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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
#1
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...
December 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29320903/air-pollution-and-human-sperm-sex-ratio
#2
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
#3
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
#4
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...
December 21, 2017: 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
#5
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
#6
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
#7
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
#8
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
https://www.readbyqxmd.com/read/28912145/dynamic-18-f-fdg-pet-lymphography-for-in-vivo-identification-of-lymph-node-metastases-in-murine-melanoma
#9
Hannah H Lockau, Volker Neuschmelting, Anuja Ogirala, Antoni Vilaseca, Jan Grimm
Objective: Positron Lymphography using (18)F-FDG followed by Cerenkov guided resection of lymph nodes in healthy mice has previously been introduced by our group. Our aim in this study was to further assess the technique`s potential beyond merely localizing sentinel lymph nodes. We now aimed to evaluate the potential of Positron Lymphography to characterize the nodes with respect to their tumor status on order to identify metastatic lymph nodes. We explored if metastatic nodes could be distinguished from normal nodes via dynamic (18)F-FDG-lymphography, in order to then be resected under Cerenkov imaging guidance...
September 14, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28904551/suppressive-effect-of-the-n-hexane-extract-of-litsea-japonica-fruit-flesh-on-monosodium-iodoacetate-induced-osteoarthritis-in-rats
#10
Seung-Hyung Kim, Hye-Jin Choi, Won-Kyung Yang, Ji-Eun Lee, Ju-Hyun Cho, In-Jae Park, Sunyoung Park, Bo-Kyung Park, Mirim Jin
We examined the antiosteoarthritic effect of the n-hexane extract of Litsea japonica fruit flesh (LJF-HE) in a rat model of monosodium-iodoacetate- (MIA-) induced osteoarthritis. LJF-HE significantly reduced the difference in weight-bearing capabilities of the hind paws between healthy and MIA-treated rats. Histological examination of the knee joints indicated that LJF-HE suppressed cartilage and bone destruction. Additionally, there were decreases in the expression of matrix metalloproteinase-2 and metalloproteinase-9 and cyclooxygenase-2 in the joints...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28901432/effects-of-coadministration-of-low-dose-cannabinoid-type-2-receptor-agonist-and-morphine-on-vanilloid-receptor-1-expression-in-a-rat-model-of-cancer-pain
#11
Mingyue Zhang, Meng Chi, Huichao Zou, Songyu Tian, Zhaodi Zhang, Guonian Wang
Morphine is widely used as an analgesic to treat moderate to severe pain, but chronic morphine use is associated with development of tolerance and dependence, which limits its analgesic efficacy. Our previous research has showed that nonanalgetic dose of a cannabinoid type 2 (CB2) receptor agonist reduced morphine tolerance in cancer pain. A previous study showed the colocalization of CB2 and transient receptor potential vanilloid 1 (TRPV1) in human and rat dorsal root ganglia (DRG) sensory neurons. Whether coadministration of a CB2 receptor agonist and morphine could reduce TRPV1 expression in morphine‑induced antinociception and tolerance in cancer pain is unclear...
November 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28887170/synthesis-and-evaluation-of-antitumor-anti-inflammatory-and-analgesic-activity-of-novel-deoxycholic-acid-derivatives-bearing-aryl-or-hetarylsulfanyl-moieties-at-the-c-3-position
#12
Irina I Popadyuk, Andrey V Markov, Ekaterina A Morozova, Valeriya O Babich, Oksana V Salomatina, Evgeniya B Logashenko, Marina A Zenkova, Tat'yana G Tolstikova, Nariman F Salakhutdinov
Novel deoxycholic acid (DCA) derivatives were stereoselectively synthesised with -OH and -CH2SR moieties at the C-3 position, where R was a substituted aryl [2-aminophenyl (8) or 4-chlorophenyl (9)] or hetaryl [1-methylimidazolyl (5), 1,2,4-triazolyl (6), 5-amino-1,3,4-thiadiazolyl (7), pyridinyl (10) or pyrimidinyl (11)]. These compounds were prepared in good yields from the C-3β-epoxy derivative 2 in the epoxide ring-opening reaction by S-nucleophiles. These derivatives were evaluated for their in vitro anti-proliferation activity in a panel of tumor cell lines...
September 5, 2017: Steroids
https://www.readbyqxmd.com/read/28881250/airborne-radionuclides-in-the-proglacial-environment-as-indicators-of-sources-and-transfers-of-soil-material
#13
Edyta Łokas, Przemysław Wachniew, Paweł Jodłowski, Michał Gąsiorek
A survey of artificial ((137)Cs, (238)Pu, (239+240)Pu, (241)Am) and natural ((226)Ra, (232)Th, (40)K, (210)Pb) radioactive isotopes in proglacial soils of an Arctic glacier have revealed high spatial variability of activity concentrations and inventories of the airborne radionuclides. Soil column (137)Cs inventories range from below the detection limit to nearly 120 kBq m(-2), this value significantly exceeding direct atmospheric deposition. This variability may result from the mixing of materials characterised by different contents of airborne radionuclides...
November 2017: Journal of Environmental Radioactivity
https://www.readbyqxmd.com/read/28874151/effects-of-mollugo-pentaphylla-extract-on-monosodium-urate-crystal-induced-gouty-arthritis-in-mice
#14
Yun Mi Lee, Eun-Jung Shon, Ohn Soon Kim, Dong-Seon Kim
BACKGROUND: Gout is an inflammatory condition induced by the deposition of monosodium urate (MSU) crystals in joints and soft tissues, and it can lead to acute or chronic arthritis. MSU are pro-inflammatory stimuli that can initiate, amplify and sustain an intense inflammatory response. In this study, we evaluated the anti-inflammatory effect of an extract of Mollugo pentaphylla (MPE) on MSU-induced gouty arthritis in a mouse model. METHOD: An MSU crystal suspension (4 mg/50 μL) was injected intradermally into the right paw...
September 6, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28791830/zirconium-the-material-of-the-future-in-modern-implantology
#15
REVIEW
Paweł Kubasiewicz-Ross, Marzena Dominiak, Tomasz Gedrange, Ute U Botzenhart
The authors present the contemporary state of knowledge concerning alternative materials for dental implantology. First of all, factors influencing osseointegration are stated. The most important factors seem to be the type of implant surface. Among the numerous parameters describing them, the most important are: average roughness and porous density. Some studies proved that materials with comparable surface roughness provide similar osseointegration. In modern implantology titanium is the material still considered as a "gold standard"...
May 2017: Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University
https://www.readbyqxmd.com/read/28609967/discovery-of-i-penicillidmus-i-in-the-bismarck-archipelago-papua-new-guinea-with-description-of-a-new-species-from-lavongai-new-hanover-island-coleoptera-staphylinidae-scydmaeninae
#16
Paweł Jałoszyński
Penicillidmus Jałoszyński, 2014 was established to accommodate two Australian species of Glandulariini. Penicillidmus masseyensis Jałoszyński, 2014 and P. unicolor Jałoszyński, 2014 are known to occur in Cape York, northern Queensland. With the adult body length ranging from 0.83 to 0.86 mm, these species are among the smallest Australian scydmaenines. Another, yet undescribed species represented by a female, is also known to occur within the same area (Jałoszyński 2014). Penicillidmus resembles similarly small adults of Microscydmus Saulcy & Croissandeau, 1893, but can be easily distinguished on the basis of remarkable cephalic and prothoracic structures...
April 18, 2017: Zootaxa
https://www.readbyqxmd.com/read/28609667/transcriptional-response-of-a-novel-hpcdpk1-kinase-gene-from-hippeastrum-x-hybr-to-wounding-and-fungal-infection
#17
Agnieszka Pawełek, Maria Duszyn, Brygida Świeżawska, Adriana Szmidt-Jaworska, Krzysztof Jaworski
Calcium dependent protein kinases (CDPK) are well established plant sensor and effectors for calcium ions and participate in regulation of multiple abiotic and biotic stress responses in plant cells. Here we present the identification and characterization of a new CDPK kinase gene from bulbous plant Hippeastrum x hybr. and examine the role of this kinase in stress responses leading to phytoalexin (PA) production in plant tissues. In the previous research, it was shown that Hippeastrum bulbs mechanically wounded or infected with Peyronellaea curtisii (=Phoma narcissi) are inducted to an antifungal red substance synthesis...
September 2017: Journal of Plant Physiology
https://www.readbyqxmd.com/read/28569387/synthesis-and-in-vitro-antioxidant-activity-study-of-some-new-piperazinyl-flavone-compounds
#18
Paweł Berczyński, Aleksandra Kładna, Irena Kruk, Elmas Sarı, Hatice Nehir Murat, Oya Bozdağ Dündar, Hassan Y Aboul-Enein
Flavones exhibit a variety of beneficial effects and are well known for their medicinal importance in several diseases, including cardiovascular, neurodegenerative and cancer. The inclusion of the piperazine ring to the flavone backbone is an important strategy in drug discovery but only a few studies have synthesized piperazinyl flavone compounds to test their biological activity. While there is a major focus on the antioxidant properties of drugs in therapy of several diseases of inflammatory origin, we synthesized a series of the novel piperazinyl flavone analogues bearing the phenyl ring with different substituents...
June 1, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28565880/etanercept-attenuates-thermal-and-mechanical-hyperalgesia-induced-by-bone-cancer
#19
Yan Yang, Juan Zhang, Qin Gao, Jinhua Bo, Zhengliang Ma
Bone cancer pain commonly occurs when tumors originating in the breast, prostate or lung metastasize to long bones, spinal vertebrae and/or the pelvis. However, the underlying mechanisms of bone cancer pain remain largely unknown. The present study aimed to determine the role of spinal tumor necrosis factor-α (TNF-α) in the development of bone cancer pain. Osteosarcoma NCTC 2472 cells were implanted into the femoral intramedullary space of C3H/HeJ mice to establish a bone cancer model. Resulting pain-related behaviors, namely spontaneous foot lifting, paw withdrawal mechanical threshold and paw withdrawal thermal latency were observed prior to inoculation and on days 3, 5, 7, 10 and 14 thereafter...
May 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28515662/tempo-functionalized-c60-fullerene-deposited-on-gold-surface-for-catalytic-oxidation-of-selected-alcohols
#20
Piotr Piotrowski, Joanna Pawłowska, Jarosław Grzegorz Sadło, Renata Bilewicz, Andrzej Kaim
C60TEMPO10 catalytic system linked to a microspherical gold support through a covalent S-Au bond was developed. The C60TEMPO10@Au composite catalyst had a particle size of 0.5-0.8 μm and was covered with the fullerenes derivative of 2.3 nm diameter bearing ten nitroxyl groups; the organic film showed up to 50 nm thickness. The catalytic composite allowed for the oxidation under mild conditions of various primary and secondary alcohols to the corresponding aldehyde and ketone analogues with efficiencies as high as 79-98%, thus giving values typical for homogeneous catalysis, while retaining at the same time all the advantages of heterogeneous catalysis, e...
2017: Journal of Nanoparticle Research: An Interdisciplinary Forum for Nanoscale Science and Technology
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