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https://www.readbyqxmd.com/read/28719844/phosphate-functionalized-4-4-armchair-cnts-as-novel-drug-delivery-systems-for-alendronate-and-etidronate-anti-osteoporosis-drugs
#1
Zahra Nikfar, Zahra Shariatinia
The ability of (4,4)-armchair CNT and its three phosphate functionalized forms (CNT-nH2PO4, n=1-3) were evaluated as novel drug delivery systems (DDSs) for the two commercially well-known anti-osteoporosis drugs namely alendronate (AL) and etidronate (ET). For this purpose, the DFT calculations were accomplished at both B3LYP and B3PW91 levels using 6-31g(d) basis set. The binding energy was increased by increasing number of H2PO4 moieties attached on the CNT with the most negative binding energy was measured for the carrier containing three phosphate groups...
July 8, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28719615/a-human-tissue-based-functional-assay-platform-to-evaluate-the-immune-function-impact-of-small-molecule-inhibitors-that-target-the-immune-system
#2
Cristina St Pierre, Jane Guo, John D Shin, Laura W Engstrom, Hyun-Hee Lee, Alan Herbert, Laura Surdi, James Baker, Michael Salmon, Sanjiv Shah, J Michael Ellis, Hani Houshyar, Michael A Crackower, Melanie A Kleinschek, Dallas C Jones, Alexandra Hicks, Dennis M Zaller, Stephen E Alves, Ravisankar A Ramadas
While the immune system is essential for the maintenance of the homeostasis, health and survival of humans, aberrant immune responses can lead to chronic inflammatory and autoimmune disorders. Pharmacological modulation of drug targets in the immune system to ameliorate disease also carry a risk of immunosuppression that could lead to adverse outcomes. Therefore, it is important to understand the 'immune fingerprint' of novel therapeutics as they relate to current and, clinically used immunological therapies to better understand their potential therapeutic benefit as well as immunosuppressive ability that might lead to adverse events such as infection risks and cancer...
2017: PloS One
https://www.readbyqxmd.com/read/28719387/pediatric-mitochondrial-diseases-and-the-heart
#3
Gregory M Enns
PURPOSE OF REVIEW: Mitochondrial disorders are an increasingly recognized cause of heart dysfunction, with the primary manifestations being cardiomyopathy and conduction defects. This review focuses on the complex genetics of mitochondrial disease and recently discovered conditions that affect mitochondrial function. RECENT FINDINGS: Next-generation sequencing techniques, especially whole-exome sequencing, have led to the discovery of a number of conditions that cause mitochondrial dysfunction and subsequent cardiac abnormalities...
July 17, 2017: Current Opinion in Pediatrics
https://www.readbyqxmd.com/read/28719360/alzheimer-s-disease-dawn-of-a-new-era
#4
Farideh Amirrad, Emira Bousoik, Kiumars Shamloo, Hassan Al-Shiyab, Viet-Huong V Nguyen, Hamidreza Montazeri Aliabadi
Alzheimer's disease (AD) is an irreversible neurodegenerative disease characterized by a progressive decline in cognition and memory, leading to significant impairment in daily activities and ultimately death. It is the most common cause of dementia, the prevalence of which increases with age; however, age is not the only predisposing factor. The pathology of this cognitive impairing disease is still not completely understood, which has limited the development of valid therapeutic options. Recent years have witnessed a wide range of novel approaches to combat this disease, so that they greatly increased our understanding of the disease and of the unique drug development issues associated with this disease...
2017: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28719354/thymol-and-carvacrol-strongly-inhibit-biofilm-formation-and-growth-of-carbapenemase-producing-gram-negative-bacilli
#5
P Raei, T Pourlak, M Y Memar, N Alizadeh, M Aghamali, E Zeinalzadeh, M Asgharzadeh, H S Kafil
Discovery of novel drugs with new mechanisms of action and without cross-reaction with current therapeutic agents is crucial in the management of infections caused by multi-drug resistant (MDR) bacteria. The aim of the present study was to investigate effects of carvacrol and thymol on biofilm formation and antimicrobial activity against different carbapenemase-producing Gram negative bacilli. The antimicrobial and antibiofilm effect of thymol and carvacrol was investigated against strains harboring different genes related to carbapenemase resistance...
May 20, 2017: Cellular and Molecular Biology
https://www.readbyqxmd.com/read/28719294/molecular-markers-for-sensitive-detection-of-plasmodium-falciparum-asexual-stage-parasites-and-their-application-in-a-malaria-clinical-trial
#6
Fitsum G Tadesse, Kjerstin Lanke, Issa Nebie, Jodie A Schildkraut, Bronner P Gonçalves, Alfred B Tiono, Robert Sauerwein, Chris Drakeley, Teun Bousema, Sanna R Rijpma
Plasmodium falciparum parasite life stages respond differently to antimalarial drugs. Sensitive stage-specific molecular assays may help to examine parasite dynamics at microscopically detectable and submicroscopic parasite densities in epidemiological and clinical studies. In this study, we compared the performance of skeleton-binding protein 1 (SBP1), ring-infected erythrocyte surface antigen, Hyp8, ring-exported protein 1 (REX1), and PHISTb mRNA for detecting ring-stage trophozoite-specific transcripts using quantitative reverse transcriptase polymerase chain reaction...
July 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28719234/the-in-vivo-effects-of-the-cb1-positive-allosteric-modulator-gat229-on-intraocular-pressure-in-ocular-normotensive-and-hypertensive-mice
#7
Elizabeth A Cairns, Anna-Maria Szczesniak, Alex J Straiker, Pushkar M Kulkarni, Roger G Pertwee, Ganesh A Thakur, William H Baldridge, Melanie E M Kelly
PURPOSE: Orthosteric cannabinoid receptor 1 (CB1) activation leads to decreases in intraocular pressure (IOP). However, use of orthosteric CB1 agonists chronically has several disadvantages, limiting their usefulness as clinically relevant drugs. Allosteric modulators interact with topographically distinct sites to orthosteric ligands and may be useful to circumvent some of these disadvantages. The purpose of this study was to investigate the effects of the novel CB1-positive allosteric modulator (PAM) GAT229 on IOP...
July 18, 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28719227/simvastatin-as-an-adjunctive-therapy-to-risperidone-in-treatment-of-autism-a-randomized-double-blind-placebo-controlled-clinical-trial
#8
Ehsan Moazen-Zadeh, Fatemeh Shirzad, Mohammad-Ali Karkhaneh-Yousefi, Rasoul Khezri, Mohammad-Reza Mohammadi, Shahin Akhondzadeh
OBJECTIVES: Providing novel treatments for autism has been a subject of long-standing research. Based on etiopathological findings, we aim at assessing potential therapeutic effects of statins, here simvastatin, on autism symptoms for the first time. METHODS: In this randomized, double-blind, placebo-controlled, parallel-group 10-week clinical trial, 70 drug-free children aged 4 to 12 years old with diagnosis of autistic disorder based on the Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition, Text Revision, who had an Aberrant Behavior Checklist-Community (ABC-C) scale irritability subscale score of ≥12, were equally randomized to receive either simvastatin (20-40 mg/day) or placebo as an adjunct to risperidone (1-2 mg/day) whereas administration of both drugs was started simultaneously from baseline...
July 18, 2017: Journal of Child and Adolescent Psychopharmacology
https://www.readbyqxmd.com/read/28719178/the-therapeutic-role-and-drug-delivery-potential-of-neuroinflammation-as-a-target-in-neurodegenerative-disorders
#9
Abhijeet Singh, Ankit Chokriwal, Madan Mohan Sharma, Devendra Jain, Juhi Saxena, Bjorn John Stephen
Neuroinflammation, the condition associated with the hyper activity of immune cells within the CNS (central nervous system) has recently been linked to a host range of neurodegenerative disorders. Targeting neuroinflammation could be of prime importance as recent research highlights the beneficial aspects associated with modulating the inflammatory mediators associated with the CNS. One of the main obstructions in neuroinflammatory treatments is the hindrance posed by the Blood Brain Barrier for the delivery of drugs...
July 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28719150/can-principles-of-the-surface-potential-be-combined-with-knowledge-of-natural-products-to-reduce-atrial-rhythm-disturbances
#10
EDITORIAL
H Ni, K Narsingani, H Zhang, W R Giles
Long lasting or chronic electrophysiological abnormalities in human atria are significant contributors to morbidity during healthy aging. Although both paroxysmal (brief) and chronic atrial fibrillation (AF) were considered to be benign; the notable association between maintained AF and stroke has resulted in AF now being a target for surgical intervention (ablation) and/or drug therapy. An interesting, forward looking paper from the Elinder Group(1) in this issue of Acta Physiologica reveals novel pharmacological agents and principles that could be the basis for more effective antiarrhythmic therapies for AF...
July 18, 2017: Acta Physiologica
https://www.readbyqxmd.com/read/28719100/deuteration-of-hyperpolarized-%C3%A2-%C3%A2-c-labelled-zymonic-acid-enables-sensitivity-enhanced-dynamic-mri-of-ph
#11
Christian Hundshammer, Stephan Düwel, Simone Köcher, Malte Gersch, Benedikt Feuerecker, Christoph Scheurer, Axel Haase, Steffen J Glaser, Markus Schwaiger, Franz Schilling
Aberrant pH is characteristic of many pathologies such as ischemia, inflammation or cancer. Therefore, a non-invasive and spatially resolved pH determination is valuable for disease diagnosis, characterization of response to treatment and the design of pH-sensitive drug delivery systems. We recently introduced hyperpolarized zymonic acid (ZA) as a novel MRI probe of extracellular pH utilizing dissolution dynamic polarization (DNP) for a more than 10,000-fold NMR signal enhancement. Here we present a strategy to enhance the sensitivity of this approach by deuteration of ZA (ZAd)...
July 18, 2017: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
https://www.readbyqxmd.com/read/28719094/discovery-and-characterization-of-a-novel-tryptophan-hydroxylase-1-inhibitor-as-a-prodrug
#12
Hailong Shi, Yaya Cui, Yifei Qin
Serotonin (5-HT) is an important neurotransmitter and paracrine signaling molecule in the gastrointestinal tract. Two distinct tryptophan hydroxylases (TPH), TPH1 and TPH2 are the rate-limiting enzymes in the 5-HT biosynthesis process. TPH1 expression is mainly limited in the enterochromaffin cells and distributed in peripheries such as the skin and gut, while TPH2 is the predominant isoform in the CNS. In this study, mol002291 was screened as a drug-like compound from the TCM database for the inhibitor of TPH...
July 18, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28719080/near-infrared-quantum-dots-in-biomedical-applications-current-status-and-future-perspective
#13
REVIEW
Peng Zhao, Quan Xu, Jia Tao, Zongwen Jin, Yue Pan, Changmin Yu, Zhiqiang Yu
To address the requirements of biomedical applications including biosensing, bioimaging, and drug delivery, fluorescent nanomaterials served as efficient tools in many cases. Among them, near-infrared quantum dots (NIR QDs) have been used as novel fluorescent labels for their binary advantages of both QDs and NIR light. In this review, through collecting references in recent 10 years, we have introduced basic structures and properties of NIR QDs and summarized the classification and the related synthetic methods...
July 18, 2017: Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology
https://www.readbyqxmd.com/read/28719060/drug-use-and-phylogenetic-clustering-of-hepatitis-c-virus-infection-among-people-who-use-drugs-in-vancouver-canada-a-latent-class-analysis-approach
#14
Brendan Jacka, Bethany Bray, Tanya L Applegate, Brandon Dl Marshall, Viviane Dias Lima, Kanna Hayashi, Kora DeBeck, Jayna Raghwani, P Richard Harrigan, Mel Krajden, Julio Montaner, Jason Grebely
BACKGROUND: This study estimated latent classes (i.e., unobserved subgroups in a population) of people who use drugs in Vancouver, Canada and examined how these classes relate to phylogenetic clustering of hepatitis C virus (HCV) infection. METHODS: HCV antibody positive people who use drugs from two cohorts in Vancouver, Canada (1996-2012) with a Core-E2 sequence were included. Time-stamped phylogenetic trees were inferred and phylogenetic clustering was determined by time to most common recent ancestor...
July 18, 2017: Journal of Viral Hepatitis
https://www.readbyqxmd.com/read/28719033/identification-of-driver-copy-number-alterations-in-diverse-cancer-types-and-application-in-drug-repositioning
#15
Wenbin Zhou, Zhangxiang Zhao, Ruiping Wang, Yue Han, Chengyu Wang, Fan Yang, Ya Han, Haihai Liang, Lishuang Qi, Chenguang Wang, Zheng Guo, Yunyan Gu
Results from numerous studies suggest an important role for somatic copy number alterations (SCNAs) in cancer progression. Our work aimed to identify the drivers (oncogenes or tumor suppressor genes) that reside in recurrently aberrant genomic regions, including a large number of genes or non-coding genes, which remain a challenge for decoding the SCNAs involved in carcinogenesis. Here, we propose a new approach to comprehensively identify drivers, using 8740 cancer samples involving 18 cancer types from The Cancer Genome Atlas (TCGA)...
July 18, 2017: Molecular Oncology
https://www.readbyqxmd.com/read/28718902/pluripotent-stem-cell-based-platforms-in-cardiac-disease-modeling-and-drug-testing
#16
N Shaheen, A Shiti, L Gepstein
The ability to generate patient/disease-specific human pluripotent stem cell (hPSC)-derived cardiomyocytes (hPSC-CMs) brings a unique value to the fields of cardiac disease modeling, drug testing, drug discovery, and precision medicine. Further integration of emerging innovative technologies such as developmental-biology inspired differentiation into chamber-specific cardiomyocyte subtypes, genome-editing, tissue-engineering, and novel functional phenotyping methodologies should facilitate even more advanced investigations...
August 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28718829/aspirin-prevention-of-colorectal-cancer-focus-on-nf-%C3%AE%C2%BAb-signalling-and-the-nucleolus
#17
REVIEW
Jingyu Chen, Lesley A Stark
Overwhelming evidence indicates that aspirin and related non-steroidal anti-inflammatory drugs (NSAIDs) have anti-tumour activity and the potential to prevent cancer, particularly colorectal cancer. However, the mechanisms underlying this effect remain hypothetical. Dysregulation of the nuclear factor-kappaB (NF-κB) transcription factor is a common event in many cancer types which contributes to tumour initiation and progression by driving expression of pro-proliferative/anti-apoptotic genes. In this review, we will focus on the current knowledge regarding NSAID effects on the NF-κB signalling pathway in pre-cancerous and cancerous lesions, and the evidence that these effects contribute to the anti-tumour activity of the agents...
July 18, 2017: Biomedicines
https://www.readbyqxmd.com/read/28718812/therapeutic-efficacy-of-the-novel-stimuli-sensitive-nano-ferritins-containing-doxorubicin-in-a-head-and-neck-cancer-model
#18
Verena Damiani, Elisabetta Falvo, Giulio Fracasso, Luca Federici, Martina Pitea, Vincenzo De Laurenzi, Gianluca Sala, Pierpaolo Ceci
Doxorubicin is employed alone or in combination for the treatment of several hematological and solid malignancies; despite its efficacy, there are associated cardiotoxicity limits both in its application in patients with heart disease risk factors and also in its long-term use. HFt-MP-PAS40 is a genetically engineered human ferritin heavy chain (HFt)-based construct able to efficiently entrap and deliver doxorubicin to cancer cells. HF-MP-PAS contains a short motif sequence (defined as MP) responsive to proteolytic cleavage by tumor matrix metalloproteases (MMPs), located between each HFt subunit and a masking polypeptide sequence rich in proline (P), alanine (A), and serine (S) residues (PAS)...
July 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28718806/the-inhibitory-activity-of-luzonicosides-from-the-starfish-echinaster-luzonicus-against-human-melanoma-cells
#19
Olesya S Malyarenko, Sergey A Dyshlovoy, Alla A Kicha, Natalia V Ivanchina, Timofey V Malyarenko, Bokemeyer Carsten, von Amsberg Gunhild, Valentin A Stonik, Svetlana P Ermakova
Malignant melanoma is the most dangerous form of skin cancer, with a rapidly increasing incidence rate. Despite recent advances in melanoma research following the approval of several novel targeted and immuno-therapies, the majority of oncological patients will ultimately perish from the disease. Thus, new effective drugs are still required. Starfish steroid glycosides possess different biological activities, including antitumor activity. The current study focused on the determination of the in vitro inhibitory activity and the mechanism of action of cyclic steroid glycosides isolated from the starfish Echinaster luzonicus-luzonicoside A (LuzA) and luzonicoside D (LuzD)-in human melanoma RPMI-7951 and SK-Mel-28 cell lines...
July 18, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28718777/an-assembly-and-interaction-of-upconversion-and-plasmonic-nanoparticles-on-organometallic-nanofibers-enhanced-multicolor-upconversion-downshifting-emission-and-plasmonic-effect
#20
Priyam Singh, Praveen Kumar Shahi, Rajiv Prakash, S B Rai
We herein present a novel inorganic-organic hybrid nanoparticle (HNPs) constituted of inorganic NPs, NaY0.78Er0.02Yb0.2F4, and organometallic nanofiber, Tb(ASA)3Phen (TAP). The X-ray diffraction, Fourier transform infrared absorption and TEM analyse reveal that, the prepared ultrafine upconversion nanoparticles {UCNPs (6-9 nm)} are dispersed on the surface of TAP nanofibers. We observe that addition of TAP in UCNPs, effectively prevents the surface quenching to boost the UC intensity and enables tuning of UC emission from green to red region by controlling the phonon frequency around Er3+ ion...
July 18, 2017: Nanotechnology
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