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https://www.readbyqxmd.com/read/28335551/molecular-basis-for-modulation-of-metabotropic-glutamate-receptors-and-their-drug-actions-by-extracellular-ca-2
#1
REVIEW
Juan Zou, Jason Y Jiang, Jenny J Yang
Metabotropic glutamate receptors (mGluRs) associated with the slow phase of the glutamatergic signaling pathway in neurons of the central nervous system have gained importance as drug targets for chronic neurodegenerative diseases. While extracellular Ca(2+) was reported to exhibit direct activation and modulation via an allosteric site, the identification of those binding sites was challenged by weak binding. Herein, we review the discovery of extracellular Ca(2+) in regulation of mGluRs, summarize the recent developments in probing Ca(2+) binding and its co-regulation of the receptor based on structural and biochemical analysis, and discuss the molecular basis for Ca(2+) to regulate various classes of drug action as well as its importance as an allosteric modulator in mGluRs...
March 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28335550/preparation-of-biodegradable-and-elastic-poly-%C3%AE%C2%B5-caprolactone-co-lactide-copolymers-and-evaluation-as-a-localized-and-sustained-drug-delivery-carrier
#2
Ji Hoon Park, Bo Keun Lee, Seung Hun Park, Mal Geum Kim, Jin Woo Lee, Hye Yun Lee, Hai Bang Lee, Jae Ho Kim, Moon Suk Kim
To develop a biodegradable polymer possessing elasticity and flexibility, we synthesized MPEG-b-(PCL-co-PLA) copolymers (PCxLyA), which display specific rates of flexibility and elasticity. We synthesize the PCxLyA copolymers by ring-opening polymerization of ε-caprolactone and l-lactide. PCxLyA copolymers of various compositions were synthesized with 500,000 molecular weight. The PCxLyA copolymers mechanical properties were dependent on the mole ratio of the ε-caprolactone and l-lactide components. Cyclic tensile tests were carried out to investigate the resistance to creep of PCxLyA specimens after up to 20 deformation cycles to 50% elongation...
March 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28335457/the-epigenetic-link-between-prenatal-adverse-environments-and-neurodevelopmental-disorders
#3
REVIEW
Marija Kundakovic, Ivana Jaric
Prenatal adverse environments, such as maternal stress, toxicological exposures, and viral infections, can disrupt normal brain development and contribute to neurodevelopmental disorders, including schizophrenia, depression, and autism. Increasing evidence shows that these short- and long-term effects of prenatal exposures on brain structure and function are mediated by epigenetic mechanisms. Animal studies demonstrate that prenatal exposure to stress, toxins, viral mimetics, and drugs induces lasting epigenetic changes in the brain, including genes encoding glucocorticoid receptor (Nr3c1) and brain-derived neurotrophic factor (Bdnf)...
March 18, 2017: Genes
https://www.readbyqxmd.com/read/28335429/the-adverse-effect-of-hypertension-in-the-treatment-of-thyroid-cancer-with-multi-kinase-inhibitors
#4
REVIEW
Ole Vincent Ancker, Markus Wehland, Johann Bauer, Manfred Infanger, Daniela Grimm
The treatment of thyroid cancer has promising prospects, mostly through the use of surgical or radioactive iodine therapy. However, some thyroid cancers, such as progressive radioactive iodine-refractory differentiated thyroid carcinoma, are not remediable with conventional types of treatment. In these cases, a treatment regimen with multi-kinase inhibitors is advisable. Unfortunately, clinical trials have shown a large number of patients, treated with multi-kinase inhibitors, being adversely affected by hypertension...
March 14, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28335413/chitin-oligosaccharide-cos-reduces-antibiotics-dose-and-prevents-antibiotics-caused-side-effects-in-adolescent-idiopathic-scoliosis-ais-patients-with-spinal-fusion-surgery
#5
Yang Qu, Jinyu Xu, Haohan Zhou, Rongpeng Dong, Mingyang Kang, Jianwu Zhao
Antibiotics are always considered for surgical site infection (SSI) in adolescent idiopathic scoliosis (AIS) surgery. However, the use of antibiotics often causes the antibiotic resistance of pathogens and side effects. Thus, it is necessary to explore natural products as drug candidates. Chitin Oligosaccharide (COS) has anti-inflammation and anti-bacteria functions. The effects of COS on surgical infection in AIS surgery were investigated. A total of 312 AIS patients were evenly and randomly assigned into control group (CG, each patient took one-gram alternative Azithromycin/Erythromycin/Cloxacillin/Aztreonam/Ceftazidime or combined daily), experiment group (EG, each patient took 20 mg COS and half-dose antibiotics daily), and placebo group (PG, each patient took 20 mg placebo and half-dose antibiotics daily)...
March 14, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28335344/a-targeted-nanoprobe-based-on-carbon-nanotubes-natural-biopolymer-chitosan-composites
#6
Baoyan Wu, Na Zhao
A novel targeting theranostic nanoprobe based on single-walled carbon nanotubes (SWCNTs)-natural biopolymer chitosan composites was developed for cancer cell targeting imaging and fluorescence imaging-guided photodynamic therapy. First, chitosan was respectively conjugated with a tumor-homing molecule folic acid, or a photosensitizing drug pyropheophorbide a using a water-soluble carbodiimide coupling chemistry. Chitosan was fluorescently labeled by fluorescein isothiocyanate via the covalently linkage of the isothiocyanate group with the amino group...
November 17, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335269/galactosylated-liposomes-for-targeted-co-delivery-of-doxorubicin-vimentin-sirna-to-hepatocellular-carcinoma
#7
Hea Ry Oh, Hyun-Young Jo, James S Park, Dong-Eun Kim, Je-Yoel Cho, Pyung-Hwan Kim, Keun-Sik Kim
The combination of therapeutic nucleic acids and chemotherapeutic drugs has shown great promise for cancer therapy. In this study, asialoglycoprotein receptors (ASGPR) targeting-ligand-based liposomes were tested to determine whether they can co-deliver vimentin siRNA and doxorubicin to hepatocellular carcinoma (HCC) selectively. To achieve this goal, we developed an ASGPR receptor targeted co-delivery system called gal-doxorubicin/vimentin siRNA liposome (Gal-DOX/siRNA-L). The Gal-DOX/siRNA-L was created via electrostatic interaction of galactose linked-cationic liposomal doxorubicin (Gal-DOX-L) on vimentin siRNA...
July 30, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335253/soft-interaction-in-liposome-nanocarriers-for-therapeutic-drug-delivery
#8
REVIEW
Domenico Lombardo, Pietro Calandra, Davide Barreca, Salvatore Magazù, Mikhail A Kiselev
The development of smart nanocarriers for the delivery of therapeutic drugs has experienced considerable expansion in recent decades, with the development of new medicines devoted to cancer treatment. In this respect a wide range of strategies can be developed by employing liposome nanocarriers with desired physico-chemical properties that, by exploiting a combination of a number of suitable soft interactions, can facilitate the transit through the biological barriers from the point of administration up to the site of drug action...
June 25, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335244/human-serum-albumin-nanoparticles-for-use-in-cancer-drug-delivery-process-optimization-and-in-vitro-characterization
#9
Nikita Lomis, Susan Westfall, Leila Farahdel, Meenakshi Malhotra, Dominique Shum-Tim, Satya Prakash
Human serum albumin nanoparticles (HSA-NPs) are widely-used drug delivery systems with applications in various diseases, like cancer. For intravenous administration of HSA-NPs, the particle size, surface charge, drug loading and in vitro release kinetics are important parameters for consideration. This study focuses on the development of stable HSA-NPs containing the anti-cancer drug paclitaxel (PTX) via the emulsion-solvent evaporation method using a high-pressure homogenizer. The key parameters for the preparation of PTX-HSA-NPs are: the starting concentrations of HSA, PTX and the organic solvent, including the homogenization pressure and its number cycles, were optimized...
June 15, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335197/cationic-nanoparticles-assembled-from-natural-based-steroid-lipid-for-improved-intracellular-transport-of-sirna-and-pdna
#10
Ruilong Sheng, Xiaoqing Zhuang, Zhao Wang, Amin Cao, Kaili Lin, Julian X X Zhu
Developing new functional biomaterials from biocompatible natural-based resources for gene/drug delivery has attracted increasing attention in recent years. In this work, we prepared a series of cationic nanoparticles (Diosarg-DOPE NPs) by assembly of a natural steroid diosgenin-based cationic lipid (Diosarg) with commercially-available helper lipid 1,2-dioleoyl-sn-glycero-3-phosphorethanolamine (DOPE). These cationic Diosarg-DOPE NPs were able to efficiently bind siRNA and plasmid DNA (pDNA) via electrostatic interactions to form stable, nano-sized cationic lipid nanoparticles instead of lamellar vesicles in aqueous solution...
April 13, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335102/efficacy-of-a-multiplex-paclitaxel-emission-stent-using-a-pluronic-%C3%A2-mixture-membrane-versus-a-covered-metal-stent-in-malignant-biliary-obstruction-a-prospective-randomized-comparative-study
#11
Sung Ill Jang, Se Joon Lee, Seok Jeong, Don Haeng Lee, Myung-Hwan Kim, Hong Jin Yoon, Dong Ki Lee
Background/Aims: A drug-eluting stent for unresectable malignant biliary obstruction was developed to increase stent patency by preventing tumor ingrowth. The safety and efficacy of a new generation of metallic stents covered with a paclitaxel-incorporated membrane using a Pluronic(®) mixture (MSCPM-II) were compared prospectively with those of covered metal stents (CMSs) in patients with malignant biliary obstructions. Methods: This study was initially designed as a prospective randomized trial but was closed early because of a high incidence of early occlusion...
March 24, 2017: Gut and Liver
https://www.readbyqxmd.com/read/28335036/validated-method-for-the-screening-and-quantification-of-baclofen-gabapentin-and-pregabalin-in-human-post-mortem-whole-blood-using-protein-precipitation-and-liquid-chromatography-tandem-mass-spectrometry
#12
Limon Nahar, Amy Smith, Rajan Patel, Rebecca Andrews, Sue Paterson
There has been a rapid increase in the number of prescriptions for baclofen (BLF), gabapentin (GBP) and pregabalin (PGL) in the UK since their introduction to therapy. Recent studies across the European Union and USA have shown the illicit abuse potential of these drugs and deaths have been observed. A simple, reliable and fully validated method was developed for the screening and quantification of BLF, GBP and PGL in human post-mortem (PM) blood. The analytes and their deuterated analogs as internal standard were extracted from blood using a single addition acetonitrile protein precipitation reaction followed by analysis using liquid chromatography-tandem mass spectrometry (LC-MS-MS) with triggered dynamic multiple reaction monitoring mode for simultaneous confirmation and quantification...
March 10, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28335023/qbd-driven-development-and-validation-of-liquid-chromatography-tandem-mass-spectrometric-method-for-the-quantitation-of-sildenafil-in-human-plasma
#13
M Saquib Hasnain, Shaukat Ali Ansari, Shireen Rao, Mohammad Tabish, Mukul Singh, Mohammad Syafiq Abdullah, Mohammed Tahir Ansari
The present work was employing the Quality by Design approach for the development and validation of a LC-MS-MS method to support the clinical advancement in determination of sildenafil in human plasma using lorazepam as an internal standard. Sample preparation involved solid phase extraction and calibration range observed between 3 and 1,700 ng/mL. The method was systematically optimized by employing Box-Behnken design and used mobile phase flow rate, pH and composition of mobile phase as the critical factors, and assessing the design for retention time and peak area as the responses...
February 27, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28334990/insulin-resistance-and-exendin-4-treatment-for-multiple-system-atrophy
#14
Fares Bassil, Marie-Hélène Canron, Anne Vital, Erwan Bezard, Yazhou Li, Nigel H Greig, Seema Gulyani, Dimitrios Kapogiannis, Pierre-Olivier Fernagut, Wassilios G Meissner
Multiple system atrophy is a fatal sporadic adult-onset neurodegenerative disorder with no symptomatic or disease-modifying treatment available. The cytopathological hallmark of multiple system atrophy is the accumulation of α-synuclein aggregates in oligodendrocytes, forming glial cytoplasmic inclusions. Impaired insulin/insulin-like growth factor-1 signalling (IGF-1) and insulin resistance (i.e. decreased insulin/IGF-1) have been reported in other neurodegenerative disorders such as Alzheimer's disease. Increasing evidence also suggests impaired insulin/IGF-1 signalling in multiple system atrophy, as corroborated by increased insulin and IGF-1 plasma concentrations in multiple system atrophy patients and reduced IGF-1 brain levels in a transgenic mouse model of multiple system atrophy...
March 14, 2017: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/28334978/therapeutic-window-of-dopamine-d2-3-receptor-occupancy-to-treat-psychosis-in-alzheimer-s-disease
#15
Suzanne Reeves, Emma McLachlan, Julie Bertrand, Fabrizia D Antonio, Stuart Brownings, Akshay Nair, Suki Greaves, Alan Smith, David Taylor, Joel Dunn, Paul Marsden, Robert Kessler, Robert Howard
Antipsychotic drugs, originally developed to treat schizophrenia, are used to treat psychosis, agitation and aggression in Alzheimer's disease. In the absence of dopamine D2/3 receptor occupancy data to inform antipsychotic prescribing for psychosis in Alzheimer's disease, the mechanisms underpinning antipsychotic efficacy and side effects are poorly understood. This study used a population approach to investigate the relationship between amisulpride blood concentration and central D2/3 occupancy in older people with Alzheimer's disease by combining: (i) pharmacokinetic data (280 venous samples) from a phase I single (50 mg) dose study in healthy older people (n = 20, 65-79 years); (ii) pharmacokinetic, 18F-fallypride D2/3 receptor imaging and clinical outcome data on patients with Alzheimer's disease who were prescribed amisulpride (25-75 mg daily) to treat psychosis as part of an open study (n = 28; 69-92 years; 41 blood samples, five pretreatment scans, 19 post-treatment scans); and (iii) 18F-fallypride imaging of an antipsychotic free Alzheimer's disease control group (n = 10, 78-92 years), to provide additional pretreatment data...
February 4, 2017: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/28334925/simultaneous-lc-ms-ms-determination-of-lopinavir-and-rifabutin-in-human-plasma
#16
Swati Jaiswal, Abhisheak Sharma, Mahendra Shukla, Jawahar Lal
Tuberculosis (TB) with human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome represents the most common infectious diseases worldwide. Anti-TB drugs are used concurrently with antiretroviral drug for treatment of TB-HIV co-morbidities. Due to lower risk of interaction with protease inhibitors, rifabutin is preferred over rifampicin in treatment of HIV and TB co-morbidity. A simple and specific liquid chromatography tandem mass spectrometry method was developed for quantification of rifabutin (RBT) and lopinavir (LPV) simultaneously in human plasma...
March 3, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28334890/application-of-ultrasound-assisted-surfactant-enhanced-emulsification-microextraction-based-on-solidi%C3%AF-cation-of-floating-organic-droplets-and-high-performance-liquid-chromatography-for-preconcentration-and-determination-of-alprazolam-and-chlordiazepoxide-in
#17
Nasser Goudarzi, Monavar Amirnavaee, Mansour Arab Chamjangali, Sahar Farsimadan
An improved microextraction method is proposed on the basis of ultrasound-assisted surfactant-enhanced emulsification and solidification of a floating organic droplet procedure combined with high performance liquid chromatography for the preconcentration and quantification of alprazolam (ALP) and chlordiazepoxide (CHL) present in a number of human serum samples. Several parameters affecting the extraction efficiency were investigated by the Plackett -Burman factorial design as the screening design. Then the response surface methodology based on the Box-Behnken design was used to optimize the effective parameters in the proposed procedure...
March 3, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28334884/improvement-in-the-prognosis-of-ovarian-cancer-in-the-era-before-addition-of-molecular-targeting-therapy
#18
Takako Shimada, Toshiaki Saito, Mototsugu Shimokawa, Kumi Shimamoto, Shuhei Matsushita, Shinichiro Yamaguchi, Kazuya Ariyoshi, Masao Okadome
Objective: The prognosis of ovarian cancer has improved because of platinum- and taxane-containing chemotherapy. We investigated the 5-year disease-specific overall survival and prognostic factors of patients with advanced ovarian cancer to elucidate the change in clinical course of ovarian cancer with the advance of chemotherapy for patients who developed relapse in the era before the addition of molecular targeting therapy. Methods: We reviewed the clinical course of 134 patients with advanced ovarian cancer (FIGO Stage III and IV) treated in the past 11 years (1999-2010)...
February 24, 2017: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28334848/systematic-review-of-surveillance-by-social-media-platforms-for-illicit-drug-use
#19
Donna M Kazemi, Brian Borsari, Maureen J Levine, Beau Dooley
Background: The use of social media (SM) as a surveillance tool of global illicit drug use is limited. To address this limitation, a systematic review of literature focused on the ability of SM to better recognize illicit drug use trends was addressed. Methods: A search was conducted in databases: PubMed, CINAHL via Ebsco, PsychINFO via Ebsco, Medline via Ebsco, ERIC, Cochrane Library, Science Direct, ABI/INFORM Complete and Communication and Mass Media Complete...
March 14, 2017: Journal of Public Health
https://www.readbyqxmd.com/read/28334726/preparation-characterization-and-anti-ulcer-efficacy-of-sanguinarine-loaded-solid-lipid-nanoparticles
#20
Qing Sun, Weifeng Li, Huani Li, Xiumei Wang, Yu Wang, Xiaofeng Niu
AIM: This study was designed to develop sanguinarine-loaded solid lipid nanoparticles (SG-SLNs) and investigate its gastroprotective effect on ethanol-induced gastric mucosal lesions in mice. METHODS: SG-SLNs were prepared by high temperature melt-cool solidification method using glycerol monostearate as the lipid and a combination of lecithin with poloxamer 188 as the surfactants. Solid lipid nanoparticles (SLNs) were designed at varying lipid concentrations (5, 10, 15, and 20 mg/mL), surfactant mixture concentrations (6, 12, and 18 mg/mL), and drug contents (5, 10, 15, and 20 mg/mL) in "one factor at a time" fashion...
March 24, 2017: Pharmacology
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