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https://www.readbyqxmd.com/read/29454290/ligand-based-computer-aided-drug-design-reveals-new-tropomycin-receptor-kinase-a-trka-inhibitors
#1
Rand Shahin, Iman Mansi, Lubna Swellmeen, Tahani Alwidyan, Nabil Al-Hashimi, Yaser Al-Qarar'h, Omar Shaheen
Targeting tropomycin kinase A (TrkA) by small molecule inhibitors is considered as a promising strategy for treating several human cancers. To achieve this goal, a ligand based QSAR model was applied using the Discovery studio 4.5 (DS 4.5). Hence, a total list of 161 TrkA inhibitors was investigated. The TrkA inhibitors were extensively explored to detect their optimal physicochemical properties and pharmacophoric binding modes, which were converted into numeric descriptors and allowed to compete within the context of the Genetic Function Algorithm (GFA) approximations to find the subset of terms that correlates best with the activity...
January 13, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29454264/development-and-validation-of-uplc-ms-ms-assay-for-quantification-of-cladrin-absolute-bioavailability-and-dose-proportionality-study-in-rats
#2
Mamunur Rashid, Sandeep K Singh, Mohd Yaseen Malik, Sadaf Jahan, Swati Chaturvedi, Isha Taneja, Kanumuri Sivarama Raju, Zaiba Naseem, J R Gayen, Muhammad Wahajuddin
Cladrin, an isoflavone is a major bioactive constituent found in stem bark of Butea monosperma with remarkable osteogenic activity. A speedy and sensitive UPLC coupled tandem mass spectrometry (UPLC-MS/MS) method was developed, validated and successfully applied to bioavailability, blood partitioning, plasma protein binding, intravenous and multiple-dose oral pharmacokinetics of cladrin in rats. Separation was done on C18 column (5.0 μm, 4.6 × 50 mm) using mobile phase containing acetonitrile and 0.10% formic acid in the ratio of 65:35 (v/v) with 0...
January 31, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29454255/effects-of-adjunctive-eslicarbazepine-acetate-on-neurocognitive-functioning-in-children-with-refractory-focal-onset-seizures
#3
Sergiusz Jóźwiak, P Veggiotti, J Moreira, H Gama, F Rocha, P Soares-da-Silva
PURPOSE: This was a phase-II, randomized, double-blind (DB), placebo-controlled study aimed to evaluate neurocognitive effects of eslicarbazepine acetate (ESL) as adjunctive therapy in pediatric patients with refractory focal-onset seizures (FOS). METHODS: Children (6-16years old) with FOS were randomized (2:1) to ESL or placebo. Treatment started at 10mg/kg/day, was up-titrated up to 30mg/kg/day (target dose), and maintained for 8weeks, followed by one-year open-label follow-up...
February 13, 2018: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/29454237/liposomes-of-dimeric-artesunate-phospholipid-a-combination-of-dimerization-and-self-assembly-to-combat-malaria
#4
Muhammad Ismail, Longbing Ling, Yawei Du, Chen Yao, Xinsong Li
Artemisinin and its derivatives are highly effective drugs in the treatment of P. falciparum malaria. However, their clinical applications face challenges because of short half-life, poor bioavailability and growing drug resistance. In this article, novel dimeric artesunate phospholipid (Di-ART-GPC) based liposomes were developed by combination of dimerization and self-assembly to address these shortcomings. Firstly, Di-ART-GPC conjugate was synthesized by a facile esterification of artesunate (ART) and glycerophosphorylcholine (GPC) and confirmed by MS, 1 H NMR and 13 C NMR...
February 10, 2018: Biomaterials
https://www.readbyqxmd.com/read/29454236/stingel-controlled-release-of-a-cyclic-dinucleotide-for-enhanced-cancer-immunotherapy
#5
David G Leach, Neeraja Dharmaraj, Stacey L Piotrowski, Tania L Lopez-Silva, Yu L Lei, Andrew G Sikora, Simon Young, Jeffrey D Hartgerink
Recent advancements in the field of immunotherapy have yielded encouraging results for the treatment of advanced cancers. Cyclic dinucleotides (CDNs) are a powerful new class of immunotherapy drugs known as STING (Stimulator of Interferon Genes) agonists, currently in clinical trials. However, previous studies of CDNs in murine cancer models have required multiple injections, and improve survival only in relatively nonaggressive tumor models. Therefore, we sought to improve the efficacy of CDN immunotherapy by developing a novel biomaterial we call "STINGel...
February 6, 2018: Biomaterials
https://www.readbyqxmd.com/read/29454235/donor-and-recipient-p450-gene-polymorphisms-influence-individual-pharmacological-effects-of-tacrolimus-in-chinese-liver-transplantation-patients
#6
Jianyu Liu, Yabo Ouyang, Dexi Chen, Bo Yao, Dongdong Lin, Zhiqiang Li, Yunjin Zang, Huan Liu, Xiaoyue Fu
The immunosuppressant drug tacrolimus (Tac) used for the prevention of immunological rejection is a metabolic substrate of cytochrome P450 enzymes. This study was designed to evaluate the short-term and long-term potential influence of single-nucleotide polymorphisms (SNPs) in CYP450 genes of liver transplant (LT) recipients as well as the donors on individual pharmacological effects of Tac and to guide individualized-medication from the perspective of pharmacogenomics. Twenty-one SNPs of the CYP450 gene were genotyped for both recipients and donors in 373 LT patients receiving Tac-based immunosuppressants...
February 14, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29454190/potholing-of-the-hydrophobic-heme-oxygenase-1-western-region-for-the-search-of-potent-and-selective-imidazole-based-inhibitors
#7
Loredana Salerno, Emanuele Amata, Giuseppe Romeo, Agostino Marrazzo, Orazio Prezzavento, Giuseppe Floresta, Valeria Sorrenti, Ignazio Barbagallo, Antonio Rescifina, Valeria Pittalà
Here we report the design, synthesis, and molecular modeling of new potent and selective imidazole-based HO-1 inhibitors in which the imidazole nucleus and the hydrophobic groups are linked by a phenylethanolic spacer. Most of the tested compounds showed a good inhibitor activity with IC 50 values in the low micromolar range, with two of them (1b and 1j) exhibiting also high selectivity toward HO-2. These results were obtained by the idea of potholing the entire volume of the principal hydrophobic western region with an appropriate ligand volume...
February 9, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29454188/modified-two-step-emulsion-solvent-evaporation-technique-for-fabricating-biodegradable-rod-shaped-particles-in-the-submicron-size-range
#8
Hanieh Safari, Reheman Adili, Michael Holinstat, Omolola Eniola-Adefeso
HYPOTHESIS: Though the emulsion solvent evaporation (ESE) technique has been previously modified to produce rod-shaped particles, it cannot generate small-sized rods for drug delivery applications due to the inherent coupling and contradicting requirements for the formation versus stretching of droplets. The separation of the droplet formation from the stretching step should enable the creation of submicron droplets that are then stretched in the second stage by manipulation of the system viscosity along with the surface-active molecule and oil-phase solvent...
February 9, 2018: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29454184/exploration-and-exploitation-of-the-environment-for-novel-specialized-metabolites
#9
REVIEW
Catarina Loureiro, Marnix H Medema, John van der Oost, Detmer Sipkema
Microorganisms are Nature's little engineers of a remarkable array of bioactive small molecules that represent most of our new drugs. The wealth of genomic and metagenomic sequence data generated in the last decade has shown that the majority of novel biosynthetic gene clusters (BGCs) is identified from cultivation-independent studies, which has led to a strong expansion of the number of microbial taxa known to harbour BGCs. The large size and repeat sequences of BGCs remain a bioinformatic challenge, but newly developed software tools have been created to overcome these issues and are paramount to identify and select the most promising BGCs for further research and exploitation...
February 14, 2018: Current Opinion in Biotechnology
https://www.readbyqxmd.com/read/29454180/tryptophan-kynurenine-and-lipid-related-metabolites-as-blood-biomarkers-for-first-episode-drug-na%C3%A3-ve-patients-with-major-depressive-disorder-an-exploratory-pilot-case-control-study
#10
Nobuki Kuwano, Takahiro A Kato, Daiki Setoyama, Mina Sato-Kasai, Norihiro Shimokawa, Kohei Hayakawa, Masahiro Ohgidani, Noriaki Sagata, Hiroaki Kubo, Junji Kishimoto, Dongchon Kang, Shigenob Kanba
BACKGROUND: Early intervention in depression has been critical to prevent its negative impact including suicide. Recent blood biomarker studies for major depressive disorder (MDD) have suggested that tryptophan-kynurenine and lipid related metabolites are involved in the pathophysiology of MDD. However, there have been limited studies investigating these blood biomarkers in first-episode drug-naïve MDD, which are particularly important for early intervention in depression. METHODS: As an exploratory pilot case-control study, we examined the above blood biomarkers, and analyzed how these biomarkers are associated with clinical variables in first-episode drug-naïve MDD patients, based on metabolome/lipidome analysis...
January 31, 2018: Journal of Affective Disorders
https://www.readbyqxmd.com/read/29454179/race-ethnicity-and-racial-group-composition-moderate-the-effectiveness-of-mindfulness-based-relapse-prevention-for-substance-use-disorder
#11
Brenna L Greenfield, Corey Roos, Kylee J Hagler, Elena Stein, Sarah Bowen, Katie A Witkiewitz
INTRODUCTION: Mindfulness-based relapse prevention has shown promise as a treatment for substance use disorder but its efficacy according to racial/ethnic minority status and group composition is unknown. METHOD: This is a secondary analysis of existing data (Bowen et al., 2014) testing individual race/ethnicity and racial/ethnic group composition as moderators of mindfulness-based relapse prevention (MBRP). Participants (N = 191; 29% female; 47% racial/ethnic minority; mean age = 39) with substance use disorder were randomized to MBRP or relapse prevention (RP)...
February 7, 2018: Addictive Behaviors
https://www.readbyqxmd.com/read/29454159/an-aligned-porous-electrospun-fibrous-membrane-with-controlled-drug-delivery-an-efficient-strategy-to-accelerate-diabetic-wound-healing-with-improved-angiogenesis
#12
Xiaozhi Ren, Yiming Han, Jie Wang, Yuqi Jiang, Zhengfang Yi, He Xu, Qinfei Ke
A chronic wound in diabetic patients is usually characterized by poor angiogenesis and delayed wound closure. The exploration of efficient strategy to significantly improve angiogenesis in the diabetic wound bed and thereby accelerate wound healing is still a significant challenge. Herein, we reported a kind of aligned porous poly (L-lactic acid) (PLLA) electrospun fibrous membranes containing dimethyloxalylglycine (DMOG)-loaded mesoporous silica nanoparticles (DS) for diabetic wound healing. The PLLA electrospun fibers aligned in a single direction and there were ellipse-shaped nano-pores in situ generated onto the surface of fibers, while the DS were well distributed in the fibers and the DMOG as well as Si ion could be controlled released from the nanopores on the fibers...
February 14, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29454157/nanofibrous-plga-electrospun-scaffolds-modified-with-type-i-collagen-influence-hepatocyte-function-and-support-viability-in-vitro
#13
Jessica H Brown, Prativa Das, Michael D DiVito, David Ivancic, Lay Poh Tan, Jason A Wertheim
A major challenge of maintaining primary hepatocytes in vitro is progressive loss of hepatocyte-specific functions, such as protein synthesis and cytochrome P450 (CYP450) catalytic activity. We developed a three-dimensional (3D) nanofibrous scaffold made from poly(L-lactide-co-glycolide) (PLGA) polymer using a newlyoptimizedwet electrospinning techniquethat resulted in a highly porous structure that accommodated inclusion of primary human hepatocytes. Extracellular matrix (ECM) proteins (type I collagen or fibronectin) at varying concentrations were chemically linked to electrospun PLGA using amine coupling to develop an in vitro culture system containing the minimal essential ECM components of the liver micro-environment that preserve hepatocyte function in vitro...
February 14, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29454114/mitochondria-targeting-mitochondrial-reactive-oxygen-species-with-mitochondriotropic-polyphenolic-based-antioxidants
#14
José Teixeira, Cláudia M Deus, Fernanda Borges, Paulo J Oliveira
Mitochondrial function and regulation of redox balance is fundamental in controlling cellular life and death pathways. Antioxidants have been used to counteract disruption of redox networks, normally associated with progressive loss of cell homeostasis and disease pathophysiology, although therapeutic success is limited mainly due to pharmacokinetic drawbacks. Attempts to improve mitochondrial function in a range of diseases spurred active drug discovery efforts. Currently, the most effective strategy to deliver drugs to mitochondria is the covalent link of lipophilic cations to the bioactive compound...
February 14, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29454108/detection-of-b-fragilis-group-and-diversity-of-bft-enterotoxin-and-antibiotic-resistance-markers-cepa-cfia-and-nim-among-intestinal-bacteroides-fragilis-strains-in-patients-with-inflammatory-bowel-disease
#15
Marjan Rashidan, Masoumeh Azimirad, Masoud Alebouyeh, Mehdi Ghobakhlou, Hamid Asadzadeh Aghdaei, Mohammad Reza Zali
We compared frequency of the members of B. fragilis group in 100 and 20 colon biopsy specimens of inflammatory bowel disease (IBD) and non-IBD patients. Agar dilution and PCR were orderly used to detect minimal inhibitory concentration of ampicillin, imipenem, and metronidazole, and carriage of related resistance genes cepA, cfi, and nim. B. fragilis group was detected in 38% of IBD (UC: 36/89; CD:1/11) and 25% (5/20) of non-IBD patients. While B. vulgatus (UC: 20/36, CD: 1/2, control: 1/6); B. fragilis (UC: 18/36, CD: 1/2, control: 5/6); B...
February 14, 2018: Anaerobe
https://www.readbyqxmd.com/read/29454097/improving-sustained-drug-delivery-from-ophthalmic-lens-materials-through-the-control-of-temperature-and-time-of-loading
#16
Ana Topete, Andreia S Oliveira, A Fernandes, T G Nunes, A P Serro, B Saramago
Although the possibility of using drug-loaded ophthalmic lens to promote sustained drug release has been thoroughly pursued, there are still problems to be solved associated to the different alternatives. In this work, we went back to the traditional method of drug loading by soaking in the drug solution and tried to optimize the release profiles by changing the temperature and the time of loading. Two materials commercially available under the names of CI26Y and Definitive 50 were chosen. CI26Y is used for intraocular lenses (IOLs) and Definitive 50 for soft contact lenses (SCLs)...
February 14, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29454091/anlotinib-inhibits-angiogenesis-via-suppressing-the-activation-of-vegfr2-pdgfr%C3%AE-and-fgfr1
#17
Binyan Lin, Xiuming Song, Dawei Yang, Dongsheng Bai, Yuyuan Yao, Na Lu
Tumor cells recruit vascular endothelial cells and circulating endothelial progenitor cells to form new vessels to support their own growth and metastasis. VEGF, PDGF-BB and FGF-2 are three major pro-angiogenic factors and applied to promote angiogenesis. In this research, we demonstrated that anlotinib, a potent multi-tyrosine kinases inhibitor (TKI), showed a significant inhibitory effect on VEGF/PDGF-BB/FGF-2-induced angiogenesis in vitro and in vivo. Wound healing assay, chamber directional migration assay and tube formation assay indicated that anlotinib inhibited VEGF/PDGF-BB/FGF-2-induced cell migration and formation of capillary-like tubes in endothelial cells...
February 14, 2018: Gene
https://www.readbyqxmd.com/read/29454083/incidence-of-acute-suppurative-sialadenitis-in-end-stage-cancer-patients-a-retrospective-observational-study
#18
Hiroaki Watanabe, Takuya Odagiri, Yasuyuki Asai
CONTEXT: Acute suppurative sialadenitis (hereafter referred to as sialadenitis) is accompanied by pain and fever and can diminish the quality of life (QOL) in end-stage cancer patients; however, its incidence is not clear. OBJECTIVES: We conducted this study to elucidate the incidence of sialadenitis in end-stage cancer patients. METHODS: Retrospective review, observational study based on patients' medical records SUBJECTS: 726 consecutive cancer patients who died on the palliative care unit of our hospital between April 2012 and November 2016 were included...
February 14, 2018: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/29454064/rna-based-micelles-a-novel-platform-for-chemotherapeutic-drug-loading-and-delivery
#19
Yi Shu, Hongran Yin, Mehdi Rajabi, Hui Li, Mario Vieweger, Sijin Guo, Dan Shu, Peixuan Guo
RNA can serve as powerful building blocks for bottom-up fabrication of nanostructures for biotechnological and biomedical applications. In addition to current self-assembly strategies utilizing base pairing, motif piling and tertiary interactions, we reported for the first time to build RNA based micellar nanoconstruct with a cholesterol molecule conjugated onto one helical end of a branched pRNA three-way junction (3WJ) motif. The resulting amphiphilic RNA micelles consist of a hydrophilic RNA head and a covalently linked hydrophobic lipid tail that can spontaneously assemble in aqueous solution via hydrophobic interaction...
February 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29454062/laser-assisted-delivery-of-synergistic-combination-chemotherapy-in-in-vivo-skin
#20
Emily Wenande, Joshua Tam, Brijesh Bhayana, Steven Kyle Schlosser, Emily Ishak, William A Farinelli, Agata Chlopik, Mai P Hoang, Omar R Pinkhasov, Peter Caravan, R Rox Anderson, Merete Haedersdal
The effectiveness of topical drugs for treatment of non-melanoma skin cancer is greatly reduced by insufficient penetration to deep skin layers. Ablative fractional lasers (AFLs) are known to enhance topical drug uptake by generating narrow microchannels through the skin, but information on AFL-drug delivery in in vivo conditions is limited. In this study, we examined pharmacokinetics, biodistribution and toxicity of two synergistic chemotherapy agents, cisplatin and 5-fluorouracil (5-FU), following AFL-assisted delivery alone or in combination in in vivo porcine skin...
February 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
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