Search results for "Tetra"

Cytoprotective organoselenium compounds for oligodendrocytes

2021

Abstract Herein we report the synthesis of peptide-like and tetrazole-based organoselenium compounds via Ugi and Ugi-azide reactions, respectively. The organoselenium compounds' intrinsic cytoprotective and antioxidant capacities were evaluated in 158 N and 158JP murine oligodendrocytes. Furthermore, their redox properties were theoretically evaluated using Molecular Operating Environment-docking studies. Most of the compounds did not exhibit any cytotoxicity against the 158JP and 158 N cells. Among the tested compounds, the tetrazole- (e.g., 6, 7, and 9) and the pseudopeptide-based organoselenium compounds (e.g., 11, 15, and 17) displayed antioxidant properties. On the other hand, the quin…

A new dual inhibitor of arachidonate metabolism isolated from Helichrysum italicum.

2003

Six acetophenones (1-6) and one gamma-pyrone (7), previously isolated from Helichrysum italicum, were tested for their ability to inhibit enzymatic and non-enzymatic lipid peroxidation, the stable 1,1-diphenyl-2-pycryl-hydrazyl free radical, superoxide scavenging and arachidonic acid metabolism. In addition, they were studied in different experimental models such as the chronic inflammation induced by 12-O-tetradecanoylphorbol 13-acetate (TPA), the phospholipase A(2)-induced mouse paw oedema test, the carrageenan-induced mouse paw oedema test, and the writhing induced by acetic acid in the mouse. Of the assayed compounds, only 1 inhibited enzymatic lipid peroxidation but had no effect on no…

Alternariol-induced cytotoxicity in Caco-2 cells. Protective effect of the phenolic fraction from virgin olive oil.

2014

The extra virgin olive oil (EVOO) has been associated to antioxidant effects. The mycotoxin alternariol (AOH) can contaminate olives. The aims of this work were to determine the cytotoxic effects and reactive oxygen species (ROS) produced by AOH, tyrosol and oleuropein (two polyphenols of olive oil) and a real EVOO extract in Caco-2 cells. The MTT assay and the ROS production by the H2-DCFDA probe were used. Results demonstrated that AOH reduces cellular proliferation depending on concentration, whereas tyrosol and oleuropein did not (12.5-100 μM). The combination of AOH + oleuropein (50 μM) increased cell proliferation (24%) whereas, AOH + tyrosol decreased (47%) it. Besides, AOH increased…

Comparative study to predict toxic modes of action of phenols from molecular structures.

2013

Quantitative structure-activity relationship models for the prediction of mode of toxic action (MOA) of 221 phenols to the ciliated protozoan Tetrahymena pyriformis using atom-based quadratic indices are reported. The phenols represent a variety of MOAs including polar narcotics, weak acid respiratory uncouplers, pro-electrophiles and soft electrophiles. Linear discriminant analysis (LDA), and four machine learning techniques (ML), namely k-nearest neighbours (k-NN), support vector machine (SVM), classification trees (CTs) and artificial neural networks (ANNs), have been used to develop several models with higher accuracies and predictive capabilities for distinguishing between four MOAs. M…

Pyrrolo[2,1-d][1,2,3,5]tetrazine-4(3H)-ones with Potent Antitumor Activity

2003

Mechanism of vascular relaxation by thaligrisine

2000

Abstract In the present study we examine the mechanism by which thaligrisine, a bisbenzyltetrahydroisoquinoline alkaloid, inhibits the contractile response of vascular smooth muscle. The work includes functional studies on rat isolated aorta and tail artery precontracted with noradrenaline or KCl. In other experiments rat aorta was precontracted by caffeine in the presence or absence of extracellular Ca 2 +. In order to assess whether thaligrisine interacts directly with calcium channel binding sites or with α-adrenoceptors we examined the effect of the alkaloid on [ 3 H]-(+)- cis diltiazem, [ 3 H]-nitrendipine and [ 3 H]-prazosin binding to cerebral cortical membranes. The functional studi…

Gene-diet interaction in plasma lipid response to plant sterols and stanols: A review of clinical trials

2021

Abstract Plant sterols and stanols (PS) are well known for their cholesterol-lowering effect by reducing intestinal absorption of cholesterol. However, genetic factors modulate the low-density lipoprotein cholesterol (LDL-C) response to PS therapy. This review examines clinical trials evaluating the impact of the main genes associated with response of plasma lipid concentrations to PS intake: APOE, CYP7A1, ABCG5/G8, NPC1L1, CETP, APOA4/A5, SCARBI, HMGCR, PPARα, LIPC, MTHFR and LPA. Evidence indicates that carriers of mutant allele of the CYP7A1 c. −204 A > C variant experience a greater plasma cholesterol reduction after PS intake, although there is discrepancy for the rest of genetic varia…

Neuronal cell cycle: the neuron itself and its circumstances.

2015

Neurons are usually regarded as postmitotic cells that undergo apoptosis in response to cell cycle reactivation. Nevertheless, recent evidence indicates the existence of a defined developmental program that induces DNA replication in specific populations of neurons, which remain in a tetraploid state for the rest of their adult life. Similarly, de novo neuronal tetraploidization has also been described in the adult brain as an early hallmark of neurodegeneration. The aim of this review is to integrate these recent developments in the context of cell cycle regulation and apoptotic cell death in neurons. We conclude that a variety of mechanisms exists in neuronal cells for G1/S and G2/M check…

High atomic yield bromine-less benzylic bromination

2002

A two-phase mixture (sodium bromide, aqueous hydrogen peroxide/carbon tetrachloride or chloroform) under visible light provides a simple and convenient system for benzylic bromination of toluenes. A high atomic yield for bromine atoms is attained. Substitution of the chlorinated solvents by other more environmentally benign organic solvents has been attempted and good results are obtained for methyl pivalate.

Protonation thermodynamics of 2,2'-bipyridyl in aqueous solution. Salt effects and weak complex formation

1993

Abstract Protonation constants of 2,2'-bipyridyl (bipy) have been determined potentiometrically, using (H + )-glass electrode, in different aqueous media (alkali and alkaline earth chlorides, tetramethylammonium chloride and tetramethylammonium iodide) at different temperatures and ionic strengths. The differences in log K H values are explained using a complex formation model. Formation thermodynamic parameters are given.