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https://www.readbyqxmd.com/read/28324785/-ub006-a-new-fatty-acid-synthase-inhibitor-and-cytotoxic-agent-without-anorexic-side-effects
#1
Kamil Makowski, Joan Francesc Mir, Paula Mera, Xavier Ariza, Guillermina Asins, Fausto G Hegardt, Laura Herrero, Jordi García, Dolors Serra
C75 is a synthetic anticancer drug that inhibits fatty acid synthase (FAS) and shows a potent anorexigenic side effect. In order to find new cytotoxic compounds that do not impact food intake, we synthesized a new family of C75 derivatives. The most promising anticancer compound among them was UB006 ((4SR,5SR)-4-(hydroxymethyl)-3-methylene-5-octyldihydrofuran-2(3H)-one). The effects of this compound on cytotoxicity, food intake and body weight were studied in UB006 racemic mixture and in both its enantiomers separately...
March 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28148395/tissue-factor-factor-viia-complex-triggers-protease-activated-receptor-2-dependent-growth-factor-release-and-migration-in-ovarian-cancer
#2
Alice Chanakira, Pamela R Westmark, Irene M Ong, John P Sheehan
OBJECTIVE: Enhanced tissue factor (TF) expression in epithelial ovarian cancer (EOC) is associated with aggressive disease. Our objective was to evaluate the role of the TF-factor VIIa-protease-activated receptor-2 (PAR-2) pathway in human EOC. METHODS: TCGA RNAseq data from EOC databases were analyzed for PAR expression. Cell and microparticle (MP) associated TF protein expression (Western blot) and MP-associated coagulant activity were determined in human EOC (SKOV-3, OVCAR-3 and CaOV-3) and control cell lines...
April 2017: Gynecologic Oncology
https://www.readbyqxmd.com/read/28003845/all-trans-retinoic-acid-and-genistein-induce-cell-apoptosis-in-ovcar-3-cells-by-increasing-the-p14-tumor-suppressor-gene
#3
Mehdi Nikbakht Dastjerdi, Saeed Zamani, Mohammad Mardani, Batool Hashemi Beni
In this study, we evaluated the effects of all-trans retinoic acid (ATRA) alone or in combination with genistein (GEN) in p14 tumor suppressor gene and subsequent apoptosis of human ovarian carcinoma cells (OVCAR-3). The cells were treated with ATRA or GEN at concentrations of 50 and 25 μM respectively, either alone or in combination for 24 and 48 h. The cell viability was evaluated using 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) assay. The percentage of cell apoptosis was determined using flow cytometry and p14 gene expression was measured using real time PCR...
December 2016: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27906095/resveratrol-and-acetyl-resveratrol-modulate-activity-of-vegf-and-il-8-in-ovarian-cancer-cell-aggregates-via-attenuation-of-the-nf-%C3%AE%C2%BAb-protein
#4
Alexandria B Tino, Kenny Chitcholtan, Peter H Sykes, Ashley Garrill
BACKGROUND: Key features of advanced ovarian cancer include metastasis via cell clusters in the abdominal cavity and increased chemoresistance. Resveratrol and derivatives of resveratrol have been shown to have antitumour properties. The purpose of this study was to investigate the effect of resveratrol and acetyl-resveratrol on 3D cell aggregates of ovarian cancer, and establish if NF-κB signalling may be a potential target. METHODS: Poly-HEMA coated wells were used to produce 3D aggregates of two ovarian cancer cell lines, SKOV-3 and OVCAR-5...
December 1, 2016: Journal of Ovarian Research
https://www.readbyqxmd.com/read/27862665/role-of-human-epididymis-protein-4-in-chemoresistance-and-prognosis-of-epithelial-ovarian-cancer
#5
Seungho Lee, Seowon Choi, Yookyung Lee, Donghae Chung, Suntaek Hong, Nohhyun Park
AIM: Human epididymis protein 4 (HE4) is a novel biomarker for epithelial ovarian cancer. This study was designed to evaluate the role of HE4 in chemo-response against anti-cancer drugs and prognosis of epithelial ovarian cancer. METHODS: HE4-depleted cells and HE4-overexpressing cells were generated. The effect of HE4 gene silencing and overexpression was examined using a cell viability assay after exposure to chemotherapeutic agents and the signaling pathway. We studied the expression of HE4 in ovarian cancer tissue and the prognostic significance...
November 12, 2016: Journal of Obstetrics and Gynaecology Research
https://www.readbyqxmd.com/read/27823852/high-paclitaxel-loaded-and-tumor-cell-targeting-hyaluronan-coated-nanoemulsions
#6
Joo-Eun Kim, Young-Joon Park
The purpose of this study was to develop hyaluronan-coated nanoemulsions (HNEs) with high solubilizing capacity and tumor cell targeting capability for the poorly soluble paclitaxel. The HNEs were composed of dl-a-tocopheryl acetate, soybean oil, polysorbate 80, and ferric chloride and were coated with hyaluronic acid (HA) as a targeting moiety. The nanoemulsions (NEs) and HNEs with or without paclitaxel (PTX) were prepared using high-pressure homogenization with a microfluidizer and were lyophilized with d-mannitol...
February 1, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/27823561/synthesis-antitubercular-and-anticancer-activities-of-p-nitrophenylethylenediamine-derived-schiff-bases
#7
Raquel S Amim, Cláudia Pessoa, Maria C S Lourenço, Marcus V N de Souza, Josane A Lessa
BACKGROUND: Schiff bases have been greatly studied in biological field due to their wide range of pharmacological activities, such as antitubercular and antitumour. In the search of novel antitubercular agents, several compounds containing pharmacophoric group of ethambutol have been synthesized and evaluated against mycobacteria species causing tuberculosis. In this work, we investigate whether ethylenediamine, Schiff base as well as nitro group together could contribute to the formation of novel molecules with dual biological activities: antitubercular and anticancer...
November 4, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27792980/synthesis-and-evaluation-of-novel-hybrids-%C3%AE-carboline-4-thiazolidinones-as-potential-antitumor-and-antiviral-agents
#8
Valéria Aquilino Barbosa, Paula Baréa, Renata Sespede Mazia, Tania Ueda-Nakamura, Willian Ferreira da Costa, Mary Ann Foglio, Ana Lucia T Goes Ruiz, João Ernesto de Carvalho, Débora Barbosa Vendramini-Costa, Celso Vataru Nakamura, Maria Helena Sarragiotto
A series of novel hybrids β-carboline-4-thiazolidinones were synthesized and evaluated for their in vitro antitumor activity against human cancer cell lines and for antiviral activity towards Herpes simplex virus type-1 (HSV-1). From the N'-(2-ylidene-4-thiazolidinone)-β-carboline-3-carbohydrazide series (9-11), compounds 9c and 11d were the most active, showing growth inhibition 50% (GI50) values less than 5 μM for all cell lines tested. Compound 9c, bearing the 4-dimethylaminophenyl group at C-1 of β-carboline was selected for further investigation concerning cell death and cell cycle profile, focusing on the human renal adenocarcinoma cell line 786-0...
November 29, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27698947/synthesis-of-thiazolidine-2-4-dione-derivatives-anticancer-antimicrobial-and-dna-cleavage-studies
#9
S Vijaya Laxmi, P Anil, G Rajitha, Asha Jyothi Rao, Peter A Crooks, B Rajitha
In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives (5a-g) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound 5d (NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound 5d was active against all the cell lines, it has shown potential activity against leukemia SR (GI50: 2...
October 2016: Journal of Chemical Biology
https://www.readbyqxmd.com/read/27689466/activation-of-estrogen-receptor-alpha-by-estradiol-and-cisplatin-induces-platinum-resistance-in-ovarian-cancer-cells
#10
Sohei Matsumura, Tsuyoshi Ohta, Keiko Yamanouchi, Zhiyang Liu, Takeshi Sudo, Takanobu Kojimahara, Manabu Seino, Megumi Narumi, Seiji Tsutsumi, Toshifumi Takahashi, Kazuhiro Takahashi, Hirohisa Kurachi, Satoru Nagase
Activation of Estrogen receptor (ER) alpha (α) promotes cell growth and influences the response of cancer cell to chemotherapeutic agents. However, the mechanism by which ERα activation antagonizes cells to chemotherapy-induced cytotoxicity remains unclear. Here, we investigated the effect of cisplatin on ERα activation. In addition, we examined whether down-regulation of ERα modulate cisplatin-mediated cytotoxicity using two human ovarian cancer cells (Caov-3 and Ovcar-3) transduced with ERα short hairpin RNA (shRNA)...
September 30, 2016: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/27688477/cure-of-human-ovarian-carcinoma-solid-xenografts-by-fractionated-211at-alpha-radioimmunotherapy-influence-of-tumor-absorbed-dose-and-effect-on-long-term-survival
#11
Tom A Bäck, Nicolas Chouin, Sture Lindegren, Helena Kahu, Holger Jensen, Per Albertsson, Stig Palm
The goal of this study was to investigate if targeted alpha therapy (TAT) could be used to successfully treat also macro tumors, in addition to its established role for treating micrometastatic and minimal disease. We used an intravenous (i.v.) fractionated regimen of alpha-radioimmunotherapy (α-RIT) in a subcutaneous (s.c.) tumor model in mice. We aimed at evaluating the absorbed dose levels required for tumor eradication and to monitor tumor growth, as well as the long-term survival after treatment. METHODS: Mice bearing s...
September 29, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27627067/are-salty-liquid-food-flavorings-in-vitro-antitumor-substances
#12
Francisco R S Carvalho, Antonio G Moura, Gardenia F Rodrigues, Narcia M F Nunes, Daisy J B Lima, Claudia Pessoa, Marcilia P Costa, Paulo M P Ferreira, Ana Paula Peron
The objective of this study was to evaluate the antiproliferative, cytotoxic and genotoxic potential of salty liquid synthetic flavorings of Butter, Cheddar Cheese and Onion. The antiproliferative potential (2.9-1500 µg/mL) was assessed by MTT assay after 72h using the human tumor lines SF-295 (glioblastoma), OVCAR-8 (ovarian), HCT-116 (colon) and HL-60 (promyelocytic leukemia) and primary cultures of murine Sarcoma 180 (S180) and peripheral blood mononuclear cells (PBMC). Allium cepa bulbs were exposed to growing respective doses (1 mL and 2 mL)...
September 2016: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/27591998/synthesis-and-evaluation-of-copper-ii-complexes-with-isoniazid-derived-hydrazones-as-anticancer-and-antitubercular-agents
#13
Gisele S S Firmino, Marcus V N de Souza, Claudia Pessoa, Maria C S Lourenco, Jackson A L C Resende, Josane A Lessa
In this study, the N,N,O metal chelator 2-pyridinecarboxaldehydeisonicotinoyl hydrazone (HPCIH, 1) and its derivatives 2-acetylpyridine-(HAPIH 2), 2-pyridineformamide-(HPAmIH, 3) and pyrazineformamide-(HPzAmIH, 4) were employed in the synthesis of four copper(II) complexes, [Cu(HPCIH)Cl2]·0.4H2O (5), [Cu(HAPIH)Cl2]·1.25H2O (6), [Cu(HPAmIH)Cl2]·H2O (7) and [Cu(HPzAmIH)Cl2]·1.25H2O (8). The compounds were assayed for their action toward Mycobacterium tuberculosis H37Rv ATCC 27294 strain and the human tumor cell lines OVCAR-8 (ovarian cancer), SF-295 (glioblastoma multiforme) and HCT-116 (colon adenocarcinoma)...
December 2016: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/27589474/differences-in-the-mechanisms-of-action-of-bde-47-and-its-metabolites-on-ovcar-3-and-mcf-7-cell-apoptosis
#14
Anna Karpeta, Ewa Łucja Gregoraszczuk
Data concerning possible carcinogenic action of polybrominated diphenyl ethers (PBDEs) in hormone-dependent tissues are limited. Our earlier studies showed that 2,2',4,4'-tetrabromodiphenyl ether (BDE-47) stimulated OVCAR-3 and MCF-7 cell proliferation, while its hydroxylated metabolites (5-OH-BDE-47 and 6-OH-BDE-47) increased estrogen receptors protein expression and extracellular signal-regulated kinase 1/2 and protein kinase Cα phosphorylation in these cell lines. In addition to cell proliferative disorder, a failure in the regulation of apoptosis can also lead to the formation and development of tumors...
September 2, 2016: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/27569743/a-novel-ief-peptide-fractionation-method-reveals-a-detailed-profile-of-n-terminal-acetylation-in-chemotherapy-responsive-and-resistant-ovarian-cancer-cells
#15
Florian Weiland, Georgia Arentz, Manuela Klingler-Hoffmann, Peter McCarthy, Noor A Lokman, Gurjeet Kaur, Martin K Oehler, Peter Hoffmann
Although acetylation is regarded as a common protein modification, a detailed proteome wide profile of this posttranslational modification may reveal important biological insight regarding differential acetylation of individual proteins. Here we optimised a novel peptide IEF fractionation method for use prior to LC-MS/MS analysis in order to obtain a more in depth coverage of N-terminally acetylated proteins from complex samples. Application of the method to the analysis of the serous ovarian cancer cell line OVCAR-5 identified 341 N-terminally acetylated proteins, 23 of which are previously un-reported...
August 29, 2016: Journal of Proteome Research
https://www.readbyqxmd.com/read/27553727/explorative-study-on-the-anticancer-activity-selectivity-and-metabolic-stability-of-related-analogs-of-aminosteroid-rm-133
#16
Martin Perreault, René Maltais, Raphaël Dutour, Donald Poirier
RM-133 is a key representative of a new family of aminosteroids reported as potent anticancer agents. Although RM-133 produced interesting results in 4 mouse xenograft cancer models when injected subcutaneously, it needs to be improved to increase its in vivo potency. Thus, to obtain an analog of RM-133 with a better drug potential, a structure-activity relationship study was conducted by synthesizing eleven RM-133-related compounds and addressing their antiproliferative activity on 3 human cancer cells (HL-60, OVCAR-3 and PANC-1) and 3 human normal cell lines (primary ovary, pancreas and renal proximal tubule) as well as their metabolic stability in human liver microsomes...
November 2016: Steroids
https://www.readbyqxmd.com/read/27444036/panobinostat-sensitizes-cyclin-e-high-homologous-recombination-proficient-ovarian-cancer-to-olaparib
#17
Andrew J Wilson, Kofi Sarfo-Kantanka, Toby Barrack, Alexandra Steck, Jeanette Saskowski, Marta A Crispens, Dineo Khabele
OBJECTIVE: Homologous recombination (HR) proficient ovarian cancers, including CCNE1 (cyclin E)-amplified tumors, are resistant to poly (ADP-ribose) polymerase inhibitors (PARPi). Histone deacetylase inhibitors (HDACi) are effective in overcoming tumor resistance to DNA damaging drugs. Our goal was to determine whether panobinostat, a newly FDA-approved HDACi, can sensitize cyclin E, HR-proficient ovarian cancer cells to the PARPi olaparib. METHODS: Expression levels of CCNE1 (cyclin E), BRCA1, RAD51 and E2F1 in ovarian tumors and cell lines were extracted from The Cancer Genome Atlas (TCGA) and Broad-Novartis Cancer Cell Line Encyclopedia (CCLE)...
October 2016: Gynecologic Oncology
https://www.readbyqxmd.com/read/27439449/radiobiological-effectiveness-of-ultrashort-laser-driven-electron-bunches-micronucleus-frequency-telomere-shortening-and-cell-viability
#18
Maria Grazia Andreassi, Andrea Borghini, Silvia Pulignani, Federica Baffigi, Lorenzo Fulgentini, Petra Koester, Monica Cresci, Cecilia Vecoli, Debora Lamia, Giorgio Russo, Daniele Panetta, Maria Tripodi, Leonida A Gizzi, Luca Labate
Laser-driven electron accelerators are capable of producing high-energy electron bunches in shorter distances than conventional radiofrequency accelerators. To date, our knowledge of the radiobiological effects in cells exposed to electrons using a laser-plasma accelerator is still very limited. In this study, we compared the dose-response curves for micronucleus (MN) frequency and telomere length in peripheral blood lymphocytes exposed to laser-driven electron pulse and X-ray radiations. Additionally, we evaluated the effects on cell survival of in vitro tumor cells after exposure to laser-driven electron pulse compared to electron beams produced by a conventional radiofrequency accelerator used for intraoperative radiation therapy...
September 2016: Radiation Research
https://www.readbyqxmd.com/read/27370528/hepta-hexa-penta-tetra-and-trisaccharide-resin-glycosides-from-three-species-of-ipomoea-and-their-antiproliferative-activity-on-two-glioma-cell-lines
#19
Ismael León-Rivera, Federico Del Río-Portilla, Raúl G Enríquez, Edgar Rangel-López, Juana Villeda, María Yolanda Rios, Gabriel Navarrete-Vázquez, Israel Hurtado-Días, Ulises Guzmán-Valdivieso, Verónica Núñez-Urquiza, Carolina Escobedo-Martínez
Six new partially acylated resin glycosides were isolated from convolvulin of Ipomoea purga, Ipomoea stans, and Ipomoea murucoides (Convolvulaceae). The structures of compounds 1-6 were elucidated by a combination of NMR spectroscopy and mass spectrometry. The structure of jalapinoside B (1) consists of a hexasaccharide core bonded to an 11-hydroxytetradecanoic (convolvulinic) acid forming a macrolactone acylated by a 2-methylbutanoyl, a 3-hydroxy-2-methylbutanoyl, and a quamoclinic acid B units. Purginoic acid A (2) contains a hexasaccharide core bonded to a convolvulinic acid acylated by a 3-hydroxy-2-methylbutanoyl unit...
March 2017: Magnetic Resonance in Chemistry: MRC
https://www.readbyqxmd.com/read/27323861/expression-of-tumor-antigens-on-primary-ovarian-cancer-cells-compared-to-established-ovarian-cancer-cell-lines
#20
Kamila Kloudová, Hana Hromádková, Simona Partlová, Tomáš Brtnický, Lukáš Rob, Jiřina Bartůňková, Michal Hensler, Michael J Halaška, Radek Špíšek, Anna Fialová
In order to select a suitable combination of cancer cell lines as an appropriate source of antigens for dendritic cell-based immunotherapy of ovarian cancer, we analyzed the expression level of 21 tumor associated antigens (BIRC5, CA125, CEA, DDX43, EPCAM, FOLR1, Her-2/neu, MAGE-A1, MAGE-A2, MAGE-A3, MAGE-A4, MAGE-A6, MAGE-A10, MAGE-A12, MUC-1, NY-ESO-1, PRAME, p53, TPBG, TRT, WT1) in 4 established ovarian cancer cell lines and in primary tumor cells isolated from the high-grade serous epithelial ovarian cancer tissue...
July 19, 2016: Oncotarget
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