Search results for "cytotoxic"
showing 10 items of 1673 documents
Cytotoxic Glial Swelling by Arachidonic Acid
1994
Arachidonic acid (AA, 20:4) is a major constituent of membrane phospholipids in brain tissue. Normally, the free fatty acid is present only in a small amount, but it accumulates under adverse conditions, such as ischemia or brain injury [1,9]. The release of free fatty acid involves activation of phospholipases and breakdown of membrane phospholipids. AA in particular is considered to mediate pathological processes. The polyunsaturated compound is a precursor of prostaglandins, leukotrienes, and oxygen-derived free radicals [11]. In cerebral ischemia concentrations of free AA of up to 0.5 mM/kg have been found in brain tissue [9].
Comparative Biological Properties and Mineralization Potential of 3 Endodontic Materials for Vital Pulp Therapy: Theracal PT, Theracal LC, and Bioden…
2021
INTRODUCTION The aim of this study was to assess the biological properties and mineralization potential of the new Theracal PT (Bisco Inc, Schaumburg, IL) compared with its predecessor Theracal LC (Bisco Inc) and the hydraulic silicate-based cement Biodentine (Septodont, Saint-Maur-des-Fosses, France) on human dental pulp stem cells (hDPSCs) in vitro. METHODS Standardized sample discs were obtained for each material (n = 30) together with 1:1, 1:2, and 1:4 material eluates. Previously characterized hDPSCs were cultured with the different materials in standardized conditions, and the following assays were performed: a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, a woun…
Introducing PeptoPlexes: Polylysine-block-Polysarcosine Based Polyplexes for Transfection of HEK 293T Cells
2014
A series of well-defined polypeptide-polypeptoid block copolymers based on the body's own amino acids sarcosine and lysine are prepared by ring opening polymerization of N-carboxyanhydrides. Block lengths were varied between 200-300 for the shielding polysarcosine block and 20-70 for the complexing polylysine block. Dispersity indexes ranged from 1.05 to 1.18. Polylysine is polymerized with benzyloxycarbonyl as well as trifluoroacetyl protecting groups at the ϵ-amine group and optimized deprotection protocols for both groups are reported. The obtained block ionomers are used to complex pDNA resulting in the formation of polyplexes (PeptoPlexes). The PeptoPlexes can be successfully applied i…
Polyacanthoside A, a new oleanane-type triterpenoid saponin with cytotoxic effects from the leaves of Acacia polyacantha (Fabaceae)
2018
The chemical investigation of the leaves and stem bark of Acacia polyacantha (Fabaceae) led to the isolation of a new oleanane-type triterpenoid saponin named polyacanthoside A 1 together with fifteen known compounds. Their structures were established from spectral , mainly HRESIMS, 1D NMR and 2D NMR and by comparison with literature data. The cytotoxicity of compound 1 and the analogues 8 as well as doxorubicin was determined in a panel of 9 cancer cell lines including sensitive and drug resistant phenotypes. Unlike the analogue 8, compound 1 as well as doxorubicin displayed cytotoxic effects in all the 9 tested cancer cell lines with IC50 values ranged from 8.90 μM (towards CCRF-CEM leuke…
Analogues of cytotoxic squamocin using reliable reactions: new insights into the reactivity and role of the α,β-unsaturated lactone of the annonaceou…
2006
Abstract A small library of squamocin analogues has been prepared and screened biologically (cytotoxicity, inhibition of mitochondrial complex I and complex III). To centre diversity on a crucial part of the molecule (i.e., the α,β-unsaturated lactone), an original and reliable lactone opening reaction has been discovered and exploited among other efficient reactions.
Design, synthesis and antiproliferative activity of methyl 4-Iodo-1-β-D-ribofuranosyl-pyrazole-3-carboxylate and related compounds
1996
Abstract In a SAR study on azole-related nucleosides we have designed some pyrazole-nucleoside analogs characterised, for the first time, by a carboxylic ester moiety. 4-Iodo-1-β-D-ribofuranosyl-pyrazole-3-carboxylate showed a wide spectrum of antiproliferative activity and a particularly low cytotoxicity against resting PBL, being, unlike the other azole nucleosides, more active than the corresponding primary amide.
Stable Expression of Heterologous Sulfotransferase in V79 Cells: Activation of Primary and Secondary Benzylic Alcohols
1994
Abstract A sulfotransferase (ST) capable of activating 1-hydroxymethylpyrene (HMP) and 9-hydroxymethylanthracene (HMA) to mutagens was purified from rat liver. This enzyme appeared to be identical with hydroxysteroid STa, whose cDNA was cloned and stably expressed in Chinese hamster V79 cells. Several primary and secondary benzylic alcohols derived from polycyclic aromatic hydrocarbons induced gene mutations, sister chromatid exchanges (SCE) and/or cytotoxicity in these cells.
Phytochemical analysis of two Weigela florida cultivars, “Pink Poppet” and “Jean’s Gold”
2020
Abstract Nine different oleanane-type glycosides were extracted and isolated by various chromatographic methods from two Weigela florida cultivars, “Pink Poppet” and “Jean’s Gold”. From the roots of W. florida “Pink Poppet”, three monodesmosidic oleanolic acid saponins 1, 4, 5 were obtained, together with one hederagenin ester 6 from the leaves, and six bidesmosidic saponins 2, 3, 6-9 were isolated from the leaves of W. florida “Jean’s Gold”. Among compounds 1-9, three were previously undescribed (1-3) and six (4-9) were already published in the literature. Their structures were assigned by spectroscopic analysis mainly 2D NMR and mass spectrometry (ESI-MS). The cytotoxicity of the isolated…
Novel Stilbene-Based Antileukemic Agents Active in P-Glycoprotein Expressing and Apoptosis-Resistant Acute Leukaemia Cell Lines.
2005
Abstract The stilbene scaffold is a basic element for a number of biologically active natural and synthetic compounds and in accordance with Evans’ definition it can be considered as a privileged structure. One of the most relevant and studied stilbenes is Resveratrol, a phytoalexin present in grapes, endowed with chemopreventive and chemotherapeutic properties and able to induce apoptosis in different cancer cell lines. Since reduced apoptosis has been implicated in the development and progression of malignant tumors and in the occurrence of chemoresistant phenotypes, resveratrol-induced apoptosis might therefore contribute to its antitumor activity. However, resveratrol is a not potent cy…
Tuning antiviral CD8 T-cell response via proline-altered peptide ligand vaccination
2019
AbstractViral escape from CD8+cytotoxic T lymphocyte responses correlates with disease progression and represents a significant challenge for vaccination. Here, we demonstrate that CD8+T cell recognition of the naturally occurring MHC-I-restricted LCMV-associated immune escape variant Y4F is restored following vaccination with a proline-altered peptide ligand (APL). The APL increases MHC/peptide (pMHC) complex stability, rigidifies the peptide and facilitates T cell receptor (TCR) recognition through reduced entropy costs. Structural analyses of pMHC complexes before and after TCR binding, combined with biophysical analyses, revealed that although the TCR binds similarly to all complexes, t…