vasculature

by Vernon W. Dolinsky and Jason R. B. Dyck

Molecules 2014, 19(9), 14919-14947; https://doi.org/10.3390/molecules190914919 - 18 Sep 2014

Cited by 29 | Viewed by 13194

Abstract

Regular exercise contributes to healthy aging and the prevention of chronic disease. Recent research has focused on the development of molecules, such as resveratrol, that activate similar metabolic and stress response pathways as exercise training. In this review, we describe the effects of [...] Read more.

Regular exercise contributes to healthy aging and the prevention of chronic disease. Recent research has focused on the development of molecules, such as resveratrol, that activate similar metabolic and stress response pathways as exercise training. In this review, we describe the effects of exercise training and resveratrol on some of the organs and tissues that act in concert to transport oxygen throughout the body. In particular, we focus on animal studies that investigate the molecular signaling pathways induced by these interventions. We also compare and contrast the effects of exercise and resveratrol in diseased states. Full article

(This article belongs to the Special Issue Resveratrol)

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17 pages, 2377 KB

Open AccessReview

1,4-Naphthoquinones: From Oxidative Damage to Cellular and Inter-Cellular Signaling

by Lars-Oliver Klotz, Xiaoqing Hou and Claus Jacob

Molecules 2014, 19(9), 14902-14918; https://doi.org/10.3390/molecules190914902 - 17 Sep 2014

Cited by 197 | Viewed by 15150

Abstract

Naphthoquinones may cause oxidative stress in exposed cells and, therefore, affect redox signaling. Here, contributions of redox cycling and alkylating properties of quinones (both natural and synthetic, such as plumbagin, juglone, lawsone, menadione, methoxy-naphthoquinones, and others) to cellular and inter-cellular signaling processes are [...] Read more.

Naphthoquinones may cause oxidative stress in exposed cells and, therefore, affect redox signaling. Here, contributions of redox cycling and alkylating properties of quinones (both natural and synthetic, such as plumbagin, juglone, lawsone, menadione, methoxy-naphthoquinones, and others) to cellular and inter-cellular signaling processes are discussed: (i) naphthoquinone-induced Nrf2-dependent modulation of gene expression and its potentially beneficial outcome; (ii) the modulation of receptor tyrosine kinases, such as the epidermal growth factor receptor by naphthoquinones, resulting in altered gap junctional intercellular communication. Generation of reactive oxygen species and modulation of redox signaling are properties of naphthoquinones that render them interesting leads for the development of novel compounds of potential use in various therapeutic settings. Full article

(This article belongs to the Special Issue Redox Active Natural Products and Their Interaction with Cellular Signalling Pathways)

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23 pages, 832 KB

Open AccessReview

Nopal Cactus (Opuntia ficus-indica) as a Source of Bioactive Compounds for Nutrition, Health and Disease

by Karym El-Mostafa, Youssef El Kharrassi, Asmaa Badreddine, Pierre Andreoletti, Joseph Vamecq, M'Hammed Saïd El Kebbaj, Norbert Latruffe, Gérard Lizard, Boubker Nasser and Mustapha Cherkaoui-Malki

Molecules 2014, 19(9), 14879-14901; https://doi.org/10.3390/molecules190914879 - 17 Sep 2014

Cited by 379 | Viewed by 47209

Abstract

Opuntia ficus-indica, commonly referred to as prickly pear or nopal cactus, is a dicotyledonous angiosperm plant. It belongs to the Cactaceae family and is characterized by its remarkable adaptation to arid and semi-arid climates in tropical and subtropical regions of the globe. [...] Read more.

Opuntia ficus-indica, commonly referred to as prickly pear or nopal cactus, is a dicotyledonous angiosperm plant. It belongs to the Cactaceae family and is characterized by its remarkable adaptation to arid and semi-arid climates in tropical and subtropical regions of the globe. In the last decade, compelling evidence for the nutritional and health benefit potential of this cactus has been provided by academic scientists and private companies. Notably, its rich composition in polyphenols, vitamins, polyunsaturated fatty acids and amino acids has been highlighted through the use of a large panel of extraction methods. The identified natural cactus compounds and derivatives were shown to be endowed with biologically relevant activities including anti-inflammatory, antioxidant, hypoglycemic, antimicrobial and neuroprotective properties. The present review is aimed at stressing the major classes of cactus components and their medical interest through emphasis on some of their biological effects, particularly those having the most promising expected health benefit and therapeutic impacts. Full article

(This article belongs to the Special Issue Redox Active Natural Products and Their Interaction with Cellular Signalling Pathways)

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17 pages, 753 KB

Open AccessReview

Hinokinin, an Emerging Bioactive Lignan

by Maria Carla Marcotullio, Azzurra Pelosi and Massimo Curini

Molecules 2014, 19(9), 14862-14878; https://doi.org/10.3390/molecules190914862 - 17 Sep 2014

Cited by 42 | Viewed by 12705

Abstract

Hinokinin is a lignan isolated from several plant species that has been recently investigated in order to establish its biological activities. So far, its cytotoxicity, its anti-inflammatory and antimicrobial activities have been studied. Particularly interesting is its notable anti-trypanosomal activity. Full article

(This article belongs to the Collection Natural Products as Leads or Drugs against Neglected Tropical Diseases)

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19 pages, 4566 KB

Open AccessArticle

Simple Rain-Shelter Cultivation Prolongs Accumulation Period of Anthocyanins in Wine Grape Berries

by Xiao-Xi Li, Fei He, Jun Wang, Zheng Li and Qiu-Hong Pan

Molecules 2014, 19(9), 14843-14861; https://doi.org/10.3390/molecules190914843 - 17 Sep 2014

Cited by 37 | Viewed by 8332

Abstract

Simple rain-shelter cultivation is normally applied during the grape growth season in continental monsoon climates aiming to reduce the occurrence of diseases caused by excessive rainfall. However, whether or not this cultivation practice affects the composition and concentration of phenolic compounds in wine [...] Read more.

Simple rain-shelter cultivation is normally applied during the grape growth season in continental monsoon climates aiming to reduce the occurrence of diseases caused by excessive rainfall. However, whether or not this cultivation practice affects the composition and concentration of phenolic compounds in wine grapes remains unclear. The objective of this study was to investigate the effect of rain-shelter cultivation on the accumulation of anthocyanins in wine grapes (Vitis vinifera L. Cabernet Sauvignon) grown in eastern China. The results showed that rain-shelter cultivation, compared with the open-field, extended the period of rapid accumulation of sugar, increased the soluble solid content in the grape berries, and delayed the senescence of the green leaves at harvest. The concentrations of most anthocyanins were significantly enhanced in the rain-shelter cultivated grapes, and their content increases were closely correlated with the accumulation of sugar. However, the compositions of anthocyanins in the berries were not altered. Correspondingly, the expressions of VvF3'H, VvF3'5'H, and VvUFGT were greatly up-regulated and this rising trend appeared to continue until berry maturation. These results suggested that rain-shelter cultivation might help to improve the quality of wine grape berries by prolonging the life of functional leaves and hence increasing the assimilation products. Full article

(This article belongs to the Special Issue Anthocyanins)

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22 pages, 734 KB

Open AccessReview

Recovery of Biomolecules from Food Wastes — A Review

by Antonietta Baiano

Molecules 2014, 19(9), 14821-14842; https://doi.org/10.3390/molecules190914821 - 17 Sep 2014

Cited by 412 | Viewed by 25028

Abstract

Food wastes are produced by a variety of sources, ranging from agricultural operations to household consumption. About 38% occurs during food processing. At present, the European Union legislation encourages the exploitation of co-products. This valorisation can be achieved through the extraction of high-value [...] Read more.

Food wastes are produced by a variety of sources, ranging from agricultural operations to household consumption. About 38% occurs during food processing. At present, the European Union legislation encourages the exploitation of co-products. This valorisation can be achieved through the extraction of high-value components such as proteins, polysaccharides, fibres, flavour compounds, and phytochemicals, which can be re-used as nutritionally and pharmacologically functional ingredients. Extraction can proceed according to solid-liquid extraction, Soxhlet extraction, pressurized fluid extraction, supercritical fluid extraction, ultrasound-assisted extraction, microwave-assisted extraction, pulsed electric field extraction, and enzyme-assisted extraction. Nevertheless, these techniques cannot be used indiscriminately and their choice depends on the type of biomolecules and matrix, the scale processing (laboratory or industrial), the ratio between production costs and economic values of the compounds to be extracted. The vegetable wastes include trimmings, peelings, stems, seeds, shells, bran, residues remaining after extraction of oil, starch, sugar, and juice. The animal-derived wastes include wastes from bred animals, wastes from seafood, wastes from dairy processing. The recovered biomolecules and by-products can be used to produce functional foods or as adjuvants in food processing or in medicinal and pharmaceutical preparations. This work is an overview of the type and amounts of food wastes; food waste legislation; conventional and novel techniques suitable for extracting biomolecules; food, medicinal and pharmaceutical uses of the recovered biomolecules and by-products, and future trends in these areas. Full article

(This article belongs to the Section Natural Products Chemistry)

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Molecules, Volume 19, Issue 9 (September 2014) – 145 articles , Pages 12898-15360

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