Bile Acid Sequestrants Based on Natural and Synthetic Gels

Bile acid sequestrants (BASs) are non-systemic therapeutic agents used for the management of hypercholesterolemia. They are generally safe and not associated with serious systemic adverse effects. Usually, BASs are cationic polymeric gels that have the ability to bind bile salts in the small intestine and eliminate them by excretion of the non-absorbable polymer–bile salt complex. This review gives a general presentation of bile acids and the characteristics and mechanisms of action of BASs. The chemical structures and methods of synthesis are shown for commercial BASs of first- (cholestyramine, colextran, and colestipol) and second-generation (colesevelam and colestilan) and potential BASs. The latter are based on either synthetic polymers such as poly((meth)acrylates/acrylamides), poly(alkylamines), poly(allylamines) and vinyl benzyl amino polymers or biopolymers, such as cellulose, dextran, pullulan, methylan, and poly(cyclodextrins). A separate section is dedicated to molecular imprinting polymers (MIPs) because of their great selectivity and affinity for the template molecules used in the imprinting technique. Focus is given to the understanding of the relationships between the chemical structure of these cross-linked polymers and their potential to bind bile salts. The synthetic pathways used in obtaining BASs and their in vitro and in vivo hypolipidemic activities are also introduced

EVALUATION OF THE INTAKE OF NITRATE, NITRITE, NITROSODIETHYLAMINE AND NITROSODIMETHYLAMINE BY FOOD CONSUMPTION

The aim of the present study was the evaluation of nitrate, nitrite, nitrosodiethylamine (NDEA) and nitrosodimethylamine (NDMA) intake by food consumption. We determined concentrations of nitrates, nitrites in 102 food samples (40 meat products, 15 fermented cheese, 25 vegetables, 22 fruits) and the concentration NDEA, NDMA in 40 meat products. Nitrates and nitrites were determined using Peter-Griess method; nitrosamines were quantified by HPLC with UV detection.  We designed vegetalian, vegetarian and conventional diets of about 2500 kcal/day.  Based of the values found, we calculated the intake of nitrates, nitrites and nitrosamines. The obtained values fits to WHO’s recommendations, except for vegetalian and conventional diet, in which the nitrate content was 3,46 respectively 1,64 times higher than the acceptable daily intake (157 mg NO3-/day)

Association and Phase Behavior of Cholic Acid-Modified Dextran and Phosphatidylcholine Liposomes

The interaction between liposomes (1,2-dimyristoyl-<i>sn</i>-glycero-3-phosphocholine (DMPC)) and a hydrophobically modified water-soluble polymer (HMP; a bile acid-modified dextran) has been investigated by isothermal titration calorimetry (ITC) and differential scanning calorimetry (DSC), combined with turbidity measurement and cryogenic scanning electron microscopy (cryo-SEM). The thermodynamic information on the association (enthalpy of interaction, enthalpy of transition of mixed vesicles to mixed micelle-like aggregates) was obtained from ITC. Further, the phase behavior for the system could be derived from the ITC measurements, and be confirmed by turbidity and cryo-SEM. The effect of cholic acid (CA) side groups on the ordered arrangement of DMPC bilayers was studied by DSC, by following the changes they induce in the gel-to-liquid crystalline liposome phase transition. The DSC results were in excellent agreement with the interpretation proposed for the ITC results. The morphology of the aggregates, as characterized by cryo-SEM, is in line with the proposed aggregate morphologies

New Quaternary Ammonium Derivatives Based on Citrus Pectin

New citrus pectin derivatives carrying pendant N,N-dimethyl-N-alkyl-N-(2-hydroxy propyl) ammonium chloride groups were achieved via polysaccharide derivatization with a mixture of N,N-dimethyl-N-alkyl amine (alkyl = ethyl, butyl, benzyl, octyl, dodecyl) and epichlorohydrin in aqueous solution. The structural characteristics of the polymers were examined via elemental analysis, conductometric titration, Fourier Transform Infrared spectroscopy (FTIR) and 1D (1H and 13C) nuclear magnetic resonance (NMR). Capillary viscosity measurements allowed for the study of viscometric behavior as well as the determination of viscosity–average molar mass for pristine polysaccharide and intrinsic viscosity ([η]) values for pectin and its derivatives. Dynamic light scattering measurements (DLS) showed that pectin-based polymers formed aggregates in aqueous solution with a unimodal distribution. Critical aggregation concentration (cac) for the hydrophobic pectin derivatives were determined using fluorescence spectroscopy. Atom force microscopy (AFM) images allowed for the investigation of the morphology of polymeric populations obtained in aqueous solution, consisting of flocs and aggregates for crude pectin and its hydrophilic derivatives and well-organized aggregates for lipophilic pectin derivatives. Antimicrobial activity, examined using the disc diffusion method, proved that all polymers were active against Staphylococcus aureus bacterium and Candida albicans yeast