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Membrane Bilayers (membrane + bilayer)
Selected AbstractsStructure elucidation, conformational analysis and thermal effects on membrane bilayers of an antimicrobial myricetin ether derivativeJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 3 2001C. Demetzos The membrane perturbing 3,7,4,,5,-tetramethyl ether of myricetin 1 was isolated from Cistus monspelien-sis L. Its structure was elucidated and its conformational properties were explored using a combination of 2D NMR spectroscopy and computational chemistry. The obtained results showed that compound 1 adopts four enantiomeric pairs of low energy conformers characterized: (a) by an aromatic ring B twisted through rotation about C2-C1, bond from the rigid isoflavone ring; (b) a 4,-O-CH3 bond oriented out of the plane with equal probability upwards or downwards the phenyl ring B, while all the other O-CH3 bonds are oriented in the plane of the aryl ring. Two of these enantiomeric pairs are lowest in energy. These possible bioactive con-formers are possibly stabilized by van Der Waals interactions. The 3,,5-diacetyl derivative 2 of compound 1 was synthesized and its structure elucidation was achieved based on the chemical shift assignment of the parent compound 1. The Differential Scanning Calorimetry (DSC) results revealed that the degree of the thermal effects exerted by the flavonoids at dipalmitoylphosphatidyl choline (DPPC) bilayers followed the order 1 > 2 > myricetin. Their antimicrobial activity against Gram positive bacteria followed the same order. [source] Skin permeation of retinol in Tween 20-based deformable liposomes: in-vitro evaluation in human skin and keratinocyte modelsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 2 2006Yu-Kyoung Oh To develop a more effective transdermal delivery method for lipophilic functional cosmetic compounds such as retinol, we formulated various deformable liposomes and compared their transdermal delivery efficiency with those of neutral or negatively-charged conventional liposomes. We tested the deformability of liposomes containing edge activators such as bile salts, polyoxyethylene esters and polyoxyethylene ethers. As indicators of deformability, we used the passed volume and phospholipid ratios during extrusion, as well as the deformability index. We found that the type of edge activator significantly affected the extent of deformability, and that Tween 20 provided the highest level of deformability. Accordingly, we used Tween 20 to formulate deformable liposomes containing retinol in the membrane bilayers, and conducted a skin permeation study in Franz diffusion cells, using dermatomed human skin and three-dimensional human keratinocyte layers. As compared with the use of conventional neutral or negatively-charged liposomes, the use of Tween 20-based deformable liposomes significantly increased the skin permeation of retinol. These results suggested that deformable liposomes might be of potential use for the formulation of retinol and other lipophilic functional cosmetic compounds. [source] Protein,membrane interactions: blood clotting on nanoscale bilayersJOURNAL OF THROMBOSIS AND HAEMOSTASIS, Issue 2009J. H. MORRISSEY Summary., The clotting cascade requires the assembly of protease,cofactor complexes on membranes with exposed anionic phospholipids. Despite their importance, protein,membrane interactions in clotting remain relatively poorly understood. Calcium ions are known to induce anionic phospholipids to cluster, and we propose that clotting proteins assemble preferentially on such anionic lipid-rich microdomains. Until recently, there was no way to control the partitioning of clotting proteins into or out of specific membrane microdomains, so experimenters only knew the average contributions of phospholipids to blood clotting. The development of nanoscale membrane bilayers (Nanodiscs) has now allowed us to probe, with nanometer resolution, how local variations in phospholipid composition regulate the activity of key protease,cofactor complexes in blood clotting. Furthermore, exciting new progress in solid-state NMR and large-scale molecular dynamics simulations allow structural insights into interactions between proteins and membrane surfaces with atomic resolution. [source] Thyroid hormones and their effects: a new perspectiveBIOLOGICAL REVIEWS, Issue 4 2000A. J. HULBERT ABSTRACT The thyroid hormones are very hydrophobic and those that exhibit biological activity are 3,,5,,3,5-Ltetraiodothyronine (T4), 3,,5,3-L-triiodothyronine (T3), 3,,5,,3-L-triiodothyronine (rT3) and 3,5,-Ldiiodothyronine (3,5-T2). At physiological pH, dissociation of the phenolic -OH group of these iodothyronines is an important determinant of their physical chemistry that impacts on their biological effects. When non-ionized these iodothyronines are strongly amphipathic. It is proposed that iodothyronines are normal constituents of biological membranes in vertebrates. In plasma of adult vertebrates, unbound T4 and T3 are regulated in the picomolar range whilst protein-bound T4 and T3 are maintained in the nanomolar range. The function of thyroid-hormone-binding plasma proteins is to ensure an even distribution throughout the body. Various iodothyronines are produced by three types of membrane-bound cellular deiodinase enzyme systems in vertebrates. The distribution of deiodinases varies between tissues and each has a distinct developmental profile. Thyroid hormones have many effects in vertebrates. It is proposed that there are several modes of action of these hormones.(1) The nuclear receptor mode is especially important in the thyroid hormone axis that controls plasma and cellular levels of these hormones.(2) These hormones are strongly associated with membranes in tissues and normally rigidify these membranes.(3) They also affect the acyl composition of membrane bilayers and it is suggested that this is due to the cells responding to thyroid-hormone-induced membrane rigidification. Both their immediate effects on the physical state of membranes and the consequent changes in membrane composition result in several other thyroid hormone effects. Effects on metabolism may be due primarily to membrane acyl changes. There are other actions of thyroid hormones involving membrane receptors and influences on cellular interactions with the extracellular matrix. The effects of thyroid hormones are reviewed and appear to be combinations of these various modes of action. During development, vertebrates show a surge in T4 and other thyroid hormones, as well as distinctive profiles in the appearance of the deiodinase enzymes and nuclear receptors. Evidence from the use of analogues supports multiple modes of action. Re-examination of data from the early 1960s supports a membrane action. Findings from receptor ,knockout' mice supports an important role for receptors in the development of the thyroid axis. These iodothyronines may be better thought of as ,vitamone' -like molecules than traditional hormonal messengers. [source] | ||||||||||