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An-Jia Wang, Kai-Xin Zhang, Yu-Lin Gao, Ai-Zhen Weng, Liu-Yang Wang, Yun-Hui Zhang, Zhi Zhang, Dong-Mei She, Jun Ning, Xiang-Dong Mei
BACKGROUND: Diamondback moth Plutella xylostella L. is a very important pest of cruciferous vegetables causing excessive economic losses worldwide. Bioactivities of halo-, diazo-, and cyclopropane acetates of P. xylostella sex pheromone have been evaluated using electrophysiology and enzyme inhibition assays. RESULTS: A total of 23 sex pheromone analogs of P. xylostella were designed and synthesized and the result shows that (11Z)-hexadec-11-en-1-yl 2,2,2-trifluoroacetate, (11Z)-hexadec-11-en-1-yl 2,2,3,3,3-pentafluoropropanoate and (11Z)-hexadec-11-en-1-yl trifluoromethanesulfonate elicited potential inhibitory effects at all doses tested in the electrophysiology and enzyme inhibition assays...
September 22, 2018: Pest Management Science
Eliandra N da Silva, José de Anchieta C Horta-Júnior, Luciane H Gargaglioni, Mirela B Dias
NEW FINDINGS: What is the central question of this study? ATP is known to modulate the chemosensitivity of some brain areas. However, whether the ATP contributes specifically to the mechanism of chemoreception in the LH/PFA remains to be determined. What is the main finding and its importance? ATP, acting on the LH/PFA, enhances the hypercapnic ventilatory response in rats during wakefulness, in the dark period. Our results highlight the importance of ATP as a modulator of central chemoreception and provide new insight regarding the mechanisms involved in LH/PFA chemosensitivity and the sleep-wake differences in the CO2 /H+ -dependent drive to breathe...
September 22, 2018: Experimental Physiology
Devin W McBride, Eric C K Gren, Wayne Kelln, William K Hayes, John H Zhang
Hemorrhagic transformation after ischemic stroke is an independent predictor for poor outcome and is characterized by blood vessel rupture leading to brain edema. To date, no therapies for preventing hemorrhagic transformation exist. Disintegrins from the venom of Crotalus atrox have targets within the coagulation cascade, including receptors on platelets. We hypothesized that disintegrins from C. atrox venom can attenuate hemorrhagic transformation by preventing activation of matrix metalloproteinase after middle cerebral artery occlusion (MCAO) in hyperglycemic rats...
September 22, 2018: Journal of Neuroscience Research
Domenica Roberto, Laurence H Klotz, Vasundara Venkateswaran
BACKGROUND: Cannabinoids have demonstrated anticarcinogenic properties in a variety of malignancies, including in prostate cancer. In the present study, we explored the anti-cancer effects of the synthetic cannabinoid WIN 55,212-2 (WIN) in prostate cancer. METHODS: Established prostate cancer cells (PC3, DU145, LNCaP) were treated with varying concentrations of WIN. Cell proliferation was determined by the MTS assay. The anti-migration and anti-invasive potential of WIN was examined by the wound healing assay and the matrigel invasion assay...
September 21, 2018: Prostate
Hsueh-Chun Wang, Shau-Ku Huang
Metformin, an anti-diabetic drug, possesses anti-inflammatory property beyond its glucose-lowering activity, but its regulatory effect on mast cells and allergic responses remains unknown, wherein the aryl hydrocarbon receptor (AhR)-ligand axis is critical in controlling mast cell activation. Herein, we provide evidence supporting the role of metformin in modulating mast cell activation by FcεR1-, AhR-mediated signaling or their combination. Metformin at relatively low doses was shown to suppress FcεR1-mediated degranulation, IL-13, TNF-α and sphingosine-1-phosphate (S1P) secretion in murine bone marrow-derived mast cells (BMMCs)...
September 22, 2018: European Journal of Immunology
Hari Prasad, Donna K Dang, Kalyan C Kondapalli, Niranjana Natarajan, Valeriu Cebotaru, Rajini Rao
We observed significant and selective up-regulation of the Na+ /H+ exchanger NHA2 (SLC9B2) in cysts of patients with autosomal dominant polycystic kidney disease. Using the MDCK model of cystogenesis, we find NHA2 increases cyst size. Silencing or pharmacological inhibition of NHA2 inhibits cyst formation in vitro. Polycystin-1 represses NHA2 expression via Ca2+ /NFAT signalling whereas the dominant negative membrane-anchored C-terminal fragment (PC1-MAT) increased NHA2 levels. Drugs (caffeine, theophylline) and hormones (vasopressin, aldosterone) known to exacerbate cysts elicit NHA2 expression...
September 22, 2018: Journal of Physiology
Stewart J Tepper
Objective - To briefly describe the history of and available data on anti-calcitonin gene-related peptide (CGRP) therapies for headache. Background - CGRP was proposed as a target for primary headache therapies. Translational research involved moving from delineating the relationships between CGRP and primary headaches and the clinical development of anti-CGRP treatments. The first anti-CGRP treatment, an intravenous CGRP-receptor antagonist or gepant, olcegepant, was described as effective in terminating migraines in humans in 2004...
September 22, 2018: Headache
N Isakakroudi, A Talebi, M Allymehr, M Tavassoli
Avian coccidiosis is the most important parasitic disease in poultry production, which inflicts numerous losses to the industry. The extensive use of anticoccidial drugs leads to parasite resistance and drug residue in poultry products. In the present study, we aimed to investigate the effects of three famous essential oils (EOs) and their combination on inactivation of mixed oocysts of Eimeria adenoides, Eimeria dispersa, Eimeria meleagrimitis, and Eimeria meleagridis. The EOs of Thymus vulgaris, Artemisia sieberi, and Mentha pulegium were prepared...
June 2018: Archives of Razi Institute
Kate H Regan, Adam T Hill
Bronchiectasis is a chronic respiratory disorder characterized by persistent productive cough and recurrent chest infections secondary to permanent structural airway damage. The current treatment strategies for this debilitating disorder are limited to prompt antibiotic treatment of infective exacerbations and regular airway clearance techniques. Despite its high morbidity and associated mortality across all age groups, it has been a neglected area of research in respiratory medicine and there remain no licensed disease-modifying therapies...
September 21, 2018: Respirology: Official Journal of the Asian Pacific Society of Respirology
Saak Victor Ovsepian, Valerie Bríd O'Leary
While the extensive hunt for therapeutics combating Alzheimer's disease (AD) has fallen short of delivering effective treatments, breakthroughs towards understanding the disease mechanisms and identifying areas for future research have nevertheless been enabled. The majority of clinical trials with β- and γ-secretase modulators have been suspended from additional studies or terminated due to toxicity issues and health concerns. The lack of progress in developing innovative AD therapies has also prompted a resurgence of interest in more traditional symptomatic treatments with cholinesterase inhibitors and N-methyl-D-aspartate receptor antagonists, as well as in the research of immune response modulators...
September 21, 2018: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
Anamika Bhargava, Sumit Saha
PURPOSE: The purpose of this review article is to discuss the potential of T-type voltage gated calcium channels (VGCCs) as drug targets in breast cancer. Breast cancer, attributable to the different molecular subtypes, has a crucial need for therapeutic strategies to counter the mortality rate. VGCCs play an important role in regulating cytosolic free calcium levels which regulate cellular processes like tumorigenesis and cancer progression. In the last decade, T-type VGCCs have been investigated in breast cancer proliferation...
September 21, 2018: Breast Cancer Research and Treatment
Patrick M Beardsley, Yan Zhang
Opioid abuse has been a global menace for centuries, but the proliferation of synthetic opioids and their use within this current decade have created epidemic-level harms in some countries. According to the United Nations Office on Drugs and Crime, almost 12 million years were estimated loss of "healthy" life resulting in premature death and disability attributable to global opioid abuse just in 2015. Law enforcement and regulatory authorities have been particularly challenged abating the spread of synthetic opioids because soon after controlling the currently recognized abused opioids, their structures are tweaked, and new entities replace them...
September 22, 2018: Handbook of Experimental Pharmacology
Nina R Ashfield-Crook, Zachary Woodward, Martin Soust, D İpek Kurtböke
Streptophages are currently being investigated to control potato common scab, however, since a majority of streptophages are reported to be polyvalent, their potential to infect beneficial soil streptomycetes during the application process may have unintended consequences. To test this hypothesis, two phytopathogenic fungi, namely Fusarium solani and Rhizoctonia solani, were tested for their detrimental effect on the test crop wheat (Triticum aestivum cv. Gutha). F. solani caused a significant root weight reduction (34%) in the wheat plant and therefore was tested further in the pot trials with actinomycetes present...
September 21, 2018: Current Microbiology
Sami Mamand, Rebecca L Allchin, Matthew J Ahearne, Simon D Wagner
Patients with peripheral T-cell lymphomas generally have poor clinical outcomes with conventional chemotherapy. Recent advances have demonstrated that a large subgroup of PTCL are derived from follicular helper (Tfh) T-cells. These cases show a characteristic pattern of gene expression, which includes high-level protein expression of interleukin-2-inducible kinase (ITK). ITK is a member of the TEC family of kinases and normally has essential functions in regulating T-cell receptor signalling and T-cell differentiation...
September 21, 2018: Scientific Reports
Niveditha Nerlakanti, Jiqiang Yao, Duy T Nguyen, Ami K Patel, Alexey M Eroshkin, Harshani R Lawrence, Muhammad Ayaz, Brent M Kuenzi, Neha Agarwal, Yunyun Chen, Steven Gunawan, Rezaul M Karim, Norbert Berndt, John Puskas, Anthony M Magliocco, Domenico Coppola, Jasreman Dhillon, Jingsong Zhang, Subramaniam Shymalagovindarajan, Uwe Rix, Youngchul Kim, Ranjan Perera, Nicholas J Lawrence, Ernst Schonbrunn, Kiran Mahajan
Resistance to Androgen receptor (AR) antagonists is a significant problem in the treatment of Castration resistant prostate cancers (CRPCs). Identification of the mechanisms by which CRPCs evade Androgen Deprivation Therapies (ADT) is critical to develop novel therapeutics. We uncovered that CRPCs rely on BRD4-HOXB13 epigenetic reprogramming for androgen-independent cell proliferation. Mechanistically, BRD4, a member of the BET bromodomain family epigenetically promotes HOXB13 expression. Consistently, genetic disruption or pharmacological suppression of HOXB13 mRNA and protein expression by the novel dual activity BET bromodomain-kinase inhibitors directly correlates with rapid induction of apoptosis, potent inhibition of tumor cell proliferation, inhibits cell migration and suppresses CRPC growth...
September 21, 2018: Molecular Cancer Therapeutics
Werner E G Müller, Maximilian Ackermann, Emad Tolba, Meik Neufurth, Ivan Ivetac, Maria Kokkinopoulou, Heinz C Schröder, Xiaohong Wang
The in vitro tube formation assay with human umbilical vein endothelial cells (HUVEC) was applied to identify the extra- and intracellular sources of metabolic energy/ATP required for cell migration during the initial stage of microvascularization. Extracellularly, the physiological energy-rich polymer, inorganic polyphosphate [polyP], applied as biomimetic amorphous calcium polyP microparticles [Ca-polyP-MP], is functioning as a substrate for ATP generation most likely via the action of the alkaline phosphatase [ALP] and the adenylate kinase [AK] T he linear Ca-polyP-MP with a size of 40 phosphate units, close to the physiological polyP in the blood platelets , were found to increase endothelial cell tube formation, as well as the intracellular ATP levels...
September 21, 2018: Biochemical Journal
Najat Dzaki, Wahidah Wahab, Azali Azlan, Ghows Azzam
CTP Synthase (CTPS) is a metabolic enzyme that is recognized as a catalyst for nucleotide, phospholipid and sialoglycoprotein production. Though the structural characteristics and regulatory mechanisms of CTPS are well-understood, little is known regarding the extent of its involvement during the early developmental stages of vertebrates. Zebrafish carries two CTPS genes, annotated as ctps1a and ctps1b. Phylogenetic analyses show that both genes had diverged from homologues in the ancestral Actinopterygii, Oreochromis niloticus...
September 18, 2018: Biochemical and Biophysical Research Communications
Camila Antia, Katherine Baquerizo, Abraham Korman, Ali Alikhan, Jonathan A Bernstein
Second-generation antihistamines are considered first-line agents in the treatment of chronic urticaria because of their safety and efficacy profile. Some patients require higher doses of H1 antihistamines alone or in combination with other classes of medications, including H2 antihistamines, leukotriene receptor antagonists, or first-generation H1 antihistamines. One major therapeutic advance has been omalizumab, a humanized monoclonal anti-immunoglobulin E that was recently approved by the US Food and Drug Administration for the treatment of chronic urticaria that is unresponsive to H1 antagonists...
October 2018: Journal of the American Academy of Dermatology
Jonathan Chee Woei Lim, Yuet Ping Kwan, Michelle Siying Tan, Melissa Hui Yen Teo, Shunsuke Chiba, Walter Wahli, Xiaomeng Wang
BACKGROUND: Peroxisome proliferator⁻activated receptor (PPAR) β/δ, a ligand-activated transcription factor, is involved in diverse biological processes including cell proliferation, cell differentiation, inflammation and energy homeostasis. Besides its well-established roles in metabolic disorders, PPARβ/δ has been linked to carcinogenesis and was reported to inhibit melanoma cell proliferation, anchorage-dependent clonogenicity and ectopic xenograft tumorigenicity. However, PPARβ/δ's role in tumour progression and metastasis remains controversial...
September 20, 2018: International Journal of Molecular Sciences
Alaa A M Osman, Moawia M A Elhassan, Blala H A AbdElrahim, Fatima H A Ahmed, Jihad B H Yousif, Malak A M Ahmed, Romisa H A Abdelhafeez, Umsalama M Y Ahmed
PURPOSE: Chemotherapy-induced nausea and vomiting (CINV) is a distressing adverse effect. Neurokinin-1 receptor antagonist (NK1RA)-containing regimens are the standard regimens for CINV prophylaxis in patients with cancer receiving highly or moderately emetogenic chemotherapy (HEC or MEC). NK1RA agents are expensive and were not registered in Sudan. Recently, regimens containing olanzapine, the available and affordable medication in Sudan, were introduced as another option. This study aimed to compare the efficacy of an olanzapine-containing regimen with the antiemetic regimen that was currently used in our institute for CINV prophylaxis in HEC/MEC settings...
September 2018: Journal of Global Oncology
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