Search results for "Chroman"
showing 10 items of 25 documents
CCDC 1409735: Experimental Crystal Structure Determination
2015
Related Article: Y. Rousselin, H. Laureano, A. Clavel|2015|Acta Crystallogr.,Sect.E:Cryst.Commun.|71|o552|doi:10.1107/S205698901501261X
Functional, textural and sensory properties of dry pasta supplemented with lyophilized tomato matrix or with durum wheat bran extracts produced by su…
2016
A study was carried out to produce functional pasta by adding bran aqueous extract (BW) and bran oleoresin (BO) obtained using ultrasound and supercritical CO2, respectively, or a powdery lyophilized tomato matrix (LT). The bioactive compounds, hydrophilic and lipophilic antioxidant activity (HAA and LAA) in vitro, were evaluated. BW supplementation did not improve antioxidant activity, whilst LT pasta showed unconventional taste and odor. BO pasta had good levels of tocochromanols (2551 μg/100 g pasta f.w.) and carotenoids (40.2 μg/100 g pasta f.w.), and the highest HAA and LAA. The oleoresin altered starch swelling and gluten network, as evidenced by scanning electron microscopy, therefor…
Is the chromanol head group of vitamin E nature's final truth on chain-breaking antioxidants?
2012
AbstractTocopherol is believed to be the most potent naturally occurring chain-breaking antioxidant. Hence, its refined phenolic head group chromanol may represent an optimum evolutionary solution to the problem of free-radical chain reactions in the lipid bilayer. To test the universal validity of this assumption beyond phenolic head groups, we have synthesized aromatic amine analogues of vitamin E and trolox with otherwise closely matching physicochemical properties: NH-toc and NH-trox. We have found that NH-toc and NH-trox were significantly more potent free radical scavengers, lipid peroxidation inhibitors and cytoprotective agents than their phenolic templates, tocopherol and trolox. I…
Quality parameters, bioactive compounds and their correlation with antioxidant capacity of commercial fruit-based baby foods
2013
Comprehensive research is required to achieve the optimization of the antioxidant protection through baby foods, in particular, the commercially available fruit-based baby foods. This study investigated the physicochemical properties, ascorbic acid (AA), total carotenoids (TC), total phenolic content (TPC), trolox equivalent antioxidant capacity (TEAC) and oxygen radical absorbance capacity (ORAC) of 23 different commercially available fruit-based baby foods. The main contribution to the total antioxidant capacity (trolox equivalent antioxidant capacity and oxygen radical absorbance capacity) was provided by ascorbic acid, followed by phenolic compounds, in accordance with a mathematical e…
Enhanced oxidative stress and increased mitochondrial mass during Efavirenz-induced apoptosis in human hepatic cells
2010
BACKGROUND AND PURPOSE Efavirenz (EFV) is widely used in the treatment of HIV-1 infection. Though highly efficient, there is growing concern about EFV-related side effects, the molecular basis of which remains elusive. EXPERIMENTAL APPROACH In vitro studies were performed to address the effect of clinically relevant concentrations of EFV (10, 25 and 50 mu M) on human hepatic cells. KEY RESULTS Cellular proliferation and viability were reduced in a concentration-dependent manner. Analyses of the cell cycle and several cell death parameters (chromatin condensation, phosphatidylserine exteriorization, mitochondrial proapoptotic protein translocation and caspase activation) revealed that EFV tr…
Bioactive chromenes from Rhyncholacis penicillata.
1994
Investigation of the aerial parts of Rhyncholacis penicillata afforded the new chromenes, 7-hydroxy-6-(3-methylbutyryl)-5-oxymethyl-chromene (rhynchonin A) and 7-hydroxy-6-(2-methylbutyryl)-6-oxymethylchromene (rhynchonin B). Structures were elucidated by spectroscopic methods and independent synthesis. Rhynchonin A showed broad insecticidal, acaricidal and nematicidal potency including strong biological activity against Heliothis zea.
Synthesis and evaluation in rats of the dopamine D2/3 receptor agonist 18F-AMC20 as a potential radioligand for PET
2015
Dopamine D2/3 receptor (D2/3R) agonist PET tracers are better suited for the imaging of synaptic dopaminergic neurotransmission than D2/3R antagonists and may also offer the opportunity to study in vivo the high-affinity state of D2/3R (D2/3RHigh). With the aim to develop 18F-labeled D2/3R agonists suitable for widespread clinical application, we report here on the synthesis and in vitro and in vivo evaluation of a D2/3R agonist ligand from the aminomethyl chromane (AMC) class-(R)-2-[(4- 18Fluorobenzylamino)methyl]chroman-7-ol (18F-AMC20). Methods: In vitro affinities of AMC20 toward dopaminergic receptor subtypes were measured in membrane homogenates prepared from HEK293 cells expressing h…
Fluorescent benzofurazan-cholic acid conjugates for in vitro assessment of bile acid uptake and its modulation by drugs.
2009
One of the most common mechanisms of hepatotoxicity is drug-induced cholestasis. Hence, new approaches for screening the cholestatic potential of drug candidates are desirable. In this context, we describe herein the use of synthetic 4-nitrobenzo-2-oxa-1,3-diazole (NBD) fluorescent conjugates of cholic acid (ChA) at positions 3alpha, 3beta, 7alpha, and 7beta for in vitro assessment of bile acid uptake. All the conjugates show a strong absorption band between 400 and 550 nm and have a fluorescence quantum yield of approximately 0.45, with an emission maximum centered at approximately 530 nm. After their photophysical characterization, 3alpha-, 3beta-, 7alpha-, and 7beta-NBD-ChA were used to …
Mitochondrial reactive oxygen species are obligatory signals for glucose-induced insulin secretion.
2009
OBJECTIVE—Insulin secretion involves complex events in which the mitochondria play a pivotal role in the generation of signals that couple glucose detection to insulin secretion. Studies on the mitochondrial generation of reactive oxygen species (ROS) generally focus on chronic nutrient exposure. Here, we investigate whether transient mitochondrial ROS production linked to glucose-induced increased respiration might act as a signal for monitoring insulin secretion. RESEARCH DESIGN AND METHODS—ROS production in response to glucose was investigated in freshly isolated rat islets. ROS effects were studied using a pharmacological approach and calcium imaging. RESULTS—Transient glucose increase …
The development of benzimidazoles as selective rho kinase inhibitors
2010
Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC(50)<10nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).