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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/29765684/clawed-forelimbs-allow-northern-seals-to-eat-like-their-ancient-ancestors
#2
David P Hocking, Felix G Marx, Renae Sattler, Robert N Harris, Tahlia I Pollock, Karina J Sorrell, Erich M G Fitzgerald, Matthew R McCurry, Alistair R Evans
Streamlined flippers are often considered the defining feature of seals and sea lions, whose very name 'pinniped' comes from the Latin pinna and pedis , meaning 'fin-footed'. Yet not all pinniped limbs are alike. Whereas otariids (fur seals and sea lions) possess stiff streamlined forelimb flippers, phocine seals (northern true seals) have retained a webbed yet mobile paw bearing sharp claws. Here, we show that captive and wild phocines routinely use these claws to secure prey during processing, enabling seals to tear large fish by stretching them between their teeth and forelimbs...
April 2018: Royal Society Open Science
https://www.readbyqxmd.com/read/29682194/a-novel-dual-pan-pim-flt3-inhibitor-sel24-exhibits-broad-therapeutic-potential-in-acute-myeloid-leukemia
#3
Wojciech Czardybon, Renata Windak, Aniela Gołas, Michał Gałęzowski, Aleksandra Sabiniarz, Izabela Dolata, Magdalena Salwińska, Paweł Guzik, Magdalena Zawadzka, Ewelina Gabor-Worwa, Bożena Winnik, Małgorzata Żurawska, Ewa Kolasińska, Ewelina Wincza, Marta Bugaj, Monika Danielewicz, Eliza Majewska, Milena Mazan, Grzegorz Dubin, Monika Noyszewska-Kania, Ewa Jabłońska, Maciej Szydłowski, Tomasz Sewastianik, Bartosz Puła, Anna Szumera-Ciećkiewicz, Monika Prochorec-Sobieszek, Elżbieta Mądro, Ewa Lech-Marańda, Krzysztof Warzocha, Jerome Tamburini, Przemysław Juszczyński, Krzysztof Brzózka
Fms-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) is one of the most common genetic lesions in acute myeloid leukemia patients (AML). Although FLT3 tyrosine kinase inhibitors initially exhibit clinical activity, resistance to treatment inevitably occurs within months. PIM kinases are thought to be major drivers of the resistance phenotype and their inhibition in relapsed samples restores cell sensitivity to FLT3 inhibitors. Thus, simultaneous PIM and FLT3 inhibition represents a promising strategy in AML therapy...
March 30, 2018: Oncotarget
https://www.readbyqxmd.com/read/29614314/glun2b-camkii-mediates-cfa-induced-hyperalgesia-via-hdac4-modified-spinal-cox2-transcription
#4
Cheng-Yuan Lai, Ming-Chun Hsieh, Yu-Cheng Ho, Gin-Den Chen, Dylan Chou, Ting Ruan, An-Sheng Lee, Hsueh-Hsiao Wang, Yat-Pang Chau, Hsien-Yu Peng, Cheng-Hung Lai
Histone deacetylase 4 (HDAC4), which actively shuttles between the nucleus and cytoplasm, is an attractive candidate for a repressor mechanism in epigenetic modification. However, the potential role of HDAC4-dependent epigenetics in the neural plasticity underlying the development of inflammatory pain has not been well established. By injecting complete Freund's adjuvant (CFA) into the hind-paw of Sprague-Dawley rats (200-250 g), we found animals displayed behavioral hyperalgesia was accompanied with HDAC4 phosphorylation and cytoplasmic redistribution in the dorsal horn neurons...
March 31, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29558661/maternal-hand-grip-strength-in-pregnancy-newborn-sex-and-birth-weight
#5
Agnieszka Żelaźniewicz, Bogusław Pawłowski
AIM: Hand grip strength (HGS) is a non-invasive measure of physical strength, overall health, and nutritional status. The aim of the study was to test if HGS and its changes in pregnancy are related with offspring sex and birth weight. METHODS: We conducted longitudinal study on 95 healthy pregnant women (mean age 29.57 ± 3.43). HGS was measured in each trimester. A woman's height and changes in weight in pregnancy were also measured. The information on a child's sex, birth weight and the pregnancy week at delivery were derived from hospital records...
April 2018: Early Human Development
https://www.readbyqxmd.com/read/29510478/in-vitro-and-in-vivo-anti-osteoarthritis-effects-of-2-3-5-4-tetrahydroxystilbene-2-o-%C3%AE-d-glucoside-from-polygonum-multiflorum
#6
Po-Wei Tsai, Yi-Hui Lee, Lih-Geeng Chen, Chia-Jung Lee, Ching-Chiung Wang
Polygonum multiflorum Thunb. is a traditional herbal medicine that is rich in polyphenols. The major compound, 2,3,5,4'-tetrahydroxystilbene-2- O -β-d-glucoside (THSG) has many pharmacological activities, such as antioxidative and free radical-scavenging properties, and the abilities to reduce hyperlipidemia, prevent lipid peroxidation, and protect the cardiovascular system. In this study, the anti-osteoarthritis (OA) effects of THSG were explored using in vitro and in vivo models. THSG inhibited nitric oxide (NO) and prostaglandin E₂ (PGE₂) production and inducible NO synthase (iNOS) and cyclooxygenase-2 expressions by lipopolysaccharide-stimulated RAW 264...
March 3, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29443860/a-novel-rat-model-of-extremity-trauma-for-pre-hospital-pain-management-research
#7
Lusha Xiang, Harold G Klemcke, Nathan A Wienandt, Kathy L Ryan, Carmen Hinojosa-Laborde
BACKGROUND: Pain management is important in pre-hospital care of patients with extremity trauma (ET). The goal of this study was to establish a rat model of ET for pre-hospital pain research, and validate it using pain behaviors and analgesics. METHODS: Rats were anesthetized using isoflurane and ET was induced in one hindlimb via clamping retrofemoral tissues for 30 sec, followed by closed fibula fracture. Rats regained consciousness after ET. Pain responses in the injured hindlimb to thermal hyperalgesia (paw withdrawal latency, PWL), mechanical allodynia (paw withdrawal pressure, PWP), and weight bearing (WB) were determined before and 90 minutes after ET...
February 14, 2018: Journal of Trauma and Acute Care Surgery
https://www.readbyqxmd.com/read/29440395/fatty-acid-binding-protein-5-controls-microsomal-prostaglandin-e-synthase-1-mpges-1-induction-during-inflammation
#8
Diane Bogdan, Jerome Falcone, Martha P Kanjiya, Sang Hoon Park, Gregory Carbonetti, Keith Studholme, Maria Gomez, Yong Lu, Matthew W Elmes, Norbert Smietalo, Su Yan, Iwao Ojima, Michelino Puopolo, Martin Kaczocha
Fatty acid-binding proteins (FABPs) are intracellular lipid carriers that regulate inflammation, and pharmacological inhibition of FABP5 reduces inflammation and pain. The mechanism(s) underlying the anti-inflammatory effects associated with FABP5 inhibition is poorly understood. Herein, we identify a novel mechanism through which FABP5 modulates inflammation. In mice, intraplantar injection of carrageenan induces acute inflammation that is accompanied by edema, enhanced pain sensitivity, and elevations in proinflammatory cytokines and prostaglandin E2 (PGE2 )...
April 6, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29392229/mice-with-cancer-induced-bone-pain-show-a-marked-decline-in-day-night-activity
#9
Lisa A Majuta, Jean-Marc G Guedon, Stefanie A T Mitchell, Michael A Kuskowski, Patrick W Mantyh
Introduction: Cancer-induced bone pain (CIBP) is the most common type of pain with cancer. In humans, this pain can be difficult to control and highly disabling. A major problem with CIBP in humans is that it increases on weight-bearing and/or movement of a tumor-bearing bone limiting the activity and functional status of the patient. Currently, there is less data concerning whether similar negative changes in activity occur in rodent models of CIBP. Objectives: To determine whether there are marked changes in activity in a rodent model of CIBP and compare this to changes in skin hypersensitivity...
September 2017: Pain Reports (Baltimore, Md.)
https://www.readbyqxmd.com/read/29372659/novel-anti-inflammatory-and-analgesic-agents-synthesis-molecular-docking-and-in-vivo-studies
#10
David Izuchukwu Ugwu, Uchechukwu Christopher Okoro, Pius Onyeoziri Ukoha, Astha Gupta, Sunday N Okafor
Twelve new derivatives of benzothiazole bearing benzenesulphonamide and carboxamide were synthesised and investigated for their in vivo anti-inflammatory, analgesic and ulcerogenic activities. Molecular docking showed an excellent binding interaction of the synthesised compounds with the receptors, with 17c showing the highest binding energy (-12.50 kcal/mol). Compounds 17c and 17i inhibited carrageenan-induced rat paw oedema at 72, 76, and 80% and 64, 73, and 78% at 1 h, 2 h, and 3 h, respectively...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29372043/mast-cells-and-pro-inflammatory-cytokines-roles-in-assessment-of-grape-seeds-extract-anti-inflammatory-activity-in-rat-model-of-carrageenan-induced-paw-edema
#11
Amany Ahmed Mohamed Abd-Allah, Nasr Abdelwahab Mohamed Nasr El-Deen, Wafaa Abdou Mohamed Mohamed, Fatma Mohamed Naguib
Objectives: Reactive oxygen species (ROS)-produced oxidative disorders were involved at the pathophysiology of many inflammatory processes via the generation of pro-inflammatory cytokines and antioxidant defense system suppression. Although herbal antioxidants as mono-therapy relief many inflammatory diseases including, autoimmunity rheumatoid arthritis, but as combination therapy with other proven anti-inflammatory drugs in order to decreasing their toxic impacts has not yet been studied clearly, especially against chemical substances that's induced local inflammation with characteristic edema...
January 2018: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/29362901/reconstructing-an-incomparable-organism-the-chalicothere-in-nineteenth-and-early-twentieth-century-palaeontology
#12
Chris Manias
Palaeontology developed as a field dependent upon comparison. Not only did reconstructing the fragmentary records of fossil organisms and placing them within taxonomic systems and evolutionary lineages require detailed anatomical comparisons with living and fossil animals, but the field also required thinking in terms of behavioural, biological and ecological analogies with modern organisms to understand how prehistoric animals lived and behaved. Yet palaeontological material often worked against making easy linkages, bringing a sense of mystery and doubt...
January 23, 2018: History and Philosophy of the Life Sciences
https://www.readbyqxmd.com/read/29324347/design-synthesis-and-biological-evaluation-of-7h-pyrrolo-2-3-d-pyrimidin-4-amine-derivatives-as-selective-btk-inhibitors-with-improved-pharmacokinetic-properties-for-the-treatment-of-rheumatoid-arthritis
#13
Linhong He, Heying Pei, Chufeng Zhang, Mingfeng Shao, Dan Li, Mingli Tang, Taijing Wang, Xiaoxin Chen, Mingli Xiang, Lijuan Chen
Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment of autoimmune diseases, such as rheumatoid arthritis (RA). We reported a series of compounds bearing 7H-pyrrolo [2,3-d]pyrimidin-4-amine scaffold that potently inhibited Btk in vitro. Analysis of the structure-activity relationships (SAR) and drug-like profiles led to the discovery of the optimal compound B16...
February 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29320903/air-pollution-and-human-sperm-sex-ratio
#14
Michał Radwan, Emila Dziewirska, Paweł Radwan, Lucjusz Jakubowski, Wojciech Hanke, Joanna Jurewicz
The present study was designed to address the hypothesis that exposure to specific air pollutants may impact human sperm Y:X chromosome ratio. The study population consisted of 195 men who were attending an infertility clinic for diagnostic purposes and who had normal semen concentration of 15-300 mln/ml (WHO, 2010). Participants represented a subset of men in a multicenter parent study conducted in Poland to evaluate environmental factors and male fertility. Participants were interviewed and provided a semen sample...
January 1, 2018: American Journal of Men's Health
https://www.readbyqxmd.com/read/29311503/a-rat-model-of-knee-osteoarthritis-suitable-for-electroacupuncture-study
#15
Yongyuan Ma, Haiyun Guo, Fuhai Bai, Ming Zhang, Liu Yang, Jiao Deng, Lize Xiong
Acupuncture is widely used for knee osteoarthritis (KOA) treatment in clinical practice. In the present study, we aimed to set a standard KOA animal model for electroacupuncture (EA) study and provide an acupuncture recipe for further KOA studies. Rats intra-articularly administered monosodium iodoacetate (MIA, 0.3, 1 or 3 mg respectively, n=12 each) were evaluated for pain-like behavior: paw withdrawal mechanical threshold, weight bearing deficit, and joint pathological changes (OARSI score) until 28 days after injury...
January 1, 2018: Experimental Animals
https://www.readbyqxmd.com/read/29274925/role-of-complement-anaphylatoxin-receptors-in-a-mouse-model-of-acute-burn-induced-pain
#16
Michael Morgan, Jennifer R Deuis, Trent M Woodruff, Richard J Lewis, Irina Vetter
The complement system is an essential component of the innate immune response. The anaphylatoxins C3a and C5a are key drivers of the complement system, acting through the receptors C3aR, C5aR1 and C5aR2 to regulate inflammation. While a role for C5a activation of C5aR1 in inflammatory and neuropathic pain has been established, the role of the complement system in burn-induced pain has not been investigated. To address this gap, we assessed the role of complement receptors C3aR, C5aR1 and C5aR2 in a mouse model of acute burn-induced pain...
February 2018: Molecular Immunology
https://www.readbyqxmd.com/read/29079220/himatanthus-drasticus-apocynaceae-latex-reduces-oxidative-stress-and-modulates-cd4-cd8-foxp3-and-hsp-60-expressions-in-sarcoma-180-bearing-mice
#17
Glauco Jonas Lemos Santos, Emanuele Silva Oliveira, Ana Débora Nunes Pinheiro, Patricia Marçal da Costa, José Claudio Carneiro de Freitas, Francisco Glauco de Araújo Santos, Fernanda Maria Machado Maia, Selene Maia de Morais, Diana Célia Sousa Nunes-Pinheiro
ETHNOPHARMACOLOGICAL RELEVANCE: In Brazil, the latex of Himatanthus drasticus is used to treat inflammation, wound healing and cancer. The present study evaluated the antitumoral potential of H. drasticus latex (HdCL) in Sarcoma 180-bearing mice (S180). MATERIALS, METHODS: HdCL was obtained in Crato-CE, Brazil. Qualitative phytochemicals assays, nuclear magnetic resonance (NMR) and microbiological analyzes were performed. Swiss mice were divided into six groups, according to tumor forms: 1) ascitic model, GI (Control; 0...
October 24, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29059223/evaluation-of-a-novel-biodegradable-thermosensitive-keto-hydrogel-for-improving-postoperative-pain-in-a-rat-model
#18
Meng-Huang Wu, Ming-Hung Shih, Wei-Bin Hsu, Navneet Kumar Dubey, Wen-Fu Lee, Tsai-Yu Lin, Meng-Yow Hsieh, Chin-Fu Chen, Kuo-Ti Peng, Tsung-Jen Huang, Chung-Sheng Shi, Ren-Shyang Guo, Chang-Jhih Cai, Chiu-Yen Chung, Chung-Hang Wong
This study evaluates the sustained analgesic effect of ketorolac-eluting thermosensitive biodegradable hydrogel in the plantar incisional pain model of the rat hind-paw. A ketorolac-embedded 2, 2'-Bis (2-oxazolin) (BOX) linking methoxy-poly(ethylene glycol) and poly(lactide-co-glycolide) (mPEG-PLGA) diblock copolymer (BOX copolymer) was synthesized as keto-hydrogel based on optimal sol-gel phase transition and in vitro drug release profile. The effect of keto-hydrogel on postoperative pain (POP) was assessed using the established plantar incisional pain model in hind-paw of rats and compared to that of ketorolac solution...
2017: PloS One
https://www.readbyqxmd.com/read/29054682/liposomalization-of-oxaliplatin-induces-skin-accumulation-of-it-but-negligible-skin-toxicity
#19
COMPARATIVE STUDY
Kentaro Nishida, Misaki Kashiwagi, Shunsuke Shiba, Kiwamu Muroki, Akihiro Ohishi, Yusuke Doi, Hidenori Ando, Tatsuhiro Ishida, Kazuki Nagasawa
Liposomalization causes alteration of the pharmacokinetics of encapsulated drugs, and allows delivery to tumor tissues through passive targeting via an enhanced permeation and retention (EPR) effect. PEGylated liposomal doxorubicin (Doxil® , Lipo-DXR), a representative liposomal drug, is well-known to reduce cardiotoxicity and increase the anti-tumor activity of DXR, but to induce the hand-foot syndrome (HFS) as a result of skin DXR accumulation, which is one of its severe adverse effects. We have developed a new liposomal preparation of oxaliplatin (l-OHP), an important anti-tumor drug for treatment of colorectal cancer, using PEGylated liposomes (Lipo-l-OHP), and showed that Lipo-l-OHP exhibits increased anti-tumor activity in tumor-bearing mice compared to the original preparation of l-OHP...
December 15, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28922386/new-carboxamide-derivatives-bearing-benzenesulphonamide-as-a-selective-cox-ii-inhibitor-design-synthesis-and-structure-activity-relationship
#20
David Izuchukwu Ugwu, Uchechukwu Chris Okoro, Hilal Ahmad
Sixteen new carboxamide derivatives bearing substituted benzenesulphonamide moiety (7a-p) were synthesized by boric acid mediated amidation of appropriate benzenesulphonamide with 2-amino-4-picoline and tested for anti-inflammatory activity. One compound 7c showed more potent anti-inflammatory activity than celecoxib at 3 h in carrageenan-induced rat paw edema bioassay. Compounds 7g and 7k also showed good anti-inflammatory activity comparable to celecoxib. Compound 7c appeared selectivity index (COX-2/COX-1) better than celecoxib...
2017: PloS One
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