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https://www.readbyqxmd.com/read/29908480/maintenance-treatment-of-recurrent-ovarian-cancer-is-it-ready-for-prime-time
#1
REVIEW
Paul DiSilvestro, Angeles Alvarez Secord
Approximately 1% of women in the United States will be diagnosed with epithelial ovarian cancer (EOC) during their lifetime. It is most likely to present at a more advanced stage, requiring aggressive therapeutic measures, and most women will succumb to this illness. Due to advancements in therapy, the oncology community has begun to shift its focus to molecular targeted agents, alternative dosing schedules, and maintenance therapy. Women who achieve a response to initial adjuvant chemotherapy may be candidates for maintenance therapy, with the goal of inducing a lasting remission or prolonging the disease-free interval before recurrence...
June 5, 2018: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/29908468/first-report-on-the-pharmacokinetic-profile-of-nimbolide-a-novel-anticancer-agent-in-oral-and-intravenous-administrated-rats-by-lc-ms-method
#2
Shandilya Mahamuni Baira, Amit Khurana, Jaganmohan Somagoni, R Srinivas, Chandraiah Godugu, M V N Kumar Talluri
Nimbolide is a novel, natural compound with promising potential as a drug candidate for anticancer activity. It is isolated from the Indian traditional medicinal plant Azadirachta indica popularly known as neem. The present study was undertaken to explore the oral bioavailability and pharmacokinetic characteristics of nimbolide in rats using the LC/QTOF/MS method. A simple protein precipitation method using acetonitrile was employed for extracting nimbolide from rat plasma. The chromatographic separation of nimbolide and the internal standard (regorafenib) was attained on an Aquity BEH C18 column (100 × 2...
June 2, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29908443/novel-pyrimidinic-selenourea-induces-dna-damage-cell-cycle-arrest-and-apoptosis-in-human-breast-carcinoma
#3
Flavio A R Barbosa, Tâmila Siminski, Rômulo F S Canto, Gabriela M Almeida, Nádia S R S Mota, Fabiana Ourique, Rozangela Curi Pedrosa, Antonio Luiz Braga
Novel pyrimidinic selenoureas were synthesized and evaluated against tumour and normal cell lines. Among these, the compound named 3j initially showed relevant cytotoxicity and selectivity for tumour cells. Three analogues of 3j were designed and synthesized keeping in view the structural requirements of this compound. Almost all the tested compounds displayed considerable cytotoxicity. However, 8a, one of the 3j analogues, was shown to be highly selective and cytotoxic, especially for breast carcinoma cells (MCF-7) (IC50  = 3...
June 11, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908440/organometallic-compounds-in-the-discovery-of-new-agents-against-kinetoplastid-caused-diseases
#4
REVIEW
Mauro Ravera, Elsa Moreno-Viguri, Rocio Paucar, Silvia Pérez-Silanes, Elisabetta Gabano
The development of safe and affordable antiparasitic agents effective against neglected tropical diseases is a big challenge of the drug discovery. The drugs currently employed have limitations such as poor efficacy, drug resistance or side effects. Thus, the search for new promising drugs is more and more crucial. Metal complexes and, in particular, organometallic compounds may expand the list of the drug candidates due to the peculiar attributes that the presence of the metal core add to the organic fragment (e...
June 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908438/targeting-rna-polymerase-i-transcription-machinery-in-cancer-cells-by-a-novel-monofunctional-platinum-based-agent
#5
Zhen-Lei Zhang, Chun-Lai Zhao, Qian Chen, Kai Xu, Xin Qiao, Jing-Yuan Xu
Aberrant ribosome biogenesis and enlarged nucleoli have long been used by pathologists as a marker of aggressive tumors. Suppression of RNA polymerase I (Pol I) transcription machinery within the nucleolus could be a direct way to trigger the nucleolar stress and to inhibit the rapid proliferation of cancer cells. Here we modified cisplatin with an analogue of the selective inhibitor of RNA polymerase I-mediated transcription BMH-21 to develop a novel platinum-based Pol I selective inhibitor. We show that this novel monofunctional platinum-based agent, P1-B1, had enhanced antitumor activity of up to 17-fold greater than the clinical drug cisplatin in cisplatin-resistant non-small cell lung cancer cells...
June 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908367/cell-proliferation-and-anti-apoptosis-essential-processes-for-recruitment-of-the-full-thermogenic-capacity-of-brown-adipose-tissue
#6
REVIEW
Jan Nedergaard, Yanling Wang, Barbara Cannon
In mice living under normal animal house conditions, the brown adipocytes in classical brown adipose tissue depots are already essentially fully differentiated: UCP1 mRNA and UCP1 protein levels are practically saturated. This means that any further recruitment - in response to cold exposure or any other browning agent - does not result in significant augmentation of these parameters. This may easily be construed to indicate that classical brown adipose tissue cannot be further recruited. However, this is far from the case: the capacity for further recruitment instead lies in the ability of the tissue to increase the number of brown-fat cells, a remarkable and highly controlled physiological recruitment process...
June 13, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29908360/heterogeneity-in-clinical-endoscopic-and-histologic-outcome-measures-and-placebo-response-rates-in-clinical-trials-of-eosinophilic-esophagitis-a-systematic-review
#7
REVIEW
Christopher Ma, Bram D van Rhijn, Vipul Jairath, Tran M Nguyen, Claire E Parker, Seema S Aceves, Glenn T Furuta, Sandeep K Gupta, David A Katzka, Ekaterina Safroneeva, Alain M Schoepfer, Alex Straumann, Jonathan M Spergel, Rish K Pai, Brian G Feagan, Ikuo Hirano, Evan S Dellon, Albert J Bredenoord
BACKGROUND & AIMS: Agents are being developed for treatment of eosinophilic esophagitis (EoE). However, it is not clear what outcome measures would best determine the efficacy and safety of these agents in clinical trials. We performed a systematic review of outcomes used in randomized placebo-controlled trials of EoE and we estimate the placebo response and rates of remission. METHODS: We searched MEDLINE, Embase, CENTRAL, ClinicalTrials.gov, and the EU Clinical Trials Register from inception through February 20, 2018 for randomized controlled trials of pharmacologic therapies for EoE...
June 13, 2018: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/29908332/enhanced-nanoparticle-uptake-into-virus-infected-cells-could-nanoparticles-be-useful-in-antiviral-therapy
#8
Yasmin Abo-Zeid, Richard A Urbanowicz, Brian J Thomson, William L Irving, Alexander W Tarr, Martin C Garnett
Virus infections cause diseases of different severity ranged from mild infection e.g. common cold into life threating diseases e.g. Human Immunodeficiency virus (HIV), Hepatitis B. Virus infections represent 44% of newly emerging infections. Although there are many efficient antiviral agents, they still have drawbacks due to accumulation at off target organs and developing of virus resistance due to virus mutation. Therefore, developing a delivery system that can selectively target drug into affected organs and avoid off target accumulation would be a highly advantageous strategy to improve antiviral therapy...
June 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29908324/pd-1-blockade-with-nivolumab-in-patients-with-recurrent-malignant-pleural-mesothelioma
#9
Josine Quispel-Janssen, Vincent van der Noort, Jeltje F de Vries, Marion Zimmerman, Ferry Lalezari, Erik Thunnissen, Kim Monkhorst, Robert Schouten, Laurel Schunselaar, Maria Disselhorst, Houke Klomp, Koen Hartemink, Sjaak Burgers, Wieneke Buikhuisen, Paul Baas
BACKGROUND: Malignant Pleural Mesothelioma (MPM) has limited treatment options and a poor outcome. PD-1/PD-L1 checkpoint inhibitors have proven efficacious in several cancer types. Nivolumab is a fully humanized monoclonal antibody against PD-1 with a favorable toxicity profile. In MPM, the immune system is considered to play an important role. We therefore tested nivolumab in recurrent MPM. METHODS: In this single center trial, patients with MPM received nivolumab 3mg/kg i...
June 13, 2018: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/29908302/inhibitory-effect-of-pxr-on-ammonia-induced-hepatocyte-autophagy-via-p53
#10
Linlin Yan, Zhanfei Chen, Luxi Wu, Yongfa Su, Xiaoqian Wang, Nanhong Tang
Pregnane X Receptor (PXR), a nuclear receptor transcription factor, participates in a wide range of physiological activities, but the regulation of ammonia-induced hepatocyte autophagy by PXR is not yet clear. In this study, the levels of down-regulated LC3B-II and up-regulated SQSTM1 were found in ammonia-induced PXR-overexpressing (PXR+) liver cells, but the opposite appeared in PXR-knockdown (PXR-) liver cells. Rifampicin, a PXR-activating agent, elicits a similar effect as PXR + cells. The mechanism analysis reveals that the levels of the energy-sensitive molecule AMPKβ1 and phosphorylated AMPKβ1 (p-AMPKβ1) in PXR - cells are higher than those in control cells, whereas the levels of this molecule in PXR + cells are lower than those in control cells...
June 13, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29908289/decreased-contractility-and-altered-responses-to-inotropic-agents-in-myocytes-from-tachypacing-induced-heart-failure-canines
#11
BaoXi Gao, Yusheng Qu, Weston Sutherland, Ray W Chui, Kim Hoagland, Hugo M Vargas
Contractility measurements using primary isolated cardiac myocytes (CM) have commonly been used in understanding the physiology and pharmacology of cellular mechanics. In the majority of studies, CM from healthy animals were used, and fewer studies were performed with CM from diseased hearts. To better understand the translational value of contractility on the cellular level of a diseased animal model, myocytes were isolated from left ventricles of a tachypacing-induced heart failure (HF) canine model, and their contractility was measured by recording sarcomere shortening using an image-based IonOptix video system...
June 13, 2018: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/29908277/dual-responsive-ipn-hydrogel-based-on-sugarcane-bagasse-cellulose-as-drug-carrier
#12
Yuanfeng Pan, Jingchun Wang, PingxiongCai, Huining Xiao
In this work, the stepwise synthesis of interpenetrating polymer network (IPN) strategy was developed in an attempt to fabricate novel hydrogels consisting of sugarcane bagasse cellulose (SBC), carboxymethylcellulose (CMC) and poly (N-isopropylacrylamide) (PNIPAm) as a dual-responsive drug carrier. The pretreated and dissolved SBC was pre-crosslinked using epichlorohydrin in the presence of CMC, followed by in-situ free-radical polymerization of NIPAm in the presence of N,N'-Methylene-bis(acrylamide) as a crosslinking agent...
June 13, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29908275/role-of-modification-route-for-zinc-oxide-nanoparticles-on-protein-structure-and-their-effects-on-glioblastoma-cells
#13
Mine Altunbek, Seda Keleştemur, Gülin Baran, Mustafa Çulha
Zinc oxide nanoparticles (ZnO) are presented as potential cancer therapeutic agent based on their surface properties. In this study, the most abundant blood proteins, albumin, fibrinogen and apo-transferrin, were covalently bound (c-ZnO NPs) and nonspecifically adsorbed (n-ZnO NPs) onto ZnO NPs to evaluate the role of modification route on protein structure and their effects on glioblastoma cells. The success of modification and structures of proteins on ZnO NPs were characterized with FT-IR. It was found that non-covalent interaction significantly damaged the secondary structure of proteins compared to those covalently attached to the ZnO nanoparticle...
June 13, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29908273/integrated-study-of-the-mechanism-of-tyrosinase-inhibition-by-baicalein-using-kinetic-multispectroscopic-and-computational-simulation-analyses
#14
Nihong Guo, Cailian Wang, Chao Shang, Xue You, Liuyang Zhang, Wenbin Liu
Controlling the activity of tyrosinase, which plays an important role in melanin synthesis, is essential endeavor in the field of medicine, food, cosmetics, and agriculture. Baicalein is a widely available inhibitor of tyrosinase. The mechanism of this inhibition was studied through an integrated approach coupling enzyme kinetics, multiple types of spectroscopy and computational simulation. Baicalein conspicuously inhibited the diphenolase activity with an IC50 value of 0.11 mM. The inhibtion kinetics indicated that baicalein was a mix-type tight binding inhibitor with a Ki of 0...
June 13, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29908257/rutin-attenuates-neurobehavioral-deficits-oxidative-stress-neuro-inflammation-and-apoptosis-in-fluoride-treated-rats
#15
Kpobari W Nkpaa, Godspower I Onyeso
Studies have shown that high exposure to fluoride (NaF) induces neurotoxicity. Rutin (RUT), a citrus flavonoid, has been reported to have antioxidant, anti-inflammatory and anti-apoptotic properties. The aim of this study was to investigate the neuroprotective mechanism(s) of RUT on NaF - induced neurotoxicity. Rats were exposed to NaF alone in drinking water at 15 mg/L alone ad libitum or orally co-treated by gavage with RUT at 50 and 100 mg/kg body weight for 31 consecutive days. A video-tracking software was used to monitor the motor and locomotive behavior during a 5 - min trial time in a novel environment...
June 13, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29908245/in-vitro-interaction-and-biocompatibility-of-titanate-nanotubes-with-microglial-cells
#16
S Sruthi, A Loiseau, J Boudon, F Sallem, L Maurizi, P V Mohanan, G Lizard, N Millot
Titanate nanotubes (TiONts) are promising agents for biomedical applications. Microglial activation and associated oxidative burst are major challenges in drug delivery applications across the brain. Here, TiONts were designed for drug delivery systems by functionalizing them with (3-aminopropyl) triethoxysilane (APTES), their interactions and biocompatibility were studied in vitro using murine microglial BV-2 cells. TiONts-APTES exposure resulted in increased ROS production and transient mitochondrial hyperpolarization...
June 13, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29908244/prompt-treatment-with-uridine-triacetate-improves-survival-and-reduces-toxicity-due-to-fluorouracil-and-capecitabine-overdose-or-dihydropyrimidine-dehydrogenase-deficiency
#17
Rolando A G Garcia, Joel A Saydoff, Michael K Bamat, Reid W von Borstel
Uridine triacetate has been shown to be an effective antidote against mortality and toxicity caused by either overdoses or exaggerated susceptibility to the widely used anticancer agents 5-fluorouracil (5-FU) and capecitabine. However, a direct assessment of efficacy based on when emergency treatment was initiated was not clinically feasible. In this study we used mouse models of 5-FU overdose and of dihydropyrimidine dehydrogenase (DPD) deficiency to compare the efficacy of uridine triacetate in reducing toxicity and mortality when treatment was initiated at time points from 4 to 144 h after administration of 5-FU...
June 13, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29908243/protective-roles-of-fenofibrate-against-cisplatin-induced-ototoxicity-by-the-rescue-of-peroxisomal-and-mitochondrial-dysfunction
#18
Se-Jin Kim, Channy Park, Joon No Lee, Raekil Park
Cisplatin is an alkylating agent that interferes with DNA replication and kills proliferating carcinogenic cells. Several studies have been conducted to attenuate the side effects of cisplatin; one such side effect in cancer patients undergoing cisplatin chemotherapy is ototoxicity. However, owing to a lack of understanding of the precise mechanism underlying cisplatin-induced side effects, management of cisplatin-induced ototoxicity remains unsolved. We investigated the protective effects of fenofibrate, a PPAR-α activator, on cisplatin-induced ototoxicity...
June 13, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29908239/the-psychostimulant-%C3%A2-cis-4-4-dimethylaminorex-4-4-dmar-interacts-with-human-plasmalemmal-and-vesicular-monoamine-transporters
#19
Julian Maier, Felix P Mayer, Dino Luethi, Marion Holy, Kathrin Jäntsch, Harald Reither, Lena Hirtler, Marius C Hoener, Matthias E Liechti, Christian Pifl, Simon D Brandt, Harald H Sitte
(±)-cis-4,4'-Dimethylaminorex (4,4'-DMAR) is a new psychoactive substance (NPS) that has been associated with 31 fatalities and other adverse events in Europe between June 2013 and February 2014. We used in vitro uptake inhibition and transporter release assays to determine the effects of 4,4'-DMAR on human high-affinity transporters for dopamine (DAT), norepinephrine (NET) and serotonin (SERT). In addition, we assessed its binding affinities to monoamine receptors and transporters. Furthermore, we investigated the interaction of 4,4'-DMAR with the vesicular monoamine transporter 2 (VMAT2) in rat phaeochromocytoma (PC12) cells and synaptic vesicles prepared from human striatum...
June 13, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29908208/nucleic-acids-binding-strategies-of-small-molecules-lessons-from-alkaloids
#20
Anirban Basu, Gopinatha Suresh Kumar
BACKGROUND: Nucleic acids are now important targets for therapeutic intervention. Alkaloids are an important class of molecules that have myriad therapeutic utility. Isoquinoline and benzophenanthridine alkaloids exhibit multiple pharmacological activities which are often related to their strong nucleic acid binding abilities. Therefore, a review of their interaction aspects with varying nucleic acid structures is essential for rational design and development as therapeutic agents. SCOPE OF THE REVIEW: This work reviews the interaction of various therapeutically important isoquinoline and benzophenanthridine alkaloids with nucleic acids...
June 13, 2018: Biochimica et Biophysica Acta
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