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Results 601 - 650 of 2862
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Makiyama Tomohiko - - 2010
Ceramide-1-phosphate (C1P) regulates cellular functions including arachidonic acid (AA) metabolism and modulates cell fate. The mechanism by which C1P is taken up is unclear, and the development of lipophilic analogs may be useful for regulating C1P's actions. We synthesized new mono- and di-methyl-ester (MM and DM, respectively) analogs of C1P ...
Wang Tao - - 2010
Polymeric micelles are used as pharmaceutical carriers to increase solubility and bioavailability of poorly water-soluble drugs. Different ligands are used to prepare targeted polymeric micelles. Earlier, we developed the method for use of specific landscape phage fusion coat proteins as targeted delivery ligands and demonstrated the efficiency of this approach ...
Pérez Martín José Manuel JM Departamento de Biología, Facultad de Ciencias, Universidad Autónoma de Madrid, Cantoblanco, Madrid, - - 2010
Propyl p-hydroxybenzoate, commonly referred to as propylparaben, is the most frequently used preservative to inhibit microbial growth and extend shelf life of a range of consumer products. The objective of this study was to provide further insight into the toxicological profile of this compound, because of the current discrepancy in ...
Metwally Kamel - - 2010
As part of our ongoing research effort to develop new antimitotic agents based on the recently reported pyrimido[4,5-c]quinoline-1(2H)-one ring skeleton, we were interested in identifying structural elements that contribute to the cytotoxicity of this class of compounds. The effect of several quinoline-ring substituents was examined and the new compounds were ...
MacDonald Chris - - 2010
The aim of this study was to use different toxicity indices to investigate the effect of N, N-Dimethylacetamide (DMA), Polyethylene glycol 400 (PEG 400), Methyl-Pyrrolidone/aromatic hydrocarbon (MPH), Cremophor((R)) EL, and Dimethylsulfoxide (DMSO) on Calu-3 cells. Membrane perturbation and cytotoxicity were investigated using lactate dehydrogenase (LDH), 3-[4, 5-Dimethylthiazol-2-yl]-2, 5-diphenyl tetrazolinium bromide ...
Gasparri Fabio - - 2010
Informa Life Sciences' Fifth Annual Conference on Cell-Based Assays, held in Cologne, Germany, included topics covering new technical developments in the field of cell-based assays. This conference report highlights selected presentations on cell-based assays for compound screening and 3D cell-based assays.
Barbosa Luiz Cláudio Almeida - - 2010
A series of twelve 2,5-bis(alkylamino)-1,4-benzoquinones were prepared in yields ranging from 9-58% via the reaction between p-benzoquinone and various amines. The structures of the synthesized compounds were confirmed by IR, 1H- and 13C-NMR and MS analyses. The phytotoxicity of the 2,5-bis(alkylamino)-1,4-benzoquinones was evaluated against two crop species, Cucumis sativus and ...
Zandi K - - 2010
BACKGROUND AND OBJECTIVES: Antitumor drug resistance and side effects of antitumor compounds are the most common problems in medicine. Therefore, finding new antitumor agents with low side effects could be interesting. This study was designed to assay antitumor activity of the extract from brown alga Sargassum oligocystum, gathered from Persian ...
Vorster Chris - - 2010
In the search for new and improved anticancer therapies, researchers have identified several potentially useful compounds. One of these agents is 2-methoxyestradiol-bis-sulphamate (2ME-BM), a sulphamoylated derivative of 2-methoxyestradiol. The objective of this study was to evaluate 2ME-BM's in vitro efficacy as antiproliferative agent in the MCF-7 breast adenocarcinoma cell line. ...
Zhang Weipeng - - 2010
The biomedical properties of novel biodegradable copoly(amino acid)s based on 6-aminocaproic acid and L-proline were analyzed in this article. The cytotoxicity of the copolymer films was tested in vitro using human embryonic kidney (HEK) 293 cells. The cell proliferation, cell cycle, cell apoptosis, and hemolysis of the polymers were also ...
Han Haiyong - - 2010
Safe and effective chemotherapeutic agents for the treatment of pancreatic cancer remain elusive. We found that chalcone epoxides (1,3-diaryl-2,3-epoxypropanones) inhibited growth in two pancreatic cancer cell lines, BxPC-3 and MIA PaCa-2. Three compounds were active, with GI(50) values of 5.6 to 15.8 microM. Compound 4a, 1,3-bis-(3,4,5-trimethoxyphenyl)-2,3-epoxypropanone, had an average GI(50) ...
Morishige T - - 2010
Recent studies have indicated that amorphous silica particles (SPs) show cytotoxicity against various types of cells, including macrophages. However, the mechanism of cell death has not been determined, and systematic investigations of the relationship between particle characteristics and cytotoxicity are still quite limited. Here, we compared the cytotoxicity of SPs ...
Shaker Kamel H - - 2010
The new cembrane diterpene (3E,11E)-cembra-3,8(19),11,15-tetraene-7alpha-ol (1), nephthenol (2), and all-trans-peridinin (3) have been isolated from the soft coral Litophyton arboreum. The tetraterpene 3, (+)-7,8-epoxy-7,8-dihydrocembrene C (4), emblide (5), sarcophytoxide (6), sarcoglaucol-16-one (7), guajacophine (8), and 1,4-peroxymuurol-5-ene (9) have been obtained from the soft coral Sarcophyton ehrenbergi. The compounds were characterized ...
Le Hegarat Ludovic - - 2010
Many chemical carcinogens require metabolic activation to form genotoxic compounds in human. Standard in vitro genotoxicity assays performed with activation systems, such as rat liver S9, are recognised to lead to a high number of false positives. The aim of this study was to evaluate the suitability of differentiated human ...
Gülden Michael - - 2010
Using C6 glioma cells in this study we investigated in detail how exposure time and cell concentration affect the cytotoxic potency of H(2)O(2) in vitro. Median cytotoxic concentrations (EC(50)) decreased from 500 to 30 μM with increasing incubation time from 1 to 24h. Twenty-four hours proved to be sufficient to ...
Scholz Anne-Kathrin - - 2010
Large-scale screens in mammalian cells demand for flexible high-throughput screening platforms that allow to analyze cellular traits on a genome-wide level or to identify small-molecule inhibitors (SMIs) from complex compound libraries. In this study we developed and tested high-density cell arrays made out of polydimethylsiloxane (PDMS) that support cell growth ...
Majumder Anurima - - 2010
Somatic mutations in the Jak2 protein, such as V617F, cause aberrant Jak/STAT signaling and can lead to the development of myeloproliferative neoplasms. This discovery has led to the search for small molecule inhibitors that target Jak2. Using structure-based virtual screening, our group recently identified a novel small molecule inhibitor of ...
Viola Giampietro - - 2010
In this paper, we have investigated the mechanism of phototoxicity of fluvastatin, an 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, in human keratinocytes cell line NCTC-2544. Fluvastatin underwent rapid photodegradation upon Ultraviolet-A (UVA) irradiation in buffered aqueous solution as shown by the changes in absorption spectra. Interestingly, no isosbestic points were observed ...
Bharate Sandip B - - 2010
The stability, hydrolysis, and uptake of the organophosphates methyl parathion and methyl paraoxon were investigated in SH-SY5Y cells. The stabilities of ((14)CH(3)O)(2)-methyl parathion ((14)C-MPS) and ((14)CH(3)O)(2)-methyl paraoxon ((14)C-MPO) at 1 microM in culture media had similar half-lives of 91.7 and 101.9 h, respectively. However, 100 microM MPO caused >95% cytotoxicity ...
Guin Sunny - - 2011
Hypoxia contributes to acquired drug resistance in various cancer cells. The underlying mechanism is cellular insensitivity regulated by hypoxia-inducible factors (HIF), which impairs drug uptake, transport, and metabolism. The current study determines anti-RON antibody-directed cytotoxicity of doxorubicin (Dox)-immunoliposomes (IL) in hypoxic colon cancer cells. Cells were cultured under hypoxia (1% ...
Aldrich Leslie N - - 2010
Herein we disclose the first total synthesis of tambjamine K and a library of unnatural analogs. Unnatural analogs were shown to be more potent in viability, proliferation, and invasion assays than the natural product in multiple cancer cell lines, with minimal to no cytotoxicity on non-transformed cell lines.
Sharmeen Sumaiya - - 2010
To identify known drugs with previously unrecognized anticancer activity, we compiled and screened a library of such compounds to identify agents cytotoxic to leukemia cells. From these screens, we identified ivermectin, a derivative of avermectin B1 that is licensed for the treatment of the parasitic infections, strongyloidiasis and onchocerciasis, but ...
Tei Lorenzo - - 2010
To design efficient targeting strategies in magnetic resonance (MR) molecular imaging applications, the formation of supramolecular adducts between (strept)avidin ((S)Av) and tribiotinylated Gd-DOTA-monoamide complexes (DOTA=1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid) was explored. Two compounds based on the trivalent core of tris(2-aminoethyl)amine each containing three biotin molecules and one (L1) or three (L2) DOTA-monoamide (DOTAMA) ...
Cui Hui-Fang - - 2010
The unique structures and properties of carbon nanotubes (CNTs) have attracted extensive investigations for many applications, such as those in the field of biomedical materials and devices, biosensors, drug delivery, and tissue engineering. Anticipated large-scale productions for numerous diversified applications of CNTs might adversely affect the environment and human health. ...
Alexandru Oana - - 2011
A major focus of brain cancer research today is to translate understanding of glioma biology into advances in treatment, by exploring the potential of target therapy. Here we investigated the ability of three compounds belonging to the chemical class of azo dyes (methyl red, methyl yellow, and helianthin) to inhibit ...
Harvey Alan L - - 2010
Natural products have been the biggest single source of anticancer drugs and there are continued efforts to explore the chemical diversity provided by nature in order to find new lead compounds. Bioassay test methods have developed into high throughput screening assays using both cell-based and molecular approaches. The various ways ...
Bayet-Robert Mathilde - - 2010
Marine plants and animals are sources of a huge number of pharmacologically active compounds, some of which exhibit antineoplastic activity of clinical relevance. However the mechanism of action of marine natural products (MNPs) is poorly understood. In this study, proton NMR spectroscopy-based metabolomics was applied to unravel biochemical disorders induced ...
Giantomassi Federica - - 2010
Asbestos fibres can be transformed into potentially non-hazardous silicates by high-temperature treatment via complete solid-state transformation. A549 cells were exposed to standard concentrations of raw cement asbestos (RCA), chrysotile and cement asbestos subjected to an industrial process at 1200 degrees C (Cry_1200 and KRY.AS, respectively), raw commercial grey cement (GC). ...
Liu Huachen - - 2010
Natural flavonoids have broad biological activity, including anticancer. In this study, a series of novel flavone derivatives were synthesized with the substitutions of chlorine, isopropyl, methoxy, and nitro groups on the benzene ring of flavone skeleton to develop effective anticancer agents. Antiproliferative assays showed that the synthesized chemicals possess notable ...
Cioce Mario - - 2010
Here we show that a subpopulation of MCF-7 breast cancer cells which stains pale to Toluidine Blue (Light Cells- LCs), is endowed with features of CSCs. LCs give rise to self-renewing mammospheres and express typical CSC markers; moreover this subpopulation is chemoresistant and highly tumorigenic in vivo. LCs can be ...
Destro Federica F BioPharmaNet, Department of Biochemistry and Molecular Biology, University of Ferrara, Ferrara, - - 2010
The rapid increase of the applications for Lab-on-a-chip devices has attracted the interest of researchers and engineers on standard process of the electronics industry for low production costs and large scale development, necessary for disposable applications. The printed circuit board technology could be used for this purpose, in particular for ...
Hondroulis Evangelia - - 2010
A whole cell based biosensor for rapid real-time testing of human and environmental toxicity of nanoscale materials is reported. Recent studies measuring nanoparticle cytotoxicity in vitro provide a final measurement of toxicity to a cell culture overlooking the ongoing cytotoxic effects of the nanoparticles over the desired timeframe. An array ...
Abate-Daga Daniel - - 2010
The suicide system TK/GCV is an enzyme/prodrug therapy that involves the transfer of the cDNA for the herpes simplex virus thymidine kinase gene (TK) into tumor cells which then sensitizes the cells to the non-toxic antiviral drug ganciclovir. Although extensively characterized, the suicide system TK/GCV conceals the details of its ...
Yang Su Hui - - 2010
In the search for potent water-soluble 3-arylisoquinolines, several 3-arylisoquinolinamines were designed and synthesized. Various substituted 3-arylisoquinolinamines exhibited strong cytotoxic activity against eight different human cancer cell lines. In particular, C-6 or C-7 dimethylamino-substituted 3-arylisoquinolinamines displayed stronger potency than the lead compound 7a. Interestingly, compounds 7b and 7c showed more effective ...
Yang Nian-Yun - - 2010
Five diterpenoids and 14 known diterpenoids were isolated from the petroleum ether extract of Pinus massoniana resin. Their structures were elucidated by spectroscopic data interpretation. The cytotoxic activities of these compounds were evaluated using the MTT method. The results showed that three of the less polar diterpenoids had strong cytotoxicity ...
Bocca Claudia - - 2010
It has been shown previously that a novel nitrooxy derivative of celecoxib exerts antiproliferative and pro-apoptotic effects in human colon cancer cells. The aim of this study was to elucidate whether these biological properties depend on COX-2 inhibition and/or NO release. Therefore, the derivative was decomposed into the parent compound ...
Cohen Evan M - - 2010
OBJECTIVE: To encapsulate 5,10,15,20-tetrakis(meso-hydroxyphenyl)porphyrin (mTHPP), a photosensitizer, into polymeric micelles; characterize the micelles; and test in vitro photodynamic therapy efficacy against human head and neck cancer cells. STUDY DESIGN: A nanoparticle design, fabrication, and in vitro testing study. SETTING: Polymer chemistry laboratory. SUBJECTS AND METHODS: Micelles encapsulating mTHPP were produced, ...
Wallenberg Marita - - 2010
The Grx (glutaredoxin) proteins are oxidoreductases with a central function in maintaining the redox balance within the cell. In the present study, we have explored the reactions between selenium compounds and the glutaredoxin system. Selenite, GS-Se-SG (selenodiglutathione) and selenocystine were all shown to be substrates of human Grx1, implying a ...
Contreras René García - - 2010
The use of dental metal alloys in the daily clinic makes it necessary to evaluate the cytotoxicity of eluted metal components against oral cells. However, the cytotoxic mechanism and the type of cell death induced by dental metals in osteoblasts have not been well characterized. This study investigated the cytotoxicity ...
Mollazadeh Samaneh - - 2010
Urinary bladder cancer is one of the most common cancers worldwide. Human transitional cell carcinoma (TCC) cells are epithelial-like adherent cells originally established from a primary bladder carcinoma. Studies have shown that TCC cells are resistant to some chemotherapeutic agents such as vincristine (VCR). In the present study, the effect ...
Kumrit Iyared - - 2010
Seven labdane-type diterpenes, coronarin E, coronarin A, yunnancoronarin A, yunnancoronarin B, hedyforrestin B, villosin, and hedyforrestin C were isolated from the rhizome of Hedychium gardnerianum and evaluated for cytotoxic activity against human small cell lung cancer (NCI-H187) and non-cancerous Vero cells. The results showed that villosin exhibited potent cytotoxic activity ...
Tostmann Alma - - 2010
Despite the important role of pyrazinamide in tuberculosis treatment, little is known about the mechanism of pyrazinamide-induced hepatotoxicity. We inhibited xanthine oxidase in HepG2 cells by using a nontoxic concentration of allopurinol, a well-known xanthine-oxidase inhibitor. This increased in vitro pyrazinamide toxicity in HepG2 cells, which suggests that the hydroxy ...
Habtemariam Solomon - - 2010
The present study examines the comparative cytotoxicity of knipholone (KP) and knipholone anthrone (KA) in leukaemic and melonocyte cancer cell lines. It was found that KA induces a rapid onset of cytotoxicity with IC(50) values ranging from 0.5 to 3.3 μM. In comparison to KA, KP was 70-480-times less toxic ...
Sandes Jana M - - 2010
We have synthesized the Morita-Baylis-Hillman adduct (MBHA) 3-hydroxy-2-methylene-3-(4-nitrophenyl)-propanenitrile (3) in quantitative yield and evaluated on Trypanosoma cruzi epimastigote and bloodstream trypomastigote forms. Compound 3 strongly inhibited epimastigote growth, with IC(50)/72hof 28.5 microM and also caused intense trypomastigotes lysis, with an IC(50)/24h of 25.5 microM. Ultrastructural analysis showed significant morphological changes ...
Miyake Katsunori - - 2010
Twenty-four quassinoids isolated from Eurycoma longifolia Jack were investigated for their cytotoxicity against a panel of four different cancer cell lines, which includes three murine cell lines [colon 26-L5 carcinoma (colon 26-L5), B16-BL6 melanoma (B16-BL6), Lewis lung carcinoma (LLC)] and a human lung A549 adenocarcinoma (A549) cell line. Among the ...
Mahmoodi Majid - - 2010
A new series of 4-aryl-4H-chromenes bearing a 2-arylthiazol-4-yl moiety at the 4-position were prepared as potential cytotoxic agents. The in-vitro cytotoxic activity of the synthesized 4-aryl-4H-chromenes was investigated in comparison with etoposide, a well-known anticancer drug, using MTT colorimetric assay. Among them, the 2-(2-chlorophenyl)thiazol-4-yl analog 4b showed the most potent ...
Vorster Christiaan Jacob Johan - - 2010
A priority in recent anti-cancer drug development has been attaining better side-effect profiles for potential compounds. To produce highly specific cancer therapies it is necessary to understand both the effects of the proposed compound on cancer and on normal cells comprising the rest of the human body. Thus in vitro ...
Rigano Daniela - - 2010
Genista species (family Leguminosae) show interesting biological properties. In this paper we describe the biological activity of the essential oils extracted from the aerial parts of G. sessilifolia DC. and G. tinctoria L. against M14 human melanoma cells, testing several biochemical parameters, such as cell vitality, cell membrane integrity and ...
Ignatova I E - - 2010
Cellular immunity was studied by flow cytometry with Becton Dickinson monoclonal antibodies in clinically healthy Macaca mulatta males before and after low-dose exposure to ionizing radiation. It was shown that T and B cells are radiosensitive, B cells being more sensitive, which is seen from a significant drop of their ...
Kowapradit Jariya - - 2010
The effect of methylated N-(4-N,N-dimethylaminocinnamyl) chitosan (TM-CM-CS) was investigated on paracellular permeability and its toxicity towards Caco-2 cells. Fluorescein isothiocyanate dextran 4,400 (FD-4) was used as the model compound for paracellular transport. The factors, i.e. the degree of quaternization (DQ) and the extent of N-substitution (ES) of the derivatives, were ...
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