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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 LN Department of Chemistry, Vanderbilt University, Nashville, TN 37232, - - 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 ...
Shokrzadeh M - - 2010
Plants are used worldwide for the treatment of diseases, and novel drugs continue to be developed through research from plants. There are more than 20,000 species of plants used in traditional medicines, and these are all potential reservoirs for new drugs. Cucurbitapepo has been used in traditional folk medicine to ...
Lima Adriano Fonseca - - 2010
To evaluate the cytotoxic effects of a bleaching agent composed of 0.01% carbamide peroxide (CP; 2.21mug/ml H(2)O(2)) on the MDPC-23 odontoblastic cell line, and to determine whether sodium ascorbate (SA) is capable of reducing, or even eliminating, the toxic effects caused by this bleaching agent. The cells were seeded in ...
de Lima Aliny Pereira - - 2010
Ruthenium(III) complexes are increasingly attracting the interest of researchers due to their promising pharmacological properties. In the present study, we investigated the ability of cis-(dichloro)tetrammineruthenium(III) chloride to produce lethal effects in human chronic myelogenous leukemia K562 cells. The MTT tetrazolium reduction test and the trypan blue exclusion assay revealed that ...
Su Quan-Guan - - 2011
To explore the potential anti-tumour activities of xanthone derivatives, 26 hydroxylxanthones and benzoxanthones and their structurally modified analogues were examined for potential cytotoxic activities against eight human cancer cell lines. Most of the xanthone derivatives exhibited a higher degree of cytotoxicity on HepG2 cells than on the other seven cancer ...
Schwanke Anja - - 2010
Aiming to address new drug targets, molecular modelling is gaining increasing importance although the prediction capability of the in silico method is still under debate. For an improved treatment of actinic keratosis and squamous cell carcinoma, inhibitors of human DNA polymerase alpha (pol alpha) are developed by docking nucleoside phosphonate ...
Gianferrara Teresa - - 2010
We report here two novel "extended-arms" porphyrins, TetbpyPP and TedabpyPP, in which four peripheral bpy fragments are connected to the meso positions of the macrocycle through flexible linkers of different length and hydrophilicity. We describe also the new, water-soluble, tetracationic conjugate [TedabpyPP{Ru([9]aneS3)Cl}(4)][Cl](4) (6). Compound 6 belongs to the series of ...
Naha Pratap C - - 2010
PNIPAM nanoparticles, with and without a covalently linked fluorescent label, were prepared by a free radical polymerisation technique. The cyto- and genotoxicity of PNIPAM nanoparticles were analysed in two representative mammalian cell lines, SW480, a colon, and HaCaT, a dermal cell line. Physical characterisation in terms of particle size and ...
Vasconcellos Marne C - - 2010
Biflorin is a natural quinone isolated from Capraria biflora L. Previous studies demonstrated that biflorin inhibits in vitro and in vivo tumor cell growth and presents potent antioxidant activity. In this paper, we report concentration-dependent cytotoxic, genotoxic, antimutagenic, and protective effects of biflorin on Salmonella tiphymurium, yeast Saccharomyces cerevisiae, and ...
Padavan Donna T - - 2011
Poly(amic acid) (PAA) derived from ethylenediaminetetracetic dianhydride shows great potential as a biomaterial suitable for biomedical applications. To evaluate this polymer class further, in vitro cell toxicity (WST-1/ECS, ELISA based) and cell compatibility (cell adhesion and cell proliferation) tests were conducted to establish structure-toxicity relationships. PAAs with a number-average molecular ...
Sun Lingmei - - 2011
The aim of this study was to demonstrate that solamargine (SM) mediates its cytotoxicity via oncosis. The cytotoxicity of SM on cancer cells was examined by 3-(4,5-dimethylthiazol)-2 and 5-diphenyltetrazolium bromide assay. Cell membrane integrity was assessed by detecting the leakage of cytoplasmic content, the release of lactate dehydrogenase (LDH), and ...
Bandgar Babasaheb P - - 2010
In the present article, we have synthesized a combinatorial library of 3,5-diaryl pyrazole derivatives using 8-(2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-5,7-dimethoxy-2-phenyl-4H-chromen-4-one (1) and hydrazine hydrate in absolute ethyl alcohol under the refluxed conditions. The structures of the compounds were established by IR, (1)H NMR and mass spectral analysis. All the synthesized compounds were evaluated for ...
El-Azab Adel S - - 2010
Novel derivatives of quinazoline (1-27) have been synthesized and tested for their antitumor activity against three tumor cell lines among these cell lines the human breast carcinoma cell line (MCF-7) in which EGFR is highly expressed. All tested compounds showed potent and selective activity against breast cancer (MCF-7) with IC(50) ...
Zuo Ai-Xue - - 2010
Three new phenolic glycosides, curculigosides F-H (1-3), were isolated from rhizomes of Curculigo orchioides Gaertn. Their structures were elucidated based on comprehensive spectroscopic analyses including IR, MS, 1D- and 2D NMR (HSQC, COSY, and HMBC). Curculigosides F-H (1-3) were evaluated for their anti-HBV activity in vitro using the HBV transfected ...
Kim Ki Hyun - - 2010
Chemical investigation of the tubers of Corydalis ternata resulted in the isolation and characterization of four new benzylisoquinoline alkaloids, epi-coryximine (1) and coryternatines A-C (2-4), along with 10 known alkaloids (5-14). Their structures were established on the basis of extensive spectroscopic data analyses and comparison with spectroscopic data reported. In ...
Llanos Gabriel G - - 2010
Seven new withanolides (1-7), along with three known ones (8-10), were isolated from the leaves of Withania aristata. Their structures were elucidated on the basis of spectroscopic analysis, including 2D NMR experiments and spectrometric techniques, and the absolute configuration of 1 and 2 was established by CD analysis. In the ...
Xiao Qin - - 2011
A cell line (FG cells) derived from a gill of the flounder, Paralichthys olivaceus were used to determine the cytotoxic effects of nonylphenol (NP). Cytotoxicity was measured by three endpoint systems: neutral red (NR) uptake assay, methyl thiazolyl tetrazolium (MTT) assay and cell protein assay. The result showed that NP ...
Moretto Johnny - - 2011
Platinum(II) metallointercalators represent a new class of DNA-damaging antitumor complexes active in cisplatin- and oxaliplatin-resistant cell lines. In the first part of our work, we have screened in vitro a serie of 18 metallointercalators with the structure [Pt(A(L))(I(L))](2+) where A(L) = ethylenediamine (EN) or diaminocyclohexane in R,R- (RR) or S,S- (SS) configuration ...
Penthala Narsimha Reddy - - 2010
A series of novel 3-hydroxy-3-(2-imino-3-methyl-5-oxoimidazolidin-4-yl)indolin-2-one analogs (3) have been synthesized under microwave irradiation and conventional heating methods. These analogs were evaluated for in vitro cytotoxicity against a panel of 57 human tumor cell lines. Compound 3o had GI(50) values of 190 nM and 750 nM against A549/ATTC non-small cell lung ...
Budman Daniel R - - 2011
Although platinum based therapy has improved short term survival of patients with metastatic ovarian cancer, the majority of patients continue to relapse and eventually die of their disease. Currently, a plethora of agents are in development, but how to combine them to enhance efficacy remains largely empiric. We have used ...
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