Search results for "amino acid"

Functionalized halloysite nanotubes: Efficient carrier systems for antifungine drugs

2018

Abstract Halloysite-cyclodextrin hybrid was employed as carrier for sustained release of clotrimazole for vaginal or buccal treatment of Candidiasis. The nanocarrier was obtained by functionalization of halloysite surface with cyclodextrin moieties by means of microwave irradiation, with the final goal to obtain a scaffold for the covalent linkage of cysteamine hydrochloride. The interaction between clotrimazole and the pristine components, namely cyclodextrin and halloysite, was thoroughly investigated by several techniques such as DSC, TGA, UV–vis spectroscopy and some adsorption studies were, also, carried out. The release of the antifungine molecule was finally investigated in a medium …

Physiopathologie de la dyslipidémie du diabète de type 2 : nouvelles perspectives

2019

Resume La dyslipidemie du diabete de type 2 (DT2) est un facteur en cause dans l’augmentation du risque cardiovasculaire au cours du DT2. La dyslipidemie du DT2 est caracterisee non seulement par des anomalies quantitatives des lipoproteines, mais aussi par des anomalies qualitatives et cinetiques a potentiel atherogene. Les anomalies quantitatives caracteristiques sont l’hypertriglyceridemie et la diminution du HDL-cholesterol. Les anomalies qualitatives comprennent une augmentation des VLDL de grande taille enrichies en cholesterol esterifie et triglycerides (VLDL1) et des LDL petites et denses, ainsi qu’une augmentation des triglycerides au sein des LDL et des HDL, une glycation des apol…

Generation of oxysterols formed by free radicals and enzymes by electrochemical oxidation

2016

International audience; It is commonly accepted that cholesterol oxide derivatives, also named oxysterols, are 27 carbon-atom molecules deriving either from enzymatic and non-enzymatic oxidation of cholesterol. Most of these compounds can be synthesized by more or less difficult and time consuming chemical reactions, and some of them have been discovered before the identification of the enzymes [mainly cytochrome P450 enzymes (CYP enzymes)] involved in their biosynthesis. A wide range of biological activities depends on oxysterols. Some oxysterols are also involved in the synthesis of cholesterol metabolites which have various properties. The paper by Weber et al. in this issue of European …

Constitutive activation of MexT by amino acid substitutions results in MexEF-OprN overproduction in clinical isolates of Pseudomonas aeruginosa

2018

ABSTRACT When overproduced, the multidrug efflux system MexEF-OprN increases the resistance of Pseudomonas aeruginosa to fluoroquinolones, chloramphenicol, and trimethoprim. In this work, we demonstrate that gain-of-function mutations in the regulatory gene mexT result in oligomerization of the LysR regulator MexT, constitutive upregulation of the efflux pump, and increased resistance in clinical isolates.

Safe intake of a plant sterol-enriched beverage with milk fat globule membrane: Bioaccessibility of sterol oxides during storage

2018

Abstract Sterols in foods are susceptible to oxidation to form oxysterols. It is interesting for consumer health to know real intake and the possible associated adverse effects associated to oxysterols. This study measured oxysterol formation and bioaccessibility (BA) in a plant sterol (PS)-enriched milk-based fruit beverage with milk fat globule membrane (MFGM) added at 0, 3 and 6 months of storage at room temperature. The same cholesterol (COPs) and phytosterol oxidation products (POPs) (exclusively from β-sitosterol) (7α/β-hydroxy, α/β-epoxy, triol and 7-keto) were detected in the beverage and its bioaccessible fraction. Total COPs and POPs contents were maintained during storage, and th…

2021

Lipids contained in the plasma membrane of platelets play an important role in platelet function. Modifications in the lipid composition can fluidify or rigidify the environment around embedded receptors, in order to facilitate the access of the receptor by the drug. However, data concerning the lipid composition of platelet plasma membrane need to be updated. In addition, data on the impact of drugs on plasma membrane composition, in particular antiplatelet agents, remain sparse. After isolation of platelet plasma membrane, we assessed, using lipidomics, the effect of ticagrelor, a P2Y12 antagonist, and its active metabolite on the lipid composition of these plasma membranes. We describe t…

NMR Investigation of Structures of G-Protein Coupled Receptor Folding Intermediates

2016

Folding of G-protein coupled receptors (GPCRs) according to the two-stage model (Popot, J. L., and Engelman, D. M. (1990) Biochemistry 29, 4031-4037) is postulated to proceed in 2 steps: partitioning of the polypeptide into the membrane followed by diffusion until native contacts are formed. Herein we investigate conformational preferences of fragments of the yeast Ste2p receptor using NMR. Constructs comprising the first, the first two, and the first three transmembrane (TM) segments, as well as a construct comprising TM1-TM2 covalently linked to TM7 were examined. We observed that the isolated TM1 does not form a stable helix nor does it integrate well into the micelle. TM1 is significant…

Recent advances inγ-aminobutyric acid (GABA) properties in pulses: an overview

2017

Beans, peas, and lentils are all types of pulses that are extensively used as foods around the world due to their beneficial effects on human health including their low glycaemic index, cholesterol lowering effects, ability to decrease the risk of heart diseases and their protective effects against some cancers. These health benefits are a result of their components such as bioactive proteins, dietary fibre, slowly digested starches, minerals and vitamins, and bioactive compounds. Among these bioactive compounds, γ-aminobutyric acid (GABA), a non-proteinogenic amino acid with numerous reported health benefits (e.g. anti-diabetic and hypotensive effects, depression and anxiety reduction) is …

2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

2016

International audience; 2,3-Dihydrobenzofurans are proposed as privileged structures and used as chemical platform to design small compound libraries. By combining molecular docking calculations and experimental verification of biochemical interference, we selected some potential inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1. Starting from low affinity natural product 1, by our combined approach we identified the compounds 19 and 20 with biological activity in the low micromolar range. Our data suggest that the 2,3-dihydrobenzofuran derivatives might be suitable bioinspired lead compounds for development of new generation mPGES-1 inhibitors with increased affinity.

Downregulation of thioredoxin-1-dependent CD95 S-nitrosation by Sorafenib reduces liver cancer

2020

Hepatocellular carcinoma (HCC) represents 80% of the primary hepatic neoplasms. It is the sixth most frequent neoplasm, the fourth cause of cancer-related death, and 7% of registered malignancies. Sorafenib is the first line molecular targeted therapy for patients in advanced stage of HCC. The present study shows that Sorafenib exerts free radical scavenging properties associated with the downregulation of nuclear factor E2-related factor 2 (Nrf2)-regulated thioredoxin 1 (Trx1) expression in liver cancer cells. The experimental downregulation and/or overexpression strategies showed that Trx1 induced activation of nitric oxide synthase (NOS) type 3 (NOS3) and S-nitrosation (SNO) of CD95 rece…