49 research outputs found

    Soil Pollution Prevention and Remediation

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    1DICATECh, Polytechnic University of Bari, Via Orabona 4, 70125 Bari, Italy 2Department of Civil and Environmental Engineering, University of California, Davis, 3105 Ghausi Hall, One Shields Avenue, Davis, CA 95616, USA 3School of Environmental Engineering, Technical University of Crete, 73100 Chania, Greece 4Dipartimento di Ingegneria Strutturale, Edile e Geotecnica, Politecnico di Torino, Corso Duca degli Abruzzi 24, 10129 Torino, Ital

    Tetrahydrohyperforin and Octahydrohyperforin Are Two New Potent Inhibitors of Angiogenesis

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    We have previously shown that hyperforin, a phloroglucinol derivative found in St. John's wort, behaves as a potent anti-angiogenic compound. To identify the reactive group(s) mainly involved in this anti-angiogenic effect, we have investigated the anti-angiogenic properties of a series of stable derivatives obtained by oxidative modification of the natural product. In addition, in the present work we have studied the role of the four carbonyl groups present in hyperforin by investigating the potential of some other chemically stable derivatives.The experimental procedures included the analysis of the effects of treatment of endothelial cells with these compounds in cell growth, cell viability, cell migration and zymographic assays, as well as the tube formation assay on Matrigel. Our study with hyperforin and eight derivatives shows that the enolized beta-dicarbonyl system contained in the structure of hyperforin has a dominant role in its antiangiogenic activity. On the other hand, two of the tested hyperforin derivatives, namely, tetrahydrohyperforin and octahydrohyperforin, behave as potent inhibitors of angiogenesis. Additional characterization of these compounds included a cell specificity study of their effects on cell growth, as well as the in vivo Matrigel plug assay.These observations could be useful for the rational design and chemical synthesis of more effective hyperforin derivatives as anti-angiogenic drugs. Altogether, the results indicate that octahydrohyperforin is a more specific and slightly more potent antiangiogenic compound than hyperforin

    The Effect of Ginger (Zingiber officinalis) and Artichoke (Cynara cardunculus) Extract Supplementation on Functional Dyspepsia: A Randomised, Double-Blind, and Placebo-Controlled Clinical Trial

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    Objective. Functional dyspepsia (FD) is a frequent clinical finding in western world. The aim of this study is to compare the efficacy of a ginger and artichoke supplementation versus placebo in the treatment of FD. Methods. A prospective multicentre, double blind, randomized, placebo controlled, parallel-group comparison of the supplement and placebo over a period of 4 weeks was performed. Two capsules/day were supplied (before lunch and dinner) to 126 FD patients (supplementation/placebo: 65/61). Results. After 14 days of treatment, only supplementation group (SG) showed a significant amelioration (SG: S = +1.195 MCA score units (u), = 0.017; placebo: P = +0.347 u, = 0.513). The intercept ( ) resulted to be significantly higher in SG than in placebo ( S − P = +0.848 u, < 0.001). At the end of the study, the advantage of SG versus placebo persists without variation ( S − P = +0.077 u, = 0.542). In SG, a significant advantage is observed for nausea ( S − P = −0.398 u, < 0.001), epigastric fullness ( S − P = −0.241, < 0.001), epigastric pain ( S − P = −0.173 u, = 0.002), and bloating ( S − P = −0.167 u, = 0.017). Conclusions. The association between ginger and artichoke leaf extracts appears safe and efficacious in the treatment of FD and could represent a promising treatment for this disease

    The reaction of hyperforin with hydride reducing agents.

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    As part of a study aimed at generating analogues of hyperforin (1), the reaction of this prenylated phloroglucinol with various hydride reducing agents was investigated. Hyperforin contains two beta-dicarbonyl systems, one of which is non-enolizable, and it was interesting to assess the relative reactivity of these structural elements in the highly compact framework of the natural product. Depending on the reducing agent employed, a surprising range of compounds could be obtained, sometimes in synthetically useful yields. The stereochemistry of the LiAlH4-reduced product was secured by X-ray analysis and served as a base for elucidating the configuration of a series of reduced and deoxygenated analogues obtained with other reducing agents. The chemoselectivity observed in these reactions is apparently the result of a combination of metal-chelation and hydrogen-bonding effects

    Synthesis and biosynthesis of isocordoin

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    In the search of a convenient synthesis for isocordoin (1), a potential anticancer natural product, 2 ' ,4 ' -dihydroxychalcone was inoculated in cell suspension cultures of Morus nigro, which were expected to contain an active prenyltransferase. After 24 hours the target compound was easily isolated from the metabolite extract. Optimization of the biotransformation resulted in a 85% yield of the prenyl derivative
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