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https://www.readbyqxmd.com/read/29778893/synthesis-of-proline-derived-benzenesulfonamides-a-potent-anti-trypanosoma-brucei-gambiense-agent
#1
David I Ugwu, Uchechukwu C Okoro, Narendra K Mishra
Thousands of death in Africa and other developing nations are still attributed to trypanosomiasis. Excessive sleep has been associated with increased inflammation. We report herein, the synthesis, antitrypanosomal and anti-inflammatory activities of eight new carboxamide derivatives bearing substituted benzenesulfonamides. The base promoted reactions of l-proline and L-4-hydroxyproline with substituted benzenesulfonyl chlorides gave the benzenesulfonamides (11a-h) in excellent yields. Boric acid mediated amidation of the benzenesulfonamides (11a-h) and p-aminobenzoic acid (12) gave the new carboxamides (13a-h) in excellent yields...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29778526/rt-qpcr-analysis-of-human-melanoma-progression-related-genes-a-novel-workflow-for-selection-and-validation-of-candidate-reference-genes
#2
Marcelina E Janik, Sabina Szwed, Paweł Grzmil, Radosław Kaczmarek, Marcin Czerwiński, Dorota Hoja-Łukowicz
The objective of this study was to identify a normalizer or combination of normalizers for quantitative evaluation of the expression of a target gene of interest during melanoma progression. Adult melanocytes, uveal primary melanoma cells and cutaneous primary and metastatic melanoma cells were used to construct a panel of 14 experimental models reflecting cancer promotion and progression. Hypoxanthine phosphoribosyltransferase 1 (HPRT1), glucuronidase beta (GUSB), ribosomal protein S23 (RPS23), phosphoglycerate kinase 1 (PGK1) and small nuclear ribonucleoprotein polypeptide A (SRNPA) were chosen as candidate housekeeping genes...
May 17, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29777135/n-methyl-d-aspartate-receptor-subtype-2b-antagonist-ro-25-6981-attenuates-neuropathic-pain-by-inhibiting-postsynaptic-density-95-expression
#3
Ling-Er Huang, Shao-Hui Guo, Lalita Thitiseranee, Yan Yang, Yan-Feng Zhou, Yong-Xing Yao
Postsynaptic density-95 (PSD-95) is a synaptic scaffolding protein that plays a crucial role in the development of neuropathic pain. However, the underlying mechanism remains unclear. To address the role of PSD-95 in N-methyl-D-aspartate receptor subtype 2B (NR2B) -mediated chronic pain, we investigated the relationship between PSD-95 activation and NR2B function in the spinal cord, by using a rat model of sciatic nerve chronic constriction injury (CCI). We demonstrate that the expression levels of total PSD-95 and cAMP response element binding protein (CREB), as well as phosphorylated NR2B, PSD-95, and CREB, in the spinal dorsal horn, and the interaction of NR2B with PSD-95 were increased in the CCI animals...
May 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29776677/myotropic-activity-of-allatostatins-in-tenebrionid-beetles
#4
Jan Lubawy, Paweł Marciniak, Mariola Kuczer, Grzegorz Rosiński
Neuropeptides control the functioning of the nervous system of insects, and they are the most diverse signalling molecules in terms of structure and function. Allatostatins are pleiotropic neuropeptides that are considered potent myoinhibitors of muscle contractions in insects. We investigated the effects caused by three distinct allatostatins, Dippu-AST1 (LYDFGL-NH2 from Diploptera punctata), Grybi-MIP1 (GWQDLNGGW-NH2 from Gryllus bimaculatus) and Trica-ASTC (pESRYRQCYFNPISCF-OH from Tribolium castaneum) on contractile activity of the myocardium, oviduct and hindgut of two tenebrionid beetles, Tenebrio molitor and Zophobas atratus...
May 9, 2018: Neuropeptides
https://www.readbyqxmd.com/read/29776484/corticotropin-releasing-factor-in-the-brain-and-blocking-spinal-descending-signals-induce-hyperalgesia-in-the-latent-sensitization-model-of-chronic-pain
#5
Wenling Chen, Yvette Taché, Juan Carlos Marvizón
Latent sensitization is a model of chronic pain in which an injury triggers a period of hyperalgesia followed by an apparent recovery, but in which pain sensitization persists but is suppressed by opioid and adrenergic receptors. One important characteristic of latent sensitization is that hyperalgesia can be triggered by acute stress. To determine whether the effect of stress is mimicked by the activation of corticotropin-releasing factor (CRF) signaling in the brain, rats with latent sensitization induced by injecting complete Freund's adjuvant (CFA, 50 μl) in one hind paw were given an intracerebroventricular (i...
June 15, 2018: Neuroscience
https://www.readbyqxmd.com/read/29776392/molecular-identification-of-tick-borne-pathogens-in-asymptomatic-individuals-with-human-immunodeficiency-virus-type-1-hiv-1-infection-a-retrospective-study
#6
Renata Welc-Falęciak, Justyna D Kowalska, Małgorzata Bednarska, Magdalena Szatan, Agnieszka Pawełczyk
BACKGROUND: The studies on the occurrence and diversity of tick-borne infections in HIV-infected individuals have been few, and the subject has been relatively neglected when compared with other common infections associated with HIV. In HIV-positive patients in whom a serological diagnostics is complicated due to reduced positive predictive value, a method where the microorganism is detected directly is of great value. Therefore, we performed a molecular study to ascertain the prevalence and incidence of tick-borne infections in HIV-infected persons in Poland, an endemic area for Ixodes ricinus ticks...
May 18, 2018: BMC Infectious Diseases
https://www.readbyqxmd.com/read/29775465/a-nocturnal-rail-with-a-simple-territorial-call-eavesdrops-on-interactions-between-rivals
#7
Lucyna Ewa Wojas, Paweł Wojciech Podkowa, Tomasz Stanisław Osiejuk
The behaviour of most animals has evolved in a communication network environment, in which signals produced by senders are perceived by many intended and unintended receivers. In this study, we tested whether the corncrake (Crex crex), a nocturnal rail species with innate (non-learned) calls, is able to eavesdrop on the interactions of conspecific males and how this eavesdropping affects subsequent responses by the eavesdropper to territorial intrusion. In the first step, simulated aggressive or neutral interactions between male dyads were presented to a focal male...
2018: PloS One
https://www.readbyqxmd.com/read/29773948/the-impact-of-total-sleep-deprivation-upon-cognitive-functioning-in-firefighters
#8
Sławomir Kujawski, Joanna Słomko, Małgorzata Tafil-Klawe, Monika Zawadka-Kunikowska, Justyna Szrajda, Julia L Newton, Paweł Zalewski, Jacek J Klawe
Introduction: Firefighters as a profession are required to maintain high levels of attention for prolonged periods. However, total sleep deprivation (TSD) could influence negatively upon performance, particularly when the task is prolonged and repetitive. Purpose: The aim of this study is to examine the influence of TSD on cognitive functioning in a group of firefighters. Subjects and methods: Sixty volunteers who were active male fire brigade officers were examined with a computerized battery test that consisted of simple reaction time (SRT) (repeated three times), choice reaction time, visual attention test, and delayed matching to sample...
2018: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/29773760/a-review-of-methods-for-preventing-pancreatic-fistula-after-distal-pancreatectomy
#9
Katarzyna Mech, Łukasz Wysocki, Tomasz Guzel, Marcin Makiewicz, Paweł Nyckowski, Maciej Słodkowski
Pancreatic fistula is one of the most severe complications after pancreatic surgeries. The risk of pancreatic fistula after distal pancreatectomy is up to 60%. Effective methods to prevent pancreatic fistula are still sought. A unified definition of pancreatic fistula, which was introduced in 2005 by the International Study Group of Pancreatic Surgery (ISGPS), has allowed for an easier diagnosis and determination of fistula severity, as well as for a reliable inter-center comparison of data. Furthermore, a number of publications point out the risk factors of pancreatic fistula, which may be classified into patient-related risk factors, such as MBI, gender, smoking tobacco or pancreatic structure; and surgery-related risk factors, such as blood loss, prolonged surgery and non-underpinning of the major pancreatic duct...
April 30, 2018: Polski Przeglad Chirurgiczny
https://www.readbyqxmd.com/read/29773758/absorbable-sutures-in-general-surgery-review-available-materials-and-optimum-choices
#10
Marcin Gierek, Katarzyna Kuśnierz, Paweł Lampe, Gabriela Ochała, Józef Kurek, Bartłomiej Hekner, Katarzyna Merkel, Jakub Majewski
Sutures are the most versatile materials used in surgery. Despite recent technological advances and availability of novel materials such as tissue cements, it appears that surgical sutures will continue to be used for many years to come. The objective of this study was to provide an overview of the most common absorbable sutures used in general surgery. The appropriate suture choice for a particular procedure is of key importance for the success of that procedure.
April 30, 2018: Polski Przeglad Chirurgiczny
https://www.readbyqxmd.com/read/29773191/anti-inflammatory-and-antinociceptive-effects-of-2-2-dipyridyl-diselenide-through-reduction-of-inducible-nitric-oxide-synthase-nuclear-factor-kappa-b-and-c-jun-n-terminal-kinase-phosphorylation-levels-in-the-mouse-spinal-cord
#11
Suzan Gonçalves Rosa, César Augusto Brüning, Ana Paula Pesarico, Ana Cristina Guerra de Souza, Cristina Wayne Nogueira
Appropriate treatment of pain requires analgesics and anti-inflammatory drugs generally associated with undesirable side effects and not fully effective in a significant proportion of patients. Organoselenium compounds elicit a plenty of pharmacological effects in different animal models. Among these compounds, the 2,2`-dipyridyl diselenide (DPD) has a potent antioxidant effect and low toxicity. In this way, the aim of this study was to investigate the possible DPD antinociceptive effect and its mechanism of action, as well as the safety of the compound...
July 2018: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/29773000/evaluation-of-antiarthritic-activity-of-butanol-fraction-of-punica-granatum-linn-rind-extract-against-freund-s-complete-adjuvant-induced-arthritis-in-rats
#12
Rupesh Kumar Gautam, Sanjay Sharma, Komal Sharma, Gaurav Gupta
Available conventional drugs produce several side effects; thus, a potent herbal drug is urgently required for the management of rheumatoid arthritis. The present investigation was performed to evaluate the antiarthritic activity of butanol fraction of Punica granatum Linn. rind methanolic extract (PGBF) against Freund's complete adjuvant (FCA)-induced arthritis in rats. An acute toxicity study of butanol fraction was conducted, accompanied by a study of its antiarthritic activity. Chromatography (thin layer chromatography and high-performance thin layer chromatography) analyses were also conducted...
2018: Journal of Environmental Pathology, Toxicology and Oncology
https://www.readbyqxmd.com/read/29772271/pain-management-after-bone-reconstruction-surgery-using-an-analgesic-bone-cement-a-functional-non-invasive-in-vivo-study-using-gait-analysis
#13
Manon Dupleichs, Martial Masson, Olivier Gauthier, Maeva Dutilleul, Jean-Michel Bouler, Elise Verron, Pascal Janvier
Postoperative pain following bone reconstruction is a serious complication that could jeopardize the global success of a surgery. This pain must be controlled and minimized during the first 3-4 postoperative days to prevent it from becoming chronic. In this study, a critical-size bone defect was created at the femoral distal end of rats and filled by an injectable calcium phosphate cement (CPC) loaded or not with local anesthetics (bupivacaine or ropivacaine). A functional evaluation of the gait was performed using the CatWalk system to compare the postoperative pain relief enhanced by the different CPCs after such a bone filling surgery...
May 14, 2018: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/29772245/ape1-ref-1-redox-function-contributes-to-inflammatory-pain-sensitization
#14
Amira Zaky, Rabia Bouali-Benazzouz, Alexandre Favereaux, Gianluca Tell, Marc Landry
Inflammatory pain is a complex and multifactorial disorder. Apurinic/apyrimidinic endonuclease 1 (APE1), also called Redox Factor-1 (Ref-1), is constitutively expressed in the central nervous system and regulates various cellular functions including oxidative stress. In the present study, we investigated APE1 modulation and associated pain behavior changes in the complete Freund's adjuvant (CFA) model of inflammatory pain in rats. In addition we tested the anti-inflammatory effects of E3330, a selective inhibitor of APE1-redox activity, in CFA pain condition...
May 14, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29771142/the-development-of-a-mouse-model-of-mtbi-induced-post-traumatic-migraine-and-identification-of-the-delta-opioid-receptor-as-a-novel-therapeutic-target
#15
Laura S Moye, Madeline L Novack, Alycia F Tipton, Harish Krishnan, Subhash C Pandey, Amynah Aa Pradhan
Background Post-traumatic headache is the most common and long-lasting impairment observed following mild traumatic brain injury, and frequently has migraine-like characteristics. The mechanisms underlying progression from mild traumatic brain injury to post-traumatic headache are not fully understood. The aim of this study was to develop a mouse model of post-traumatic headache and identify mechanisms and novel targets associated with this disorder. Methods We combined the closed head weight-drop method and the nitroglycerin chronic migraine model...
January 1, 2018: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/29770986/the-influence-of-binding-site-geometry-on-anion-binding-selectivity-a-case-study-of-macrocyclic-receptors-built-on-an-azulene-skeleton
#16
Dawid Lichosyt, Sylwia Wasiłek, Paweł Dydio, Janusz Jurczak
The understanding of the host-guest interactions lies at the very heart of supramolecular chemistry. Often a minute change to the structure of a receptor can have a dramatic impact on the binding selectivity. Herein, we studied the influence of small perturbations in biding site geometry for a series of five closely correlated macrocyclic tetra-amide receptors, constructed from building blocks out of a pool of azulene-based units. The solid-state structures revealed that the conformational preferences of the free receptors are driven by the inherent preferences of the building blocks, yet in some cases the macrocyclic topology is able to override these to promote pre-organized conformations favorable for anion binding...
May 17, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29770441/evaluation-of-the-anti-inflammatory-activity-of-tinospora-cordifolia-willd-miers-chloroform-extract-a-preclinical-study
#17
Sheena Philip, Greeshma Tom, Asha V Vasumathi
OBJECTIVES: Tinospora cordifolia (Willd.) Miers is an inevitable ingredient of Ayurvedic rasayanas for the treatment of disorders with unregulated inflammation. However, studies regarding the mechanism of anti-inflammatory potential of this plant at the molecular level are lacking. METHODS: In vitro evaluations were conducted in RAW264.7 macrophages which were preincubated with chloroform extract of T. cordifolia (CETC) and subsequently stimulated with LPS. The expressions of COX-2, TNF-α and iNOS genes were analysed by SQRT-PCR and Western blot, cytokines (IL-6, IL-1β and PGE2 ) levels by ELISA, NF-κB activation and p38 MAPK phosphorylation by Immunoblot and confocal imaging...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29769077/magnetic-field-distribution-modulation-of-intrathecal-delivered-ketorolac-iron-oxide-nanoparticle-conjugates-produce-excellent-analgesia-for-chronic-inflammatory-pain
#18
Ping-Ching Wu, Dar-Bin Shieh, Hung-Tsung Hsiao, Jeffery Chi-Fei Wang, Ya-Chi Lin, Yen-Chin Liu
BACKGROUND: Nanoparticles have become one of the most promising among the potential materials used for biomedical applications. However, few researchers have focused on their effects on analgesia. Despite the fact that various nanoparticles have been evaluated for drug delivery and MRI imaging contrast enhancement in clinical settings, no reports have investigated the in vivo synergy of ketorolac iron-oxide nanoparticle conjugates to improve the analgesic effect. METHODS: Ketorolac conjugated magnetic iron oxide nanoparticles (Keto-SPIO) were synthesized via two-stage additions of protective agents and chemical co-precipitation...
May 16, 2018: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/29768200/sensory-afferents-use-different-coding-strategies-for-heat-and-cold
#19
Feng Wang, Erik Bélanger, Sylvain L Côté, Patrick Desrosiers, Steven A Prescott, Daniel C Côté, Yves De Koninck
Primary afferents transduce environmental stimuli into electrical activity that is transmitted centrally to be decoded into corresponding sensations. However, it remains unknown how afferent populations encode different somatosensory inputs. To address this, we performed two-photon Ca2+ imaging from thousands of dorsal root ganglion (DRG) neurons in anesthetized mice while applying mechanical and thermal stimuli to hind paws. We found that approximately half of all neurons are polymodal and that heat and cold are encoded very differently...
May 15, 2018: Cell Reports
https://www.readbyqxmd.com/read/29766765/control-of-transitions-between-locomotor-like-and-paw-shake-like-rhythms-in-a-model-of-a-multistable-central-pattern-generator
#20
Jessica Rae Parker, Brain Bondy, Boris I Prilutsky, Gennady S Cymbalyuk
The ability of the same neuronal circuit to control different motor functions is an actively debated concept. Previously, we have shown in a model that a single multistable CPG could produce two different rhythmic motor patterns, slow and fast, corresponding to cat locomotion and paw-shaking. A locomotor-like rhythm (~2 Hz) and a paw-shake-like rhythm (~10 Hz) did coexist and, by applying a single pulse of current, we could switch the CPG from one regime to another (Bondy et al. 2016). Here, we investigate roles of slow intrinsic ionic currents in this multistability...
May 16, 2018: Journal of Neurophysiology
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