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https://www.readbyqxmd.com/read/28735523/histochemistry-and-immunolocalisation-of-glucokinin-in-antidiabetic-plants-used-in-traditional-mexican-medicine
#1
Guillermo Laguna-Hernández, Carlos A Rio-Zamorano, Itzel G Meneses-Ochoa, Alicia E Brechú-Franco
Mexico is a megadiverse country that has 3,600 to 4,000 species of medicinal plants, of which approximately 800 are used to treat conditions related to diabetes mellitus (DM). DM is a chronic degenerative disease of energy metabolism that exists as two types: type 1 (DM1) and type 2 (DM2). DM is considered a public health problem that affects 7% of the Mexican population older than 20 years. DM is clinically controlled with hypoglycaemic drugs, alpha-glucosidase inhibitors, insulin secretion stimulants or the direct application of insulin...
June 21, 2017: European Journal of Histochemistry: EJH
https://www.readbyqxmd.com/read/28735510/fxa-inhibition-by-rivaroxaban-modifies-mechanisms-associated-with-the-pathogenesis-of-human-abdominal-aortic-aneurysms
#2
G Moñux, J J Zamorano-León, P Marqués, B Sopeña, J M García-García, G Laich de Koller, B Calvo-Rico, M A García-Fernandez, J Serrano, A López-Farré
AIM: To evaluate if Rivaroxaban, an oral factor Xa (FXa) inhibitor, could in vitro modify the expression of inflammatory and oxidative stress biomarkers in abdominal aortic aneurysmal (AAA) sites showing intraluminal thrombus. METHODS: AAA sites with intraluminal mural thrombus were obtained from six patients undergoing elective AAA repair. In addition, control abdominal aortic samples were obtained from six organ donors. AAA sites were incubated in the presence and absence of 50 nmol/L Rivaroxaban...
July 23, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28735439/surgical-management-of-periocular-cancers-high-and-low-risk-features-drive-treatment
#3
REVIEW
Richard C Allen
PURPOSE OF REVIEW: Recent advances in the treatment of eyelid tumors have centered on the excision, evaluation of margins, role of sentinel lymph node biopsy, and adjunctive/adjuvant systemic and radiation therapy. The purpose of this review is to elaborate on these advances. RECENT FINDINGS: Mohs excision of basal cell carcinoma and squamous cell carcinoma continues to provide the greatest success in complete excision of the cancer, especially in those cases of high-risk disease including medial canthal location and recurrent disease...
September 2017: Current Oncology Reports
https://www.readbyqxmd.com/read/28735432/eucalyptol-sabinene-and-cinnamaldehyde-potent-inhibitors-of-salmonella-target-protein-l-asparaginase
#4
Archana Vimal, Dharm Pal, Timir Tripathi, Awanish Kumar
Salmonella typhimurium is a severe threat to human life. The treatment became more difficult with the emergence of multidrug resistance. In the present in silico study, a novel drug target L-asparaginase was tested against three ligands eucalyptol, sabinene, and cinnamaldehyde, major components of cardamom, nutmeg, and cinnamon, respectively. The lowest docking score was obtained for sabinene followed by eucalyptol and cinnamaldehyde i.e. -5.648, -3.939 and -3.469. The docking score of sabinene is also better than the standard drug, Ciprofloxacin (-4...
August 2017: 3 Biotech
https://www.readbyqxmd.com/read/28735419/modulation-of-human-kv4-3-kchip2-channel-inactivation-kinetics-by-cytoplasmic-ca-2
#5
Christiane Groen, Robert Bähring
The transient outward current (I to) in the human heart is mediated by Kv4.3 channels complexed with Kv channel interacting protein (KChIP) 2, a cytoplasmic Ca(2+)-binding EF-hand protein known to modulate Kv4.3 inactivation gating upon heterologous co-expression. We studied Kv4.3 channels co-expressed with wild-type (wt) or EF-hand-mutated (ΔEF) KChIP2 in human embryonic kidney (HEK) 293 cells. Co-expression took place in the absence or presence of BAPTA-AM, and macroscopic currents were recorded in the whole-cell patch-clamp configuration with different free Ca(2+) concentrations in the patch-pipette...
July 22, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28735378/a-phase-i-ii-trial-and-pharmacokinetic-study-of-mithramycin-in-children-and-adults-with-refractory-ewing-sarcoma-and-ews-fli1-fusion-transcript
#6
Patrick J Grohar, John Glod, Cody J Peer, Tristan M Sissung, Fernanda I Arnaldez, Lauren Long, William D Figg, Patricia Whitcomb, Lee J Helman, Brigitte C Widemann
PURPOSE: In a preclinical drug screen, mithramycin was identified as a potent inhibitor of the Ewing sarcoma EWS-FLI1 transcription factor. We conducted a phase I/II trial to determine the dose-limiting toxicities (DLT), maximum tolerated dose (MTD), and pharmacokinetics (PK) of mithramycin in children with refractory solid tumors, and the activity in children and adults with refractory Ewing sarcoma. PATIENTS AND METHODS: Mithramycin was administered intravenously over 6 h once daily for 7 days for 28 day cycles...
July 22, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28735369/ethylene-sensitivity-and-relative-air-humidity-regulate-root-hydraulic-properties-in-tomato-plants
#7
Monica Calvo-Polanco, Pablo Ibort, Sonia Molina, Juan Manuel Ruiz-Lozano, Angel María Zamarreño, Jose María García-Mina, Ricardo Aroca
The effect of ethylene and its precursor ACC on root hydraulic properties, including aquaporin expression and abundance, is modulated by relative air humidity and plant sensitivity to ethylene. Relative air humidity (RH) is a main factor contributing to water balance in plants. Ethylene (ET) is known to be involved in the regulation of root water uptake and stomatal opening although its role on plant water balance under different RH is not very well understood. We studied, at the physiological, hormonal and molecular levels (aquaporins expression, abundance and phosphorylation state), the plant responses to exogenous 1-aminocyclopropane-1-carboxylic acid (ACC; precursor of ET) and 2-aminoisobutyric acid (AIB; inhibitor of ET biosynthesis), after 24 h of application to the roots of tomato wild type (WT) plants and its ET-insensitive never ripe (nr) mutant, at two RH levels: regular (50%) and close to saturation RH...
July 22, 2017: Planta
https://www.readbyqxmd.com/read/28735240/therapeutic-effects-of-l-cysteine-in-newborn-mice-subjected-to-hypoxia-ischemia-brain-injury-via-the-cbs-h2s-system-role-of-oxidative-stress-and-endoplasmic-reticulum-stress
#8
Song Liu, Danqing Xin, Lingxiao Wang, Tiantian Zhang, Xuemei Bai, Tong Li, Yunkai Xie, Hao Xue, Shishi Bo, Dexiang Liu, Zhen Wang
Neonatal hypoxic-ischemic (HI) injury is a major cause of neonatal death and neurological dysfunction. H2S has been shown to protect against hypoxia-induced injury and apoptosis of neurons. L-Cysteine is catalyzed by cystathionine-β-synthase (CBS) in the brain and sequentially produces endogenous H2S. The present study was designed to investigate whether L-Cysteine could attenuate the acute brain injury and improve neurobehavioral outcomes following HI brain injury in neonatal mice by releasing endogenous H2S...
July 14, 2017: Redox Biology
https://www.readbyqxmd.com/read/28735226/perinatal-fluoxetine-effects-on-social-play-the-hpa-system-and-hippocampal-plasticity-in-pre-adolescent-male-and-female-rats-interactions-with-pre-gestational-maternal-stress
#9
Mary Gemmel, Mariah Hazlett, Eszter Bögi, Sonsoles De Lacalle, Lesley A Hill, Nikolaos Kokras, Geoffrey L Hammond, Christina Dalla, Thierry D Charlier, Jodi L Pawluski
Selective serotonin reuptake inhibitor medications (SSRIs) are the first lines of treatment for maternal affective disorders, and are prescribed to up to 10% of pregnant women. Concern has been raised about how perinatal exposure to these medications affect offspring neurobehavioral outcomes, particularly those related to social interactions, as recent research has reported conflicting results related to autism spectrum disorder (ASD) risk in children prenatally exposed to SSRIs. Therefore, the aim of this work was to investigate the effects of perinatal exposure to the SSRI fluoxetine on social play behaviors and the hypothalamic pituitary adrenal system, using a model of pre-gestational maternal stress...
July 15, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28735213/chemoselective-synthesis-and-biological-evaluation-of-arylated-2-trifluoromethyl-quinolines-as-nucleotide-pyrophosphatase-npps-inhibitors
#10
David Kuhrt, Syeda Abida Ejaz, Saira Afzal, Shafi Ullah Khan, Joanna Lecka, Jean Sévigny, Peter Ehlers, Anke Spannenberg, Jamshed Iqbal, Peter Langer
A new approach to arylated 2-trifluoromethylquinolines based on novel regioselective Suzuki-Miyaura coupling reactions has been developed. Moreover, site-selective, chemo-selective amination reactions were performed. The new 2-trifluoromethylquinoline derivatives were tested as potential NPPs inhibitors and evaluated for their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs and nucleoside triphosphate diphosphohydrolases (NTPDases). Several derivatives were active on a nanomolecular concentration...
July 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28735097/protecting-the-heart-through-mk2-modulation-toward-a-role-in-diabetic-cardiomyopathy-and-lipid-metabolism
#11
REVIEW
Matthieu Ruiz, Lise Coderre, Bruce Gordon Allen, Christine Des Rosiers
Various signaling pathways have been identified in the heart as important players during development, physiological adaptation or pathological processes. This includes the MAPK families, particularly p38MAPK, which is involved in several key cellular processes, including differentiation, proliferation, apoptosis, inflammation, metabolism and survival. Disrupted p38MAPK signaling has been associated with several diseases, including cardiovascular diseases (CVD) as well as diabetes and its related complications...
July 19, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28735060/individual-roles-of-brain-and-serum-alcohol-dehydrogenase-isoforms-in-regulation-of-alcohol-consumption-in-spf-wistar-rats
#12
Vsevolod V Pavshintsev, Nikita A Mitkin, Olga Y Frolova, Ekaterina A Kushnir, Olga A Averina, Maxim L Lovat
Alcohol dehydrogenases (ADH) are key enzymes of ethanol metabolism that mediate its oxidation to acetaldehyde. ADHs are also able to oxidize some types of neurotransmitters such as dopamine, serotonin and norepinephrine. Increased level of ADHs activity, induced by chronic alcohol consumption, is presumably associated with disturbed neurotransmitters metabolism that leads to stable alcohol craving. As earlier reported, intraperitoneal administration of 4-methilpirasole (non-specific inhibitor of ADHs) has shown to provide a short-term anti-alcoholic effect, but individual roles of ADH isoforms in this process were still unclear...
July 19, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28735057/brazil-s-resolutions-to-regulate-the-sale-of-antibiotics-impact-on-consumption-and-escherichia-coli-resistance-rates
#13
Karen P H Mattos, Marília B Visacri, Júlia C F Quintanilha, Gustavo R Lloret, Maria A Cursino, Anna S Levin, Carlos E Levy, Patricia Moriel
OBJECTIVE: The aim of this study was to determine the impact of two resolutions to restrict antibiotic use (RDCs no. 44/2010 and 20/2011) in the Campinas metropolitan area (Sao Paulo, Brazil) on antibiotic consumption, resistance rates, and trends in Escherichia coli-causing community-acquired urinary tract infection (UTI). METHODS: The annual retail sale information of antibiotics from drugstores in the Campinas metropolitan area between 2008 and 2012 were obtained through the Intercontinental Medical Statistics Health of Brazil...
July 19, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28735002/immobilization-of-%C3%AE-galactosidase-on-surface-modified-cobalt-multiwalled-carbon-nanotube-nanocomposite-improves-enzyme-stability-and-resistance-to-inhibitor
#14
Maryam Khan, Qayyum Husain, Rani Bushra
The present study aimed to work out a high yield procedure for immobilization of Aspergillus oryzae β-galactosidase on polyaniline cobalt multiwalled carbon nanotubes nanocomposite (PANI/Co/MWCNTNC) by physical adsorption and covalent attachment via glutaraldehyde. The binding was confirmed by scanning and transmission electron microscopy along with Fourier transform-infrared spectroscopy. The immobilization yields obtained for adsorbed and cross-linked enzymes were 93% and 97%, respectively. The covalently immobilized enzyme was remarkably more stable at extremes of pH and temperature compared to native and adsorbed enzymes...
July 19, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28734998/oxidative-stress-with-tau-hyperphosphorylation-in-memory-impaired-1-2-diacetylbenzene-treated-mice
#15
Sin-Woo Kang, Sung Jin Kim, Min-Sun Kim
Long-term exposure to organic solvent may be related to the incidence of neuronal diseases, such as, Alzheimer's disease, depression, multiple sclerosis, dementia, Parkinson's disease. Previously, the authors reported 1,2-diacetylbenzene (DAB; a neurotoxic metabolite of 1,2-diethylbenzene) causes central and peripheral neuropathies that lead to motor neuronal deficits. Furthermore, it is known DAB increases oxidative stress and protein adduct levels and impairs hippocampal neurogenesis in mice. The authors examined the relevance of oxidative stress and tau hyperphosphorylation in the hippocampus...
July 19, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28734986/exogenous-hedgehog-antagonist-delays-but-does-not-prevent-fracture-healing-in-young-mice
#16
Xiaochen Liu, Jennifer A McKenzie, Clayton W Maschhoff, Michael J Gardner, Matthew J Silva
Fracture healing recapitulates many aspects of developmental osteogenesis. The hedgehog (Hh) signaling pathway, essential to skeletal development, is upregulated during fracture healing, although its importance is unclear. Our goal was to assess the functional importance of Hh signaling in endochondral fracture healing. We created closed, transverse diaphyseal femur fractures in mice, stabilized with an intramedullary pin, and administered a systemic Hh inhibitor or vehicle. Because Hh pathway activation is mediated by the receptor Smoothened (Smo), we used the Smo antagonist GDC-0449 (GDC, 50mg/kg, twice daily) to target the pathway...
July 19, 2017: Bone
https://www.readbyqxmd.com/read/28734982/isolation-and-characterization-of-renin-like-aspartic-proteases-from-echis-ocellatus-venom
#17
M C Wilkinson, D J H Nightingale, R A Harrison, S C Wagstaff
Three aspartic proteases (SVAPs) have been isolated from venom of the saw-scaled viper, Echis ocellatus. In confirmation of prior transcriptomic predictions, all three forms match to sequences of either of the two SVAP transcripts (EOC00051 and EOC00123), have a molecular weight of 42 kDa and possess a single N-glycan. The SVAPs act in a renin-like manner, specifically cleaving human and porcine angiotensinogen into angiotensin-1 and possess no general protease activity. Their activity is completely inhibited by the aspartyl protease inhibitor Pepstatin A...
July 19, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28734977/modulation-of-the-interaction-between-human-p450-3a4-and-b-megaterium-reductase-via-engineered-loops
#18
Silvia Castrignanò, Serena D'Avino, Giovanna Di Nardo, Gianluca Catucci, Sheila J Sadeghi, Gianfranco Gilardi
Chimerogenesis involving cytochromes P450 is a successful approach to generate catalytically self-sufficient enzymes. However, the connection between the different functional modules should allow a certain degree of flexibility in order to obtain functional and catalytically efficient proteins. We previously applied the molecular Lego approach to develop a chimeric P450 3A4 enzyme linked to the reductase domain of P450 BM3 (BMR). Three constructs were designed with the connecting loop containing no glycine, 3 glycine or 5 glycine residues and showed a different catalytic activity and coupling efficiency...
July 19, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28734932/a-pyridone-derivative-activates-serca2a-by-attenuating-the-inhibitory-effect-of-phospholamban
#19
Manami Kaneko, Hisato Yamamoto, Hiroki Sakai, Yusuke Kamada, Toshiki Tanaka, Shuji Fujiwara, Synsuke Yamamoto, Hiroki Takahagi, Hideyuki Igawa, Shizuo Kasai, Masakuni Noda, Makoto Inui, Tomoyuki Nishimoto
The cardiac sarco/endoplasmic reticulum Ca(2+)-dependent ATPase 2a (SERCA2a) plays a central role in Ca(2+) handling within cardiomyocytes and is negatively regulated by phospholamban (PLN), a sarcoplasmic reticulum (SR) membrane protein. The activation of SERCA2a, which has been reported to improve cardiac dysfunction in heart failure, is a potential therapeutic approach for heart failure. Therefore, we developed a novel small molecule, compound A and characterized it both in vitro and in vivo. Compound A activated the Ca(2+)-dependent ATPase activity of cardiac SR vesicles but not that of skeletal muscle SR vesicles that lack PLN...
July 19, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28734929/aripiprazole-prevents-renal-ischemia-reperfusion-injury-in-rats-probably-through-nitric-oxide-involvement
#20
Hanieh Gholampour, Leila Moezi, Hamed Shafaroodi
Renal ischemia/reperfusion (I/R) injury is strongly related to morbidity and mortality. Oxidative stress, inflammation, and apoptosis play key roles in renal dysfunction following renal I/R. Aripiprazole is an atypical antipsychotic which used for the treatment of schizophrenia and bipolar disorder. Recent studies have reported aripiprazole as displaying certain anti-inflammatory effects. Regarding the underlying mechanisms of renal ischemia-reperfusion, therefore, nephroprotective effects might be predicted to be seen with aripiprazole...
July 19, 2017: European Journal of Pharmacology
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