Search results for "cyclic"
showing 10 items of 2439 documents
0131 : Impact of overweight on anthracycline and trastuzumab-induced cardiotoxicity: experimental study in mice
2015
Trastuzumab (TRZ), a humanized monoclonal antibody against Human Epidermal Growth Factor Receptor 2 (HER2) oncogene, is believed to potentiate doxorubicin (DOX) cardiotoxicity, resulting in left ventricular dysfunction. Few data indicate that overweight could influence DOX-induced cardiotoxicity, and no study has already evaluated the impact of moderate overweight on the cardiotoxic effect of DOX alone or in combination with TRZ. Immediately after birth, litters of C57BL/6 mice were either maintained at 10 (normal litter, NL), or reduced to 3 (small litter, SL) in order to induce programming of ~15% overweight through postnatal overfeeding. At 4 months, in order to evaluate the potentiation…
Doxorubicin induces wide-spread transcriptional changes in the myocardium of hearts distinguishing between mice with preserved and impaired cardiac f…
2021
Abstract Aims Doxorubicin (DOX) is an important drug for the treatment of various tumor entities. However, the occurrence of heart failure limits its application. This study investigated differential gene expression profiles in the left and right ventricles of DOX treated mice with either preserved or impaired myocardial function. We provide new mechanistic insights into the pathophysiology of DOX-induced heart failure and have discovered pathways that counteract DOX-induced cardiotoxicity. Main methods We used in total 48 male mice and applied a chronic low dose DOX administration (5 mg/kg per injection, in total 20 mg/kg over 4 weeks) to induce heart failure. Echocardiographic parameters …
Iron overload does not potentiate doxorubicin induced cardiotoxicity in vivo in mice and in vitro in cardiomyocytes cell cultures
2013
Background: Doxorubicin (DOX), an anticancer anthracycline, is known to induce serious cardiotoxicity, which is believed to be mediated by oxidative stress and complex interactions with iron. However, the relations between iron metabolism and DOX-induced cardiotoxicity remain a matter of controversy. Methods: Firstly, we used an in vivo murine model of iron overloading (IO) where male C57BL/6 mice received during 3 weeks (D0-D20) a daily dextran-iron injection (15 mg/kg/day.) and then (D21) a single dose of 6 mg/kg DOX. We evaluated cardiac function with echocardiography, myocardial gene's expression, nitro-oxidative stress levels and iron status. Secondly, the anti-proliferative activity o…
Inhibition of class I histone deacetylase with an apicidin derivative prevents cardiac hypertrophy and failure
2008
AIMS: Recent studies have demonstrated the importance of chromatin remodelling via histone acetylation/deacetylation for the control of cardiac gene expression. Specific histone deacetylases (HDACs) can, in fact, play a positive or negative role in determining cardiac myocyte (CM) size. Here, we report on the effect on hypertrophy development of three inhibitors (HDACi) of class I HDACs. METHODS AND RESULTS: The compounds were first analysed in vitro by scoring hypertrophy, expression of foetal genes, and apoptosis of neonatal rat CMs stimulated with phenylephrine, an alpha1-adrenergic agonist. This initial screening indicated that a truncated derivative of apicidin with class I HDAC specif…
Inorganic Nitrate Therapy Improves Doxorubicin-Induced Cardiomyopathy
2011
The anthracycline doxorubicin (DOX) is a potent and effective antineoplastic antibiotic agent widely used in the treatment of a broad range of forms of cancer. The clinical use of DOX is limited by cardiotoxicity, which increases dose dependently and may lead to dilated cardiomyopathy and clinical
Modulating effects of humic acids on genotoxicity induced by water disinfectants in Cyprinus carpio
2005
The use of chlorinated disinfectants during drinking-water production has been shown to generate halogenated compounds as a result of interactions of humic acids with chlorine. Such chlorinated by-products have been shown to induce genotoxic effects and consumption of chlorinated drinking-water has been correlated with increased risk for cancer induction in human populations. The aim of this work was to test the potential genotoxic effects on circulating erythrocytes of the fish Cyprinus carpio exposed in vivo to well-waters disinfected with sodium hypochlorite (NaClO), chlorine dioxide (ClO2) or peracetic acid (CH3COO2H, PAA), in the absence or presence of standard humic acids (HA). The ef…
Stereoselective construction of the tetracyclic scalarane skeleton from carvone
1999
The tetracyclic scalarane skeleton 22 has been constructed from (S)-(+)-carvone using two intramolecular Diels–Alder reactions as key synthetic steps. Abad Somovilla, Antonio, Antonio.Abad@uv.es ; Agullo Blanes, M Consuelo, Consuelo.Agullo@uv.es ; Cuñat Romero, Ana Carmen, Ana.Cunat@uv.es ; Llosa Blasco, Maria Carmen, Carmen.Llosa@uv.es
Synthesis, In Vitro and In Silico Analysis of New Oleanolic Acid and Lupeol Derivatives against Leukemia Cell Lines: Involvement of the NF-κB Pathway
2022
Oleanolic acid (OA) and Lupeol (LU) belong to the class of natural triterpenes and are endowed with a wide range of biological activities, including cytotoxicity toward several cancer cell lines. In this context, we investigated a set of compounds obtained from the two natural precursors for the cytotoxicity against leukemia HL60 cells and the multidrug-resistant (MDR) variant HL60R. Six new semi-synthetic triterpenes have been synthetized, fully characterized, and were investigated together with other triterpenes compounds for their pharmacological mechanism of action. The interaction of the more cytotoxic compounds with the nuclear factor kappa B (NF-κB) pathway has been also evalua…
Efficient electroorganic synthesis of 2,3,6,7,10,11-hexahydroxytriphenylene derivatives
2012
2,3,6,7,10,11-Hexahydroxytriphenylene of good quality and purity can be obtained via anodic treatment of catechol ketals and subsequent acidic hydrolysis. The electrolysis is conducted in propylene carbonate circumventing toxic and expensive acetonitrile. The protocol is simple to perform and superior to other chemical or electrochemical methods. The key of the method is based on the low solubility of the anodically trimerized product. The shift of potentials is supported by cyclic voltammetry studies.
A Versatile and Convenient Method for the Functionalization of Porphyrins
2001
International audience; The condensation of 3-(chloromethyl)benzoyl chloride with different atropisomers of meso-(tetra-o-aminophenyl)porphyrin (TAPP), followed by the reaction of a series of nucleophilic reagents leads, among others, to precursors of biomimetic models of heme proteins such as cytochrome c oxidase (CcO). This synthesis can also be applied as an efficient two-step reaction to obtain highly functionalized porphyrin derivatives potentially useful for cation binding.