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https://www.readbyqxmd.com/read/28821163/metformin-maintains-mucosal-integrity-in-experimental-model-of-colitis-by-inhibiting-oxidative-stress-and-pro-inflammatory-signaling
#1
Abhimanu Pandey, Sneh Verma, Vijay L Kumar
Metformin, an antidiabetic drug, is well known for its multifarious properties and its ability to modulate inflammatory cascade. Ulcerative colitis (UC) is an inflammatory condition of the colon where drugs exhibiting anti-inflammatory property have been shown to induce and maintain remission. The objective of the present study was to evaluate the efficacy of metformin against acetic-acid induced colitis in rat. The study included five groups of rats namely normal control, experimental control, drug treated groups (50 and 500mg/kg of metformin, MET50, MET500 and 300mg/kg of mesalazine, MSZ300)...
August 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28821159/inhibition-of-dna-pk-enhances-chemosensitivity-of-b-cell-precursor-acute-lymphoblastic-leukemia-cells-to-doxorubicin
#2
Fatemeh Alikarami, Majid Safa, Mohammad Faranoush, Parisa Hayat, Ahmad Kazemi
DNA damage repair pathways greatly affect the response to genotoxic drugs in cancer cells, so inhibition of such pathways could be a potentially useful strategy to enhance chemosensitivity. DNA-dependent protein kinase (DNA-PK) plays a crucial role in the repair of DNA double-strand breaks (DSBs) that are probably one of the most detrimental types of DNA damage. It has been shown that DNA-PK is highly expressed in B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells. Less well appreciated was the effect of DNA-PK inhibition on sensitivity of BCP-ALL cells to DNA-damaging agents...
August 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28821097/thiolated-pectin-doxorubicin-conjugates-synthesis-characterization-and-anticancer-activity-studies
#3
Kamonrak Cheewatanakornkool, Sathit Niratisai, Somkamol Manchun, Crispin R Dass, Pornsak Sriamornsak
In this paper, pectin was cross-linked by a coupling reaction with either thioglycolic acid or cystamine dihydrochloride to form thiolated pectins. The thiolated pectins were then coupled with doxorubicin (DOX) derivative to obtain thiolated pectin-DOX conjugates by two different methods, disulfide bond formation and disulfide bond exchange. The disulfide bond exchange method provided a simple, fast, and efficient approach for synthesis of thiolated pectin-DOX conjugates, compared to the disulfide bond formation...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28821011/the-photodynamic-action-of-pheophorbide-a-induces-cell-death-through-oxidative-stress-in-leishmania-amazonensis
#4
Nathielle Miranda, Hélito Volpato, Jean Henrique da Silva Rodrigues, Wilker Caetano, Tânia Ueda-Nakamura, Sueli de Oliveira Silva, Celso Vataru Nakamura
Leishmaniasis is a disease caused by hemoflagellate protozoa, affecting millions of people worldwide. The difficulties of treating patients with this parasitosis include the limited efficacy and many side effects of the currently available drugs. Therefore, the search for new compounds with leishmanicidal action is necessary. Photodynamic therapy has been studied in the medical field because of its selectivity, utilizing a combination of visible light, a photosensitizer compound, and singlet oxygen to reach the area of treatment...
August 11, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28820965/systematic-identification-of-mcu-modulators-by-orthogonal-interspecies-chemical-screening
#5
Daniela M Arduino, Jennifer Wettmarshausen, Horia Vais, Paloma Navas-Navarro, Yiming Cheng, Anja Leimpek, Zhongming Ma, Alba Delrio-Lorenzo, Andrea Giordano, Cecilia Garcia-Perez, Guillaume Médard, Bernhard Kuster, Javier García-Sancho, Dejana Mokranjac, J Kevin Foskett, M Teresa Alonso, Fabiana Perocchi
The mitochondrial calcium uniporter complex is essential for calcium (Ca(2+)) uptake into mitochondria of all mammalian tissues, where it regulates bioenergetics, cell death, and Ca(2+) signal transduction. Despite its involvement in several human diseases, we currently lack pharmacological agents for targeting uniporter activity. Here we introduce a high-throughput assay that selects for human MCU-specific small-molecule modulators in primary drug screens. Using isolated yeast mitochondria, reconstituted with human MCU, its essential regulator EMRE, and aequorin, and exploiting a D-lactate- and mannitol/sucrose-based bioenergetic shunt that greatly minimizes false-positive hits, we identify mitoxantrone out of more than 600 clinically approved drugs as a direct selective inhibitor of human MCU...
August 17, 2017: Molecular Cell
https://www.readbyqxmd.com/read/28820953/a-fluorescence-based-high-throughput-assay-for-the-identification-of-anticancer-reagents-targeting-fructose-1-6-bisphosphate-aldolase
#6
Eun Jeong Cho, Ashwini K Devkota, Gabriel Stancu, Ramakrishna Edupunganti, Garth Powis, Kevin N Dalby
A high rate of glycolysis, which supplies energy and materials for anabolism, is observed in a wide range of tumor cells, making it a potential pathway to control cancer growth. ALDOA is a multifunctional enzyme in the glycolytic pathway and also promotes HIF-1α, which is of importance in hypoxic solid tumors. The current method for assaying ALDOA activity involves monitoring the consumption of NADH in vitro using absorbance or intrinsic fluorescence via a coupled enzymatic reaction. Here, we report the development of a homogeneous biochemical assay that can overcome limitations of current methods, in particular for the application of high-throughput drug screening...
August 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28820943/the-active-site-flexibility-of-mycobacterium-tuberculosis-isocitrate-lyase-in-dimer-form
#7
Yie-Vern Lee, Sybing Choi, Habibah Wahab, Yee Siew Choong
Tuberculosis (TB) still remains as global threat due to the emerging of drug resistant strain. Instead of focus on drug target of active stage TB, we are highlighting the isocitrate lyase (ICL) at the dormant stage TB. ICL is one of the persistent factors for Mycobacterium tuberculosis (MTB) to survive during dormant phase. In addition, the absent of ICL in human has made ICL a potential drug target for TB therapy. However, the dynamics details of ICL which could give insights to the ICL-ligand interaction is yet to be solved...
August 18, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28820879/a-kinetic-view-of-gpcr-allostery-and-biased-agonism
#8
J Robert Lane, Lauren T May, Robert G Parton, Patrick M Sexton, Arthur Christopoulos
G-protein-coupled receptors (GPCRs) are one of the most tractable classes of drug targets. These dynamic proteins can adopt multiple active states that are linked to distinct functional outcomes. Such states can be differentially stabilized by ligands interacting with the endogenous agonist-binding orthosteric site and/or by ligands acting via spatially distinct allosteric sites, leading to the phenomena of 'biased agonism' or 'biased modulation'. These paradigms are having a major impact on modern drug discovery, but it is becoming increasingly apparent that 'kinetic context', at the level of both ligand-receptor and receptor-signal pathway kinetics, can have a profound impact on the observation and quantification of these phenomena...
August 18, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28820621/-doctors-killed-my-baby-argumentative-patterns-in-medical-disputes-in-china
#9
Dawei Pan
The recent surge in medical disputes requires that more attention be paid to the voices of laypeople. This article explores the argumentative nature of the public discourse of the reported "malpractice mobs" that strive to convince members of the public (in the place of health or legal experts) that they have been victims of medical errors and injustice. This case-based qualitative empirical study uses a pragma-dialectical approach to suggest a prototypical pattern of such public appeals that contains a basic argumentative pattern and various types of extensions...
August 18, 2017: Health Communication
https://www.readbyqxmd.com/read/28820585/chemo-enzymatic-assembly-of-isotopically-labeled-folates
#10
Antonio Angelastro, William Michael Dawson, Louis Y P Luk, E Joel Loveridge, Rudolf K Allemann
Pterin-containing natural products have diverse functions in life but an efficient and easy scheme for their in vitro synthesis is not available. Here, we report a chemo-enzymatic 14-step, one-pot synthesis that can be used to generate 13C- and 15N-labeled dihydrofolates (H2F) from glucose, guanine and p-aminobenzoyl-L-glutamic acid. This synthesis stands out from previous approaches to produce H2F in that the average yield of each step is >91% and it requires only one single purification step. The use of a one-pot reaction allowed us to overcome potential problems with individual steps during the synthesis...
August 18, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28820568/enhanced-drug-delivery-into-cell-cytosol-via-glycoprotein-h-derived-peptide-conjugated-nanoemulsions
#11
Teresa Fotticchia, Raffaele Vecchione, Pasqualina Liana Scognamiglio, Daniela Guarnieri, Vincenzo Calcagno, Concetta Di Natale, Chiara Attanasio, Maria De Gregorio, Chiara Di Cicco, Vincenzo Quagliariello, Nicola Maurea, Antonio Barbieri, Luca Raiola, Rosario Vincenzo Iaffaioli, Paolo Antonio Netti
The key role of nanocarriers in improving the pharmacological properties of commonly used drugs is recognized worldwide. It is also known that in the development of new effective nanocarriers the use of targeting moieties integrated on their surface is essential. Herein, we propose a nanocarrier based on an oil in water nanoemulsion coated with a membranotropic peptide derived from the glycoprotein H of Herpes simplex virus 1, known as gH625, in order to reduce endo-lysosomal accumulation and to enhance cytosolic localization...
August 18, 2017: ACS Nano
https://www.readbyqxmd.com/read/28820454/personal-hygiene-practices-among-urban-homeless-persons-in-boston-ma
#12
Jessica H Leibler, Daniel D Nguyen, Casey León, Jessie M Gaeta, Debora Perez
Persons experiencing homelessness in the United States experience significant barriers to self-care and personal hygiene, including limited access to clean showers, laundry and hand washing facilities. While the obstacles to personal hygiene associated with homelessness may increase risk of infectious disease, hygiene-related behaviors among people experiencing homelessness has received limited attention. We conducted a cross-sectional study of individuals experiencing homelessness in Boston, MA (n = 194) to identify hygiene-related self-care practices and risk factors for reduced hygiene in this population...
August 18, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28820390/small-molecule-inhibitors-of-dna-pk-for-tumor-sensitization-to-anticancer-therapy
#13
M Pospisilova, M Seifrtova, M Rezacova
The most sensitive cell structure - a DNA molecule, is the common target of cancer therapy. DNA damage response (controlled by enzymes from the phosphatidylinositol 3-kinase-related kinases family - PIKK) presents many encouraging targets for improving both conventional cytotoxic anticancer therapy and individualized monotherapy. DNA-dependent protein kinase (DNA-PK) is a member of the PIKK superfamily and plays an important role in the detection and repair of DNA double-strand breaks via the non-homologous end-joining pathway...
June 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28820267/causes-and-significance-of-increased-compound-potency-in-cellular-or-physiological-contexts
#14
Adam G Schwaid, Ivan Cornella-Taracido
Compound potency is a key metric that is often used to drive medicinal chemistry programs. Compound potency is also taken into account when identifying the mechanism of action of compounds whose pharmacological target is unknown, particularly when these compounds are identified in phenotypic screens. Often compound potency is determined from assays using recombinantly generated, purified protein. It is well understood in the medicinal chemistry community that potency measured with recombinant enzyme and potency measured in cell may not entirely coincide...
August 18, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28820055/an-update-on-circumventing-multidrug-resistance-in-cancer-by-targeting-p-glycoprotein
#15
Xiaoqian Yang, Xiaoduan Li, Zhenfeng Duan, Xipeng Wang
BACKGROUND: The ultimate emergence of multidrug resistance remains a severe limitation of chemotherapy treatment for patients with cancer. The best-characterized cause of drug resistance involves the overexpression of P-glycoprotein (Pgp), which decreases the intracellular accumulation of chemotherapeutic agents in drug-resistant cancer cells. Thus, Pgp has become an attractive potential target for treating chemotherapy-resistant cancer, butthe outcomes of using chemotherapy in combination with Pgp inhibitors in clinical trials to date have been disappointing...
June 22, 2017: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/28820054/qsar-modeling-of-histamine-h3r-antagonists-inverse-agonists-as-future-drugs-for-neurodegenerative-diseases
#16
Michelle Fidelis Corrêa, João Paulo Dos Santos Fernandes
Histamine H3 receptor (H3R) is associated with several neuropsychological diseases. It is predominantly expressed in the central nervous system as presynaptic receptor, especially in regions associated with cognition and behavior, and is responsible for modulate the synthesis and release of histamine and other neurotransmitters such as acetylcholine, dopamine and serotonin. Therefore, H3R is an important target involved in several CNS disorders, such as narcolepsy, attention deficit hyperactivity disorder and schizophrenia...
August 17, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28820000/novel-combination-strategies-for-enhancing-efficacy-of-immune-checkpoint-inhibitors-in-the-treatment-of-metastatic-solid-malignancies
#17
Michael J Flynn, James M G Larkin
Immune-checkpoint inhibitor (ICPI) drugs, which include antibodies against CTLA-4, PD-1 and PD-L1, have been shown to induce durable complete responses in a proportion of patients with particular efficacy demonstrated in both the first line and refractory setting in advanced NSCLC and melanoma. However, these drugs remain effective only in a minority of unselected patients. Areas covered: This review will focus on mechanisms of resistance to ICPI and underline the importance of identification of novel predictive markers of responsiveness...
August 18, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28819983/an-evaluation-of-the-effectiveness-of-a-risk-based-monitoring-approach-implemented-with-clinical-trials-involving-implantable-cardiac-medical-devices
#18
Christopher A Diani, Angie Rock, Phil Moll
Background Risk-based monitoring is a concept endorsed by the Food and Drug Administration to improve clinical trial data quality by focusing monitoring efforts on critical data elements and higher risk investigator sites. BIOTRONIK approached this by implementing a comprehensive strategy that assesses risk and data quality through a combination of operational controls and data surveillance. This publication demonstrates the effectiveness of a data-driven risk assessment methodology when used in conjunction with a tailored monitoring plan...
August 1, 2017: Clinical Trials: Journal of the Society for Clinical Trials
https://www.readbyqxmd.com/read/28819929/a-comparative-study-of-the-adhesion-of-biosynthesized-gold-and-conjugated-gold-prodigiosin-nanoparticles-to-triple-negative-breast-cancer-cells
#19
S O Dozie-Nwachukwu, J D Obayemi, Y Danyuo, N Anuku, O S Odusanya, K Malatesta, W O Soboyejo
This paper explores the adhesion of biosynthesized gold nanoparticles (AuNPs) and gold (Au) nanoparticle/prodigiosin (PG) drug nanoparticles to breast cancer cells (MDA-MB-231 cells). The AuNPs were synthesized in a record time (less than 30 s) from Nauclea latifolia leaf extracts, while the PG was produced via bacterial synthesis with Serratia marcescens sp. The size distributions and shapes of the resulting AuNPs were characterized using transmission electron microscopy (TEM), while the resulting hydrodynamic diameters and polydispersity indices were studied using dynamic light scattering (DLS)...
August 17, 2017: Journal of Materials Science. Materials in Medicine
https://www.readbyqxmd.com/read/28819800/nanotechnology-from-in-vivo-imaging-system-to-controlled-drug-delivery
#20
REVIEW
Maria Mir, Saba Ishtiaq, Samreen Rabia, Maryam Khatoon, Ahmad Zeb, Gul Majid Khan, Asim Ur Rehman, Fakhar Ud Din
Science and technology have always been the vitals of human's struggle, utilized exclusively for the development of novel tools and products, ranging from micro- to nanosize. Nanotechnology has gained significant attention due to its extensive applications in biomedicine, particularly related to bio imaging and drug delivery. Various nanodevices and nanomaterials have been developed for the diagnosis and treatment of different diseases. Herein, we have described two primary aspects of the nanomedicine, i.e...
August 17, 2017: Nanoscale Research Letters
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