Search results for "Propionate"

Phospholipid-polyaspartamide micelles for pulmonary delivery of corticosteroids

2011

A novel drug delivery system for beclomethasone dipropionate (BDP) has been constructed through self-assembly of a pegylated phospholipid-polyaminoacid conjugate. This copolymer was obtained by chemical reaction of α,β-poly(N-2-hydroxyethyl)-DL-aspartamide (PHEA) with 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethyleneglycol)2000] (DSPE-PEG(2000)-NH(2)). Benefiting from the amphiphilic structure with the hydrophilic shell based on both PHEA and PEG and many hydrophobic stearoyl tails, PHEA-PEG(2000)-DSPE copolymer was able to self assemble into micelles in aqueous media above a concentration of 1.23 × 10(-7)M, determined by fluorescence studies. During the self-assembling …

Biocompatible polymers coated Solid Lipid Microparticles (SLM) for pulmonary delivery

2015

Effects of extra-fine inhaled beclomethasone/formoterol on both large and small airways in asthma

2010

Background: Airway inflammation in asthma involves both large and small airways, and the combination of inhaled corticosteroids (ICS) and long acting beta-2 agonists (LABA) is the mainstay of therapy. Available inhaled combinations differ in terms of drug delivery to the lung and the ability to reach small airways. Aim: To evaluate whether treatment with an extra-fine inhaled combination provides additional effects vs a nonextra-fine combination on airway function. Methods: After a 1- to 4-week run-in period, patients with asthma were randomized to a double blind, double dummy, 12-week treatment with either extra-fine beclomethasone/formoterol (BDP/F) 400/24 lg daily or fluticasone propiona…

IκB kinase-driven nuclear factor-κB activation in patients with asthma and chronic obstructive pulmonary disease.

2011

Background Nuclear factor-κB (NF-κB) is a transcriptional factor of different inflammatory patterns involved in asthma and chronic obstructive pulmonary disease (COPD) that is tightly controlled by IκB kinase (IKK) complex. Objective We investigated the dysregulation of IKK-driven NF-κB activation in patients with asthma and COPD. Methods We assessed IKKα and IKKβ expression and activation, their regulation by glucocorticosteroids, and their involvement in IL-8 synthesis in PBMCs isolated from asthmatic patients, healthy smokers (HSs), patients with COPD, and control subjects. PBMCs from control subjects were stimulated with TNF-α and cigarette smoke extract in the presence or absence of fl…

Screening for potential fermentative hydrogen production from black water and kitchen waste in on-site UASB reactor at 20 degrees C.

2008

The potential of black water and a mixture of black water and kitchen waste as substrates for on-site dark fermentative hydrogen production was screened in upflow anaerobic sludge blanket reactors at 20 degrees C. Three different inocula were used with and without heat treatment. With glucose, the highest specific hydrogenogenic activity was 69 ml H2 g volatile solids(-1) d(-1) in batch assays and the highest hydrogen yield 0.44 mol H2 mol glucose(-1) in upflow anaerobic sludge bed reactor. The mixture of black water and kitchen waste degraded readily into volatile fatty acids in the reactors, thus showing potential for hydrogen production. In the conditions applied, however, the highest en…

Effects of Beclomethasone dipropionate and Formoterol in reducing oxidative stress induced by cigarette smoke extracts and IL-17

2011

Rationale: Oxidative stress is involved in airway inflammatory diseases. Inhaled-corticosteroids reduce airway inflammation and the combination with long-acting β2 agonists enhances this effect. Objective: to investigate whether Cigarette smoke extracts (CSE) and Interleukin-17A (IL-17A) activate airway epithelial cells to release markers of oxidative/nitrosative stress and to investigate the effect of beclomethasone dipropionate (BDP) and formoterol. Methods: Human bronchial epithelial cells (16HBE) were stimulated with different concentrations of CSE (from 0 to 10%) to evaluate the expression of IL-17 receptor (IL-17R). 16HBE were also stimulated with CSE (2.5%) with and withouth rhIL-17A…

Synthesis and in Vitro Evaluation of Biotinylated RG108:  A High Affinity Compound for Studying Binding Interactions with Human DNA Methyltransferases

2006

Small-molecule inhibitors of DNA methyltransferases such as RG108 represent promising candidates for cancer drug development. We report the synthesis and in vitro analysis of a biotinylated RG108 conjugate, 2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-3-(5-[3-[5-(2-oxo-hexahydro-thieno[3,4-d]imidazol-4-yl)pentanoylamino]propoxy]-1H-indol-3-yl)propionic acid (bio-RG108), for the evaluation of interactions with DNA methyltransferase enzymes. The structural design of the chemically modified inhibitor was aided by molecular modeling, which suggested the possibility for extensive chemical modifications at the 5-position of the tryptophan moiety in RG108. The inhibitory activity of the corresponding d…

Fluticasone furoate maintains epithelial homeostasis via leptin/leptin receptor pathway in nasal cells

2014

Leptin is involved in the lung epithelial homeostasis. Its role in the nasal tract is largely unknown. Allergic rhinitis (AR) is induced by the allergen exposure leading to consequential structural abnormalities in the nasal epithelium. Topical corticosteroids are recommended as first-line therapy in AR. Parietaria pollen is one of the most important allergenic sources in the southern Europe. In vitro, in human nasal epithelial cell line RPMI 2650, we aimed to determine whether allergen stimulation acts on leptin/leptin receptor pathway and how fluticasone furoate (FF) influences this pathway. The effects of the major allergen recombinant Par j 1 (rPar j 1), of FF, of leptin, and of TGF-b1 …

Multixenobiotic resistance efflux activity in Daphnia magna and Lumbriculus variegatus

2014

Multixenobiotic resistance is a phenomenon in which ATP-binding cassette (ABC) family proteins transfer harmful compounds out of cells. Daphnia magna and Lumbriculus variegatus are model species in aquatic ecotoxicology, but the presence and activity of ABC proteins have not been well described in these species. The aim of this work was to study the presence, activity, and inhibition of ABC transport proteins in D. magna and L. variegatus. The presence of abcb1 and abcc transcripts in 8-9-day-old D. magna was investigated by qRT-PCR. The activity of MXR in D. magna and L. variegatus was explored by influx of the fluorescent ABC protein substrates rhodamine B and calcein-AM, with and without…

Novel GPR120 agonist TUG891 modulates fat taste perception and preference and activates tongue-brain-gut axis in mice

2020

GPR120 is implicated as a lipid receptor in the oro-sensory detection of dietary fatty acids. However, the effects of GPR120 activation on dietary fat intake or obesity are not clearly understood. We investigated to determine whether the binding of TUG891, a novel GPR120 agonist, to lingual GPR120 modulates fat preference in mice. We explored the effects of TUG891 on obesity-related hormones and conducted behavioral choice tests on mice to better understand the physiologic relevance of the action of TUG891. In cultured mouse and human taste bud cells (TBCs), TUG891 induced a rapid increase in Ca2+ by acting on GPR120. A long-chain dietary fatty acid, linoleic acid (LA), also recruited Ca2+ …