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https://www.readbyqxmd.com/read/28635673/toxicity-of-naphthalene-and-benzene-on-tribollium-castaneum-herbst
#1
Nerlis Pajaro-Castro, Karina Caballero-Gallardo, Jesus Olivero-Verbel
Naphthalene and benzene are widely-used volatile organic compounds. The aim of this research was to examine the toxicological effects of naphthalene and benzene against Tribolium castaneum as an animal model. Adult insects were exposed to these aromatic compounds to assess mortality after 4-48 h of exposure. The lethal concentration 50 (LC50) for naphthalene, naphthalin, and benzene were 63.6 µL/L, 20.0 µL/L, and 115.9 µL/L in air, respectively. Real-time polymerase chain reaction (PCR) analysis revealed expression changes in genes related to oxidative stress and metabolism [Glutathione S-Transferase (Gst), and Cytochrome P450 6BQ8 (Cyp6bq8)]; reproduction and metamorphosis [Hormone receptor in 39-like protein (Hr39), Ecdysone receptor: (Ecr), and Chitin synthase 2 (Chs2)]; and neurotransmission [Histamine-gated chloride channel 2 (Hiscl2)] in insects exposed for 4 h to 70...
June 21, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28629736/kfp-h008-blocks-gastric-acid-secretion-through-inhibiting-h-k-atpase
#2
Cheng-Yuan Li, Mei Su, Yun-Yi Yan, Lin Zhou, Lu-Yao Ao, Wei-Rong Fang, Yun-Man Li
1-(5-(1H-indol-5-yl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl)-N-methylmethanamine (KFP-H008),a novel and potent potassium-competitive acid blocker for the treatment of acid secretion related diseases, has not been reported previously. In this study, we demonstrated that KFP-H008 inhibits basal acid secretion, 2-deoxy-D-glucose- (2DG-) stimulated gastric acid secretion in rats. KFP-H008 blocked histamine-stimulated acid secretion in rats and heidenhain pouch dogs and reversed acid output in isolated gastric perfusion under histamine stimulation...
June 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28629594/the-discovery-of-benzoxazine-sulfonamide-inhibitors-of-nav1-7-tools-that-bridge-efficacy-and-target-engagement
#3
Daniel S La, Emily A Peterson, Christiane Bode, Alessandro A Boezio, Howard Bregman, Margaret Y Chu-Moyer, James Coats, Erin F DiMauro, Thomas A Dineen, Bingfan Du, Hua Gao, Russell Graceffa, Hakan Gunaydin, Angel Guzman-Perez, Robert Fremeau, Xin Huang, Christopher Ilch, Thomas J Kornecook, Charles Kreiman, Joseph Ligutti, Min-Hwa Jasmine Lin, Jeff S McDermott, Isaac Marx, David J Matson, Stefan I McDonough, Bryan D Moyer, Hanh Nho Nguyen, Kristin Taborn, Violeta Yu, Matthew M Weiss
The voltage-gated sodium channel NaV1.7 has received much attention from the scientific community due to compelling human genetic data linking gain- and loss-of-function mutations to pain phenotypes. Despite this genetic validation of NaV1.7 as a target for pain, high quality pharmacological tools facilitate further understanding of target biology, establishment of target coverage requirements and subsequent progression into the clinic. Within the sulfonamide class of inhibitors, reduced potency on rat NaV1...
June 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28628008/basophil-histamine-release-to-amoxicilloyl-poly-l-lysine-compared-to-amoxicillin-in-patients-with-ige-mediated-allergic-reactions-to-amoxicillin
#4
F Arribas, S Falkencrone, J Sola, M P Gomez-Serranillos, J J Laguna, M I Montañez, T D Fernandez, D Rodríguez, F Pineda, P Stahl Skov, C Mayorga, M J Torres
BACKGROUND: Amoxicillin (AX) is the betalactam most often involved in IgE-mediated reactions and the diagnosis is mainly based on skin testing (ST) although without optimal sensitivity. We have produced a newly AX derivative, amoxicilloyl-poly-L-lysine (APL), and have analysed its IgE recognition by passive histamine release test (pHRT). METHODS: Patients (N=19) with confirmed AX allergy and with specific IgE positive to AX and controls (N=10) with good tolerance to AX were included...
June 19, 2017: Journal of Investigational Allergology & Clinical Immunology
https://www.readbyqxmd.com/read/28627593/suppressive-effect-of-an-aqueous-extract-of-diospyros-kaki-calyx-on-dust-mite-extract-2-4-dinitrochlorobenzene-induced-atopic-dermatitis-like-skin-lesions
#5
Ju-Hee Yu, Meiling Jin, Young-Ae Choi, Na-Hee Jeong, Jeong-Sook Park, Tae-Yong Shin, Sang-Hyun Kim
Atopic dermatitis (AD) is a common chronic inflammatory skin disease, affecting 10-20% of individuals worldwide. Therefore, the discovery of drugs for treating AD is an attractive subject and important to human health. Diospyros kaki and Diospyros kaki (D. kaki) folium exert beneficial effects on allergic inflammation. However, the effect of D. kaki calyx on AD remains elusive. The present study evaluated the effects of an aqueous extract of D. kaki calyx (AEDKC) on AD-like skin lesions using mouse and keratinocyte models...
June 12, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28627122/a-biotinylated-peptide-bp21-as-a-novel-potent-anti-anaphylactic-agent-targeting-platelet-activating-factor
#6
Akira Sato, Keiichi Ebina
Platelet-activating factor (PAF) is an important mediator of anaphylaxis and is therefore an anti-anaphylactic drug target. We recently reported that synthetic N-terminally biotinylated peptides (BP4-BP29) inhibit PAF by directly interacting with PAF and its metabolite/precursor lyso-PAF. In this study, we investigated whether the biotinylated peptides can inhibit anaphylactic reactions in vivo. In mouse models of anaphylaxis, one of the peptides, BP21, markedly and dose-dependently inhibited hypothermia with a maximum dose-response within 30 min after administration, even at doses 20 times lesser than doses of the known PAF antagonist CV-3988...
June 19, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28626527/systematic-data-mining-reveals-synergistic-h3r-mchr1-ligands
#7
David Schaller, Stefanie Hagenow, Gina Alpert, Alexandra Naß, Robert Schulz, Marcel Bermudez, Holger Stark, Gerhard Wolber
In this study, we report a ligand-centric data mining approach that guided the identification of suitable target profiles for treating obesity. The newly developed method is based on identifying target pairs for synergistic positive effects and also encompasses the exclusion of compounds showing a detrimental effect on obesity treatment (off-targets). Ligands with known activity against obesity-relevant targets were compared using fingerprint representations. Similar compounds with activities to different targets were evaluated for the mechanism of action since activation or deactivation of drug targets determines the pharmacological effect...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28624934/low-serum-diamine-oxidase-dao-activity-levels-in-patients-with-migraine
#8
Joan Izquierdo-Casas, Oriol Comas-Basté, M Luz Latorre-Moratalla, Marian Lorente-Gascón, Adriana Duelo, M Carmen Vidal-Carou, Luis Soler-Singla
Histamine intolerance is a disorder in the homeostasis of histamine due to a reduced intestinal degradation of this amine, mainly caused by a deficiency in the enzyme diamine oxidase (DAO). Among the several multi-faced symptoms associated with histamine intolerance, headache is one of the most recognized and disabling consequences. The aim of this study was to determine the prevalence of DAO deficiency in patients with a confirmed migraine diagnosis according to the current International Headache Society (IHS) and in non-migraine subjects...
June 17, 2017: Journal of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28624575/intestinal-fungal-dysbiosis-associates-with-visceral-hypersensitivity-in-patients-with-irritable-bowel-syndrome-and-rats
#9
Sara Botschuijver, Guus Roeselers, Evgeni Levin, Daisy M Jonkers, Olaf Welting, Sigrid Em Heinsbroek, Heleen H de Weerd, Teun Boekhout, Matteo Fornai, Ad A Masclee, Frank H J Schuren, Wouter J de Jonge, Jurgen Seppen, Rene M van den Wijngaard
BACKGROUND & AIMS: Visceral hypersensitivity is one feature of irritable bowel syndrome (IBS). Bacterial dysbiosis might be involved in activation of nociceptive sensory pathways, but there have been few studies of the role of the mycobiome (the fungal microbiome) in development of IBS. We analyzed intestinal mycobiomes of patients with IBS and a rat model of visceral hypersensitivity. METHODS: We used internal transcribed spacer 1-based metabarcoding to compare fecal mycobiomes of 18 healthy volunteers with those of 39 patients with IBS (with visceral hypersensitivity or normal levels of sensitivity)...
June 14, 2017: Gastroenterology
https://www.readbyqxmd.com/read/28622592/second-generation-h1-antihistamines-interaction-with-food-and-alcohol-a-systematic-review
#10
REVIEW
Paweł Paśko, Tomasz Rodacki, Renata Domagała-Rodacka, Krzysztof Palimonka, Monika Marcinkowska, Danuta Owczarek
Histamine is a mediator of many physiological processes. It plays an important role in modulating allergy reactions and immune system responses. H1 receptor is a therapeutic target for drugs applied in allergic diseases such as allergic rhinoconjunctivitis, urticarial, or atopic dermatitis. H1-antihistamines display different chemical structures, pharmacokinetics and a potential for drug-drug and drug-food interactions. Drug-food interactions are known to reduce therapeutic effects of the medicine, as well as to induce a potent adverse drug reactions...
June 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28618071/histamine-receptor-2-modifies-inkt-cell-activity-within-the-inflamed-lung
#11
R Ferstl, R Frei, W Barcik, E Schiavi, K Wanke, M Ziegler, N Rodriguez-Perez, D Groeger, P Konieczna, S Zeiter, D Nehrbass, Roger Lauener, C A Akdis, L O'Mahony
BACKGROUND: Histamine is a key immunoregulatory mediator and can dampen proinflammatory responses via activation of histamine receptor 2 (H2 R). The aim of this study was to determine the role of H2 R in modulating lung inflammatory responses. METHODS: H2 R was blocked using famotidine or activated using dimaprit in both the ovalbumin (OVA) and house dust mite extract (HDM) murine models of respiratory inflammation. H2 R-deficient animals and CD1d/ H2 R-deficient animals were utilized to examine the CD1d presentation of lipid antigens (αGal-Cer or OCH) to invariant Natural Killer T (iNKT) cells...
June 15, 2017: Allergy
https://www.readbyqxmd.com/read/28618014/dual-mode-optical-sensing-of-histamine-at-nanomolar-concentrations-in-complex-biological-fluids-and-living-cells
#12
Santanu Bhattacharya, Nilanjan Dey, Asfa Ali, Santosh Podder, Shamik Majumdar, Dipankar Nandi
An easily synthesizable fluorescein-based luminescent dye has been utilized for dual-mode detection of histamine at a nanomolar concentration at pH 7.0 in water. The specific response with histamine was achieved by imidazole catalyzed 'imine' formation reaction. The protocol was subsequently applied for the estimation of histamine in complex biological milieu such as human blood serum and urine samples. Furthermore, the dose-dependent cellular uptake of histamine and de novo synthesis (by thapsigargin treatment) was visualized in RAW 264...
June 15, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28617575/external-influences-on-invertebrate-brain-histamine-and-related-compounds-via-an-automated-derivatization-method-for-capillary-electrophoresis
#13
Sandrine Parrot, Mónica Pavón Vergés, Marie-Jeanne Perrot-Minnot, Luc Denoroy
Histamine has been shown to modulate visual system and photic behavior in arthropods. However, few methods are available for the direct quantification of histamine and its precursor and metabolites in arthropod brain. In this work, a method for the separation of histamine, its precursor histidine and its metabolite N-methyl-histamine from brain extracts of a freshwater crustacean has been developed using capillary electrophoresis with laser-induced fluorescence detection. Molecules were tagged on their primary amine function with naphthalene-2,3-dicarboxaldehyde, but derivatized histamine and N-methyl-histamine exhibited poor stability in contrast to derivatized histidine...
June 15, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28616446/treatment-with-anti-fc%C3%AE%C2%B5ri%C3%AE-antibody-exacerbates-eae-and-t-cell-immunity-against-myelin
#14
Silvia Musio, Massimo Costanza, Pietro Luigi Poliani, Elena Fontana, Manuela Cominelli, Gabriella Abolafio, Lawrence Steinman, Rosetta Pedotti
OBJECTIVE: To investigate the effects of targeting the high-affinity receptor for immunoglobulin E (FcεRI), that plays a central role in allergic responses and is constitutively expressed on mast cells and basophils, in clinical disease and autoimmune T-cell response in experimental MS. METHODS: Experimental autoimmune encephalomyelitis (EAE) was induced in C57BL/6 mice by immunization with myelin oligodendrocyte glycoprotein 35-55. Anti-FcεRI α-chain antibody was administered intraperitoneally...
May 2017: Neurology® Neuroimmunology & Neuroinflammation
https://www.readbyqxmd.com/read/28616043/angioedema-suppressed-by-a-combination-of-anti-histamine-and-leukotriene-modifier
#15
Brendan N Wong, Peter Vadas
RATIONALE: Angioedema without co-existent urticaria is due to a limited number of causes, including hereditary and acquired C1 esterase inhibitor deficiency, drug-induced angioedema or idiopathic histaminergic or non-histaminergic angioedema. We describe a cohort of patients with recurrent angioedema whose clinical features and response to medications are distinct from the causes above. METHODS: Patients were accrued retrospectively from an academic allergy practice between 2007 and 2014...
2017: Allergy, Asthma, and Clinical Immunology
https://www.readbyqxmd.com/read/28615015/the-gastroprotective-effect-of-ethyl-acetate-fraction-of-hot-water-extract-of-trichosanthes-cucumerina-linn-and-its-underlying-mechanisms
#16
Ramani Karunakaran, M Ira Thabrew, G Mayuri Thammitiyagodage, B Prasanna Galhena, L D A Menuka Arawwawala
BACKGROUND: Antacids, anticholinergic drugs, histamine H2- receptor antagonists and irreversible proton pump inhibitors have been used for the treatment of gastric ulcers. However, prolonged use of these drugs may lead to series of adverse effects such as diarrhea, headache, rash, hypertension, muscular and joint pain. Therefore, there is an urgent need of more effective and safer treatments with fewer side effects. The aim of the present study was to scientifically evaluate the gastroprotective activity of fractions of the hot water extract of Trichosanthes cucumerina Linn (Family: Cucurbitaceae) aerial parts with a view to identifying the fraction with the best gastroprotective activity and the possible mechanism/s by which this fraction exert gastroprotection...
June 14, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28614417/antipsychotic-medications-and-stroke-in-schizophrenia-a-case-crossover-study
#17
Wen-Yin Chen, Lian-Yu Chen, Hsing-Cheng Liu, Chi-Shin Wu, Shu-Yu Yang, Chun-Hung Pan, Shang-Ying Tsai, Chiao-Chicy Chen, Chian-Jue Kuo
BACKGROUND: The association between antipsychotic use and the risk of stroke in schizophrenic patients is controversial. We sought to study the association in a nationwide cohort with schizophrenia. METHODS: Using a retrospective cohort of patients with schizophrenia (N = 31,976) derived from the Taiwan National Health Insurance Research Database, 802 new-onset cases of stroke were identified within 10 years of follow-up (from 2000 through 2010). We designed a case-crossover study using 14-day windows to explore the risk factors of stroke and the association between antipsychotic drugs and the risk of stroke...
2017: PloS One
https://www.readbyqxmd.com/read/28614190/non-histaminergic-and-mechanical-itch-sensitization-in-atopic-dermatitis
#18
H H Andersen, J Elberling, H Sølvsten, G Yosipovitch, L Arendt-Nielsen
Chronic or episodic severe itch is recurrent in atopic dermatitis (AD). Non-histaminergic neuronal itch pathways are suggested to dominate in AD itch, contributing to an "itch-scratch-itch cycle" that prolongs and worsens itch, pain, and skin lesions. We hypothesized that non-histaminergic neuronal sensitization contributes to itch in AD. Hence, we compared sensitivity to thermal, mechanical, and chemical pruritic stimuli in AD patients and controls. The study comprised 25 AD patients with chronic itch and 25 healthy controls...
June 9, 2017: Pain
https://www.readbyqxmd.com/read/28613003/systematic-review-pharmacotherapy-for-high-output-enterostomies-or-enteral-fistulas
#19
REVIEW
F E E de Vries, L F Reeskamp, O van Ruler, I van Arum, W Kuin, G Dijksta, J W Haveman, M A Boermeester, M J Serlie
BACKGROUND: High-output enterocutaneous fistula or enterostomies can cause intestinal failure. There is a wide variety of options in medical management of patients with high output. AIM: To systematically review the literature on available pharmacotherapy to reduce output and to propose an algorithm for standard of care. METHODS: Relevant databases were systematically reviewed to identify studies on pharmacotherapy for reduction in (high-) output enterostomies or fistula...
June 14, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28613002/the-catalytic-mechanism-of-the-pyridoxal-5-phosphate-dependent-enzyme-histidine-decarboxylase-a-computational-study
#20
Henrique Silva Fernandes, Maria João Ramos, Nuno M F S A Cerqueira
The catalytic mechanism of histidine decarboxylase (HDC), a pyridoxal-5'-phosphate (PLP)-dependent enzyme, was studied by using a computational QM/MM approach following the scheme M06-2X/6-311++G(3df,2pd):Amber. The reaction involves two sequential steps: the decarboxylation of l-histidine and the protonation of the generated intermediate from which results histamine. The rate-limiting step is the first one (ΔG(≠) =17.6 kcal mol(-1) ; ΔGr =13.7 kcal mol(-1) ) and agrees closely with the available experimental kcat (1...
June 14, 2017: Chemistry: a European Journal
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