Synthesis of New Tetrazole Derivatives of α,α‐Trehalose

Five new nitrogen heterocycles, mono‐and disubstituted tetrazoles with potential synthetic and pharmacological interest, were synthesized from α, α‐trehalose via the alkylation of commercial tetrazoles. This method appears to have broad scope with respect to the variations at positions 1 and 2 of tetrazole.     

Pd-catalyzed asymmetric conjugate addition of arylboronic acids to 2-nitroacrylates: a facile route to β-homophenylglycines

Asymmetric conjugate addition of arylboronic acids to 2-nitroacrylamide in the presence of cationic palladium–Chiraphos complex proceeds with high yield and enantioselectivity (73–89% ee) using as low as 0.05–0.25 mol % of the catalyst. The adducts can be smoothly transformed into the corresponding β²-homophenylglycines in two simple steps.     

Preparation and characterization of microcapsules loaded with polyphenols-enriched Uncaria tomentosa extract using spray-dryer technique

Journal of Thermal Analysis and Calorimetry - This work prepared and characterized microcapsule of Uncaria tomentosa (UT) in order to standardize a spray-dryer Uncaria tomentosa extract. The UT...     

Nutritional Value and Preventive Role of Nigella sativa L. and Its Main Component Thymoquinone in Cancer: An Evidenced-Based Review of Preclinical and Clinical Studies

In recent times, scientific attention has been paid to different foods and their bioactive components for the ability to inhibit the onset and progress of different types of cancer. Nigella sativa extract, powder and seed oil and its main components, thymoquinone and α-hederin, have showed potent anticancer and chemosensitizing effects against various types of cancer, such as liver, colon, breast, renal, cervical, lung, ovarian, pancreatic, prostate and skin tumors, through the modulation of various molecular signaling pathways. Herein, the purpose of this review was to highlight the anticancer activity of Nigella sativa and it constitutes, focusing on different in vitro, in vivo and clinical studies and projects, in order to underline their antiproliferative, proapoptotic, cytotoxic and antimetastatic effects. Particular attention has been also given to the synergistic effect of Nigella sativa and it constitutes with chemotherapeutic drugs, and to the synthesized analogs of thymoquinone that seem to enhance the chemo-sensitizing potential. This review could be a useful step towards new research on N. sativa and cancer, to include this plant in the dietary treatments in support to conventional therapies, for the best achievement of therapeutic goals.     

Metabolomics Insights of the Immunomodulatory Activities of Phlorizin and Phloretin on Human THP-1 Macrophages

Dihydrochalcones, phlorizin (PZ) and its aglycone phloretin (PT), have evidenced immunomodulatory effects through several mechanisms. However, the differential metabolic signatures that lead to these properties are largely unknown. Since macrophages play an important role in the immune response, our study aimed to characterise human THP-1 macrophages under PZ and PT exposure. A multiplatform-based untargeted metabolomics approach was used to reveal metabolites associated with the anti-inflammatory mechanisms triggered by the dihydrochalcones in LPS-stimulated macrophages, for the first time. Results showed differential phenotypic response in macrophages for all treatments. Dihydrochalcone treatment in LPS-stimulated macrophages mimics the response under normal conditions, suggesting inhibition of LPS response. Antagonistic effects of dihydrochalcones against LPS was mainly observed in glycerophospholipid and sphingolipid metabolism besides promoting amino acid biosynthesis. Moreover, PT showed greater metabolic activity than PZ. Overall, the findings of this study yielded knowledge about the mechanisms of action PZ and PT at metabolic level in modulating inflammatory response in human cells.     

Development of a Simple and Fast Electrochemical Method for Screening and Stoichiometric Determination of Dimenhydrinate

Dimenhydrinate (DIM) is a salt composed by the combination of two active pharmaceutical ingredients: diphenhydramine (DIP) and 8‐chlorotheophylline (CTP). In this work, the use of batch injection analysis with multiple pulse amperometric detection (BIA‐MPA) was proposed for the first time for fast stoichiometric determination of DIM. DIP (cation) and CTP (anion) were determined simultaneously in pharmaceutical samples with a simple and fast injection procedure (70 injections h^?1). Additional strategies were also proposed for rapid screening of samples containing the DIM salt. By a simple injection of a sample into the BIA system (without using of calibration curve), reliable information about stoichiometry of the DIM salt (1 : 1; DIP:CTP) and presence or absence of interfering species (electroactive) can be achieved.     

Solubility enhancement of ibuprofen using tri-ureasil-PPO hybrid: structural,cytotoxic, and drug release investigation

Herein, we used tri-ureasil organic–inorganic hybrid material (tU5000) in order to enhance the solubility of nonsteroidal anti-inflammatory drugs and fine tuning the drug delivery profile. For the first time, we used tU5000 as a film-forming agent in order to provide an alternative vehicle for transdermal drug delivery systems which the cell viability of practically 100 % for the highest and the lowest tested concentrations of pure tU5000 indicated that the material was not cytotoxic. The physicochemical properties of the tU5000 drug carrier and drug-loaded hybrids were systematically studied using powder X-ray diffraction, differential scanning calorimetry, small-angle X-ray scattering, and Fourier-transform infrared spectroscopy. The structural changes of tU5000 as well as the relationships between the drug content and in vitro drug release behaviors were investigated. The results showed that the ibu molecules were homogeneously distributed in the tU5000 xerogels contributing to fine-tuning the drug delivery profile. Considering the ability to incorporated high drug content, simple and mild preparation procedure by one-pot sol–gel route, high stability of the materials, sustained-release property, this class of hybrid based on polymers and inorganic compounds may have potential applications in the design of pharmaceutical formulation as ophthalmic (contact lenses), transdermal (patches) and implantable (soft tissue) drug delivery systems.     

Mukaiyama–Michael Reactions with trans‐2,5‐Diarylpyrrolidine Catalysts: Enantioselectivity Arises from Attractive Noncovalent Interactions,Not from Steric Hindrance

The scope of the enantioselective Mukaiyama–Michael reactions catalyzed by trans‐2,5‐diphenylpyrrolidine has been expanded to include both α‐ and β‐substituted enals. However, the rationalization of the observed enantioselectivity is far from obvious since the catalyst is not very sterically hindered. DFT calculations were carried out to rationalize the observed stereoselectivities. Transition states of the C?C bond formation between iminium intermediates and silyloxyfurans were located and their relative energies were used to estimate the stereoselectivity data. We find excellent agreement between the predicted and observed stereoselectivities. The analysis of intermolecular forces reveals that the enantioselectivity is mostly due to stabilizing noncovalent interactions between the reacting partners, not due to steric hindrance. The role of attractive noncovalent interactions in enantioselective catalysis may be underappreciated.     

Bacterial cellulose/triethanolamine based ion-conducting membranes

New bacterial cellulose (BC)–triethanolamine (TEA) ion-conducting membranes have been prepared and characterized. The samples were obtained by soaking BC membranes in triethanolamine aqueous solutions and drying. The scanning electron microscopy pictures revealed that the incorporation of TEA in BC membranes covers the cellulose microfibrils. Raman spectra exhibited BC and TEA characteristic group frequencies and thermal analysis evidenced an influence of TEA content on the sample thermal stability. The ion-conductivity as a function of the temperature showed an Arrhenius behavior increasing from 1.8 × 10^?5 S/cm at room temperature to 7.0 × 10^?4 S/cm at 80 °C for the BC–TEA 1 M sample.