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https://www.readbyqxmd.com/read/27914040/formulation-optimization-and-ex-vivo-and-in-vivo-evaluation-of-celecoxib-microemulsion-based-gel-for-transdermal-delivery
#1
Mengyuan Cao, Lili Ren, Guoguang Chen
Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). Hence, the formulation of CXB was selected for solubilization and bioavailability. To find out suitable formulation for microemulsion, the solubility of CXB in triacetin (oil phase), Tween 80 (surfactant), and Transcutol-P (co-surfactant) was screened respectively and optimized by using orthogonal experimental design. The Km value and concentration of oil, Smix, and water were confirmed by pseudo-ternary phase diagram studies and central composite design...
December 2, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27913752/expression-and-bioactivity-of-human-alpha-fetoprotein-in-a-bac-to-bac-system
#2
Bo Lin, Kun Liu, Wenting Wang, Wei Li, Xu Dong, Yi Chen, Yan Lu, Junli Guo, Mingyue Zhu, Mengsen Li
Alpha-fetoprotein (AFP) is an early serum growth factor in fetal embryonic development and hepatic oncogenesis. A growing number of investigations of AFP as a tumor-specific biomarker have concluded that AFP is an important target for cancer treatment. AFP also plays an immunomodulatory role in the treatment of several autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, and thyroiditis. In an effort to support biochemical screening and drug design and discovery, we attempted to express and purify human AFP in a Bac-to-Bac system...
December 2, 2016: Bioscience Reports
https://www.readbyqxmd.com/read/27913699/risk-and-association-of-hla-with-oxcarbazepine-induced-cutaneous-adverse-reactions-in-asians
#3
Chun-Bing Chen, Yi-Hsin Hsiao, Tony Wu, Mo-Song Hsih, Wichittra Tassaneeyakul, Teekayu P Jorns, Chonlaphat Sukasem, Chien-Ning Hsu, Shih-Chi Su, Wan-Chun Chang, Rosaline Chung-Yee Hui, Chia-Yu Chu, Yi-Ju Chen, Ching-Ying Wu, Chao-Kai Hsu, Tsu-Man Chiu, Pei-Lun Sun, Hua-En Lee, Chin-Yi Yang, Pei-Han Kao, Chih-Hsun Yang, Hsin-Chun Ho, Jing-Yi Lin, Ya-Ching Chang, Ming-Jing Chen, Chun-Wei Lu, Chau Yee Ng, Kang-Ling Kuo, Chien-Yio Lin, Ching-Sheng Yang, Ding-Ping Chen, Pi-Yueh Chang, Tsu-Lan Wu, Yu-Jr Lin, Yi-Ching Weng, Tseng-Tong Kuo, Shuen-Iu Hung, Wen-Hung Chung
OBJECTIVE: To investigate the risk and genetic association of oxcarbazepine-induced cutaneous adverse reactions (OXC-cADRs), including Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN), in Asian populations (Chinese and Thai). METHODS: We prospectively enrolled patients with OXC-cADRs in Taiwan and Thailand from 2006 to 2014, and analyzed the clinical course, latent period, drug dosage, organ involvement, complications, and mortality. We also investigated the carrier rate of HLA-B*15:02 and HLA-A*31:01 of patients with OXC-cADRs and compared to OXC-tolerant controls...
December 2, 2016: Neurology
https://www.readbyqxmd.com/read/27913670/screening-for-chemical-modulators-for-lrrk2
#4
REVIEW
Heather Mortiboys
After the discovery of leucine-rich repeat kinase 2 (LRRK2) as a risk factor for sporadic Parkinson's disease (PD) and mutations in LRRK2 as a cause of some forms of familial PD, there has been substantial interest in finding chemical modulators of LRRK2 function. Most of the pathogenic mutations in LRRK2 are within the enzymatic cores of the protein; therefore, many screens have focused on finding chemical modulators of this enzymatic activity. There are alternative screening approaches that could be taken to investigate compounds that modulate LRRK2 cellular functions...
December 15, 2016: Biochemical Society Transactions
https://www.readbyqxmd.com/read/27913567/drug-repositioning-screens-identify-triamterene-as-a-selective-drug-for-the-treatment-of-dna-mismatch-repair-deficient-cells
#5
Delphine Guillotin, Philip Austin, Rumena Begum, Marta O Freitas, Ashirwad Merve, Tim Brend, Susan C Short, Silvia Marino, Sarah A Martin
PURPOSE: The DNA Mismatch repair (MMR) pathway is required for the maintenance of genome stability. Unsurprisingly, mutations in MMR genes occur in a wide range of different cancers. Studies thus far have largely focused on specific tumor types or MMR mutations, however it is becoming increasingly clear that a therapy targeting MMR-deficiency in general would be clinically very beneficial. EXPERIMENTAL DESIGN: Based on a drug-repositioning approach, we screened a large panel of cell lines with various MMR deficiencies from a range of different tumor types with a compound drug library of previously approved drugs...
December 2, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27913498/long-term-risk-of-second-malignancy-and-cardiovascular-disease-after-hodgkin-lymphoma-treatment
#6
Flora E van Leeuwen, Andrea K Ng
Long-term survivors of Hodgkin lymphoma (HL) experience several late adverse effects of treatment, with second malignant neoplasms (SMNs) and cardiovascular diseases (CVDs) being the leading causes of death in these patients. Other late effects have also been identified, such as pulmonary dysfunction, endocrinopathies (thyroid dysfunction, infertility), neck muscle atrophy, and persistent fatigue. HL survivors have two- to fourfold increased risks to develop SMNs and CVD compared with the general population...
December 2, 2016: Hematology—the Education Program of the American Society of Hematology
https://www.readbyqxmd.com/read/27913311/should-travelers-be-screened-for-multi-drug-resistant-mdr-bacteria-after-visiting-high-risk-areas-such-as-india
#7
Eskild Petersen, Jalila Mohsin
No abstract text is available yet for this article.
November 29, 2016: Travel Medicine and Infectious Disease
https://www.readbyqxmd.com/read/27913030/confounding-variables-and-the-performance-of-triggers-in-detecting-unreported-adverse-drug-reactions
#8
Fabiana Rossi Varallo, Carolina Dagli-Hernandez, Caroline Pagotto, Tales Rubens de Nadai, Maria Teresa Herdeiro, Patricia de Carvalho Mastroianni
PURPOSE: This study explored the performance of trigger in detecting adverse drug reactions (ADRs), the confounding variables impairing the causal association of the ADRs, and the underreporting rate by hospital health professionals. METHODS: A 6-month cross-sectional study was conducted in a public general hospital. Data collection was conducted in 2 stages: (1) screening of patient hospitalizations to identify suspected ADRs with 9 triggers developed by the Institute of Healthcare Improvement; and (2) chart review to perform the causality assessment of the suspected ADRs identified, to describe the confounding variables associated with detection of suspected ADRs that were not drug induced, and to analyze the positive predictive value of triggers in recognizing ADRs...
November 29, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27912146/inosine-acedoben-dimepranol-promotes-an-early-and-sustained-increase-in-the-natural-killer-cell-component-of-circulating-lymphocytes-a-clinical-trial-supporting-anti-viral-indications
#9
S Rumel Ahmed, Amy S Newman, James O'Daly, Sean Duffy, Gillian Grafton, Catherine A Brady, S John Curnow, Nicholas M Barnes, John Gordon
Inosine Acedoben Dimepranol (IAD), licensed for the treatment of cell-mediated immune deficiencies associated with viral infections, has been reported to impact a variety of immune parameters both in vitro and in vivo. Here we report the results from a clinical trial where multiple lymphocyte subsets - CD19+ B cells, CD3+ T cells, CD4+ T-helper cells, FoxP3(hi)/CD25(hi)/CD127(lo) regulatory T cells (Tregs), CD3-/CD56+ NK cells, and CD3+/CD56+ NKT cells - were, together with serum immunoglobulins and IgG subclasses, followed during 14days of IAD administration to ten healthy volunteers; these selected from 27 individuals pre-screened in vitro for their capacity to respond to IAD as gauged by increases in the percentage of Treg and/or NKT cells arising in PHA-stimulated cultures...
November 29, 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27911980/cell-based-dna-demethylation-detection-system-for-screening-of-epigenetic-drugs-in-2d-3d-and-xenograft-models
#10
Khushboo Agrawal, Viswanath Das, Miroslav Otmar, Marcela Krečmerová, Petr Džubák, Marián Hajdúch
Aberrant DNA methylation that results in silencing of genes has remained a significant interest in cancer research. Despite major advances, the success of epigenetic therapy is elusive due to narrow therapeutic window. A wide variety of naturally occurring epigenetic agents and synthetic molecules that can alter methylation patterns exist, however, their usefulness in epigenetic therapy remains unknown. This underlines the need for effective tumor models for large-scale screening of drug candidates with potent hypomethylation activity...
December 2, 2016: Cytometry. Part A: the Journal of the International Society for Analytical Cytology
https://www.readbyqxmd.com/read/27911825/elucidating-the-druggable-interface-of-protein-protein-interactions-using-fragment-docking-and-coevolutionary-analysis
#11
Fang Bai, Faruck Morcos, Ryan R Cheng, Hualiang Jiang, José N Onuchic
Protein-protein interactions play a central role in cellular function. Improving the understanding of complex formation has many practical applications, including the rational design of new therapeutic agents and the mechanisms governing signal transduction networks. The generally large, flat, and relatively featureless binding sites of protein complexes pose many challenges for drug design. Fragment docking and direct coupling analysis are used in an integrated computational method to estimate druggable protein-protein interfaces...
November 29, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27911816/rapid-emergence-and-mechanisms-of-resistance-by-u87-glioblastoma-cells-to-doxorubicin-in-an-in-vitro-tumor-microfluidic-ecology
#12
Jeonghun Han, Yukyung Jun, So Hyun Kim, Hong-Hoa Hoang, Yeonjoo Jung, Suyeon Kim, Jaesang Kim, Robert H Austin, Sanghyuk Lee, Sungsu Park
In vitro prediction of the probable rapid emergence of resistance to a drug in tumors could act to winnow out potential candidates for further costly development. We have developed a microfluidic device consisting of ∼500 hexagonal microcompartments that provides a complex ecology with wide ranges of drug and nutrient gradients and local populations. This ecology of a fragmented metapopulation induced the drug resistance in stage IV U87 glioblastoma cells to doxorubicin in 7 d. Exome and transcriptome sequencing of the resistant cells identified mutations and differentially expressed genes...
November 22, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27911484/platinum-complex-assemblies-as-luminescent-probes-and-tags-for-drugs-and-toxins-in-water
#13
Stephan Sinn, Frank Biedermann, Luisa De Cola
A reactive phosphorescent probe for aza-heterocyclic drugs and toxins was developed, affording a supramolecular emission-switch-on chemosensor in water. Complex formation of the heterocycles with a platinum(II) precursor proceeds readily at ambient conditions, allowing for facile analyte screening. 52 structurally diverse compounds were tested, out of which 23 pyridines, imidazole, and triazoles formed strongly emissive complex aggregates. Importantly, they all can be clearly distinguished from each other through a principal component analysis, but often already by simple visual inspection, e...
December 1, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27911362/automated-acoustic-dispensing-for-the-serial-dilution-of-peptide-agonists-in-potency-determination-assays
#14
Jacqueline Naylor, Alessandra Rossi, Christopher Brankin, David C Hornigold
As with small molecule drug discovery, screening for peptide agonists requires the serial dilution of peptides to produce concentration-response curves. Screening peptides affords an additional layer of complexity as conventional tip-based sample handling methods expose peptides to a large surface area of plasticware, providing an increased opportunity for peptide loss via adsorption. Preventing excessive exposure to plasticware reduces peptide loss via adherence to plastics and thus minimizes inaccuracies in potency prediction, and we have previously described the benefits of non-contact acoustic dispensing for in vitro high-throughput screening of peptide agonists(1)...
November 10, 2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27911223/advances-in-capillary-electrophoresis-and-the-implications-for-drug-discovery
#15
Claire M Ouimet, Cara I D'Amico, Robert T Kennedy
Many screening platforms are prone to assay interferences that can be avoided by directly measuring the target or enzymatic product. Capillary electrophoresis (CE) and microchip electrophoresis (MCE) have been applied in a variety of formats to drug discovery. CE provides direct detection of the product allowing for the identification of some forms of assay interference. The high efficiency, rapid separations, and low volume requirements make CE amenable to drug discovery. Areas Covered: This article describes advances in capillary electrophoresis throughput, sample introduction, and target assays as they pertain to drug discovery and screening...
December 2, 2016: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/27910927/novel-chemoimmunotherapeutic-strategy-for-hepatocellular-carcinoma-based-on-a-genome-wide-association-study
#16
Kaku Goto, Dorcas A Annan, Tomoko Morita, Wenwen Li, Ryosuke Muroyama, Yasuo Matsubara, Sayaka Ito, Ryo Nakagawa, Yasushi Tanoue, Masahisa Jinushi, Naoya Kato
Pharmacotherapeutic options are limited for hepatocellular carcinoma (HCC). Recently, we identified the anti-tumor ligand MHC class I polypeptide-related sequence A (MICA) gene as a susceptibility gene for hepatitis C virus-induced HCC in a genome-wide association study (GWAS). To prove the concept of HCC immunotherapy based on the results of a GWAS, in the present study, we searched for drugs that could restore MICA expression. A screen of the FDA-approved drug library identified the anti-cancer agent vorinostat as the strongest hit, suggesting histone deacetylase inhibitors (HDACis) as potent candidates...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27910869/multiparameter-mechanical-and-morphometric-screening-of-cells
#17
Mahdokht Masaeli, Dewal Gupta, Sean O'Byrne, Henry T K Tse, Daniel R Gossett, Peter Tseng, Andrew S Utada, Hea-Jin Jung, Stephen Young, Amander T Clark, Dino Di Carlo
We introduce a label-free method to rapidly phenotype and classify cells purely based on physical properties. We extract 15 biophysical parameters from cells as they deform in a microfluidic stretching flow field via high-speed microscopy and apply machine-learning approaches to discriminate different cell types and states. When employing the full 15 dimensional dataset, the technique robustly classifies individual cells based on their pluripotency, with accuracy above 95%. Rheological and morphological properties of cells while deforming were critical for this classification...
December 2, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27910855/l-type-calcium-channels-regulate-filopodia-stability-and-cancer-cell-invasion-downstream-of-integrin-signalling
#18
Guillaume Jacquemet, Habib Baghirov, Maria Georgiadou, Harri Sihto, Emilia Peuhu, Pierre Cettour-Janet, Tao He, Merja Perälä, Pauliina Kronqvist, Heikki Joensuu, Johanna Ivaska
Mounting in vitro, in vivo and clinical evidence suggest an important role for filopodia in driving cancer cell invasion. Using a high-throughput microscopic-based drug screen, we identify FDA-approved calcium channel blockers (CCBs) as potent inhibitors of filopodia formation in cancer cells. Unexpectedly, we discover that L-type calcium channels are functional and frequently expressed in cancer cells suggesting a previously unappreciated role for these channels during tumorigenesis. We further demonstrate that, at filopodia, L-type calcium channels are activated by integrin inside-out signalling, integrin activation and Src...
December 2, 2016: Nature Communications
https://www.readbyqxmd.com/read/27910812/inflammatory-markers-associated-with-abdominal-aortic-aneurysm
#19
Sarah Lindberg, Moncef Zarrouk, Jan Holst, Anders Gottsäter
PURPOSE: Inflammation with leukocytic infiltration, degradation of extracellular matrix (ECM), and depletion of vascular smooth muscle cells (VSMC) are pathological hallmarks of abdominal aortic aneurysm (AAA). The aim of this study was to further evaluate relationships between AAA and inflammatory biomarkers, interleukin-6 (IL-6), tumour necrosis factor-α (TNF-α), endothelin-1 (ET-1) and soluble urokinase-type plasminogen activator receptor (suPAR), by comparing levels in 65-year-old men with and without AAA at ultrasound screening...
September 1, 2016: European Cytokine Network
https://www.readbyqxmd.com/read/27910784/hepatoprotective-effect-of-tricholoma-giganteum-agaricomycetes-in-a-nonalcoholic-fatty-liver-disease-rat-model
#20
Ramar Govindaraj, Michael Gabriel Paulraj, Erenius Toppo, Perumal Pandikumar, Savarimuthu Ignacimuthu, Naif Abdhullah Al-Dhabi
Different concentrations of standardized ethanolic extract from the basidiocarps of Tricholoma giganteum Massee (TgEtOH) were screened for hepatoprotective effects in an animal model of rats with nonalcoholic fatty liver disease (NAFLD) fed a high-fat and high-fructose diet. After 4 weeks of treatment with TgEtOH, the relative liver weights, serum lipid concentrations, and biochemical profiles were found to be normal in treated animals compared with those given a standard drug. The macroscopic and histopathological studies clearly indicated that 200 mg/kg of ethanolic extract was effective in ameliorating the abnormalities of NAFLD...
2016: International Journal of Medicinal Mushrooms
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