Safety issues in nutraceutical exploitation of Chlorella vulgaris, Arthrospira Platensis and Scenedesmus sp. microalgae

Microalgae contain many bioactive compounds, which may be exploited in food and nutraceutical fields. Bisphenol A (BPA) is a contaminant in microalgae that may be released from polymeric plastics. Since it is responsible for toxic effects on humans, the European legislation set the legal BPA limit within foods at 50 µg kg−1 of food weight. In this work, a fast ultrasounds solid-liquid extraction of BPA from commercial microalgal powders of Chlorella vulgaris, Arthrospira Platensis and Scenedesmus sp. was optimized. To increase selectivity, BPA was derivatized by using N,O-bis(trimethylsilyl)trifluoroacetamide/trimethylchlorosilane (BSTFA-TMCS) and it was analysed by GC-MS in selected ion monitoring mode. A design of experiment (DOE) optimization study of the reaction conditions was performed. The analytical method was validated by determining selectivity, linearity (R2= 0.99999 ± 3.3165E-07), precision, accuracy (99.92 ± 9.83E-02 %), recovery (99.65 ± 3.61E-02 %) and sensitivity (LoD= 0.547 ± 9.94E-02 µg kg−1; LoQ= 1.823 ± 3.31E-1 µg kg−1). The overall method proved to be fast, with high recovery and suitable to selectively and sensitively determine the content of BPA, eliminating the interferences from extraction and allowing to control the safety profile of microalgae. Dried microalgae cultivated in a polycarbonate reactor, were found to contain an amount of BPA 6 times exceeding the legal limit

Structure-activity relationships of novel substituted naphthalene diimides as anticancer agents

Novel 1,4,5,8-naphthalenetetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity on a wide number of different tumor cell lines. The prototypes of the present series were derivatives 1 and 2 characterized by interesting biological profiles as anticancer agents. The present investigation expands on the study of structure-activity relationships of prototypes 1 and 2, namely, the influence of the different substituents of the phenyl rings on the biological activity. Derivatives 3-22, characterized by a different substituent on the aromatic rings and/or a different chain length varying from two to three carbon units, were synthesized and evaluated for their cytostatic and cytotoxic activities. The most interesting compound was 20, characterized by a linker of three methylene units and a 2,3,4-trimethoxy substituent on the two aromatic rings. It displayed antiproliferative activity in the submicromolar range, especially against some different cell lines, the ability to inhibit Taq polymerase and telomerase, to trigger caspase activation by a possible oxidative mechanism, to downregulate ERK 2 protein and to inhibit ERKs phosphorylation, without acting directly on microtubules and tubuline. Its theoretical recognition against duplex and quadruplex DNA structures have been compared to experimental thermodynamic measurements and by molecular modeling investigation leading to putative binding modes. Taken together these findings contribute to define this compound as potential Multitarget-Directed Ligands interacting simultaneously with different biological targets. \ua9 2012 Elsevier Masson SAS. All rights reserved

Risultati prova di esame di laboratorio del Corso di Aanalisi dei prodotti per la salute 1, Turno B

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Risultati prova finale Analisi farmaceutica 1 modulo analisi qualitativa

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