Search results for "Toxicity"

Oxidative stress response of tumor cells: microarray-based comparison between artemisinins and anthracyclines

2004

The antimalarial artemisinins also reveal profound cytotoxic activity against tumor cells. Artemisinins harbor an endoperoxide bridge whose cleavage results in the generation of reactive oxygen species (ROS) and/or artemisinin carbon-centered free radicals. Established cancer drugs such as anthracyclines also form ROS and free radicals that are responsible for the cardiotoxicity of anthracyclines. In contrast, artemisinins do not reveal cardiotoxicity. In the present investigation, we compared the cytotoxic activities of different artemisinins (artemisinin, artesunate, arteether, artemether, artemisitene, dihydroartemisinylester stereoisomers) in 60 cell lines of the National Cancer Institu…

Toxicity of the antimalarial artemisinin and its dervatives.

2010

As long as no effective malaria vaccine is available, chemotherapy belongs to the most important weapons fighting malaria. One of the most promising new drug developments is the sesquiterpene artemisinin (ARS) and its derivatives, e.g., artemether, arteether, and sodium artesunate. Large clinical studies and meta-analyses did not show serious side effects, although proper monitoring of adverse effects in developing countries might not be a trivial task. There is a paucity of large-scale clinical trials suitable to detect rare but significant toxicity. Therefore, a final and definitive statement on the safety of artemisinins still cannot be made. In contrast, animal experiments show consider…

Arterial hypertension in cancer: The elephant in the room

2019

The great therapeutical success achieved by oncology is counterbalanced by growing evidences of cardiovascular (CV) toxicity due to many antineoplastic treatments. Cardiac adverse events may cause premature discontinuation of effective oncologic treatments or occur as late events undermining the oncologic success. Arterial hypertension is both the most common comorbidity in cancer patients and a frequent adverse effect of anticancer therapies. A pre-existing hypertension is known to increase the risk of other cardiac adverse events due to oncologic treatments, in particular heart failure. Moreover, as a strict association between cancer and CV diseases has emerged over the recent years, var…

Safer chemicals using less animals: kick-off of the European ONTOX project

2021

The 3Rs concept, calling for replacement, reduction and refinement of animal experimentation, is receiving increasing attention around the world, and has found its way to legislation, in particular in the European Union. This is aligned by continuing high-level efforts of the European Commission to support development and implementation of 3Rs methods. In this respect, the European project called "ONTOX: ontology-driven and artificial intelligence-based repeated dose toxicity testing of chemicals for next generation risk assessment" was recently initiated with the goal to provide a functional and sustainable solution for advancing human risk assessment of chemicals without the use of animal…

Use of atropine-treated Daphnia magna survival for detection of environmental contamination by acetylcholinesterase inhibitors.

2003

The toxicity of cholinesterase-inhibiting compounds (e.g., carbamates and organophosphates) is due to a decrease in acetylcholine metabolism, which results in a continuous stimulation of cholinergic receptors (muscarinic and nicotinic) that can be fatal. The goal of this study was to evaluate the protective effect of atropine (muscarinic receptor antagonist) against paraoxon-induced toxicity to Daphnia magna using its survival rate for the detection of environmental contamination by cholinesterase-inhibiting compounds. As expected, paraoxon was lethal to D. magna in a concentration-dependent manner. Noteworthy, the pretreatment of these organisms with atropine dramatically increased their s…

Folate-targeted supramolecular vesicular aggregates based on polyaspartyl-hydrazide copolymers for the selective delivery of antitumoral drugs.

2010

Supramolecular vesicular aggregates (SVAs) have the advantage of combining the safe and biocompatible properties of colloidal vesicular carriers based on phospholipids with those of polymeric materials, i.e. polyaspartyl-hydrazide (PAHy) copolymers. To provide SVAs with a certain tumour selectivity, folate moieties were chemically conjugated to PAHy copolymers. Physicochemical properties (mean sizes, polydispersity index and zeta potential) of folate-targeted SVAs (FT-SVAs) loaded with gemcitabine were evaluated. The antiproliferative and anticancer activity of gemcitabine-loaded FT-SVAs was evaluated against two cancer cell lines, i.e. MCF-7 cells which over-express the folate receptor and…

Synthesis and characterization of some dibutylbis{5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoato}tin(IV) compounds. Toxicity studies of di- and tri-or…

2003

The preparation and spectroscopic characterization of some complexes of the type Bu2Sn(LH)2 (LH = 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoate) are reported. On the basis of spectroscopic evidence (1H, 13C, 119Sn NMR, IR and 119mSn Mossbauer) the compounds were judged to adopt the usual dicarboxylato structural type with a skew trapezoidal arrangement. This was further confirmed by X-ray crystallography in the case of Bu2Sn(L5H)2 (L5H = 5-[(E)-2-(4-chlorophenyl)-1-diazenyl]-2-hydroxybenzoate). Toxicity studies of the di- and tri-organotin compounds on the second larval instar of Aedes aegypti mosquito larvae are reported. Copyright © 2003 John Wiley & Sons, Ltd.

Microwave-Assisted Synthesis of New Selenazole Derivatives with Antiproliferative Activity

2013

New aryl-hydrazinyl-1,3-selenazole and aroyl-hydrazonyl-1,3-selenazoles were synthesized via Hantzsch type condensation reactions of selenosemicarbazides with α-halogenocarbonyl derivatives, under classical versus microwave heating conditions. Excellent yields and shorter reaction times were obtained under irradiation conditions. The structures of the synthesized compounds were assigned based on spectroscopic data (FT-IR, 1 H-NMR), MS and elemental analysis. Selenazole derivatives were screened for their anti-proliferative effects against two leukemia cell lines (CCRF-CEM and HL60) and three carcinoma cell lines (MDA-MB231, HCT116 and U87MG).

Single dose prulifloxacina can improve BCG tollerability

2010

Toward the development of metal-based synthetic nucleases: DNA binding and oxidative DNA cleavage of a mixed copper(II) complex with N-(9H-purin-6-yl…

2009

Abstract The complex [Cu(N9-ABS)(phen) 2 ]·3.6H 2 O, H 2 N9-ABS  = N -(9 H -purin-6-yl)benzenesulfonamide and phen = 1,10-phenanthroline, has been synthesized and then characterized with the aid of X-ray diffraction, analytical, and spectroscopic techniques. The geometry of Cu(II) is distorted square pyramidal with the equatorial positions occupied by three N atoms from two phenantroline molecules and one N atom from the adenine ring of the sulfonamide ligand. The interaction of the complex with DNA was studied by means of viscosity measurements and fluorescence spectroscopy. The results pointed to a classic intercalation of the complex between the DNA base pairs. The complex was found to b…