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https://www.readbyqxmd.com/read/28915356/real-time-apoptosis-and-viability-high-throughput-screening-of-3d-multicellular-tumor-spheroids-using-the-celigo-image-cytometer
#1
Sarah Kessel, Scott Cribbes, Surekha Bonasu, Jean Qiu, Leo Li-Ying Chan
Three-dimensional tumor spheroid models have been increasingly used to investigate and characterize cancer drug compounds. Previously, the Celigo image cytometer has demonstrated its utility in a high-throughput screening manner for evaluating potential drug candidates in a 3D multicellular tumor spheroid (MCTS) primary screen. In addition, we have developed real-time kinetic caspase 3/7 apoptosis and propidium iodide viability 3D MCTS assays, both of which can be used in a secondary screen to better characterize the hit compounds...
September 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28903178/the-effects-of-%C3%AE-caryophyllene-oxide-and-trans-nerolidol-on-the-efficacy-of-doxorubicin-in-breast-cancer-cells-and-breast-tumor-bearing-mice
#2
Veronika Hanušová, Kateřina Caltová, Hana Svobodová, Martin Ambrož, Adam Skarka, Natálie Murínová, Věra Králová, Pavel Tomšík, Lenka Skálová
BACKGROUND: One approach to improve effect of chemotherapy is combination of classical cytostatic drugs with natural compounds, e. g. sesquiterpenes. In our previous study, sesquiterpenes β-caryophyllene oxide (CAO) and trans-nerolidol (NER) improved the anti-proliferative effect of doxorubicin (DOX) in intestinal cancer cell lines. PURPOSE: The present study was designed to evaluate the effect of CAO and NER on DOX efficacy, focusing on cell proliferation, migration, apoptosis and DOX accumulation in breast cancer cells MDA-MB-231 and MCF7 in vitro and in mice bearing solid Ehrlich tumors (EST) in vivo...
September 9, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28902204/rational-design-and-structure-activity-relationship-studies-of-quercetin-amino-acid-hybrids-targeting-the-anti-apoptotic-protein-bcl-xl
#3
Tahsin F Kellici, Maria V Chatziathanasiadou, Min-Sung Lee, Nisar Sayyad, Elena G Geromichalou, Eirinaios I Vrettos, Antonis D Tsiailanis, Seung-Wook Chi, George D Geromichalos, Thomas Mavromoustakos, Andreas G Tzakos
Anti-apoptotic proteins, like the Bcl-2 family proteins, present an important therapeutic cancer drug target. Their activity is orchestrated through neutralization upon interaction of pro-apoptotic protein counterparts that leads to immortality of cancer cells. Therefore, generating compounds targeting these proteins is of immense therapeutic importance. Herein, Induced Fit Docking (IFD) and Molecular Dynamics (MD) simulations were performed to rationally design quercetin analogues that bind in the BH3 site of the Bcl-xL protein...
September 13, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28901962/ability-of-polymer-bound-p-glycoprotein-inhibitor-ritonavir-to-overcome-multidrug-resistance-in-various-resistant-neuroblastoma-cell-lines
#4
Eva Koziolová, Petr Chytil, Tomáš Etrych, Olga Janoušková
Polymer prodrugs can considerably improve the treatment of tumors with multidrug resistance, often caused by overexpression of P-glycoprotein (P-gp). Here, we present the effect of the N-(2-hydroxypropyl) methacrylamide-based polymer conjugate with P-gp inhibitor ritonavir (RIT) on the increase of free doxorubicin (DOX) and polymer-bound DOX cytotoxicity in the human neuroblastoma 4 cell line and its resistant clones to different cytostatics. The increase in cytotoxicity after polymer-RIT conjugate pretreatment was higher for the lines overexpressing P-gp and less pronounced for those with decreased P-gp levels...
September 8, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28898049/analysis-of-plasmodium-vivax-chloroquine-resistance-transporter-pvcrt-mutant-isoforms
#5
Matthew R Hassett, Bryce E Riegel, Paul Samuel Callaghan, Paul David Roepe
Chloroquine (CQ) resistance (CQR) in Plasmodium falciparum malaria is widespread and has limited the use of CQ in many regions of the globe. Malaria caused by the related human parasite P. vivax is as widespread as is P. falciparum malaria and has been treated with CQ as extensively as has P. falciparum, suggesting that P. vivax parasites have been selected with CQ as profoundly as have P. falciparum parasites. Indeed, a growing number of clinical reports have presented data suggesting increased P. vivax CQR...
September 12, 2017: Biochemistry
https://www.readbyqxmd.com/read/28893108/comparative-efficacy-evaluation-of-catheter-intraperitoneal-chemotherapy-normothermic-and-hyperthermic-chemoperfusion-in-a-rat-model-of-ascitic-ovarian-cancer
#6
V G Bespalov, I K Alvovsky, G V Tochilnikov, A N Stukov, E A Vyshinskaya, A L Semenov, I N Vasilyeva, O A Belyaeva, G S Kireeva, K Y Senchik, J D Von, L A Krasilnikova, V A Alexandrov, N N Khromov-Borisov, D A Baranenko, A M Belyaev
OBJECTIVES: The choice of an optimal administration route for intraperitoneal (IP) chemotherapy and a suitable chemotherapeutic regime in the treatment of ovarian cancer remains a controversy. We investigated survival outcomes according to catheter intraperitoneal chemotherapy (CIPC), normothermic and hyperthermic chemoperfusion (NIPEC and HIPEC) with cytostatic drugs dioxadet and cisplatin in rats with transplantable ascitic ovarian cancer. METHODS: Ascitic liquid containing 1·10(7) tumor cells was inoculated to female Wistar rats and 48 hours after rats received dioxadet and cisplatin at the maximum tolerated doses...
September 11, 2017: International Journal of Hyperthermia
https://www.readbyqxmd.com/read/28892751/poly-2-ethyl-2-oxazoline-conjugates-with-doxorubicin-for-cancer-therapy-in%C3%A2-vitro-and-in%C3%A2-vivo-evaluation-and-direct-comparison-to-poly-n-2-hydroxypropyl-methacrylamide-analogues
#7
Ondrej Sedlacek, Bryn D Monnery, Jana Mattova, Jan Kucka, Jiri Panek, Olga Janouskova, Anita Hocherl, Bart Verbraeken, Maarten Vergaelen, Marie Zadinova, Richard Hoogenboom, Martin Hruby
We designed and synthesized a new delivery system for the anticancer drug doxorubicin based on a biocompatible hydrophilic poly(2-ethyl-2-oxazoline) (PEtOx) carrier with linear architecture and narrow molar mass distribution. The drug is connected to the polymer backbone via an acid-sensitive hydrazone linker, which allows its triggered release in the tumor. The in vitro studies demonstrate successful cellular uptake of conjugates followed by release of the cytostatic cargo. In vivo experiments in EL4 lymphoma bearing mice revealed prolonged blood circulation, increased tumor accumulation and enhanced antitumor efficacy of the PEtOx conjugate having higher molecular weight (40 kDa) compared to the lower molecular weight (20 kDa) polymer...
September 6, 2017: Biomaterials
https://www.readbyqxmd.com/read/28883724/nanomedicinal-products-a-survey-on-specific-toxicity-and-side-effects
#8
Walter Brand, Cornelle W Noorlander, Christina Giannakou, Wim H De Jong, Myrna W Kooi, Margriet Vdz Park, Rob J Vandebriel, Irene Em Bosselaers, Joep Hg Scholl, Robert E Geertsma
Due to their specific properties and pharmacokinetics, nanomedicinal products (NMPs) may present different toxicity and side effects compared to non-nanoformulated, conventional medicines. To facilitate the safety assessment of NMPs, we aimed to gain insight into toxic effects specific for NMPs by systematically analyzing the available toxicity data on approved NMPs in the European Union. In addition, by comparing five sets of products with the same active pharmaceutical ingredient (API) in a conventional formulation versus a nanoformulation, we aimed to identify any side effects specific for the nano aspect of NMPs...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28882945/melatonin-synergizes-the-chemotherapeutic-effect-of-cisplatin-in-ovarian-cancer-cells-independently-of-mt1-melatonin-receptors
#9
Agata Zemła, Irmina Grzegorek, Piotr Dzięgiel, Karolina Jabłońska
BACKGROUND/AIM: Melatonin (MLT), through the interaction with membrane melatonin receptors MT1, can improve the effectiveness of cytostatic agents, including cisplatin (CP). The aim of this study was to examine the synergistic effect of MLT and CP in three cell lines: IOSE 364, SK-OV-3 and OVCAR-3, as well as to assess the role of MT1 receptors in this mechanism. MATERIALS AND METHODS: Using the SRB assay we investigated the effect of different concentrations of CP and MLT on cell viability...
September 2017: In Vivo
https://www.readbyqxmd.com/read/28869461/effects-of-tacrolimus-or-sirolimus-on-the-adhesion-of-vascular-wall-cells-controlled-in-vitro-comparison-study
#10
A Krüger-Genge, B Hiebl, R P Franke, A Lendlein, F Jung
In drug eluting stents the cytostatic drugs Sirolimus or Tacrolimus are used to inhibit blood vessel restenosis by limiting the proliferation of smooth muscle cells. However, the cytostatic activity of both drugs was shown to be not cell specific and could also affect the stent endothelialisation, respectively. Currently, only limited in vitro data are available about the impact of Sirolimus and Tacrolimus on endothelial cell proliferation over a broad concentration range. To answer this question the following study was performed...
August 28, 2017: Clinical Hemorheology and Microcirculation
https://www.readbyqxmd.com/read/28868810/five-year-follow-up-of-the-endothelial-progenitor-cell-capturing-stent-versus-the-paxlitaxel-eluting-stent-in-de-novo-coronary-lesions-with-a-high-risk-of-coronary-restenosis
#11
Pier Woudstra, Deborah N Kalkman, Marcel A Beijk, Margo Klomp, Peter Damman, Karel T Koch, Jose P S Henriques, Jan Baan, Marije M Vis, Jan J Piek, Jan G P Tijssen, Robbert J de Winter
OBJECTIVES: To assess the long-term safety and clinical efficacy of the Genous endothelial progenitor cell capturing stent (ECS) compared with the TAXUS Liberté paclitaxel-eluting stent (PES) in lesions with a high risk of restenosis. BACKGROUND: Instead of the use of cytotoxic or cytostatic drugs in drug-eluting stents, a "pro-healing" approach in ECS may overcome impeded healing response due to delayed functional endothelialization of the stent struts. METHODS: In the prospective, randomized TRIAS pilot study 193 patients with coronary artery lesions carrying a high risk of restenosis were included (ECS: n = 98, PES: n = 95)...
September 4, 2017: Catheterization and Cardiovascular Interventions
https://www.readbyqxmd.com/read/28861328/targeting-myc-sensitizes-malignant-mesothelioma-cells-to-pak-blockage-induced-cytotoxicity
#12
Yinfei Tan, Eleonora Sementino, Jonathan Chernoff, Joseph R Testa
Clinical management of malignant mesothelioma (MM) is very challenging due to marked resistance of this tumor to chemotherapy. Various mechanisms lead to a less than ideal drug concentration inside of MM cells, diminishing cytotoxicity. Consequently, single cytotoxic drugs achieve very modest response rates in MM patients, and combination regimens using standard and novel therapies have achieved only limited improvement in overall survival. Here, we demonstrate that MYC has either proliferative or pro-survival effects in MM cells during normal or stressed conditions, respectively...
2017: American Journal of Cancer Research
https://www.readbyqxmd.com/read/28857796/local-anesthetics-inhibit-the-growth-of-human-hepatocellular-carcinoma-cells
#13
Grégoire Le Gac, Gaëlle Angenard, Bruno Clément, Bruno Laviolle, Cédric Coulouarn, Hélène Beloeil
BACKGROUND: Hepatocellular carcinoma (HCC) is an aggressive cancer with limited therapeutic options. Retrospective studies have shown that the administration of local anesthetics (LAs) during cancer surgery could reduce cancer recurrence. Besides, experimental studies reported that LAs could inhibit the growth of cancer cells. Thus, the purpose of this study was to investigate the effects of LAs on human HCC cells. METHODS: The effects of 2 LAs (lidocaine and ropivacaine) (10 to 10 M) were studied after an incubation of 48 hours on 2 HCC cell lines, namely HuH7 and HepaRG...
August 29, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28855512/atrx-is-a-regulator-of-therapy-induced-senescence-in-human-cells
#14
Marta Kovatcheva, Will Liao, Mary E Klein, Nicolas Robine, Heather Geiger, Aimee M Crago, Mark A Dickson, William D Tap, Samuel Singer, Andrew Koff
Senescence is a state of stable cell cycle exit with important implications for development and disease. Here, we demonstrate that the chromatin remodeling enzyme ATRX is required for therapy-induced senescence. ATRX accumulates in nuclear foci and is required for therapy-induced senescence in multiple types of transformed cells exposed to either DNA damaging agents or CDK4 inhibitors. Mobilization into foci depends on the ability of ATRX to interact with H3K9me3 histone and HP1. Foci form soon after cells exit the cell cycle, before other hallmarks of senescence appear...
August 30, 2017: Nature Communications
https://www.readbyqxmd.com/read/28841513/synthesis-and-biological-investigation-of-2-4-substituted-quinazolines-as-highly-potent-inhibitors-of-breast-cancer-resistance-protein-abcg2
#15
Michael K Krapf, Jennifer Gallus, Michael Wiese
Expression of ABCG2, a member of the ABC transporter superfamily, has been correlated to the clinical outcome of multiple cancers and is often associated with the occurrence of multidrug resistance (MDR) in chemotherapy. Inhibition of the transport protein by potent and selective inhibitors might be a way to treat cancer more efficiently and improve the therapy of cancer patients. Recently we reported the synthesis of new inhibitors based on a quinazoline scaffold. In the present study more structural variations were explored...
August 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28841172/zytoprotektion-mit-amifostin-ethyol-%C3%A2-in-der-chemotherapie-meta-analyse-zum-pharmakokinetischen-interaktionspotential-mit-zytostatika
#16
Martin Czejka, Johannes Schüller, Heidemarie Kletzl
The cytoprotective agent amifostine (AMI) is capable to protect healthy cells (contrary to tumor cells) due to higher activity of alkaline phosphatase at the membrane site of normal cells. In seven clinical trials the influence of AMI on the pharmacokinetics of different cytostatics was investigated. Preadministration of AMI increased Cmax of doxorubicin (+ 44 %, p < 0.06), epirubicin (+ 31 %, P < 0.08), mitomycin C (+ 41 %, p < 0.01) and docetaxel (+ 31 % and + 17 %, not significant). In contrary, the peak concentration of pirarubicin , the tetrahydropyranyl-prodrug of doxorubicin was decreased (- 50 %, P < 0...
August 25, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28840740/-two-perspectives-on-venous-thromboembolism-in-oncology
#17
Patrik Palacka, Jana Hirmerová
An increased risk of venous thromboembolism (VTE) in patients with malignancy compared with the current population is determined by risk factors including the use of anticancer treatments, in particular some hormonal drugs, cytostatics, vascular endothelial growth factor (VEGF) inhibitors and epidermal receptor growth factor (EGFR) inhibitors, immunomodulators, and erythropoietins. The population of cancer patients is divided into a group of individuals with a history of malignant disease in complete remission and patients with active (locally advanced or metastatic) malignant disease in terms of approach to VTE...
2017: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/28837922/development-of-glut4-selective-antagonists-for-multiple-myeloma-therapy
#18
Changyong Wei, Richa Bajpai, Horrick Sharma, Monique Heitmeier, Atul D Jain, Shannon M Matulis, Ajay K Nooka, Rama K Mishra, Paul W Hruz, Gary E Schiltz, Mala Shanmugam
Cancer cells consume more glucose to fuel metabolic programs fundamental to sustaining their survival, growth and proliferation. Among the fourteen SLC2A family members, GLUTs 1 and 4 are high-affinity glucose transporters. GLUT4 (SLC2A4) is highly expressed in muscle and adipose tissue. Basally retained within the cell, GLUT4 traffics to the plasma membrane (PM) in response to insulin and exercise-stimulation. The plasma cell malignancy multiple myeloma (MM) exhibits increased constitutive expression of GLUT4 on the PM, co-opting use of GLUT4 for survival and proliferation...
August 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28835384/ezh2-inhibition-by-tazemetostat-results-in-altered-dependency-on-b-cell-activation-signaling%C3%A2-in-dlbcl
#19
Dorothy Brach, Danielle Johnston-Blackwell, Allison Drew, Trupti Lingaraj, Vinny Motwani, Natalie M Warholic, Igor Feldman, Christopher Plescia, Jesse J Smith, Robert A Copeland, Heike Keilhack, Elayne Chan-Penebre, Sarah K Knutson, Scott A Ribich, Alejandra Raimondi, Michael J Thomenius
The EZH2 small molecule inhibitor tazemetostat (EPZ-6438) is currently being evaluated in phase II clinical trials for the treatment of non-Hodgkin's Lymphoma (NHL).  We have previously shown that EZH2 inhibitors display an anti-proliferative effect in multiple pre-clinical models of NHL, and that models bearing gain-of-function mutations in EZH2 were consistently more sensitive to EZH2 inhibition than lymphomas with wild-type (WT) EZH2 Here, we demonstrate that cell lines bearing EZH2 mutations show a cytotoxic response, while cell lines with WT-EZH2 show a cytostatic response and only tumor growth inhibition without regression in a xenograft model...
August 23, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28834581/pyrrolo-2-3-d-pyrimidine-7-deazapurine-as-a-privileged-scaffold-in-design-of-antitumor-and-antiviral-nucleosides
#20
REVIEW
Pavla Perlíková, Michal Hocek
7-Deazapurine (pyrrolo[2,3-d]pyrimidine) nucleosides are important analogues of biogenic purine nucleosides with diverse biological activities. Replacement of the N7 atom with a carbon atom makes the five-membered ring more electron rich and brings a possibility of attaching additional substituents at the C7 position. This often leads to derivatives with increased base-pairing in DNA or RNA or better binding to enzymes. Several types of 7-deazapurine nucleosides with potent cytostatic or cytotoxic effects have been identified...
August 23, 2017: Medicinal Research Reviews
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