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Quadros Edward V - - 2010
Cellular uptake of cobalamin (Cbl) occurs by endocytosis of transcobalamin saturated with Cbl by the transcobalamin receptor (TCblR/CD320). The cell cycle-associated overexpression of this receptor in many cancer cells provides a suitable target for delivering chemotherapeutic drugs and cytotoxic molecules to these cells while minimizing the effect on the normal ...
Movia Dania - - 2010
The in vitro toxic response of spiropyrans in cellular models has not been previously addressed, despite the fact that such photoswitchable molecules have shown great potential as versatile and tunable components for bionanodevices and imaging agents. In this study, we examine the cytotoxic effects of a spiropyran, namely, 8-methoxy-6-nitro-BIPS (1',3'-dihydro-1'-ethanol-3',3'-dimethyl-8-methoxy-6-nitro-spiro(2H-1-benzopyran-2,2'-(2H)-indole) ...
Bourthoumieu S - - 2010
It is important to determine the possible effects of exposure to radiofrequency (RF) radiation on the genetic material of cells since damage to the DNA of somatic cells may be linked to cancer development or cell death and damage to germ cells may lead to genetic damage in next and ...
Fiori Jessica - - 2011
Guaiazulene (GA) is widely used as a natural ingredient in many health care products and solutions. Although it has been reported to have interesting biological effects, GA and azulene derivatives have been proven to be cytotoxic against normal human cells and human tumor cells; moreover, guaiazulene has shown photomutagenic properties ...
Pilloni Martina - - 2010
High energy ball milling (HEBM) has been used for the first time to prepare PEGylated magnetite-silica (Fe(3)O(4)-SiO(2)) nanocomposites intended to be used for biological purposes. Surface amine groups were introduced by a silanization reaction involving 3-aminopropyl triethoxysilane (APTS) followed by PEGylation to yield long-term stable and stealth nanocomposites of 200nm ...
Backorová M - - 2011
One of the ways for searching for potentially new anti-cancer drugs is the testing of various naturally synthesized compounds. Lichens are a source of unique chemical agents of which some have already been proved to be effective against various cancer in vitro models. Our study reports on the sensitivity of ...
Lessa Josane A - - 2010
2-acetylpyridine N(4)-phenyl thiosemicarbazone (H2Ac4Ph), and its N(4)-ortho-tolyl (H2Ac4oT), N(4)-meta-tolyl (H2Ac4mT), N(4)-para-tolyl (H2Ac4pT), N(4)-ortho-chlorophenyl (H2Ac4oClPh), N(4)-meta-chlorophenyl (H2Ac4mClPh) and N(4)-para-chlorophenyl (H2Ac4pClPh) derivatives were assayed for their cytotoxicity against RT2 (expressing p53 protein) and against T98 (expressing mutant p53 protein) glioma cells. The compounds were highly cytotoxic against RT2 (IC50=24-1.4 nM) and T98 ...
Rakotonandrasana Olga L - - 2010
In a screening program directed to the discovery of new anticancer agents from Madagascan plants, ethyl acetate extracts of Croton barorum and C. goudotii showed strong cytotoxic activity, with 100% inhibition at 10 μg/mL in a primary screen using the murine lymphocytic leukemia P388 cell line. Bioassay-guided fractionation led to ...
Queiroz Maria-João R P - - 2010
A wide variety of new bi(hetero)aryl derivatives of the thieno[3,2-b]pyridine skeleton was obtained in high to excellent yields (65-91%) by Suzuki-Miyaura cross-coupling of the methyl 3-amino-6-bromothieno[3,2-b]pyridine-2-carboxylate, recently reported by us, with aryl or heteroaryl pinacolboranes or potassium trifluoroborates. The coupling products obtained were evaluated for their growth inhibitory effect on ...
Clark Cheryl A - - 2010
Curcumin appears to be a safe, bioactive food compound that is a potential chemopreventive for patients at a high risk for head and neck squamous cell carcinoma (HNSCC). Identification and validation of intermediate endpoints is an important step in evaluating chemopreventive agents. AKT/MTOR pathway biomarkers are intrinsic to the carcinogenic ...
Lai Yisheng - - 2010
A series of novel furoxan-based nitric oxide (NO)-releasing derivatives of glycyrrhetinic acid (GA) were designed, synthesized, and evaluated for their in vitro cytotoxicity against human hepatocellular carcinoma (HCC) and non-tumor liver cells. Five furoxan/GA hybrids, 7b-d, 7f, and 7g, displayed potent cytotoxicity against HCC cells (IC(50): 0.25-1.10 μM against BEL-7402 ...
Das Swagatika - - 2010
The concept of sequential cytotoxicity, which states that successive chemical attacks on cellular constituents can be more deleterious to neoplasms than normal cells, was evaluated using a series of 3,5-bis(benzylidene)-1-diethylphosphono-4-oxopiperidines 1 and related phosphonic acids 2, which were screened against a panel of malignant and normal cell lines. The compounds ...
Kalam Yasmean - - 2011
Acanthophis genus (i.e. death adders) and the Naja genus (i.e. cobras) belong to the family elapidae. The current study compared the in vitro cytotoxicity of venoms from four Acanthophis spp. and three Naja spp. on rat aortic smooth muscle cells, A7r5, and rat skeletal muscle cells, L6. The ability of ...
Siddiqui Akhtar A Department of Basic Pharmaceutical Sciences, College of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209-0497, United - - 2010
In this study, solid lipid nanoparticles (SLN) loaded with MBO-asGCS oligonucleotide were prepared, characterized and evaluated for cytotoxicity against NCI/ADR-RES human ovary cancer cells. Two types of cetyltrimethyl ammonium bromide (CTAB) stabilized SLN, with or without ceramide VI, were prepared by mixed homogenization/ultrasonication technique. Complexes were characterized for size, zeta-potential, ...
Sun Haiying - - 2010
A series of compounds were designed and synthesized as antagonists of cIAP-1/2 and XIAP based upon our previously identified lead compound SM-122 (1). The most potent of these (7) binds to XIAP, cIAP-1, and cIAP-2 proteins with K(i) values of 36, <1, and <1.9 nM, respectively. Consistent with its potent ...
Zheng Yunquan - - 2010
Six pigments were separated from Monascus product, and some derivatives were chemically synthesized. The cytotoxicity of different Monascus pigments to various human cancer cells (SH-SY5Y, HepG2, HT-29, BGC-823, AGS, and MKN45) was evaluated. Rubropunctatin showed the greatest anticancer effect within the tested compounds. The inhibition effect of rubropunctatin was higher ...
Cappella Paolo - - 2010
Analysis of cell cycle progression by 5-bromo-2'-deoxyuridine (BrdU) incorporation is commonly used for evaluating the mode of action of anticancer drugs, but usually requires a high number of cells and large amounts of monoclonal antibodies. In addition, manual sample handling is not suitable for high throughput. To circumvent these limitations, ...
Ostacolo Luisanna - - 2010
In this paper we have investigated the behavior of core-shell poly(ethylene oxide)-poly(epsilon-caprolactone) (PEO-PCL) micelles derived from copolymers with linear triblock (TR) and 4-arm star-diblock (ST) architectures for the delivery of docetaxel (DTX). DTX was loaded inside micelles (DTX-TR(m) and DTX-ST(m)) with high efficiency and released slowly for more than two ...
Unlu Mehmet - - 2010
The essential oil from the bark of Cinnamomum zeylanicum Blume was analyzed by GC-MS and bioassays were carried out. Nine constituents representing 99.24% of the oil were identified by GC-MS. The major compounds in the oil were (E)-cinnamaldehyde (68.95%), benzaldehyde (9.94%) and (E)-cinnamyl acetate (7.44%). The antimicrobial activity of the ...
Andres-Hernando Ana - - 2010
Chronic analgesic abuse has been shown to induce severe renal injury characterized by renal papillary necrosis (RPN), an injury detectable at late stage. While direct toxicity of the drug may exist, the molecular mechanisms underlying analgesics induction of RPN remain unknown. A major limitation to study the pathogenesis of RPN ...
Rudolf R - - 2012
The aim of this work was to study the cytotoxicity of different fractions of gold nanoparticles prepared by ultrasonic spray pyrolysis from gold scrap. The target cells were rat thymocytes, as a type of nonproliferating cells, and L929 mouse fibroblasts, as a type of continuous proliferating cells. Fractions 1 and ...
Zhang Ting - - 2010
Two new eudesmane-type sesquiterpene lactones were isolated from the roots of Inula racemosa and their structures were elucidated as 3β-hydroxy-11α,13-dihydroalantolactone (1) and 11α-hydroxy-eudesm-5-en-8β,12-olide (2). Their cytotoxic activities against five human cancer cell lines had been tested and compound 2 exhibited weak cytotoxic activity against BEL-7402 and HCT-8 cell lines. The ...
Aranha Andreza Maria Fábio - - 2010
This in vitro study evaluated the cytotoxicity of an experimental restorative composite resin subjected to different light-curing regimens. Forty round-shaped specimens were prepared and randomly assigned to four experimental groups (n=10), as follows: in Group 1, no light-curing; in Groups 2, 3 and 4, the composite resin specimens were light-cured ...
Male Keith B - - 2010
In an effort to develop a noninvasive method for assessment of cyanobacterial toxins in drinking water, plausible cytotoxicity/inhibition of microcystin-LR and cylindrospermopsin was evaluated by cell-substrate impedance sensing (ECIS) using three different cell lines. Sf9 insect cells were attached to concanavalin A coated gold electrodes, whereas Chinese hamster ovary (CHO) ...
Van der Heggen Maarten - - 2010
The effect of Pb on Saccharomyces cerevisiae cell structure and function was examined. Membrane integrity was assessed by the release of UV-absorbing compounds and by the intracellular K(+) efflux. No leakage of UV(260)-absorbing compounds or loss of K(+) were observed in Pb (until 1,000 μmol/l) treated cells up to 30 ...
Pedrini Fernanda Spezia - - 2010
New compounds with biological targets and less cytotoxicity to normal cells are necessary for cancer therapy. In this work ten synthetic chalcones derived from 2-naphtaldehyde were evaluated for their cytotoxic effect in murine acute lymphoblastic leukemia cells L-1210. A series of ten chalcones derived from 2-naphtaldehyde and corresponding acetophenones were ...
Liu Wei - - 2010
This work investigated the cytotoxicities of three silver nanoparticles (SNPs) SNP-5, SNP-20 and SNP-50 with different sizes ( approximately 5 nm, approximately 20 nm and approximately 50 nm) using four human cell models (A549, SGC-7901, HepG2 and MCF-7). Endpoints included cell morphology, cell viability, cellular membrane integrity, oxidative stress and ...
Rabolli Virginie - - 2010
Identifying the physico-chemical characteristics of nanoparticles (NPs) that drive their toxic activity is the key to conducting hazard assessment and guiding the design of safer nanomaterials. Here we used a set of 17 stable suspensions of monodisperse amorphous silica nanoparticles (SNPs) with selected variations in size (diameter, 2-335 nm), surface ...
Pati Hari N - - 2010
A series of 1,3-diaryl-2-propenones 2a-j and analogous 2-benzylidene-1,3-indandiones 3a-j were evaluated against various neoplasms and normal cells. In general, greater cytotoxic potencies and selective toxicity to human malignant cells were observed by the compounds in series 2 rather than 3. In particular, 2i emerged as a lead molecule having an ...
Shin Hye Kyung - - 2010
Colorectal cancer (CRC) is one of the commonest malignant disorders and frequently associated with high expression of epidermal growth factor receptor (EGFR), resulting in advanced disease and a poor prognosis. In this study, we investigated the radiosensitizing effects of the selective EGFR inhibitor cetuximab in human CRC cell lines. Four ...
Cvikl B - - 2011
To investigate whether zoledronate (ZOL) can cause a cytotoxic response in dental pulp-derived cells (DPCs) in vitro. Cell activity was assessed utilizing MTT tests, (3) [H]thymidine, and (3) [H]leucine incorporation assays in human DPCs in response to ZOL. Cell activity assays were also preformed on calcium phosphate-coated plates. Cell death ...
Toyama Takashi - - 2010
We examined the contribution of carbon monoxide (CO), an enzymatic product of heme oxygenase (HO), to methylmercury (MeHg) cytotoxicity in SH-SY5Y cells, because this gas molecule is reported to activate Nrf2, which plays a protective role against MeHg-mediated cell damage. Exposure of SH-SY5Y cells to CO gas resulted in protection ...
Gehring Sonja - - 2011
Statins are inhibitors of the cholesterol synthesis pathway with pleiotropic effects, while thiazolidinediones (TDZ) are peroxisomal proliferator activator receptor γ (PPAR-γ) agonists with potent proapoptotic activity. For both groups of substances a cytotoxic effect against several human tumors is presumed. Direct comparison of several statins and TDZ has not been ...
Hirano Seishiro - - 2010
Carbon nanotubes (CNT) are cytotoxic to several cell types. However, the mechanism of CNT toxicity has not been fully studied, and dosimetric analyses of CNT in the cell culture system are lacking. Here, we describe a novel, high throughput method to measure cellular uptake of CNT using turbimetry. BEAS-2B, a ...
Hashimoto Kiyohiro - - 2011
In the OECD Guideline 487, a total of four extended exposure treatment conditions are proposed for the in vitro micronucleus (MNvit) assay in the presence and absence of a cytokinesis block and with or without a recovery period. This guideline also states that rodent cell lines and human lymphocytes can ...
Yang Su Hui - - 2010
Various substituted 3-aryl-1-isoquinolinamines were designed and synthesized based on the previously constructed CoMFA model. Most of the synthesized compounds showed excellent potency in eight different human tumor cell lines as expected. In order to find the exact cytotoxic mechanism of these 3-aryl-1-isoquinolinamines, we analyzed the cell cycle dynamics by flow ...
da Silva Bruna Polacchine - - 2010
Leishmaniasis is one of the major infectious diseases affecting the poorest regions of the world. The present study evaluated the antileishmanial activity of a guaianolide purified from the hydroalcoholic extract of aerial parts of Tanacetum parthenium (L.) Schultz Bip. The isolated compound showed activity against the promastigote form of Leishmania ...
Hasima Noor - - 2010
Medicinal plants containing active natural compounds have been used as an alternative treatment for cancer patients in many parts of the world especially in Asia (Itharat et al. 2004). In this report, we describe the cytotoxic and apoptotic properties of 1'S-1'-acetoxyeugenol acetate (AEA), an analogue of 1'S-1'-acetoxychavicol acetate (ACA), isolated ...
Zeng Xiu-Xiu - - 2010
Novel thienopyridine derivatives 1b-1r were synthesized, based on a hit compound 1a that was found in a previous cell-based screening of anticancer drugs. Compounds 1a-1r have the following features: (1) their anticancer activity in vitro was first reported by our group. (2) The most potent analog 1g possesses hepatocellular carcinoma ...
Gerashchenko Bogdan I - - 2010
Radiosensitization of mammalian cells by heat is believed to involve the inhibition of repair of DNA double-strand breaks (DSBs). The Mre11 complex (composed of Mre11, Rad50, and Nbs1) is involved in DSB repair and forms foci at sites of radiation-induced DSBs. Heat induces the translocation of a significant amount of ...
Lam Rosanna Y Y - - 2010
To investigate the efficacy of traditional Chinese medicine (TCM) in the treatment of hyperpigmentation problems, extracts of herbs selected based on traditional Chinese medical literature were screened. Forty extracts were extracted from 10 selected herbs using hexane, dichloromethane, methanol and water. They were then screened using melan-a cells, an immortalized ...
Richter Patricia A - - 2010
Cytotoxic properties of tobacco smoke are associated with chronic tobacco-related diseases. The cytotoxicity of tobacco smoke can be tested with short-term predictive assays. In this study, we compare eight mainstream cigarette smoke condensates (CSCs) from commercial and experimental cigarettes in three different cytotoxicity assays with unique and overlapping endpoints. The ...
Yan Ye - - 2011
The aims of this study were to isolate sesquiterpene compounds from the largehead atractylodes rhizome (LAR) and to investigate their effects on B16 cancer cells. A total of 8 sesquiterpenes from LAR were identified, of which eudesm-4 (15), 7-diene-9α, 11-diol (7) was isolated for the first time. All 8 compounds ...
Nestor Marika - - 2011
The monoclonal antibody cetuximab, targeting the epidermal growth factor receptor (EGFR), is a promising molecular targeting agent to be used in combination with radiation for anticancer therapy. In this study, effects of cetuximab in combination with alpha-emitting radioimmunotherapy (RIT) in a panel of cultured human squamous cell carcinomas (SCCs) were ...
Wada Koji - - 2011
The cytotoxicity of three alkaloids from the roots of Aconitum yesoense var. macroyesoense as well as 36 semi-synthetic C(20)-diterpenoid atisine-type alkaloid derivatives against A549 human lung carcinoma cells was examined. Ten acylated alkaloid derivatives, pseudokobusine 11-veratroate (9), 11-anisoate (12), 6,11-dianisoate (14), 11-p-nitrobenzoate (18), 11,15-di-p-nitrobenzoate (22), 11-cinnamate (25) and 11-m-trifluoromethylbenzoate (27), ...
Bae Won-Jung - - 2010
The aim of this study was to investigate the cellular effects of newly developed calcium phosphate-based sealers (CAPSEAL I and II) using cultured human periodontal ligament cells (HPDLCs) compared with epoxy resin sealer (AH26; Dentsply, DeTrey, Konstanz, Germany), zinc oxide eugenol [ZOE] sealer (extended working time [EWT]; Kerr Corporation, Orange, ...
Feliu Lidia - - 2010
Antimicrobial peptides have been considered as potential candidates for cancer therapy. We report here the cytotoxicity of a library of 66 antibacterial cyclodecapeptides on human carcinoma cell lines, and their effects on apoptosis [as assessed by cleavage of poly(ADP-ribose) polymerase (PARP)] and cell signaling proteins (p53 and ERK1/2) in cultured ...
Yoon Il Sang - - 2010
Parkinson's disease (PD) is a neurodegenerative disease featured by selective loss of substantia nigra neurons. Rotenone administration in animals induces neurodegeneration accompanied by α-synuclein-positive Lewy body-like inclusions, recapturing typical histopathological features of PD. In an effort to screen for small-molecule agents to reverse rotenone-induced cytotoxicity, we developed and validated a ...
Zhao Yu - - 2012
A novel series of 4β-[(4-substituted) aroylthiourea] derivatives of podophyllotoxin were synthesized and their abilities to inhibit the growth of cancer cells were investigated by MTT assay. Compound 4a possessed the highest cytotoxicity on HepG2, A549 and HCT-116 cancer cell lines with the IC(50) values of 0.1 μM. Apoptosis in HCT-116 cells ...
Xiong Xiang Yuan - - 2012
In order to prepare targeted drug carriers, previously a biotin group has been attached by our group to the end of Pluronic F87/poly(lactic acid) and Pluronic P85/poly(lactic acid) block co-polymers to obtain B-F87-PLA and B-P85-PLA, respectively. In this paper, the active targeting properties of B-F87-PLA and B-P85-PLA nanoparticles in vitro ...
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