Characterization, stability and solubility of co-amorphous systems of glibenclamide and L-arginine at different pH

Purpose: To investigate the stability and solubility of co-amorphous systems of glibenclamide (GBC) with L-arginine (L-Arg) at different pH values. Methods: Three co-amorphous solids of GBC and L-Arg were obtained by fast solvent evaporation using 2:1, 1:1 and 1:2 stoichiometries. All co-amorphous systems were characterized by XRPD, FTIR, RAMAN and NMR-solid state as well as thermal techniques such as DSC and TGA. The stability of coamorphous systems was evaluated by indicative stability and stability in relevant physiological media was measured at different pH values. Results: The chemical characterization suggest that there was no proton transference between L-Arg and GBC indicative of co-amorphous solids. Stability studies showed that all the co-amorphous solids are unstable under humid conditions and only the co-amorphous system of GBC: L-Arg 1:2 was stable in all the pH values tested. Solubility studies at different pH values showed that the co-amorphous GBC: L-Arg 1:1 and 1:2, showed increasing solubility values even at pH < 7 (0.6468 mg/mL at pH 1.2 for coamorphous GBC: L-Arg 1:2 at the first hour) where free GBC was not soluble. Conclusion: Co-amorphous systems of GBC and L-Arg, is an interesting strategy to increase the solubility of poorly-soluble drugs at acidic pH values Keywords: Co-amorphous; Glibenclamide; L-Arginine; Solubility; Stabilit

Isolation of green coffee chlorogenic acids using activated carbon

Chlorogenic acids, which are interesting natural antioxidants widespread in the plant kingdom, were extracted and purified from Mexican green coffee beans (Coffea arabica) using different methods. The final objective was to find an easy way to extract high-value molecules from a complex mixture, avoiding as much as possible the use of toxic solvents. Three extraction methods (hot water at 80 8C, aqueous methanol 70% (v/v), and aqueous isopropanol 60% (v/v)) were tested in combination with two isolating methods (activated carbon, different solvents). The extracted amounts of chlorogenic acids with the six treatments (4.67–5.87% dry basis) presented no significant differences. The one using hot water for extraction and of activated carbon for isolation, was the simplest and the most environmentally friendly. Thus it can be used as a previous step to obtain from green coffee a mixture rich in chlorogenic acids which can be further fractionated to purify a specific chlorogenic acid (i.e. in this work, 5-O-caffeoyl quinic acid using a silica gel column). Chlorogenic acids can be used as natural antioxidants in food or non-food products. To the best of our knowledge, activated carbon has not been used to isolate chlorogenic acids from green coffee

Sclerin, a New Cytotoxic Cyclononapeptide from <i>Annona scleroderma</i>

A new cytotoxic cyclononapeptide, sclerin, cyclo(&#8315;Dab1&#8315;Ser2&#8315;Tyr3&#8315;Gly4&#8315;Thr5&#8315;Val6&#8315;Ala7&#8315; Ile8&#8315;Pro9&#8315;) (1), was isolated from the methanol extract of the seeds of Annona scleroderma, together with the known metabolite, cyclosenegalin A, cyclo(&#8315;Pro1&#8315;Gly2&#8315;Leu3&#8315;Ser4&#8315;Ala5&#8315;Val6&#8315;Thr7&#8315;) (2). The planar structures for the two compounds were established by comprehensive analysis of NMR and ESI-HRMS data, and the absolute stereochemistry was stablished by Marfey&#8217;s method. Compound 1 showed moderate cytotoxic activity against the human prostate carcinoma cell line DU-145 at &#181;M concentration

Waste residues from Opuntia ficus indica for peroxidase-mediated preparation of phenolic dimeric compounds

A methodology to detect peroxidase activity in Opuntia ficus indica cladodes waste extracts was performed and then used towards phenolic compounds. The extracts were able to dimerize three different molecules. Dimeric compounds were produced with yields ranging from 11% to 55%. The influence of H2O2 concentration was also tested, finding better yields when the peroxide-to-substrate ratio was 1:1. Some water-miscible solvents were used trying to increase overall yields, but no-significant positive results were found. In fact, one of them, THF, seemed to inhibit dimerization reaction. Hence, we have tested an alternative natural peroxidase source obtained from the wastes of a local highly-consumed vegetable and studied their enzymatic activity towards the preparation of biologically active, valuable compounds. Keywords: Opuntia ficus cladodes, Food waste residues, Peroxidase, Oxidative coupling, Phenolic compounds, Dimerization reaction

Where Brain, Body and World Collide

The production cross section of electrons from semileptonic decays of beauty hadrons was measured at mid-rapidity (|y| &lt; 0.8) in the transverse momentum range 1 &lt; pt &lt; 8 Gev/c with the ALICE experiment at the CERN LHC in pp collisions at a center of mass energy sqrt{s} = 7 TeV using an integrated luminosity of 2.2 nb^{-1}. Electrons from beauty hadron decays were selected based on the displacement of the decay vertex from the collision vertex. A perturbative QCD calculation agrees with the measurement within uncertainties. The data were extrapolated to the full phase space to determine the total cross section for the production of beauty quark-antiquark pairs