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https://www.readbyqxmd.com/read/28088690/electrochemical-studies-of-dna-interaction-and-antimicrobial-activities-of-mn-ii-fe-iii-co-ii-and-ni-ii-schiff-base-tetraazamacrocyclic-complexes
#1
Anuj Kumar, Vinod Kumar Vashistha, Prashant Tevatia, Randhir Singh
Tetraazamacrocyclic complexes of Mn(II), Fe(III), Co(II) and Ni(II) have been synthesized by template method. These tetraazamacrocycles have been analyzed with various techniques like molar conductance, IR, UV-vis, mass spectral and cyclic voltammetric studies. On the basis of all these studies, octahedral geometry has been assigned to these tetraazamacrocyclic complexes. The DNA binding properties of these macrocyclic complexes have been investigated by electronic absorption spectra, fluorescence spectra, cyclic voltammetric and differential pulse voltammetric studies...
January 6, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28088632/nanosized-complexation-assemblies-housed-inside-reverse-micelles-churn-out-monocytic-delivery-cores-for-bendamustine-hydrochloride
#2
Yuvraj Singh, Anumandla Chandrashekhar, Jaya Gopal Meher, K K Durga Rao Viswanadham, Vivek K Pawar, Kavit Raval, Komal Sharma, Pankaj K Singh, Animesh Kumar, Manish K Chourasia
OBJECTIVE: We explore a plausible method of targeting bendamustine hydrochloride (BM) to circulatory monocytes by exploiting their intrinsic endocytic/phagocytic capability. METHODS: We do so by complexation of sodium alginate and chitosan inside dioctyl sulfo succinate sodium (AOT) reverse micelles to form bendamustine hydrochloride loaded nanoparticles (CANPs). Dynamic light scattering, electrophoretic mobility and UV spectroscopy were used to detail intra-micellar complexation dynamics and to prove that drug was co-captured during interaction of carbohydrate polymers...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088442/the-in-vivo-fate-of-nanocrystals
#3
REVIEW
Yi Lu, Jianping Qi, Xiaochun Dong, Weili Zhao, Wei Wu
There has been significant research interest in, and development of, nanocrystals in recent years for the delivery of poorly water-soluble drugs via various routes. However, there is a common misinterpretation of nanocrystallization as an approach to modulate, and more specifically to enhance, the dissolution of drug crystals. Nevertheless, it is possible for nanocrystals to interact with biological tissues because nanocrystals can survive for a longer duration in vivo compared with XXXX. Therefore, understanding the in vivo fate of nanocrystals and determining its contribution to XXXX is of tremendous significance for optimizing the performance of nanocrystals...
January 11, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28088085/new-pyridazinone-4-carboxamides-as-new-cannabinoid-receptor-type-2-inverse-agonists-synthesis-pharmacological-data-and-molecular-docking
#4
Giulio Ragusa, María Gómez-Cañas, Paula Morales, Carmen Rodríguez-Cueto, María R Pazos, Battistina Asproni, Elena Cichero, Paola Fossa, Gerard A Pinna, Nadine Jagerovic, Javier Fernández-Ruiz, Gabriele Murineddu
In the last few years, cannabinoid type-2 receptor (CB2R) selective ligands have shown a great potential as novel therapeutic drugs in several diseases. With the aim of discovering new selective cannabinoid ligands, a series of pyridazinone-4-carboxamides was designed and synthesized, and the new derivatives tested for their affinity toward the hCB1R and hCB2R. The 6-(4-chloro-3-methylphenyl)-2-(4-fluorobenzyl)-N-(cis-4-methylcyclohexyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide (9) displayed high CB2-affinity (KiCB2 = 2...
January 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28088076/in%C3%A2-vivo-visualization-of-endogenous-mir-21-using-hyaluronic-acid-coated-graphene-oxide-for-targeted-cancer-therapy
#5
Do Won Hwang, Han Young Kim, Fangyuan Li, Ji Yong Park, Dohyun Kim, Jae Hyung Park, Hwa Seung Han, Jung Woo Byun, Yun-Sang Lee, Jae Min Jeong, Kookheon Char, Dong Soo Lee
Oncogene-targeted nucleic acid therapy has been spotlighted as a new paradigm for cancer therapeutics. However, in vivo delivery issues and uncertainty of therapeutic antisense drug reactions remain critical hurdles for a successful targeted cancer therapy. In this study, we developed a fluorescence-switchable theranostic nanoplatform using hyaluronic acid (HA)-conjugated graphene oxide (GO), which is capable of both sensing oncogenic miR-21 and inhibiting its tumorigenicity simultaneously. Cy3-labeled antisense miR-21 peptide nucleic acid (PNA) probes loaded onto HA-GO (HGP21) specifically targeted CD44-positive MBA-MB231 cells and showed fluorescence recovery by interacting with endogenous miR-21 in the cytoplasm of the MBA-MB231 cells...
December 31, 2016: Biomaterials
https://www.readbyqxmd.com/read/28088050/pharmacists-knowledge-of-issues-in-pharmacotherapy-of-epilepsy-using-antiepileptic-drugs-a-cross-sectional-study-in-palestinian-pharmacy-practice
#6
Ramzi Shawahna, Ahlam Atrash, Aman Jebril, Areen Khalaf, Eman Shaheen, Hala Tahboosh
OBJECTIVE: Antiepileptic drugs (AEDs) are mainstay in controlling epileptic seizures. As experts in medications, pharmacists should be able to ensure accuracy of dosing regimens, explain adverse effects, and screen for and alert people with epilepsy (PWE) and their physicians to possible drug-drug interactions (DDIs). The aim of this study was to evaluate pharmacists' knowledge of issues in pharmacotherapy of epilepsy using AEDs. METHODS: This was a cross-sectional observational study conducted in the Palestinian pharmacy practice...
January 11, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28088032/oral-cannabidiol-does-not-produce-a-signal-for-abuse-liability-in-frequent-marijuana-smokers
#7
Shanna Babalonis, Margaret Haney, Robert J Malcolm, Michelle R Lofwall, Victoria R Votaw, Steven Sparenborg, Sharon L Walsh
BACKGROUND: Cannabidiol (CBD) is a naturally occurring constituent of the marijuana plant. In the past few years, there has been great interest in the therapeutic effects of isolated CBD and it is currently being explored for numerous disease conditions (e.g., pain, epilepsy, cancer, various drug dependencies). However, CBD remains a Schedule I drug on the U.S. Controlled Substances Act (CSA). Despite its status, there are no well-controlled data available regarding its abuse liability...
December 14, 2016: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28088003/the-effect-of-the-antioxidant-on-the-properties-of-thiolated-poly-aspartic-acid-polymers-in-aqueous-ocular-formulations
#8
Mária Budai-Szűcs, Gabriella Horvát, Benjámin Gyarmati, Barnabás Áron Szilágyi, András Szilágyi, Szilvia Berkó, Rita Ambrus, Piroska Szabó-Révész, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Caramella, Erzsébet Csányi
Thiolated polymers are a promising new group of excipients, but their stability against atmospheric oxidation has not been investigated in detail, and only a few efforts have been made to improve their stability. The oxidation of the thiol groups in solutions of thiolated polymers may result in a decrease of mucoadhesion and unpredictable in situ gelation. The aims of our work were to study the stability of aqueous solutions of thiolated polymers and the effects of stabilizing agents. We investigated thiolated poly(aspartic acid) polymers stabilized with dithiothreitol, glutathione or acetylcysteine...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087739/tnf-signaling-through-rip1-kinase-enhances-sn38-induced-death-in-colon-adenocarcinoma
#9
Lucia Cabal-Hierro, Peter J O'Dwyer
: Elucidation of tumor necrosis factor (TNF)-directed mechanisms for cell death induction and maintenance of tumor growth has revealed a role for receptor-interacting protein kinases 1 and 3 (RIPK1/RIP1 and RIPK3/RIP3), components of the necrosome complex, as determinants of cell fate. Here the participation of TNF signaling was analyzed with regard to the cytotoxic action of different DNA damaging agents in a panel of colon cancer cells. While most of these cell lines were insensitive to TNF, combination with these drugs increased sensitivity by inducing cell death and DNA damage, especially in the case of the topoisomerase inhibitor SN38...
January 13, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28087697/development-of-high-affinity-and-high-specificity-inhibitors-of-metalloproteinase-14-through-computational-design-and-directed-evolution
#10
Valeria Arkadash, Gal Yosef, Jason Shirian, Itay Cohen, Yuval Horev, Moran Grossman, Irit Sagi, Evette S Radisky, Julia M Shifman, Niv Papo
Degradation of the extracellular matrices in the human body is controlled by matrix metalloproteinases (MMPs), a family of more than 20 homologous enzymes. Imbalance in MMP activity can result in many diseases, such as arthritis, cardiovascular diseases, neurological disorders, fibrosis, and cancers. Thus, MMPs present attractive targets for drug design and have been a focus for inhibitor design for as long as three decades. Yet, to date, all MMP inhibitors have failed in clinical trials because of their broad activity against numerous MMP family members and the serious side effects of the proposed treatment...
January 13, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28087443/an-update-on-the-physiological-and-therapeutic-relevance-of-gpcr-oligomers
#11
REVIEW
Batoul Farran
The traditional view on GPCRs held that they function as single monomeric units composed of identical subunits. This notion was overturned by the discovery that GPCRs can form homo- and hetero-oligomers, some of which are obligatory, and can further assemble into receptor mosaics consisting of three or more protomers. Oligomerisation exerts significant impacts on receptor function and physiology, offering a platform for the diversification of receptor signalling, pharmacology, regulation, crosstalk, internalization and trafficking...
January 10, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28087379/pegylated-liposomes-for-topical-vaginal-therapy-improve-delivery-of-interferon-alpha
#12
May Wenche Jøraholmen, Purusotam Basnet, Ganesh Acharya, Nataša Škalko-Basnet
Recent studies regarding mucosal drug delivery indicate that nanosystems with surface-available polyethylene glycol (PEG) are able to penetrate mucus barrier, assure closer contact with the epithelium, and improve drug delivery to vagina. In the present work, we developed the mucus-penetrating PEGylated liposomes containing interferon alpha-2b (IFN α-2b), destined to provide localized therapy for human papilloma virus (HPV) vaginal infections. The PEGylated liposomes were of a mean size of 181 ± 8 nm, bearing a negative zeta potential of - 13 mV and an entrapment efficiency of 81 ± 10 %...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087374/what-stoichiometries-determined-by-mass-spectrometry-reveal-about-the-ligand-binding-mode-to-g-quadruplex-nucleic-acids
#13
Michael J Lecours, Adrien Marchand, Ahdia Anwar, Corinne Guetta, W Scott Hopkins, Valérie Gabelica
G-quadruplexes (G4s) have become important drug targets to regulate gene expression and telomere maintenance. Many studies on G4 ligand binding focus on determining the ligand binding affinities and selectivities. Ligands, however, can also affect the G4 conformation. Here we explain how to use electrospray ionization mass spectrometry (ESI-MS) to monitor simultaneously ligand binding and cation binding stoichiometries. The changes in potassium binding stoichiometry upon ligand binding hint at ligand-induced conformational changes involving a modification of the number of G-quartets...
January 10, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28087355/generation-of-quercetin-cellulose-acetate-phthalate-systems-for-delivery-by-supercritical-antisolvent-process
#14
I García-Casas, A Montes, C Pereyra, E J Martínez de la Ossa
Supercritical antisolvent process (SAS) has been used to precipitate microparticles of quercetin, a plant pigment found in many foods and used for medical treatments, pharmaceutical and cosmetic industries, together with nanoparticles of cellulose acetate phthalate (CAP), a polymer quite frequently used in drug delivery. Previously, precipitation of nanoparticles of CAP by the same process was studied at different conditions of pressure, temperature, CO2and solution flow rates, nozzle diameter and initial concentration of the solution...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28087354/effect-of-piroxicam-on-lipid-membranes-drug-encapsulation-and-gastric-toxicity-aspects
#15
Natalia Wilkosz, Sami Rissanen, Małgorzata Cyza, Renata Szybka, Maria Nowakowska, Alex Bunker, Tomasz Róg, Mariusz Kepczynski
Uptake of piroxicam, a non-steroidal anti-inflammatory drug, from the intestines after oral intake is limited due to its low solubility and its wide use is associated with several side effects related to the gastrointestinal tract. In this study, all-atom molecular dynamics (MD) simulations and fluorescent spectroscopy were employed to investigate the interaction of piroxicam in neutral, zwitterionic, and cationic forms with lipid bilayers composed of phosphatidylcholine, cholesterol, and PEGylated lipids. Our study was aimed to assess the potential for encapsulation of piroxicam in liposomal carriers and to shed more light on the process of gastrointestinal tract injury by the drug...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28087343/calcium-remodeling-in-colorectal-cancer
#16
REVIEW
Carlos Villalobos, Diego Sobradillo, Miriam Hernández-Morales, Lucía Núñez
: Colorectal cancer (CRC) is the third most frequent form of cancer and the fourth leading cause of cancer-related death in the world. Basic and clinical data indicate that aspirin and other non-steroidal anti-inflammatory drugs (NSAIDs) may prevent colon cancer but mechanisms remain unknown. Aspirin metabolite salicylate and other NSAIDs may inhibit tumor cell growth acting on store-operated Ca(2+) entry (SOCE), suggesting an important role for this pathway in CRC. Consistently, SOCE is emerging as a novel player in different forms of cancer, including CRC...
January 10, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28087315/assessing-light-independent-effects-of-hypericin-on-cell-viability-ultrastructure-and-metabolism-in-human-glioma-and-endothelial-cells
#17
Veronika Huntosova, Marta Novotova, Zuzana Nichtova, Lucia Balogova, Maria Maslanakova, Dana Petrovajova, Katarina Stroffekova
Cell exposure to light-independent effects of photosensitizers (PS) used in PDT is clinically relevant when PS affect the pro-apoptotic cascade.In many malignant cells, Hypericin (Hyp) has PS displayed light-dependent anti-proliferative and cytotoxic effects with no cytotoxicity in the dark. Recent studies have shown that Hyp also exhibited light-independent cytotoxic effects in a wide range of concentrations. The molecular mechanisms underlying Hyp light-independent (dark) toxicity may be due to its interaction with different molecules at the Hyp accumulation sites including mitochondria, and these mechanisms are not understood in detail...
January 10, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28087250/pharmacology-of-cannabinoids-in-the-treatment-of-epilepsy
#18
REVIEW
Tyler E Gaston, Daniel Friedman
The use of cannabis products in the treatment of epilepsy has long been of interest to researchers and clinicians alike; however, until recently very little published data were available to support its use. This article summarizes the available scientific data of pharmacology from human and animal studies on the major cannabinoids which have been of interest in the treatment of epilepsy, including ∆9-tetrahydrocannabinol (∆9-THC), cannabidiol (CBD), ∆9-tetrahydrocannabivarin (∆9-THCV), cannabidivarin (CBDV), and ∆9-tetrahydrocannabinolic acid (Δ9-THCA)...
January 10, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28086980/inflammation-in-epileptogenesis-after-traumatic-brain-injury
#19
REVIEW
Kyria M Webster, Mujun Sun, Peter Crack, Terence J O'Brien, Sandy R Shultz, Bridgette D Semple
BACKGROUND: Epilepsy is a common and debilitating consequence of traumatic brain injury (TBI). Seizures contribute to progressive neurodegeneration and poor functional and psychosocial outcomes for TBI survivors, and epilepsy after TBI is often resistant to existing anti-epileptic drugs. The development of post-traumatic epilepsy (PTE) occurs in a complex neurobiological environment characterized by ongoing TBI-induced secondary injury processes. Neuroinflammation is an important secondary injury process, though how it contributes to epileptogenesis, and the development of chronic, spontaneous seizure activity, remains poorly understood...
January 13, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28086831/evaluation-of-the-cytotoxicity-of-the-bithionol-cisplatin-combination-in-a-panel-of-human-ovarian-cancer-cell-lines
#20
Vijayalakshmi N Ayyagari, Tsung-Han Jeff Hsieh, Paula L Diaz-Sylvester, Laurent Brard
BACKGROUND: Combination drug therapy appears a promising approach to overcome drug resistance and reduce drug-related toxicities in ovarian cancer treatments. In this in vitro study, we evaluated the antitumor efficacy of cisplatin in combination with Bithionol (BT) against a panel of ovarian cancer cell lines with special focus on cisplatin-sensitive and cisplatin-resistant cell lines. The primary objectives of this study are to determine the nature of the interactions between BT and cisplatin and to understand the mechanism(s) of action of BT-cisplatin combination...
January 13, 2017: BMC Cancer
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