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Li Wen-Tai - - 2010
2-Amino-1-arylidenaminoimidazoles, a novel class of orally (po) active microtubule-destabilizing anticancer agents, were synthesized. The compounds were designed from a hit compound identified in a drug discovery platform by using cancer cell-based high throughput screening assay. Selective synthesized compounds exerted cell cytotoxicity against human cancer cells. The underlying mechanisms for the ...
Mazué Frédéric - - 2010
Resveratrol is the subject of intense research because of the abundance of this compound in the human diet and as one of the most valuable natural chemopreventive agents. Further advances require new resveratrol analogs be used to identify the structural determinants of resveratrol for the inhibition potency of cell proliferation ...
Kowapradit Jariya - - 2010
The aim of this study was to investigate the effects of a type of hydrophobic moiety, extent of N-substitution (ES), and degree of quaternization (DQ) of chitosan (CS) on the transepithelial electrical resistance and permeability of Caco-2 cells monolayer, using fluorescein isothiocyanate dextran 4,400 (FD-4) as the model compound for ...
Li Ji - - 2010
Aristolochic acid nephropathy, a progressive tubulointerstitial renal disease, is primarily caused by aristolochic acid I (AA-I) intoxication. Aristololactam I (AL-I), the main metabolite of AA-I, may also participate in the processes that lead to renal damage. To investigate the role and mechanism of the AL-I-mediated cytotoxicity, we determined and compared ...
Murgia Sergio - - 2010
Here, monoolein-based nanoparticles (NPs), obtained through fragmentation of bulk liquid crystalline phases, and stabilized by two different emulsifiers, namely, Pluronic F127 (PF127) and lauroylcholine chloride (LCh), are investigated for structural features and for short-term in vitro cytotoxicity. Depending on the emulsifiers, different morphologies of the lipid NPs (cubosomes and liposomes) ...
Takahashi Yuuka - - 2011
The aim of this study was to evaluate the biological activity and pharmacological activity of several amphiphilic liquid-crystalline compounds (LCs), i.e. phenylpyrimidine derivatives possessing D-glucamine and cyanobiphenyl derivatives with a terminal hydroxyl unit, to explore novel anti-cancer functions of the LCs. The anti-cancer properties of the LCs were investigated in ...
Benites Julio - - 2011
We describe the biological activity of some furylbenzo- and naphthoquinones (furylquinones) on hepatocarcinoma cells and healthy rat liver slices. The effects of furylquinones on cancer cells (Transplantable Liver Tumor, TLT) were assessed by measuring cell death (membrane cell lysis); intracellular contents of ATP and GSH and the activity of caspase-3 ...
Hakimi Osnat - - 2010
Recent years have seen an increased interest in the use of natural and modified silks for tissue engineering. Despite longstanding concerns regarding the biocompatibility of silk sutures, only a few studies have been carried out to investigate the biocompatibility of natural silk fibers. Here, we report an in vitro assessment ...
Yenjai Chavi - - 2010
Flavones 1-4 isolated from Kaempferia parviflora were used for structural modification. Sixteen flavonoid derivatives, including four new derivatives, were synthesized and evaluated for cytotoxicity against KB and NCI-H187 cell lines. Flavanones 2a-4a demonstrated higher cytotoxic activity than the parent compounds. Cytotoxicity against KB cell line of oxime 1c was about ...
Espi?a Bego?a - - 2010
The metabolism of toxins that have accumulated in fish and shellfish is considered a detoxification process, as happens with pectenotoxins (PTXs) in the Japanese scallop Patinopecten yessoensis. PTXs are macrolactones that display hepatotoxicity in mice, principally by capping or sequestering actin, their molecular target. PTX-2, which is considered to be ...
Powell K Leslie - - 2010
Sulfur mustard (bis-(2-chloroethyl)sulfide) is a well-known chemical warfare agent that induces debilitating cutaneous toxicity in exposed individuals. It is also known to be carcinogenic and mutagenic because of its ability to damage DNA via electrophilic attack. We previously showed that a nucleophilic scavenger, 2,6-dithiopurine (DTP), reacts chemically with several electrophilic ...
Appels Natalie M G M - - 2011
AZD3409 is a novel DPTI that has potent activity against both FTase and GGTase-1. The in vitro inhibition profile of AZD3409 was characterized using three different cell lines: mouse embryogenic fibroblasts, transfected with H-Ras(V12) (MEF), A549 cells (Ki4B-Ras mutation) and MCF-7 cells (no Ras mutation). Both cytotoxicity and levels of ...
Popsavin Velimir - - 2010
This paper describes a straightforward divergent synthesis of (+)-goniofufurone mimics (4, 5 and 6) starting from d-xylose. In a preliminary bioassay, analogues 4 and 5 exhibited a submicromolar antiproliferative activity towards HL-60 cells, while the corresponding parent compound 1 was completely inactive against this cell line. At the same time, ...
Rapozzi Valentina - - 2010
This paper describes the synthesis of pi-extended squaraines and their photooxidation properties and gives an in-depth characterization of these molecules as photosensitizing agents. Squaraines show a strong absorption in the tissue transparency window (600-800 nm), and upon irradiation, they undergo a photooxidation process, leading to the formation of peroxide and ...
Burja Bojan - - 2010
A series of pyrazolone-fused combretastatins and precursors were synthesized and their cytotoxicity as well as antitubulin potential was evaluated. The hydrazide 9f and the pyrazolone-fused combretastatins 12a, 12b and 12c were highly cytotoxic against various tumor cell lines including cisplatin resistant cells. The same compounds were also the best inhibitors ...
Wise John Pierce JP - - 2010
In this study we directly compared soluble and particulate chromate cytotoxicity and genotoxicity in human (Homo sapiens) and sea lion (Eumetopias jubatus) lung fibroblasts. Our results show that hexavalent chromium induces increased cell death and chromosome damage in both human and sea lion cells with increasing intracellular chromium ion levels. ...
Hackenberg Stephan - - 2010
Nanomaterials are defined as substances with at least one dimension smaller than 100nm in size and are used for a multitude of purposes. Titanium dioxide nanoparticles (TiO(2)-NPs) are an important material used as an additive in pharmaceutical and cosmetic products. Due to their high surface-to-mass index, TiO(2) nanoparticles show different ...
Johnson George E GE Institute of Life Science, School of Medicine, Swansea University, Singleton Park, Swansea, UK. - - 2010
Sudan-1 and para red are industrial dyes that have been illegally added to some foodstuffs, leading to withdrawal of the adulterated products throughout the UK since 2003. This resulted in international concern that arose because Sudan-1 is classified by International Agency for Research on Cancer as a Category 3 carcinogen. ...
Perchellet Elisabeth M - - 2010
Substituted quinolines (PQ code number), which reduce colony formation and increase gap junctional intercellular communication, were tested for their ability to interact with various molecular targets in murine and human tumor cell lines in vitro. Various markers of tumor cell metabolism, DNA fragmentation, mitotic disruption, apoptosis induction and growth factor ...
Fernández-Herrera María A - - 2010
Certain steroidal compounds have demonstrated an antiproliferative effect against several tumor cell lines; however, their complete role on cancer cells is not currently established. Herein, we report the synthesis and evaluation of two new 26-hydroxy-22-oxocholestanic steroids on cervical cancer CaSki cells. The title compounds were prepared from diosgenin and hecogenin ...
Sharma Sheela - - 2010
Previously, we developed a 30-day transformation assay (focus inhibition, FIA) of rat tracheal epithelial (RTE) cells to identify cancer preventive agents. This study reports nuclear density (ND) as a morphometric biomarker for efficacy evaluation of at an early stage before transformed foci appear. Positive (oltipraz, D-carvone, fumaric acid, and 2-amino-4-methylpyridine ...
Schr?terov? L - - 2010
We characterized the effect of phytic acid (inositol hexaphosphate, IP6) as a potential adjuvant in treatment of colorectal carcinoma and evaluated the optimal concentration and treatment time to produe the maximal therapeutic effect. There is some evidence that myoinositol (Ins) can potentiate anti-cancer effects of IP6. Therefore, we tested both ...
Inoue Sadako - - 2010
N-Glycolylneuraminic acid (Neu5Gc) is the second most populous sialic acid (Sia). The only known biosynthetic pathway of Neu5Gc is the hydroxylation of cytidine-5'-monophosphate-N-acetylneuraminic acid (CMP-Neu5Ac), catalyzed by CMP-Neu5Ac hydroxylase (CMAH). Neu5Gc is abundantly found in mammals except for human, in which CMAH is inactivated due to mutation in the CMAH ...
Asp V - - 2010
Adrenocortical carcinoma (ACC) is a rare malignant disease with poor prognosis. The main pharmacological choice, o,p'-DDD (mitotane), produces severe adverse effects. Since o,p'-DDD is a chiral molecule and stereoisomers frequently possess different pharmacokinetic and/or pharmacodynamic properties, we isolated the two o,p'-DDD enantiomers, (R)-(+)-o,p'-DDD and (S)-(-)-o,p'-DDD, and determined their absolute structures. ...
Bhatia Amit - - 2010
AIM: Tamoxifen is a nonsteroidal estrogen receptor modulator indicated in the treatment of breast cancer. Apoptosis has been reported to be a major mechanism for its antitumor effect. Tamoxifen has also shown significant potential in treating various dermatological disorders including psoriasis, characterized by hyperproliferation of epidermal keratinocytes. An endeavor was ...
Chung Ill-Min - - 2010
The methanolic extract of the rhizomes parts of Agelica purpuraefolia was investigated for its activity against chloroquine-sensitive strains of Plasmodium falciparum using the parasite lactate dehydrogenase assay method. Two natural khellactone, (+)-4'-Decanoyl-cis-khellactone (1) and (+)-3'-Decanoyl-cis-khellactone (2) were isolated from the rhizomes parts of A. purpuraefolia. Two compounds were evaluated for ...
Clemente Alfonso - - 2010
Bowman-Birk inhibitors (BBI) from soybean and related proteins are naturally occurring protease inhibitors with potential health-promoting properties within the gastrointestinal tract. In this work, we have investigated the effects of soybean BBI proteins on HT29 colon adenocarcinoma cells, compared with non-malignant colonic fibroblast CCD-18Co cells. Two major soybean isoinhibitors, IBB1 ...
Yen Chiao-Ting - - 2010
The synthesis and cytotoxic evaluation of a series of Fmoc-based dipeptides are described. Among the thirty compounds, 4a, 8a, 12a, 2b, 4b, 10b, 3c, 4c and 6c showed potent activity against HepG2, Hep3B, MCF-7, MDA-MB-231, A549 and Ca9-22 human cancer cell lines. The most active compounds (10a and 10c) showed ...
Midura-Nowaczek Krystyna - - 2010
The effect of H-EACA-L-Cys(S-Bzl)-OH, H-EACA-L-Leu-OH, H-EACA-L-Nle-OH and EACA on the viability of MCF-7 and fibroblast cells was examined. The antibacterial activity of these compounds was also tested. H-EACA-L-Leu-OH and H-EACA-L-Nle-OH showed cytotoxic activity against MCF-7 and fibroblast cell lines, particularly in the highest studied 20 mM concentration. None of the ...
Du Lin - - 2010
Four new alkaloids, including two new meleagrin analogs, meleagrin D (1) and E (2), and two new diketopiperazines, roquefortine H (3) and I (4), were isolated from a deep ocean sediment-derived fungus Penicillium sp. Meleagrin D (1) and E (2) possess unprecedented acetate-mevalonate-derived side chains on the imidazole moiety. These ...
Pan Li - - 2010
Cytotoxicity-guided fractionation of a methanol extract of the leaves and twigs of Rolandra fruticosa using the HT-29 human colon cancer cell line led to the isolation of seven sesquiterpene lactones, including the hitherto unknown isorolandrolide, 13-methoxyisorolandrolide (1), and bourbonenolide, 2alpha,13-diacetoxy-4alpha-hydroxy-8alpha-isobutyroyloxybourbonen-12,6alpha-olide (2), as well as five known compounds, 13-acetoxyrolandrolide (3), 8-desacyl-13-acetoxyrolandrolide-8-O-tiglate ...
Issa Samar - - 2010
The synthesis, structure elucidation and antitumoral activity of novel heterocyclic compounds containing a carbazole nucleus are reported. Oxazinocarbazoles were synthesized by application of the Mannich reaction to the corresponding hydroxylated derivatives leading to 41 new molecules. Their cytotoxic activity was evaluated against various human tumor cell lines including three leukemic ...
Ding Lan - - 2011
Four xanthones were isolated from Gentianopsis paludosa Ma and were identified by modern spectroscopic methods. Cytotoxicity of the four xanthones was tested on HepG2 cells and HL-60 cells by sulphorhodamine B (SRB) assay. Clonogenic survival assay, trypan blue exclusion method, AO/EB staining and DNA fragmentation assay were conducted to investigate ...
Yosifov Deyan Y - - 2011
Erufosine is an i.v. injectable alkylphosphocholine which is active against various haematological malignancies in vitro. In the present study, its effects on multiple myeloma (MM) cell lines and on murine and human hematopoietic progenitor cells (HPCs) were investigated. The following MM cell lines were used: RPMI-8226, U-266 and OPM-2. The ...
El-Deeb Ibrahim M - - 2010
Novel derivatives of 5-(substituted)benzylidene-3-(4-substituted)phenylsulfonylimidazolidine-2,4-diones (3a-r), 1-(4-substituted)phenylsulfonyl-3-(4-substituted)phenylpyrimidine-2,4,6-(1H,3H,5H)-triones (6a-l), and 3-(4-substituted)phenyl-1-(4-substituted)phenylsulfonylquinazoline-2,4(1H,3H)- diones (8a-l) have been synthesized and tested for their antitumor activity against 60 tumor cell lines taken from 9 different organs. The tested compounds have showed good inhibitory effect at the ovarian cancer (IGROV1) cell line. A significant inhibition for (RXF393) ...
LaCerte Carolyne - - 2010
Depleted uranium (DU) is commonly used in military applications and consequently exposure to soldiers and non-combatants is potentially frequent and widespread. DU is suspected to be a carcinogen, potentially affecting the bronchial cells of the lung. Few studies have considered DU in human bronchial cells. Accordingly, we determined the cytotoxicity ...
Hu Xiaoke - - 2010
In this study, we used a systematic approach to study and compare the in vitro cytotoxicity of selected engineered carbon nanotubes (CNTs) to test cell lines including human skin keratinocytes, lung cells and lymphocytes. Results of fluorescein diacetate (FDA) uptake in T4 lymphocyte A3 cells indicated cytotoxicity caused by single-walled ...
Ko Jen-Chung - - 2010
Emodin, a tyrosine kinase inhibitor, is a natural anthraquinone derivative found in the roots and rhizomes of numerous plants. Emodin exhibits anticancer effects against a variety of cancer cells, including lung cancer cells. ERCC1 and Rad51 proteins are essential for nucleotide excision repair and homologous recombination, respectively. Furthermore, ERCC1 and ...
Jin Shiwei - - 2010
Recently, the environmental residues of polybrominated diphenyl ethers (PBDEs) have markedly increased. In particular, the levels of certain PBDE congeners in fish have raised concern regarding potential risks associated with dietary PBDEs exposures. However, little is known regarding PBDE-mediated cell injury in relevant in vitro fish cell models. In this ...
Tu Huang-Yao - - 2010
A series of novel 2',5'-dimethoxylchalcone derivatives including 18 new compounds were synthesized and evaluated for cytotoxicities against two human cancer cell lines, NTUB1 (human bladder cancer cell line) and PC3 (human prostate cancer cell line). All these derivatives except for 21 exhibited significant cytotoxic effect against NTUB1 and PC3 cell ...
Yang Xinmei - - 2010
Ethacrynic acid (EA) is a glutathione S-transferase P1-1 (GST P1-1) inhibitor with weak antiproliferative ability in tumor cells. By use of the principle of bioisosterism, a series of novel EA oxadiazole analogues were designed and synthesized. The structure-activity relationships of inhibiting GST P1-1 activity and cell proliferation of those EA ...
Kumar Ravi - - 2010
A series of tetrahydro-beta-carbolines and 1,3,5-triazine hybrids have been synthesized and evaluated for their cytotoxicity against a panel of eight human cancer cell lines and normal human fibroblasts (NIH3T3). It led us to discovery of racemic compounds 69, 71 and 75, which are selectively cytotoxic towards KB (oral cancer) cell ...
Zakharova Ol'ga D - - 2010
Fluorinated derivatives of 1,4-naphthoquinone are highly potent inhibitors of Cdc25A and Cdc25 phosphatases and growth of tumor cells. Five new N-substituted polyfluorinated derivatives of 2-amino-1,4-naphthoquinone were synthesized and their mutagenic and antioxidant properties in Salmonella cells, as well as cytotoxicity in human myeloma (RPMI 8226), human mammary adenocarcinoma (MCF-7), mouse ...
Mercey Emilie - - 2010
We report the fabrication of a 3D micropatterned agarose substrate that enables the culture of single or multiple cells. Patterning was performed on dried agarose using deep UV irradiation leading to 6-microm-deep micropatterns of 25-70 microm in diameter. Cell adhesion was facilitated by the specific grafting of ECM (extra cellular ...
Kirkland David - - 2010
This paper summarises the data for 14 different chemicals tested for induction of micronuclei (MN) in 5 different cell types across 12 different laboratories. All 14 chemicals induced biologically and statistically significant increases in MN frequency in the different cell types (L5178Y, TK6, CHO, CHL, V79) in the absence of ...
Carlson Coby B - - 2010
The authors recently reported the development and application of multiple LanthaScreen cellular assays to interrogate specific steps within the PI3K/Akt pathway. The importance of this signaling cascade in regulating fundamental aspects of cell growth and survival, as well as in the progression of cancer, underscores the need for portable cell-based ...
Parimi Srinivas - - 2010
We report on the role of PAMAM dendrimer concentration and generation (G2, G4, G6) on cell growth and cytotoxicity in HEK293T and HeLa cell lines and make comparisons with dendrimer-induced leakage from liposomes to probe the mechanisms in action. Specifically, we observed a striking transition from cell growth enhancement to ...
Pissuwan Dakrong - - 2010
The RAFT technique has been increasingly used to generate polymers for potential biological applications. However, to-date, the toxicity of the RAFT-polymers has received limited attention. In this study, the in vitro cytotoxicity of three different, RAFT-synthesized, water-soluble polymers was investigated using three different adherent cell lines via CellTiter-Blue cell viability ...
Sun Min - - 2010
Two series of novel diaryl ureas have been designed and synthesized, with their in vitro antitumor effect screened on human non-small cell lung cancer (NSCLC) cell line A549 and human breast cancer cell line MDA-MB-231. Some target compounds demonstrated significant inhibitory activities against both cell lines. Compared to contrast drug ...
Wang Pan - - 2010
The cytotoxic effect of protoporphyrin IX disodium salt (PPIX) on isolated Ehrlich ascetic tumor (EAT) cells induced by ultrasound exposure was investigated. Tumor cells suspended in air-saturated phosphate buffer solution (PBS, pH 7.2) were exposed to ultrasound at 2.2MHz for up to 60 s in the presence and absence of ...
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