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https://www.readbyqxmd.com/read/29793150/exploring-the-victimization%C3%A2-early-substance-misuse-relationship-in-search-of-moderating-and-mediating-effects
#1
Glenn D Walters, Dorothy L Espelage
This study was designed to address two research questions. The first research question asked whether physical abuse victimization at the hands of parents/guardians, bullying victimization at the hands of peers, and the abuse x bullying interaction encouraged early involvement in substance misuse. The second research question inquired as to whether the victimization‒substance misuse relationship was mediated by variables proposed by various theories and research studies-specifically, cognitive impulsivity, negative affect, and low self-esteem...
May 21, 2018: Child Abuse & Neglect
https://www.readbyqxmd.com/read/29792929/recent-advances-in-intra-articular-drug-delivery-systems-for-osteoarthritis-therapy
#2
REVIEW
Pierre Maudens, Olivier Jordan, Eric Allémann
Osteoarthritis (OA) is the most common degenerative disease of the joint. Despite many reports and numerous clinical trials, OA is not entirely understood, and there is no effective treatment available for this disease. To satisfy this unmet medical need, drug delivery systems (DDSs) containing disease-modifying OA drugs (DMOADs) for intra-articular (IA) administration are required to improve the health of OA patients. DDSs should provide controlled and/or sustained drug release, enabling long-term treatment with a reduced number of injections...
May 21, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29792889/ros-triggered-degradable-iron-chelating-nanogels-safely-improving-iron-elimination-in-vivo
#3
Zhi Liu, Jing Qiao, Tamas Nagy, May P Xiong
Iron-mediated generation of highly toxic Reactive Oxygen Species (ROS) plays a major role in the process leading to iron overload-related diseases. The long-term subcutaneous administration of Deferoxamine (DFO) is currently clinically-approved to improve patient symptoms and survival. However, non-specific toxicity and short circulation times of the drug in humans often leads to poor patient compliance. Herein, thioketal-based ROS-responsive polymeric nanogels containing DFO moieties (rNG-DFO) were designed to chelate iron and to degrade under oxidative stimuli into fragments <10 nm to enhance excretion of iron-bound chelates...
May 21, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29792714/docking-screens-for-dual-inhibitors-of-disparate-drug-targets-for-parkinson-s-disease
#4
Mariama Jaiteh, Alexey Zeifman, Marcus Saarinen, Per Svenningsson, José M Brea, Maria Isabel Loza, Jens Carlsson
Modulation of multiple biological targets with a single drug can lead to synergistic therapeutic effects and has been demonstrated to be essential for efficient treatment of CNS disorders. However, rational design of compounds that interact with several targets is very challenging. Here, we demonstrate that structure-based virtual screening can guide the discovery of multi-target ligands of unrelated proteins relevant for Parkinson's disease. A library with 5.4 million molecules was docked to crystal structures of the A2A adenosine receptor (A2AAR) and monoamine oxidase B (MAO-B)...
May 24, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29792572/galnac-sirna-conjugates-leading-the-way-for-delivery-of-rnai-therapeutics
#5
Aaron D Springer, Steven F Dowdy
Short-interfering RNA (siRNA)-induced RNAi responses have great potential to treat a wide variety of human diseases from cancer to pandemic viral outbreaks to Parkinson's Disease. However, before siRNAs can become drugs, they must overcome a billion years of evolutionary defenses designed to keep invading RNAs on the outside cells from getting to the inside of cells. Not surprisingly, significant effort has been placed in developing a wide array of delivery technologies. Foremost of these has been the development of N-acetylgalactosamine (GalNAc) siRNA conjugates for delivery to liver...
May 24, 2018: Nucleic Acid Therapeutics
https://www.readbyqxmd.com/read/29792360/newer-human-inosine-5-monophosphate-dehydrogenase-2-himpdh2-inhibitors-as-potential-anticancer-agents
#6
Chetan P Shah, Prashant S Kharkar
Human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2), being an age-old target, has attracted attention recently for anticancer drug development. Mycophenolic acid (MPA), a well-known immunosuppressant drug, was used a lead structure to design and develop modestly potent and selective analogues. The steep structure-activity relationship (SAR) requirements of the lead molecule left little scope to synthesise newer analogues. Here, newer MPA amides were designed, synthesised and evaluated for hIMPDH2 inhibition and cellular efficacy in breast, prostate and glioblastoma cell lines...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29792353/gastroretentive-raft-liquid-delivery-system-as-a-new-approach-to-release-extension-for-carrier-mediated-drug
#7
Samar M Abouelatta, Ahmed A Aboelwafa, Omaima N El-Gazayerly
Gabapentin (GBP), an antiepileptic and anti-neuropathic agent, suffers from short half-life (5-7 h), has narrow absorption window, and is absorbed via carrier-mediated mechanism resulting in frequent dosing, poor compliance, and poor bioavailability (<60%). Moreover, GBP is a freely water-soluble drug, thus it is considered a challenging candidate to be formulated as extended release dosage form. In this study, raft forming systems were investigated as a potential drug delivery system for prolonging gastric residence time of GBP...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29792292/identifying-medication-management-smartphone-app-features-suitable-for-young-adults-with-developmental-disabilities-delphi-consensus-study
#8
Teresa M Salgado, Alexa Fedrigon, Donna Riccio Omichinski, Michelle A Meade, Karen B Farris
BACKGROUND: Smartphone apps can be a tool to facilitate independent medication management among persons with developmental disabilities. At present, multiple medication management apps exist in the market, but only 1 has been specifically designed for persons with developmental disabilities. Before initiating further app development targeting this population, input from stakeholders including persons with developmental disabilities, caregivers, and professionals regarding the most preferred features should be obtained...
May 23, 2018: JMIR MHealth and UHealth
https://www.readbyqxmd.com/read/29792196/ethnozoological-study-of-traditional-medicinal-appreciation-of-animals-and-their-products-among-the-indigenous-people-of-metema-woreda-north-western-ethiopia
#9
Fasil Adugna Kendie, Sileshi Andualem Mekuriaw, Melkamu Andargie Dagnew
BACKGROUND: Using animals for different purposes goes back to the dawn of mankind. Animals served as a source of food, medicine, and clothing for humans and provided other services. This study was designed to undertake a cross-sectional ethnozoological field survey among the residents of Metema Woreda from November 2015 to May 2016. METHODS: Data were collected through studied questionnaires, interviews, and focus group discussions with 36 purposively selected respondents...
May 23, 2018: Journal of Ethnobiology and Ethnomedicine
https://www.readbyqxmd.com/read/29792151/pyrazole-and-imidazo-1-2-b-pyrazole-derivatives-as-new-potential-anti-tuberculosis-agents
#10
Elda Meta, Chiara Brullo, Michele Tonelli, Scott G Franzblau, Yuehong Wang, Rui Ma, Wan Baojie, Beatrice Silvia Orena, Maria Rosalia Pasca, Olga Bruno
BACKGROUND: We screened a large library of differently decorated imidazo-pyrazole and pyrazole derivatives as possible new antitubercular agents and this preliminary screening showed that many compounds are able to totally inhibit Mycobacterium growth (>90 %). Among the most active compounds, we selected some new possible hits based on their similarities and, at the same time, their novelty respect to the pipeline drugs. METHODS: In order to increase the potency and obtain more information about structure activity relationship (SAR), we design and synthesized three new series of compounds (2a-e, 3a-e, and 4a-l)...
May 23, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29792145/1-2-4-oxadiazole-as-a-privileged-scaffold-for-anti-inflammatory-and-analgesic-activities-a-complete-review
#11
Gita Chawla, Chanda Ranjan, Anees A Siddiqui
1,2,4-Oxadiazole is one of the important heterocycles used by medicinal chemists in designing a new therapeutic molecule. The compounds containing this nucleus are reported to have a wide range of pharmaceutical and biological applications including anti-inflammatory and analgesic activities. The fused and pendent 1,2,4-oxadiazole moiety has been traced in a number of well established, commercially available drugs. This review article provides an up to date information about techniques adopted for the synthesis of 1,2,4-oxadiazoles, and their therapeutic importance as an anti-inflammatory and analgesic agents...
May 23, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29792142/collaboration-of-the-joint-research-centre-and-the-european-customs-laboratories-for-identification-of-new-psychoactive-substances
#12
Claude Guillou, Fabiano Reniero, Joana Lobo Pereira Vicente, Margaret Holland, Kamil Kolar, Hubert Chassaigne, Salvatore Tirendi, Herve Schepers
The emergence of designer drugs as substances of abuse has seen a dramatic increase over the last few years. Customs officials are responsible for the control of products entering the European Union (EU) market. This control applies to chemicals in general, pharmaceutical products and medicines. Numerous products imported from non-EU countries, often -declared as 'bath salts' or 'fertilizers', may in fact contain new psychoactive substance (NPS). These are not necessarily controlled under international law, but are subject to monitoring in agreement with EU legislation...
May 23, 2018: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/29792137/recent-trends-in-nanocrystals-for-pharmaceutical-applications
#13
Leming Sun, Yanzi Hu, Lianbing Zhang
BACKGROUND: As the quick development of modern methods and technologies currently, more and more drugs have been invented with a better efficiency. However, the poor water solubility has limited the drugs' pharmaceutical application. METHODS: Tremendous research has been put in the design and development of nanocrystals for pharmaceutical applications over the past few decades. The nanocrystals not only have the chance to solve the poor solubility problem, but also could conquer the bioavailability and even the specific delivery problems...
May 23, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29792071/phosphoramidates-and-phosphonamidates-protides-with-antiviral-activity
#14
Magdalena Slusarczyk, Michaela Serpi, Fabrizio Pertusati
Following the first report on the nucleoside phosphoramidate (ProTide) prodrug approach in 1990 by Chris McGuigan, the extensive investigation of ProTide technology has begun in many laboratories. Designed with aim to overcome limitations and the key resistance mechanisms associated with nucleoside analogues used in the clinic (poor cellular uptake, poor conversion to the 5'-monophosphate form), the ProTide approach has been successfully applied to a vast number of nucleoside analogues with antiviral and anticancer activity...
January 2018: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/29792032/a-tict-based-turn-on-fluorogenic-nano-probe-for-realtime-detection-of-serum-albumin-in-physiological-condition
#15
Soham Samanta, Senjuti Halder, Gopal Das
Two, cyanine based fluorescent probes L [(E)-2-(4-(diethylamino)-2-hydroxystyryl)-3-ethyl-1,1-dimethyl-1H-benzo[e]indol-3-ium iodide] and L1 [(E)-3-ethyl-1,1-dimethyl-2-(4-nitrostyryl)-1H-benzo[e]indol-3-ium iodide] have been designed and synthesized. Among these two probes; TICT (twisted intramolecular charge transfer) based probe L can preferentially self-assemble to form nanoaggregates. L displayed a selective TURN-ON fluorescence response towards HSA and BSA in ~100% aqueous PBS buffer medium which is noticeable through naked eye whereas L1 failed to sense these albumin proteins...
May 24, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29791923/inhaled-treprostinil-prodrug-lipid-nanoparticle-formulations-provide-long-acting-pulmonary-vasodilation
#16
Franziska G Leifer, Donna M Konicek, Kuan-Ju Chen, Adam J Plaunt, Dany Salvail, Charles E Laurent, Michel R Corboz, Zhili Li, Richard W Chapman, Walter R Perkins, Vladimir S Malinin
Treprostinil (TRE), a prostanoid analogue approved in the USA for the treatment of pulmonary arterial hypertension, requires continuous infusion or multiple dosing sessions per day for inhaled and oral routes of administration due to its short half-life. The inhaled drug is known to induce adverse systemic and local effects including headache, nausea, cough, and throat irritation which may be due at least in part to transiently high drug concentrations in the lungs and plasma immediately following administration [1]...
May 23, 2018: Drug Research
https://www.readbyqxmd.com/read/29791803/bacteria-activated-janus-particles-driven-by-chemotaxis
#17
Zihan Huang, Pengyu Chen, Guo-Long Zhu, Ye Yang, Ziyang Xu, Li-Tang Yan
In the development of biocompatible nano/micro-motors for drug and cargo delivery, motile bacteria represent an excellent energy source for biomedical applications. Despite intense research of the fabrication of bacteria-based motors, how to effectively utilize the instinctive responses of bacteria to environmental stimuli in the fabrication process, particularly, chemotaxis, remains an urgent and critical issue. Here, by developing a molecular-dynamics model of bacterial chemotaxis, we present an investigation of the transport of a bacteria-activated Janus particle driven by chemotaxis...
May 23, 2018: ACS Nano
https://www.readbyqxmd.com/read/29791472/pioglitazone-abolishes-autistic-like-behaviors-via-the-il-6-pathway
#18
Thiago Berti Kirsten, Renato C Casarin, Maria M Bernardi, Luciano F Felicio
Autism is characterized by social deficits, communication abnormalities, and repetitive behaviors. The risk factors appear to include genetic and environmental conditions, such as prenatal infections and maternal dietary factors. Previous investigations by our group have demonstrated that prenatal exposure to lipopolysaccharide (LPS), which mimics infections by gram-negative bacteria, induces autistic-like behaviors. No effective treatment yet exists for autism. Therefore, we used our rat model to test a possible treatment for autism...
2018: PloS One
https://www.readbyqxmd.com/read/29791433/the-belfast-youth-development-study-byds-a-prospective-cohort-study-of-the-initiation-persistence-and-desistance-of-substance-use-from-adolescence-to-adulthood-in-northern-ireland
#19
Kathryn Higgins, Aisling McLaughlin, Oliver Perra, Claire McCartan, Mark McCann, Andrew Percy, Julie-Ann Jordan
BACKGROUND: Substance misuse persists as a major public health issue worldwide with significant costs for society. The development of interventions requires methodologically sound studies to explore substance misuse causes and consequences. This Cohort description paper outlines the design of the Belfast Youth Development (BYDS), one of the largest cohort studies of its kind in the UK. The study was established to address the need for a long-term prospective cohort study to investigate the initiation, persistence and desistance of substance use, alongside life course processes in adolescence and adulthood...
2018: PloS One
https://www.readbyqxmd.com/read/29790875/visible-light-induced-electropolymerization-of-suspended-hydrogel-bioscaffolds-in-a-microfluidic-chip
#20
Pan Li, Haibo Yu, Na Liu, Feifei Wang, Gwo-Bin Lee, Yuechao Wang, Lianqing Liu, Wen Jung Li
The development of microengineered hydrogels co-cultured with cells in vitro could advance in vivo bio-systems in both structural complexity and functional hierarchy, which holds great promise for applications in regenerative tissues or organs, drug discovery and screening, and bio-sensors or bio-actuators. Traditional hydrogel microfabrication technologies such as ultraviolet (UV) laser or multiphoton laser stereolithography and three-dimensional (3D) printing systems have advanced the development of 3D hydrogel micro-structures but need either expensive and complex equipment, or harsh material selection with limited photoinitiators...
May 23, 2018: Biomaterials Science
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