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https://www.readbyqxmd.com/read/28346967/anticoagulation-therapy-in-children
#1
Vlad Calin Radulescu
Venous thromboembolism (VTE) is very uncommon in children and adolescents compared with older adults, though its incidence has significantly increased over the past two decades. Given the rarity of the condition, the data on pediatric VTE lag behind the adult experience and consequently the management of VTE in children is, in large part, modeled on the adult strategies. This approach has certain limitations, given that young children have developmental particularities of the hemostatic system and differences in the pharmacokinetics and pharmacodynamics of various anticoagulant agents...
March 27, 2017: Seminars in Thrombosis and Hemostasis
https://www.readbyqxmd.com/read/28346873/design-synthesis-docking-studies-and-biological-evaluation-of-novel-chalcone-derivatives-as-potential-histone-deacetylase-inhibitors
#2
Mamdouh F A Mohamed, Montaser Sh A Shaykoon, Mostafa H Abdelrahman, Bakheet E M Elsadek, Ahmed S Aboraia, Gamal El-Din A A Abuo-Rahma
A group of novel chalcone derivatives comprising hydroxamic acid or 2-aminobenzamide group as zinc binding groups (ZBG) were synthesized. The structure of the prepared compounds was fully characterized by IR, NMR and elemental microanalyses. Most of the tested compounds displayed strong to moderate HDAC inhibitory activity. Some of these compounds showed potent anti-proliferative activity against human HepG2, MCF-7 and HCT-116 cell lines. In particular, compounds 4a and 4b exhibited significant anti-proliferative activity against the three cell lines compared to SAHA as reference drug and displayed promising profile as anti-tumor candidates...
March 19, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28346814/nicotinamide-riboside-a-form-of-vitamin-b3-and-nad-precursor-relieves-the-nociceptive-and-aversive-dimensions-of-paclitaxel-induced-peripheral-neuropathy-in-female-rats
#3
Marta V Hamity, Stephanie R White, Roxanne Y Walder, Mark S Schmidt, Charles Brenner, Donna L Hammond
Injury to sensory afferents may contribute to the peripheral neuropathies that develop after administration of chemotherapeutic agents. Manipulations that increase levels of nicotinamide adenine dinucleotide (NAD) can protect against neuronal injury. This study examined whether nicotinamide riboside (NR), a third form of vitamin B3 and precursor of NAD, diminishes tactile hypersensitivity and place escape-avoidance behaviors in a rodent model of paclitaxel-induced peripheral neuropathy. Female Sprague-Dawley rats received 3 intravenous injections of 6...
January 30, 2017: Pain
https://www.readbyqxmd.com/read/28346540/fragment-library-screening-identifies-hits-that-bind-to-the-non-catalytic-surface-of-pseudomonas-aeruginosa-dsba1
#4
Biswaranjan Mohanty, Kieran Rimmer, Róisín M McMahon, Stephen J Headey, Mansha Vazirani, Stephen R Shouldice, Mathieu Coinçon, Stephanie Tay, Craig J Morton, Jamie S Simpson, Jennifer L Martin, Martin J Scanlon
At a time when the antibiotic drug discovery pipeline has stalled, antibiotic resistance is accelerating with catastrophic implications for our ability to treat bacterial infections. Globally we face the prospect of a future when common infections can once again kill. Anti-virulence approaches that target the capacity of the bacterium to cause disease rather than the growth or survival of the bacterium itself offer a tantalizing prospect of novel antimicrobials. They may also reduce the propensity to induce resistance by removing the strong selection pressure imparted by bactericidal or bacteriostatic agents...
2017: PloS One
https://www.readbyqxmd.com/read/28346237/current-and-future-pharmacologic-treatment-of-nonalcoholic-steatohepatitis
#5
Bubu A Banini, Arun J Sanyal
PURPOSE OF REVIEW: Nonalcoholic steatohepatitis (NASH), the aggressive form of nonalcoholic fatty liver disease (NAFLD), can progress to cirrhosis and hepatocellular cancer in 5-15% of patients and is rapidly becoming the leading cause for end-stage liver disease. Dietary caloric restriction and exercise, currently the cornerstone of therapy for NAFLD, can be difficult to achieve and maintain, underscoring the dire need for pharmacotherapy. This review presents the agents currently used in managing NAFLD and their pharmacologic targets...
March 24, 2017: Current Opinion in Gastroenterology
https://www.readbyqxmd.com/read/28346211/stability-of-two-antifungal-agents-fluconazole-and-miconazole-compounded-in-humco-recura-topical-cream-to-determine-beyond-use-date
#6
Pradeep Gautam, Bob Light, Troy Purvis
A novel compounding vehicle (RECURA) has previously been proven to penetrate the nail bed when compounded with the antifungal agent miconazole or fluconazole, providing for an effective treatment for onychomycosis. In this study, miconazole and fluconazole were compounded separately in RECURA compounding cream, and they were tested at different time points (0, 7, 14, 28, 45, 60, 90, and 180 days) to determine the beyond-use date of those formulations. The beyond-use date testing of both formulations (10% miconazole in RECURA and 10% fluconazole in RECURA) proved them to be physically, chemically, and microbiologically stable under International Conference of Harmonisation controlled room temperature (25°C ± 2°C/60% RH ±5%) for at least 180 days from the date of compounding...
March 2017: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28345337/light-up-mitophagy-in-live-cells-with-dual-functional-theranostic-phosphorescent-iridium-iii-complexes
#7
Mu-He Chen, Fang-Xin Wang, Jian-Jun Cao, Cai-Ping Tan, Liang-Nian Ji, Zong-Wan Mao
Phosphorescent Ir(III) complexes are ideal candidates to construct novel multifunctional theranostic platforms that enable the integration of imaging capabilities and anticancer properties. Selective autophagy of mitochondria, termed mitophagy, is an important cellular process that selectively degrades dysfunctional mitochondria. Until now, the regulation of mitophagy is still poorly understood. Herein, we present two phosphorescent cyclometalated iridium(III) complexes (Ir1 and Ir2) that can accumulate in mitochondria and induce mitophagy...
March 27, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28345206/treatment-with-direct-acting-antiviral-agents-of-hepatitis-c-virus-infection-in-injecting-drug-users-a-prospective-study
#8
Lucio Boglione, Simone Mornese Pinna, Amedeo De Nicolò, Jessica Cusato, Giuseppe Cariti, Giovanni Di Perri, Antonio D'Avolio
In this prospective study, we evaluated the effectiveness and tolerability of novel therapies against hepatitis C virus (HCV) in a cohort of PWID enrolled at our centre from April 2015 to July 2016. In this analysis, a total of 174 patients were included: 11 (6.3%) were treated with pegylated-interferon (PEG-IFN) and ribavirin (RBV) containing regimens, 163 (93.7%) with IFN-free treatments. RBV has been used in 70 patients (40.2%); 59 (33.9%) patients were in opioid substitution therapy (OST) with methadone or buprenorphine...
March 26, 2017: Journal of Viral Hepatitis
https://www.readbyqxmd.com/read/28345190/new-medicinal-products-for-chronic-heart-failure-advances-in-clinical-trial-design-and-efficacy-assessment
#9
REVIEW
Martin R Cowie, Gerasimos S Filippatos, Maria de Los Angeles Alonso Garcia, Stefan D Anker, Anna Baczynska, Daniel M Bloomfield, Maria Borentain, Karsten Bruins Slot, Maureen Cronin, Pieter A Doevendans, Amany El-Gazayerly, Claudio Gimpelewicz, Narimon Honarpour, Salim Janmohamed, Heidi Janssen, Albert M Kim, Dominik Lautsch, Ian Laws, Martin Lefkowitz, Jose Lopez-Sendon, Alexander R Lyon, Fady I Malik, John J V McMurray, Marco Metra, Santiago Figueroa Perez, Marc A Pfeffer, Stuart J Pocock, Piotr Ponikowski, Krishna Prasad, Isabelle Richard-Lordereau, Lothar Roessig, Giuseppe M C Rosano, Warren Sherman, Wendy Gattis Stough, Karl Swedberg, Benoit Tyl, Faiez Zannad, Caroline Boulton, Pieter De Graeff
Despite the availability of a number of different classes of therapeutic agents with proven efficacy in heart failure, the clinical course of heart failure patients is characterized by a reduction in life expectancy, a progressive decline in health-related quality of life and functional status, as well as a high risk of hospitalization. New approaches are needed to address the unmet medical needs of this patient population. The European Medicines Agency (EMA) is undertaking a revision of its Guideline on Clinical Investigation of Medicinal Products for the Treatment of Chronic Heart Failure...
March 27, 2017: European Journal of Heart Failure
https://www.readbyqxmd.com/read/28344576/genomic-characterization-of-recent-chicken-anemia-virus-isolates-in-china
#10
Yang Li, Lichun Fang, Shuai Cui, Jiayuan Fu, Xiaohan Li, Huanmin Zhang, Zhizhong Cui, Shuang Chang, Weifeng Shi, Peng Zhao
Chicken anemia virus (CAV) causes diseases in young chickens, which include increased pathogenicity of secondary infectious agents, generalized lymphoid depletion, and immunodepression. In the present study, we have identified 22 CAV strains isolated from several commercial chicken farms in Northern China during 2014-2015. In addition, two CAVs were also isolated from stray mouse and dog feces, respectively. To our knowledge, this is the first report of identification of CAV from mouse and dog feces. Phylogenetic analysis of 121 full-length CAV genome sequences showed that all available CAV could be classified into eight lineages, supported by phylogenetic trees estimated using different methods...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28344479/synthesis-of-chalcone-incorporated-quinazoline-derivatives-as-anticancer-agents
#11
Sapavat Madhavi, Reddymasu Sreenivasulu, Jyothsna Pragathi Yazala, Rudraraju Ramesh Raju
A series of ten novel chalcone incorporated quinazoline derivatives (11a-11j) were designed and synthesized. All the synthesized compounds were evaluated for their anticancer activities against four human cancer cell lines (A549, HT-29, MCF-7 and A375). Among them, four compounds, 11f, 11g, 11i and 11j showed more potent anticancer activity than the control drug, Combretastatin - A4.
February 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28344475/antiproliferative-and-apoptotic-effect-of-morus-nigra-extract-on-human-prostate-cancer-cells
#12
Ibrahim Turan, Selim Demir, Kagan Kilinc, Nesibe Arslan Burnaz, Serap Ozer Yaman, Kubra Akbulut, Ahmet Mentese, Yuksel Aliyazicioglu, Orhan Deger
Background: Morus nigra L. belongs to the family Moraceae and is frequently used in traditional medicine. Numerous studies have investigated the antiproliferative effects of various extracts of different Morus species, but studies involving the in vitro cytotoxic effect of M. nigra extract are very limited. The purpose of this study was to evaluate the phenolic composition and antioxidant activity of dimethyl sulfoxide extract of M. nigra (DEM) and to investigate, for the first time, the probable cytotoxic effect in human prostate adenocarcinoma (PC-3) cells together with the mechanism involved...
February 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28344015/transdermal-delivery-of-atorvastatin-calcium-from-novel-nanovesicular-systems-using-polyethylene-glycol-fatty-acid-esters-ameliorated-effect-without-liver-toxicity-in-poloxamer-407-induced-hyperlipidemic-rats
#13
Mohamed O Mahmoud, Heba M Aboud, Amira H Hassan, Adel A Ali, Thomas P Johnston
CONTEXT: Atorvastatin calcium (ATV), a cholesterol-lowering agent, suffers from poor systemic availability (14%) after oral administration in addition to other side effects on the gastrointestinal tract, liver and muscle. OBJECTIVE: The goal of the present investigation was to improve ATV bioavailability and overcome complications attendant with peroral administration by developing a new nanovesicular system encapsulating ATV for its delivery via the transdermal route...
March 23, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28343773/enhancing-heterologous-protection-in-pigs-vaccinated-with-chimeric-porcine-reproductive-and-respiratory-syndrome-virus-containing-the-full-length-sequences-of-shuffled-structural-genes-of-multiple-heterologous-strains
#14
Debin Tian, Dianjun Cao, C Lynn Heffron, Danielle M Yugo, Adam J Rogers, Christopher Overend, Shannon R Matzinger, Sakthivel Subramaniam, Tanja Opriessnig, Tanya LeRoith, Xiang-Jin Meng
Porcine reproductive and respiratory syndrome virus (PRRSV) is the causative agent of arguably the most economically important global swine disease. The extensive genetic variation of PRRSV strains is a major obstacle for heterologous protection of current vaccines. Previously, we constructed a panel of chimeric viruses containing only the ectodomain sequences of DNA-shuffled structural genes of different PRRSV strains in the backbone of a commercial vaccine, and found that one chimeric virus had an improved cross-protection efficacy...
March 23, 2017: Vaccine
https://www.readbyqxmd.com/read/28343293/pharmacokinetic-and-pharmacodynamic-considerations-in-the-treatment-of-chronic-lymphocytic-leukemia-ibrutinib-idelalisib-and-venetoclax
#15
REVIEW
Madeline Waldron, Allison Winter, Brian T Hill
Management of chronic lymphocytic leukemia has changed markedly over the last several years with the emergence of several novel oral agents targeting B-cell receptor and Bcl-2 signaling pathways. For patients requiring treatment, ibrutinib, idelalisib, and venetoclax offer unique clinical benefits with a different set of therapeutic considerations compared with traditional parenteral therapy. Despite the conveniences afforded by oral therapy, these agents also carry unique logistical obstacles. Drug interactions with agents that are metabolized via the cytochrome P450 3A4 pathway are possible with all three agents...
March 25, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28343119/synergistically-enhanced-stability-of-laccase-immobilized-on-synthesized-silver-nanoparticles-with-water-soluble-polymers
#16
M N M Cunha, H P Felgueiras, I Gouveia, A Zille
Silver nanoparticles (AgNPs) were synthesized by citrate reduction method in the presence of polymers, poly(ethylene glycol) (PEG), poly(vinyl alcohol) (PVA) and chitosan, used as stabilizing agents, and an oxidoreductase enzyme, laccase (Lac), with the goal of expanding the NPs antimicrobial action. AgNPs were characterized by UV-vis spectrometry, dynamic light scattering and transmission electron microscopy. As protecting agents, PEG and PVA promoted the formation of spherical uniformly-shaped, small-sized, monodispersed AgNPs (≈20nm)...
March 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28342971/a-novel-dual-glp-1-gip-receptor-agonist-alleviates-cognitive-decline-by-re-sensitizing-insulin-signaling-in-the-alzheimer-icv-stz-rat-model
#17
Lijuan Shi, Zhihua Zhang, Lin Li, Christian Hölscher
Alzheimer's disease (AD) is a progressive neurodegenerative disorder, accompanied by memory loss and cognitive impairments, and there is no effective treatment for it at present. Since type 2 diabetes (T2DM) has been identified as a risk factor for AD, the incretins glucagon-like peptide 1 (GLP-1) and glucose dependent insulinotropic polypeptide (GIP), promising antidiabetic agents for the treatment of type 2 diabetes, have been tested in models of neurodegenerative disease including AD and achieved good results...
March 22, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28342744/synthesis-and-anti-cancer-activity-of-chiral-tetrahydropyrazolo-1-5-a-pyridine-fused-steroids
#18
Susana M M Lopes, Emanuel P Sousa, Luísa Barreira, Cátia Marques, Maria João Rodrigues, Teresa M V D Pinho E Melo
Regio- and stereoselective synthesis of novel chiral 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused steroids via [8π+2π] cycloaddition of diazafulvenium methides with steroidal scaffolds is reported. The biological evaluation of the new family of hexacyclic steroids as anti-cancer agents was also carried out. Hexacyclic steroids bearing a benzyl group at C-22, derived from 16-dehydropregnenolone and 16-dehydroprogesterone, show considerable cytotoxicity against EL4 (murine T-lymphoma) in contrast with the corresponding C-22-unsubstituted derivatives showing low cytotoxicity...
March 22, 2017: Steroids
https://www.readbyqxmd.com/read/28342399/design-synthesis-and-biological-evaluation-of-pegylated-xenopus-glucagon-like-peptide-1-derivatives-as-long-acting-hypoglycemic-agents
#19
Jing Han, Yiyun Wang, Qinghua Meng, Guangchao Li, Fangmin Huang, Su Wu, Yingying Fei, Feng Zhou, Junjie Fu
In order to develop novel long-acting GLP-1 derivatives, a peptide hybrid (1a) from human GLP-1 and Xenopus GLP-1 discovered in our previous research was selected as the lead compound. Exendin-4 inspired modification resulted in peptide 1b with enhanced glucose-lowering activity. Cysteine mutated 1b derivatives with reserved bioactivity were further site-specifically connected with mPEG2000-MAL to provide conjugates 3a-h, among which 3d and 3e were found to have significantly improved hypoglycemic activity and insulinotropic ability than GLP-1...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28342031/ibrutinib-in-cll-a-focus-on-adverse-events-resistance-and-novel-approaches-beyond-ibrutinib
#20
REVIEW
Varinder Kaur, Arjun Swami
Bruton's tyrosine kinase (BTK), a mediator in B cell receptor signaling has been successfully exploited as a therapeutic target in treatment of chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL). Ibrutinib is a BTK inhibitor that has shown excellent efficacy in treatment-naïve, heavily pre-treated, and high-risk CLL/SLL. With remarkable efficacy, good oral bioavailability, and modest adverse events profile, ibrutinib use is likely to continue to increase. As data with ibrutinib use in CLL matures, concerns regarding adverse events and drug resistance have emerged...
March 24, 2017: Annals of Hematology
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