32 research outputs found
Influence of Anodic Conditions on Self-ordered Growth of Highly Aligned Titanium Oxide Nanopores
Self-aligned nanoporous TiO2templates synthesized via dc current electrochemical anodization have been carefully analyzed. The influence of environmental temperature during the anodization, ranging from 2 °C to ambient, on the structure and morphology of the nanoporous oxide formation has been investigated, as well as that of the HF electrolyte chemical composition, its concentration and their mixtures with other acids employed for the anodization. Arrays of self-assembled titania nanopores with inner pores diameter ranging between 50 and 100 nm, wall thickness around 20–60 nm and 300 nm in length, are grown in amorphous phase, vertical to the Ti substrate, parallel aligned to each other and uniformly disordering distributed over all the sample surface. Additional remarks about the photoluminiscence properties of the titania nanoporous templates and the magnetic behavior of the Ni filled nanoporous semiconductor Ti oxide template are also included
The fatty-acid amide hydrolase inhibitor URB597 does not affect triacylglycerol hydrolysis in rat tissues
Structure-property relationships of a class of carbamate-based fatty acid amide hydrolase (FAAH) inhibitors: chemical and biological stability
Cyclohexylcarbamic acid aryl esters are a class of fatty acid amide hydrolase (FAAH) inhibitors, which includes the reference compound URB597. The reactivity of their carbamate fragment is involved in pharmacological activity and may affect their pharmacokinetic and toxicological properties. We conducted in vitro stability experiments in chemical and biological environments to investigate the structure-stability relationships in this class of compounds. The results show that electrophilicity of the carbamate influences chemical stability, as suggested by the relation between the rate constant of alkaline hydrolysis (log k(pH9)) and the energy of the lowest unoccupied molecular orbital (LUMO). Introduction of small electron-donor substituents at conjugated positions of the O-aryl moiety increased the overall hydrolytic stability of the carbamate group without affecting FAAH inhibitory potency, whereas peripheral non-conjugated hydrophilic groups, which favor FAAH recognition, helped decrease oxidative metabolism in the liver
Synthesis and Quantitative Structure-Activity Relationship of Fatty Acid Amide Hydrolase Inhibitors: Modulation at the N-Portion of Biphenyl-3-yl Alkylcarbamates.
Alkylcarbamic acid biphenyl-3-yl esters are a class of fatty acid amide hydrolase (FAAH) inhibitors that comprises cyclohexylcarbamic acid 3′-carbamoylbiphenyl-3-yl ester (URB597), a compound with analgesic,
anxiolytic-like and antidepressant-like properties in rat and mouse models. Here, we extended the
structure-activity relationships (SARs) for this class of compounds by replacing the cyclohexyl ring of the
parent compound cyclohexylcarbamic acid biphenyl-3-yl ester (URB524) (FAAH IC50: 63 nM) with a
selected set of substituents of different size, shape, flexibility, and lipophilicity. Docking experiments and
linear interaction energy (LIE) calculations indicated that the N-terminal group of O-arylcarbamates fits
within the lipophilic region of the substrate-binding site, mimicking the arachidonoyl chain of anandamide.
Significant potency improvements were observed for the beta-naphthylmethyl derivative 4q (IC50 ) 5.3 nM)
and its 3′-carbamoylbiphenyl-3-yl ester 4z (URB880, IC50 ) 0.63 nM), indicating that shape complementarity
and hydrogen bonds are crucial to obtain highly potent inhibitors
Trophoblast cells are able to regulate monocyte activity to control Toxoplasma gondii infection
Distribution et abondance de microorganismes méthagéniques et méthatrophes dans les cours d'eau européens
International audienceGlobally, streams and rivers emit a significant amount of methane, a highly potent greenhouse gas. However, little is known about stream sediment microbial communities, driving the net methane balance in these systems, especially on their distribution and composition at large spatial scales. Within the project Euro Methane we investigated the diversity and abundance of methanogenic archaea and methane-oxidizing bacteria across 16 European streams (from northern Spain to central Sweden) via 16S rRNA sequencing and qPCR. We determined environmental drivers of both abundance and community composition and explored the link to measured potential methane production and oxidation rates of the respective sediments. We found that the community composition of methane-oxidizing bacteria significantly differed among the studied streams, while methanogenic archaea were more homogeneously distributed. Beyond the overall diversity trends, indicator species for stream types were identified. Methanogenic Methanosaeta sp. and methane-oxidizing Methyloglobulus sp. increased with geographical latitude and dominated in headwater streams (orders 1-3) with high oxygen levels and high proportions of pristine land within the catchment, while methanogenic Methanomethylovorans sp. and methane-oxidizing Methylocaldum spp. were more common in larger streams (orders 4-6) with higher discharge and agricultural influence. Potential methane production rates significantly increased with abundance of methanogenic archaea, while potential methane oxidation rates did not show significant correlations with methane oxidizing bacteria, presumably due to the more diverse physiological capabilities of this microbial group. Our study represents a holistic large-scale biogeographical overview of two microbial groups to enhance our understanding of the methane cycle within a heretofore understudied ecosystem