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https://www.readbyqxmd.com/read/28749624/synthesis-characterization-and-evaluation-of-cytotoxic-effects-of-novel-hybrid-steroidal-heterocycles-as-peg-based-nanoparticles
#1
Mervat M Abd Elhalim, Nasser S M Ismail, Shaymaa M M Yahya, Yasmin Y Omar, Ahmed A Abd Rabou, Deena S Lasheen, Mahmoud F Zawrah, Gamal A Elmegeed
Anticancer agents featuring hybrid molecules can improve effectiveness and diminish drug resistance. The current study aimed to introduce newly synthesized heterocyclic steroids of promising anticancer effects loaded in polyethylene glycol (PEG)•based nanoparticles form. Several heterocyclic steroids (1-9) were synthesized via multicomponent reactions (MCRs) and confirmed via the analytical and spectral data. Compounds 1, 2, 3, 4, 5, 6, 7 and 9, were investigated individually in their free and PEG based nano-size hybrid forms as anticancer agents against three human cell lines: hepatocellular carcinoma cells (HepG2); breast cancer cells (MCF-7); and colon cancer cells (HCT116)...
July 27, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28749594/seizure-activity-per-se-does-not-induce-tissue-damage-markers-in-human-neocortical-focal-epilepsy
#2
Laura Rossini, Rita Garbelli, Vadym Gnatkovsky, Giuseppe Didato, Flavio Villani, Roberto Spreafico, Francesco Deleo, Giorgio Lo Russo, Giovanni Tringali, Francesca Gozzo, Laura Tassi, Marco de Curtis
Objective The contribute of recurring seizures to the progression of epileptogenesis is debated. Seizure-induced brain damage is not conclusively demonstrated both in humans and in animal models of epilepsy. We evaluated the expression of brain injury biomarkers on post-surgical brain tissue obtained from 20 patients with frequent seizures and a long history of drug-resistant focal epilepsy. Methods The expression patterns of specific glial, neuronal and inflammatory molecules was evaluated by immunohistochemistry in the core of type II focal cortical dysplasias (FCD-II), at the FCD boundary (perilesion) and in the adjacent normal-appearing area included in the epileptogenic region...
July 27, 2017: Annals of Neurology
https://www.readbyqxmd.com/read/28749581/prediction-of-transporter-mediated-drug-drug-interactions-for-baricitinib
#3
Maria M Posada, Ellen A Cannady, Christopher D Payne, Xin Zhang, James A Bacon, Y Anne Pak, J William Higgins, Nazila Shahri, Stephen D Hall, Kathleen M Hillgren
Baricitinib, an oral selective Janus kinase 1 and 2 inhibitor, undergoes active renal tubular secretion. Baricitinib was not predicted to inhibit hepatic and renal uptake and efflux drug transporters, based on the ratio of the unbound maximum eliminating-organ inlet concentration and the in vitro half-maximal inhibitory concentrations (IC50 ). In vitro, baricitinib was a substrate for organic anion transporter (OAT)3, multidrug and toxin extrusion protein (MATE)2-K, P-glycoprotein (P-gp), and breast cancer resistance protein (BCRP)...
July 27, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/28749544/combined-eeg-fmri-and-esi-improves-localisation-of-paediatric-focal-epilepsy
#4
Maria Centeno, Tim M Tierney, Suejen Perani, Elhum A Shamshiri, Kelly StPier, Charlotte Wilkinson, Daniel Konn, Serge Vulliemoz, Frédéric Grouiller, Louis Lemieux, Ronit M Pressler, Christopher A Clark, J Helen Cross, David W Carmichael
Objective Surgical treatment in epilepsy is effective if the epileptogenic zone (EZ) can be correctly localized and characterized. Here we use simultaneous Electroencephalography-functional MRI (EEG-fMRI) data to derive EEG-fMRI and Electrical Source Imaging (ESI) maps. Their yield and their individual and combined ability to 1) localize the epileptogenic zone and 2) predict seizure outcome was then evaluated. Methods Fifty-three children with drug-resistant epilepsy underwent EEG-fMRI. Interictal discharges were mapped using both EEG-fMRI haemodynamic responses and Electrical Source Imaging (ESI)...
July 27, 2017: Annals of Neurology
https://www.readbyqxmd.com/read/28749468/wwox-sensitises-ovarian-cancer-cells-to-paclitaxel-via-modulation-of-the-er-stress-response
#5
Szymon Janczar, Jaya Nautiyal, Yi Xiao, Edward Curry, Mingjun Sun, Elisa Zanini, Adam Jw Paige, Hani Gabra
There are clear gaps in our understanding of genes and pathways through which cancer cells facilitate survival strategies as they become chemoresistant. Paclitaxel is used in the treatment of many cancers, but development of drug resistance is common. Along with being an antimitotic agent paclitaxel also activates endoplasmic reticulum (ER) stress. Here, we examine the role of WWOX (WW domain containing oxidoreductase), a gene frequently lost in several cancers, in mediating paclitaxel response. We examine the ER stress-mediated apoptotic response to paclitaxel in WWOX-transfected epithelial ovarian cancer (EOC) cells and following siRNA knockdown of WWOX...
July 27, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28749461/dnmt1-maintained-hypermethylation-of-kr%C3%A3-ppel-like-factor-5-involves-in-the-progression-of-clear-cell-renal-cell-carcinoma
#6
Rong-Jie Fu, Wei He, Xiao-Bo Wang, Lei Li, Huan-Bin Zhao, Xiao-Ye Liu, Zhi Pang, Guo-Qiang Chen, Lei Huang, Ke-Wen Zhao
Clear cell renal cell carcinoma (ccRCC) is the major subtype of renal cell carcinoma (RCC) that is resistant to conventional radiation and chemotherapy. It is a challenge to explore effective therapeutic targets and drugs for this kind of cancer. Transcription factor Krüppel-like factor 5 (KLF5) exerts diverse functions in various tumor types. By analyzing cohorts of the Cancer Genome Atlas (TCGA) data sets, we find that KLF5 expression is suppressed in ccRCC patients and higher level of KLF5 expression is associated with better prognostic outcome...
July 27, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28749433/hbv-drug-resistance-substitutions-existed-before-the-clinical-approval-of-nucleos-t-ide-analogues-a-bioinformatic-analysis-by-genbank-data-mining
#7
Xizhan Xu, Kuanhui Xiang, Mingze Su, Yao Li, Wei Ji, Yutang Li, Hui Zhuang, Tong Li
Naturally occurring nucleos(t)ide analogue resistance (NUCr) substitution frequencies in the reverse transcriptase (RT) of the hepatitis B virus (HBV) were studied extensively after the clinical approval of nucleos(t)ide analogues (NUCs; year of approval 1998). We aimed to study NUCr substitutions in HBV RT sequences obtained before 1998 and better understand the evolution of RT sequences without NUC pressures. Our strategy was to retrieve HBV sequences from GenBank deposited before 1998. The initial search used the keywords "hepatitis B virus" or "HBV" and 1139 sequences were found...
July 27, 2017: Viruses
https://www.readbyqxmd.com/read/28749390/extensively-drug-resistant-tuberculosis-in-india-current-evidence-on-diagnosis-management
#8
REVIEW
Rajendra Prasad, Abhijeet Singh, Viswesvaran Balasubramanian, Nikhil Gupta
Emergence of extensively drug-resistant tuberculosis (XDR-TB) has significantly threatened to jeopardize global efforts to control TB, especially in HIV endemic regions. XDR-TB is mainly an iatrogenically created issue, and understanding the epidemiological and risk factors associated with it is of paramount importance in curbing this menace. Emergence of this deadly phenomenon can be prevented by prompt diagnosis and effective treatment with second-line drugs in rifampicin-resistant TB (RR-TB) as well as multidrug-resistant TB (MDR-TB) patients...
March 2017: Indian Journal of Medical Research
https://www.readbyqxmd.com/read/28749272/ketamine-medetomidine-and-ketamine-medetomidine-midazolam-anesthesia-in-captive-cheetahs-acinonyx-jubatus-comparison-of-blood-pressure-and-kidney-blood-flow
#9
Julia Stagegaard, Arne Hørlyck, Helle B Hydeskov, Mads F Bertelsen
Six clinically healthy captive cheetahs ( Acinonyx jubatus ) were anesthetized twice using two different drug combinations to investigate if blood pressure and kidney blood flow are affected by medetomidine dosage. Protocol KM (2.0 mg/kg ketamine and 0.05 mg/kg medetomidine) was compared with protocol KMM (2.0 mg/kg ketamine, 0.02 mg/kg medetomidine, and 0.1 mg/kg midazolam). Heart rate (HR), respiratory rate (RR), body temperature, end-tidal carbon dioxide pressure (ETCO2), and anesthetic depth were monitored every 10 min...
June 2017: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
https://www.readbyqxmd.com/read/28749255/pharmacokinetics-of-orally-administered-voriconazole-in-african-penguins-spheniscus-demersus-after-single-and-multiple-doses
#10
Michael W Hyatt, Nathan P Wiederhold, William W Hope, Katharine E Stott
Aspergillosis is a common respiratory fungal disease in African penguins ( Spheniscus demersus ) under managed care, and treatment failures with itraconazole due to drug resistance are increasingly common, leading to recent use of voriconazole. Empirical dosing with voriconazole based on other avian studies has resulted in adverse clinical drug effects in penguins. The objective of this study was to determine oral voriconazole pharmacokinetics (PK) in African penguins (n = 18). Single and once daily multiple oral doses of 5 mg/kg voriconazole were evaluated with a 4-mo washout period between trials...
June 2017: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
https://www.readbyqxmd.com/read/28749251/identification-of-spirocyclic-or-phosphate-substituted-quinolizine-derivatives-as-novel-hiv-1-integrase-inhibitors-a-patent-evaluation-of-wo2016094197a1-wo2016094198a1-and-wo2016154527a1
#11
Xiqiang Cheng, Ping Gao, Lin Sun, Ye Tian, Peng Zhan, Xinyong Liu
Highly active antiretroviral therapy (HAART) has been widely adopted to control the HIV-1 infection successfully. HIV-1 integrase (IN) inhibitors are primary drugs in HAART regimens targeting integration step in the HIV-1 life cycle. However, due to the emergence of viral resistance and cross-resistance amongst drugs, there is a pressing need for new and potent IN inhibitors. This review covers the three patents describing spirocyclic and phosphate substituted quinolizine derivatives as novel HIV-1 IN inhibitors for the discovery of new anti-HIV-1 drug candidates...
July 27, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28749250/discovery-of-thalicthuberine-as-a-novel-antimitotic-agent-from-nature-that-disrupts-microtubule-dynamics-and-induces-apoptosis-in-prostate-cancer-cells
#12
Claire Levrier, Anja Rockstroh, Brian Gabrielli, Maria Kavallaris, Melanie Lehman, Rohan A Davis, Martin C Sadowski, Colleen C Nelson
We report for the first time the mechanism of action of the natural product thalicthuberine (TH) in prostate and cervical cancer cells. TH induced a strong accumulation of LNCaP cells in mitosis, severe mitotic spindle defects and asymmetric cell divisions, ultimately leading to mitotic catastrophe accompanied by cell death through apoptosis. However, unlike microtubule-binding drugs (vinblastine and paclitaxel), TH did not directly inhibit tubulin polymerization when tested in a cell-free system, whereas it reduced cellular microtubule polymer mass in LNCaP cells...
July 27, 2017: Cell Cycle
https://www.readbyqxmd.com/read/28749197/cardiovascular-benefits-and-safety-of-non-insulin-medications-used-in-the-treatment-of-type-2-diabetes-mellitus
#13
Srikanth Yandrapalli, George Jolly, Adam Horblitt, Abdallah Sanaani, Wilbert S Aronow
Diabetes mellitus is a growing in exponential proportions. If the current growth trend continues, it may result in every third adult in the United States having diabetes mellitus by 2050, and every 10(th) adult worldwide. Type 2 diabetes mellitus (T2DM) confers a 2- to 3-fold increased risk of cardiovascular (CV) events compared with non-diabetic patients, and CV mortality is responsible for around 80% mortality in this population. Patients with T2DM can have other features of insulin resistance-metabolic syndrome like hypertension, lipid abnormalities, and obesity which are all associated with increased CV disease and stroke risk even in the absence of T2DM...
July 27, 2017: Postgraduate Medicine
https://www.readbyqxmd.com/read/28749195/hippo-pathway-contributes-to-cisplatin-resistant-induced-emt-in-nasopharyngeal-carcinoma-cells
#14
Shuo Li, Xiaomeng Zhang, Rongkai Zhang, Zibin Liang, Wei Liao, Zhengde Du, Chunsheng Gao, Fei Liu, Yunping Fan, Haiyu Hong
Nasopharyngeal carcinoma (NPC) is a kind of head-neck malignant tumor derived from the nasopharyngeal epithelium and is mainly prevalent in Southern China and Southeast Asia countries. Cisplatin (DDP) provides the first-line therapeutic administration in NPC patients. However, chemoresistance has been a main barrier and caused bad treatment outcome in NPC therapy. To understand the molecular mechanism of acquired resistance to DDP, multiple methods were performed to examine the morphocytology and molecular changes in DDP-resistant NPC cells...
July 27, 2017: Cell Cycle
https://www.readbyqxmd.com/read/28749169/effects-of-sodium-glucose-cotransporter-2-inhibitors-on-serum-uric-acid-in-type-2-diabetes-mellitus
#15
Hala Ahmadieh, Sami Azar
Hyperuricemia has been linked to metabolic syndrome, cardiovascular disease, and chronic kidney disease. Hyperuricemia and type 2 diabetes mellitus were inter-related, type 2 diabetes mellitus was more at risk of having a higher serum uric acid level, and also individuals with higher serum uric acid had higher risk of developing type 2 diabetes in the future. Insulin resistance seems to play an important role in the causal relationship between metabolic syndrome, type 2 diabetes, and hyperuricemia. Oral diabetic drugs that would have additional beneficial effects on reducing serum uric acid levels are of importance...
July 27, 2017: Diabetes Technology & Therapeutics
https://www.readbyqxmd.com/read/28748919/changing-concepts-in-hypertension-management
#16
REVIEW
P S Gudsoorkar, S W Tobe
Hypertension is the most common modifiable risk factor for cardiovascular disease and death, and lowering blood pressure with anti-hypertensive drugs reduces target organ damage and prevents cardiovascular disease outcomes. The recent trials SPRINT and HOPE-3 will lead to changes in the way we manage hypertension and impact on clinical practice guidelines. These studies also demonstrate the shift toward automated blood pressure measurements. We have reviewed these studies and others to put them in context with the guidelines that have come before and to describe how they will impact on hypertension treatment thresholds and targets, the treatment of hypertension in the elderly, and changing approaches to the management of hypertension including resistant hypertension...
July 27, 2017: Journal of Human Hypertension
https://www.readbyqxmd.com/read/28748768/allosteric-targeting-of-aurora-a-kinase-using-small-molecules-a-step-forward-towards-next-generation-medicines
#17
Resmi C Panicker, Anthony G Coyne, Rajavel Srinivasan
Aurora A (AurA) kinase is a key mitotic protein essential for carrying out numerous cellular functions. Overexpression or malfunction of this enzyme results in numerous human diseases most notably in cancer. Several small molecule inhibitors targeting the ATP binding site of this enzyme are in various stages of clinical development. However, ATP binding site inhibitors can result in selectivity problems often leading to undesirable off-target effects. Moreover, these drugs are prone to drug resistance problem rendering them unfit for long-term administration...
July 27, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28748603/graphene-quantum-dots-downregulate-multiple-multidrug-resistant-genes-via-interacting-with-their-c-rich-promoters
#18
Chao Luo, Yanfang Li, Lijuan Guo, Fangwei Zhang, Hui Liu, Jiali Zhang, Jing Zheng, Jingyan Zhang, Shouwu Guo
Multidrug resistance (MDR) is the major factor in the failure of many forms of chemotherapy, mostly due to the increased efflux of anticancer drugs that mediated by ATP-binding cassette (ABC) transporters. Therefore, inhibiting ABC transporters is one of effective methods of overcoming MDR. However, high enrichment of ABC transporters in cells and their broad substrate spectra made to circumvent MDR are almost insurmountable by a single specific ABC transporter inhibitor. Here, this study demonstrates that graphene quantum dots (GQDs) could downregulate the expressions of P-glycoprotein, multidrug resistance protein MRP1, and breast cancer resistance protein genes via interacting with C-rich regions of their promoters...
July 27, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28748397/activity-of-the-novel-siderophore-cephalosporin-cefiderocol-against-multidrug-resistant-gram-negative-pathogens
#19
J Dobias, V Dénervaud-Tendon, L Poirel, P Nordmann
The novel siderophore cephalosporin cefiderocol (S-649266) with potent activity against Gram-negative pathogens was recently developed (Shionogi & Co., Ltd.). Here, we evaluated the activity of this new molecule and comparators against a collection of previously characterized Gram-negative isolates using broth microdilution panels. A total of 753 clinical multidrug-resistant Gram-negative isolates collected from hospitals worldwide were tested against cefiderocol and antibiotic comparators (ceftolozane-tazobactam [CT], meropenem [MEM], ceftazidime [CAZ], ceftazidime-avibactam [CZA], colistin [CST], aztreonam [ATM], amikacin [AMK], ciprofloxacin [CIP], cefepime [FEP], and tigecycline [TGC]) for their susceptibility...
July 26, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28748348/impact-of-genetic-polymorphisms-on-phenytoin-pharmacokinetics-and-clinical-outcomes-in-the-middle-east-and-north-africa-region
#20
REVIEW
Renée Dagenais, Kyle John Wilby, Hazem Elewa, Mary H H Ensom
BACKGROUND: Genetic polymorphisms are known to influence outcomes with phenytoin yet effects in the Middle East and North Africa region are poorly understood. OBJECTIVES: The objective of this systematic review was to evaluate the impact of genetic polymorphisms on phenytoin pharmacokinetics and clinical outcomes in populations originating from the Middle East and North Africa region, and to characterize genotypic and allelic frequencies within the region for genetic polymorphisms assessed...
July 26, 2017: Drugs in R&D
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