Search results for "Esters"
showing 10 items of 305 documents
Interactions of human P-glycoprotein transport substrates and inhibitors at the drug binding domain: Functional and molecular docking analyses
2015
Rhodamine 123 (R123) transport substrate sensitizes P-glycoprotein (P-gp) to inhibition by compound 2c (cis-cis) N,N-bis(cyclohexanolamine)aryl ester isomer in a concentration-dependent manner in human MDR1-gene transfected mouse T-lymphoma L5178 cells as shown previously. By contrast, epirubicin (EPI) concentration changes left unaltered 2c IC50 values of EPI efflux. To clarify this discrepancy, defined molecular docking (DMD) analyses of 12 N,N-bis(cyclohexanolamine)aryl esters, the highly flexible aryl ester analog 4, and several P-gp substrate/non-substrate inhibitors were performed on human P-gp drug- or nucleotide-binding domains (DBD or NBD). DMD measurements yielded lowest binding e…
Large-scale screening of lipase acid deficiency in at risk population
2021
International audience; BACKGROUND: Lysosomal acid lipase deficiency (LALD, OMIM#278000) is a rare lysosomal disorder with an autosomal recessive inheritance. The main clinical manifestations are related to a progressive accumulation of cholesteryl esters, triglycerides or both within the lysosome in different organs such as the liver, spleen, and cardiovascular system. A wide range of clinical severity is associated with LALD including a severe very rare antenatal/neonatal/infantile phenotype named Wolman disease and a late-onset form named cholesteryl ester storage disease (CESD). METHODS: This study aimed to investigate a cohort of at-risk patients (4174) presenting with clinical or biol…
Synthesis and stereochemical studies of 2-substituted thiazolidine-4-carboxamide derivatives
2000
A series of new 2-substituted thiazolidine-4-carboxamide derivatives which have potentially useful immunological properties, have been synthesized in a stereoselective manner by coupling 2-subsituted thiazolidine-4-carboxylic acids with amines or amino esters. The structure of these compounds was established by combination of NMR methods and by X-ray analysis.
PHEA-PLA biocompatible nanoparticles by technique of solvent evaporation from multiple emulsions
2015
Nanocarriers of amphiphilic polymeric materials represent versatile delivery systems for poorly water soluble drugs. In this work the technique of solvent evaporation from multiple emulsions was applied to produce nanovectors based on new amphiphilic copolymer, the α,β-poly(N-2-hydroxyethyl)-DL-aspartamide-polylactic acid (PHEA-PLA), purposely synthesized to be used in the controlled release of active molecules poorly soluble in water. To this aim an amphiphilic derivative of PHEA, a hydrophilic polymer, was synthesized by derivatization of the polymeric backbone with hydrophobic grafts of polylactic acid (PLA). The achieved copolymer was thus used to produce nanoparticles loaded with α toc…
A 3D‑scaffold of PLLA induces the morphological differentiation and migration of primary astrocytes and promotes the production of extracellular vesi…
2019
The present study analyzed the ability of primary rat astrocytes to colonize a porous scaffold, mimicking the reticular structure of the brain parenchyma extracellular matrix, as well as their ability to grow, survive and differentiate on the scaffold. Scaffolds were prepared using poly-L-lactic acid (PLLA) via thermally-induced phase separation. Firstly, the present study studied the effects of scaffold morphology on the growth of astrocytes, evaluating their capability to colonize. Specifically, two different morphologies were tested, which were obtained by changing the polymer concentration in the starting solution. The structures were characterized by scanning electron microscopy, and a…
PLLA scaffolds with controlled architecture as potential microenvironment for in vitro tumor model
2019
Abstract The "microenvironment" where a tumor develops plays a fundamental role in determining its progression, the onset of metastasis and, eventually, its resistance to therapies. Tumor cells can be considered more or less invasive depending both on the nature of the cells and on the site where they are located. Commonly adopted laboratory culture protocols for the investigation of tumor cells take usually place on standard two-dimensional supports. However, such cultures do not allow for reproduction of the biophysical properties of the tumor’s microenvironment, thus causing the cells to lose most of their relevant characteristics. In this work MDA-MB 231 breast cancer cells were cultiva…
Synthesis, Structural Analysis, Fiber Formation and Preliminary Anticancer Characterization of the Organotin Polyether from Dibutyltin Dichloride and…
2012
The organotin polyether derived from reaction of dibutyltin dichloride and 2,5-dimethyl-3-hexyne-2,5-diol was rapidly synthesized employing classical interfacial polymerization in 65% yield and a chain length of 360 units. IR results are consistent with the polyether structure. Bands characteristic of the formation of the Sn-O are present and bands characteristic of the Sn-Cl are absent. F MALDI MS results in the low mass range gives ion fragment clusters to five units. Isotopic abundance matches for tin are consistent with its presence in these ion fragment clusters. In the high mass range ion fragment clusters to greater than 300 units are found. The products offer outstanding inhibition …
Diagnostic problems and postnatal follow-up in congenital toxoplasmosis
2007
Aim. In order to assess the consequences of different clinica] approaches in the prenata] management of congenital toxoplasmosis, we retrospectively reviewed 58 pregnant women with Toxoplasma seroconversion and prospec tively enrolled their 59 infants, referred to us from 1999 to 2004. Metbods. Data on clinica!, laboratocy and de mographic characteristics of the pregnant women were collected. Their children were entered intoa 48-month follow-up progcamme in which clinica , instrumental, ophthalmo logic and serologic evaluations were carried out at birth, at 1, 3, 6, 9, 15, 18, 24, 36 and at 48 months of life. Paediatric treatment with Spiramycin alone or alternated with Pyrime thamine-S…
Determination of ethyl sulfate – a marker for recent ethanol consumption – in human urine by CE with indirect UV detection
2006
A CE method for the determination of the ethanol consumption marker ethyl sulfate (EtS) in human urine was developed. Analysis was performed in negative polarity mode with a background electrolyte composed of 15 mM maleic acid, 1 mM phthalic acid, and 0.05 mM cetyltrimethylammonium bromide (CTAB) at pH 2.5 and indirect UV detection at 220 nm (300 nm reference wavelength). This buffer system provided selective separation conditions for EtS and vinylsulfonic acid, employed as internal standard, from urine matrix components. Sample pretreatment of urine was minimized to a 1:5 dilution with water. The optimized CE method was validated in the range of 5-700 mg/L using seven lots of urine. Intra-…
Treatment of malar and midfacial fractures with osteoconductive forged unsintered hydroxyapatite and poly-L-lactide composite internal fixation devic…
2013
Purpose To evaluate the internal fixation of malar and midfacial fractures, long-term results, and biocompatibility of osteoconductive internal fixation devices composed of a forged composite of unsintered hydroxyapatite and poly-L-lactide (F-u-HA/PLLA). Materials and Methods From January 2006 to June 2010, 29 patients (24 males and 5 females; age 33 ± 15 years) were included in the present prospective study. The fracture type was malar in 24 patients, midfacial in 5, isolated orbital floor blowout in 2, and frontal sinus, cranial base in 2 patients. The fractures were fixed with internal fixation devices; these were plates and screws composed of F-u-HA/PLLA. The 24 patients with malar frac…