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51.
Irene Bravo-Osuna Christine Vauthier Alessandra Farabollini Gioconda Millotti Gilles Ponchel 《Journal of nanoparticle research》2008,10(8):1293-1301
Surface modified nanoparticles composed of poly(isobutylcyanoacrylate) (PIBCA) cores surrounded by a chitosan and thiolated
chitosan gel layer were prepared and characterized in previous works. The presence of such biopolymers on the nanoparticle
surface conferred those nanosystems interesting characteristics that might partially overcome the gastrointestinal enzymatic
barrier, improving the oral administration of pharmacologically active peptides. In the present work, the antiprotease behaviour
of this family of core–shell nanoparticles was in vitro tested against two model metallopeptidases present in the gastrointestinal
tract (GIT): Carboxypeptidase A -CP A- (luminal protease) and Leucine Aminopeptidase M -LAP M- (membrane protease). As previous
step, the zinc-binding capacity of these nanoparticles was evaluated. Interestingly, an improvement of both the zinc-binding
capacity and the antiprotease effect of chitosan was observed when the biopolymers (chitosan and thiolated chitosan) were
used as coating component of the core–shell nanoparticles, in comparison with their behaviour in solution, thanks to the different
biopolymer chains rearrangement. The presence of amino, hydroxyl and thiol groups on the nanoparticle surface promoted zinc
binding and hence the inhibition of the metallopeptidases analysed. On the contrary, the occurrence of a cross-linked structure
in the gel layer surrounding the PIBCA cores of thiolated formulations, due to the formation of interchain and intrachain
disulphide bonds, partially limited the inhibition of the proteases. The low accessibility of cations to the active groups
of the cross-linked polymeric shell was postulated as a possible explanation of this behaviour. Results obtained in this work
make this family of surface-modified nanocarriers promising candidates for the successfull administration of pharmacologically
active peptides and proteins by the oral route. 相似文献
52.
A new proof of the characterization of the Chinese postman polyhedra is given. In developing this proof, a theorem of Gomory about homomorphic lifting of facets for group polyhedra is generalized to subproblems. Some results for the Chinese postman problem are generalized to binary group problems. In addition, a connection is made between Fulkerson's blocking polyhedra and a blocking pair of binary group problems. A connection is also developed between minors and lifting of facets for group problems. 相似文献
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55.
Lorne Tallet Emilie Frisch Mgane Bornerie Claire Medemblik Benoît Frisch Philippe Lavalle Gilles Guichard Cline Douat Antoine Kichler 《Molecules (Basel, Switzerland)》2022,27(5)
There is an urgent need to develop new therapeutic strategies to fight the emergence of multidrug resistant bacteria. Many antimicrobial peptides (AMPs) have been identified and characterized, but clinical translation has been limited partly due to their structural instability and degradability in physiological environments. The use of unnatural backbones leading to foldamers can generate peptidomimetics with improved properties and conformational stability. We recently reported the successful design of urea-based eukaryotic cell-penetrating foldamers (CPFs). Since cell-penetrating peptides and AMPs generally share many common features, we prepared new sequences derived from CPFs by varying the distribution of histidine- and arginine-type residues at the surface of the oligourea helix, and evaluated their activity on both Gram-positive and Gram-negative bacteria as well as on fungi. In addition, we prepared and tested new amphiphilic block cofoldamers consisting of an oligourea and a peptide segment whereby polar and charged residues are located in the peptide segment and more hydrophobic residues in the oligourea segment. Several foldamer sequences were found to display potent antibacterial activities even in the presence of 50% serum. Importantly, we show that these urea-based foldamers also possess promising antifungal properties. 相似文献
56.
Mei Wang Chantal Septier Hlne Brignot Christophe Martin Francis Canon Gilles Feron 《Molecules (Basel, Switzerland)》2022,27(5)
Astringency is an important sensory characteristic of food and beverages containing polyphenols. However, astringency perception in elderly people has not been previously documented. The aim of the present work was to evaluate sensitivity to astringency as a function of age, salivary flow and protein amount. Fifty-four panellists, including 30 elderly people (age = 75 ± 4.2 years) and 24 young people (age = 29.4 ± 3.8 years), participated in this study. Astringency sensitivity was evaluated by the 2-alternative forced choice (2-AFC) procedure using tannic acid solutions. Whole saliva was collected for 5 min before and after the sensory tests. The results showed that the astringency threshold was significantly higher in the elderly group than the young group. No correlation was observed between the salivary protein amount and threshold value. However, a negative correlation between salivary flow and threshold was observed in the young group only. These results showed a difference in oral astringency perception as a function of age. This difference can be linked to salivary properties that differ as a function of age. 相似文献
57.
The perturbation of the racemic equilibrium of luminescent D3 lanthanide(III) complexes by added chiral agents, such as amino acids, may be a useful technique for determining the absolute configuration of the added species. It is shown in this work, however, that simple interpretation of the equilibrium shift of racemic tris-terdentate complexes of Tb(III) with 2,6-pyridine-dicarboxylate by amino acids, as measured by the sign of the resultant circularly polarized luminescence (CPL) in terms of specific structural characteristics is not possible. CPL results for a number of derivatized amino acids are also presented, and some insights into the nature of the chiral discriminatory forces that might be exploited in this kind of study are discussed. 相似文献
58.
The sound field inside a model human ear canal has been computed, to show both longitudinal variations along the canal length and transverse variations through cross-sectional slices. Two methods of computation were used. A modified horn equation approach parametrizes the sound field with a single coordinate, the position along a curved center axis-this approach can accommodate the curvature and varying cross-sectional area of the ear canal but cannot compute transverse variations of the sound field. A boundary element method (BEM) was also implemented to compute the full three-dimensional sound field. Over 2000 triangular mesh elements were used to represent the ear canal geometry. For a plane piston source at the entrance plane, the pressure along the curved center axis predicted by the two methods is in good agreement, for frequencies up to 15 kHz, for four different ear canals. The BEM approach, though, reveals spatial variations of sound pressure within each canal cross section. These variations are small below 4 kHz, but increase with frequency, reaching 1.5 dB at 8 kHz and 4.5 dB at 15 kHz. For source configurations that are more realistic than a simple piston, large transverse variations in sound pressure are anticipated in the vicinity of the source. 相似文献
59.
Johannes Karges Uttara Basu Olivier Blacque Hui Chao Gilles Gasser 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2019,131(40):14472-14478
The use of photodynamic therapy (PDT) to treat cancer has received increasing attention over the last years. However, the clinically used photosensitisers (PSs) have some limitations that include poor aqueous solubility, hepatotoxicity, photobleaching, aggregation, and slow clearance from the body, so the design of new classes of PSs is of great interest. We present the use of bis(dipyrrinato)zinc(II) complexes with exceptionally long lifetimes as efficient PDT PSs. Based on the heavy‐atom effect, intersystem crossing of these complexes changes the excited state from singlet to a triplet state, thereby enabling singlet oxygen generation. To overcome the limitation of quenching effects in water and improve water solubility, the lead compound 3 was encapsulated in a polymer matrix. It showed impressive phototoxicity upon irradiation at 500 nm in various monolayer cancer cells as well as 3D multicellular tumour spheroids, without observed dark toxicity. 相似文献
60.
Trouche N Wieckowski S Sun W Chaloin O Hoebeke J Fournel S Guichard G 《Journal of the American Chemical Society》2007,129(44):13480-13492
Synthetic multivalent ligands, owing to the presence of multiple copies of a recognition motif attached to a central scaffold, can mediate clustering of cell surface receptors and thereby function as effector molecules. This paper dissects the relationship between structure and effector function of synthetic multivalent ligands targeting CD40, a cell surface receptor of the tumor necrosis factor receptor (TNF-R) superfamily. Triggering CD40 signaling in vivo can be used to enhance immunity against intracellular pathogens or tumors. A series of multimeric molecules has been prepared by systematically varying the shape and the valency of the central scaffold, the nature and the length of the linker as well as the sequence of the receptor binding motif. The data reported here (i) suggest that radial distribution of CD40-binding units and C3-symmetry are preferred for optimal binding to CD40 and signaling, (ii) underscore the importance of choosing an appropriate linker to connect the receptor binding motif to the central scaffold, and (iii) show the versatility of planar cyclic alpha- and beta-peptides as templates for the design of CD40L mimetics. In particular, the (Ahx)3-B trimeric scaffold-linker combination equally accommodated binding elements derived from distinct CD40L hot-spot regions including AA" loop and beta-strand E. The use of miniCD40Ls such as those reported here is complementary to other approaches (recombinant ligands, agonistic anti-receptor antibodies) and may find interesting therapeutic applications. Furthermore, the results disclosed in this paper provide the basis for future design of other TNF family member mimetics. 相似文献