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Babak Behnam Azad, Daniel P Holt, Hayden T Ravert, Andrew G Horti, Robert F Dannals
In this concise practitioner protocol, the radiochemical synthesis of [18 F]FNDP suitable for human PET studies is described and the results from validation productions are presented. The high specific activity radiotracer product is prepared as a sterile, apyrogenic solution that conforms to current Good Manufacturing Practice (cGMP) requirements.
March 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Věra Čertíková Chábová, Petr Kujal, Petra Škaroupková, Zdeňka Varňourková, Šárka Vacková, Zuzana Husková, Soňa Kikerlová, Janusz Sadowski, Elzbieta Kompanowska-Jezierska, Iwona Baranowska, Sung Hee Hwang, Bruce D Hammock, John D Imig, Vladimír Tesař, Ludek Červenka
BACKGROUND/AIMS: We found recently that increasing renal epoxyeicosatrienoic acids (EETs) levels by blocking soluble epoxide hydrolase (sEH), an enzyme responsible for EETs degradation, shows renoprotective actions and retards the progression of chronic kidney disease (CKD) in Ren-2 transgenic hypertensive rats (TGR) after 5/6 renal ablation (5/6 NX). This prompted us to examine if additional protection is provided when sEH inhibitor is added to the standard renin-angiotensin system (RAS) blockade, specifically in rats with established CKD...
March 6, 2018: Kidney & Blood Pressure Research
P Kala, L Sedláková, P Škaroupková, L Kopkan, Z Vaňourková, M Táborský, A Nishiyama, S H Hwang, B D Hammock, J Sadowski, V Melenovský, J D Imig, L Červenka
We showed recently that increasing kidney epoxyeicosatrienoic acids (EETs) by blocking soluble epoxide hydrolase (sEH), an enzyme responsible for EETs degradation, retarded the development of renal dysfunction and progression of aorto-caval fistula(ACF)-induced congestive heart failure (CHF) in Ren-2 transgenic hypertensive rats (TGR). In that study the final survival rate of untreated ACF TGR was only 14 % but increased to 41 % after sEH blockade. Here we examined if sEH inhibition added to renin-angiotensin system (RAS) blockade would further enhance protection against ACF-induced CHF in TGR...
March 12, 2018: Physiological Research
Arun Bahadur Gurung, Bishwarjit Mayengbam, Atanu Bhattacharjee
Soluble epoxide hydrolase (sEH), a key enzyme belonging to cytochrome P450 pathway of arachidonic acid cascade is a novel therapeutic drug target against atherosclerosis. The enzyme breaks down epoxyeicosatrienoic acid (EETs) to dihydroxy-eicosatrienoic acids (DHETs) and reduces beneficial cardiovascular properties of EETs. Thus, the present work is aimed at identification of potential leads as sEH inhibitors which will sustain the beneficial properties of EETs in vivo. PubChem and ZINC databases were screened for drug-like compounds based on Lipinski's rule of five and in silico toxicity filters...
March 6, 2018: Computational Biology and Chemistry
Suixia Li, Panpan Wang, Jialin Zhao, Luhong Zhou, Pengfei Zhang, Chengyu Fu, Jianghong Meng, Xin Wang
The aim of this study was to investigate the toxin gene profile and antimicrobial resistance of Staphylococcus aureus isolates from raw chicken in the People's Republic of China. In total, 289 S. aureus isolates were characterized by antimicrobial susceptibility testing, and genes encoding enterotoxins, exfoliative toxins, Panton-Valentine leukocidin, and toxic shock syndrome toxin were revealed by PCR. Overall, 46.0% of the isolates were positive for one or more toxin genes. A high proportion of toxin genes were pvl (26...
April 2018: Journal of Food Protection
K K Fursova, M P Shchannikova, I V Loskutova, A O Shepelyakovskaya, A G Laman, A M Boutanaev, S L Sokolov, O A Artem'eva, D A Nikanova, N A Zinovieva, F A Brovko
Mastitis, a major veterinary problem widespread in many regions, is caused mainly by Staphylococcus spp. However, there is no current reliable information about the role of Staphylococcus aureus and their toxins in the development of mastitis in cows in the territory of the Russian Federation. The aim of this investigation was to determine the profile of exotoxins of S. aureus from cow milk from farms of Central Russia. A total of 60 isolates of S. aureus were obtained from milk samples of cows with the subclinical form of mastitis...
February 21, 2018: Journal of Dairy Science
Bingbing Li, Xu Li, Yangu Pan, Jiang Qiu, Dajun Zhang
A self-enhancing humor style (SEHS) plays an important role in the regulation of negative emotion through humorous perspective-taking. Following the mind-reading theories of humor, we investigated the relationship between gray-matter volume (GMV) of brain areas related to theory of mind and SEHS in young college students, using voxel-based morphometry analysis. We then performed a voxel-wise analysis of covariance to assess any moderation effect of cognitive empathy on the relationship. Results demonstrated that higher SEHS scores were associated with larger GMV of the precuneus in the group with high cognitive empathy, but there was no association in the group with low cognitive empathy...
February 22, 2018: Scientific Reports
Jang Hoon Kim, In Sook Cho, Jaihyuk Ryu, Ji Sun Lee, Jong Seong Kang, Si Yong Kang, Young Ho Kim
Anthocyanin derivatives are well-known secondary constituents contained in fruits. The inhibitory activity of anthocyanin derivatives toward soluble epoxide hydrolase (sEH) was tested for potential applications in the treatment of cardiovascular diseases. Anthocyanin derivatives 1-5 showed dose-dependent inhibitory activity toward sEH, with IC 50 values ranging from 4.3 ± 0.2 to 25.3 ± 2.6 μM. Lineweaver-Burk plots showed that all anthocyanin derivatives preferentially interacted with allosteric sites instead of active sites as noncompetitive (1-3) and mixed (4 and 5) inhibitors...
February 12, 2018: International Journal of Biological Macromolecules
W Swardfager, M Hennebelle, D Yu, B D Hammock, A J Levitt, K Hashimoto, A Y Taha
The common and severe psychiatric disorders, including major depressive disorder (MDD) and bipolar disorder (BD), are associated with inflammation, oxidative stress and changes in peripheral and brain lipid metabolism. Those pathways are implicated in the premature development of vascular and metabolic comorbidities, which account for considerable morbidity and mortality, including increased dementia risk. During endoplasmic reticulum stress, the soluble epoxide hydrolase (sEH) enzyme converts anti-inflammatory fatty acid epoxides generated by cytochrome p450 enzymes into their corresponding and generally less anti-inflammatory, or even pro-inflammatory, diols, slowing the resolution of inflammation...
February 2, 2018: Neuroscience and Biobehavioral Reviews
Emilio Márquez-Contreras, Nieves Martell-Claros, Sara Márquez-Rivero, Enrique Hermida-Campa, Carmen Gracia-Diez, Eugenio Sanchez-López, Vicente Gil-Guillén
OBJECTIVE: To assess the efficacy of a mixed intervention, educational and reminder calendar of the intake, as a strategy to improve therapeutic adherence with dabigatran in patients with non-valvular atrial fibrillation (NVAF). METHODS: Prospective, longitudinal, multicenter study, carried out in 110 specialized healthcare centers in Spain. 726 patients treated with dabigatran prescribed for stroke prevention were included. A cluster randomization was performed based on two groups: 1) Control Group (CG) as usual clinical practice and Intervention Group (IG) with a mixed strategy: a) Healthcare education and b) Use of a reminder calendar for taking the anticoagulant medication...
January 31, 2018: Current Medical Research and Opinion
Sean D Kodani, Saavan Bhakta, Sung Hee Hwang, Svetlana Pakhomova, Marcia E Newcomer, Christophe Morisseau, Bruce D Hammock
Multi-target inhibitors have become increasing popular as a means to leverage the advantages of poly-pharmacology while simplifying drug delivery. Here, we describe dual inhibitors for soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FAAH), two targets known to synergize when treating inflammatory and neuropathic pain. The structure activity relationship (SAR) study described herein initially started with t-TUCB (trans-4-[4-(3-trifluoromethoxyphenyl-l-ureido)-cyclohexyloxy]-benzoic acid), a potent sEH inhibitor that was previously shown to weakly inhibit FAAH...
January 4, 2018: Bioorganic & Medicinal Chemistry Letters
Amy A Rand, Patrick O Helmer, Bora Inceoglu, Bruce D Hammock, Christophe Morisseau
Liquid chromatography-tandem mass spectrometry (LC-MS/MS) is a useful tool to characterize the behavior of natural lipids within biological matrices. We report a LC-MS/MS method developed specifically to analyze CYP products of the arachidonoyl ethanolamide (anandamide, AEA), the epoxyeicosatrienoic acid ethanolamides (EET-EAs) and their hydrolyzed metabolites, and the dihydroxyeicosatrienoic acid ethanolamides (DHET-EAs). This method was used to measure EET-EA biotransformation to DHET-EAs by two human epoxide hydrolases: the soluble EH (sEH) and the microsomal EH (mEH)...
2018: Methods in Molecular Biology
Min Gao, Rui Wang, Fabiao Yu, Lingxin Chen
As a crucial member in antioxidant regulatory systems, sulfane sulfur plays essential roles in cytoprotective mechanisms by directly eliminating ROS and altering ROS-mediated redox signaling. Despite the rising interests in sulfane sulfur, there only a few bio-compatible methods are available for its direct detection. Moreover, most of the existing methods cannot meet the requirements of real-time detection due to the reactive and labile chemical properties of sulfane sulfur. Therefore, we strive to clarify the mutual relationship between mitochondria sulfane sulfur and ROS under hypoxia stress...
January 11, 2018: Biomaterials
Idil Bastan, Xiao Na Ge, Mythili Dileepan, Yana G Greenberg, Alonso G Guedes, Sung Hee Hwang, Bruce D Hammock, Robert J Washabau, Savita P Rao, P Sriramarao
Prevalence of food allergies in the United States is on the rise. Eosinophils are recruited to the intestinal mucosa in substantial numbers in food allergen-driven gastrointestinal (GI) inflammation. Soluble epoxide hydrolase (sEH) is known to play a pro-inflammatory role during inflammation by metabolizing anti-inflammatory epoxyeicosatrienoic acids (EETs) to pro-inflammatory diols. We investigated the role of sEH in a murine model of food allergy and evaluated the potential therapeutic effect of a highly selective sEH inhibitor (trans-4-{4-[3-(4-trifluoromethoxyphenyl)-ureido]-cyclohexyloxy}-benzoic acid [t-TUCB])...
January 17, 2018: Journal of Leukocyte Biology
Ryohei Hirose, Takaaki Nakaya, Yuji Naito, Tomo Daidoji, Hiroaki Yasuda, Hideyuki Konishi, Yoshito Itoh
BACKGROUND AND AIMS: Development of high-performance submucosal injection materials (SIMs) contribute to the advancement of endoscopic therapy for early-stage gastrointestinal neoplasms. This study aimed to develop a new ex vivo model that mimics the human gastrointestinal tract to evaluate the performance (the height and duration of the submucosal elevation) of various SIMs in detail. METHODS: A new ex vivo model that applies a constant tension to the tested specimen (the porcine gastric specimen) was developed...
January 5, 2018: Journal of the Mechanical Behavior of Biomedical Materials
Alessandro Di Rienzo, Denise Brunozzi, Mauro Dobran, Maurizio Iacoangeli, Roberto Colasanti, Rikin Trivedi, Massimo Scerrati
OBJECTIVE: We present our experience with a modification of the conventional techniques for the removal of large Spinal Epidural Haematomas (SEHs), based on multilevel "skip hemilaminectomies". METHODS: Eleven patients with SEHs extending over 5 or more spinal segments were treated at our institution using a modified hemilaminectomy technique from 2008 to 2014. This procedure, that we called "skip hemilaminectomy" consists in performing consecutive, alternating, unilateral laminar decompressions at two to three levels, followed by sublaminar undercutting, ipsi- and contralateral flavectomy, plus haematoma removal...
January 8, 2018: World Neurosurgery
You-Lin Tain, Wei-Chia Lee, Kay L H Wu, Steve Leu, Julie Y H Chan
Widespread consumption of high-fructose and high-fat diets relates to the global epidemic of hypertension. Hypertension may originate from early life by a combination of prenatal and postnatal nutritional insults. We examined whether maternal high-fructose diet increases vulnerability to post-weaning high-fructose or high-fat diets induced hypertension in adult offspring and determined the underlying mechanisms. Pregnant Sprague-Dawley rats received regular chow (ND) or chow supplemented with 60% fructose (HFR) during the entire pregnancy and lactation periods...
January 9, 2018: Nutrients
Li-Hsin Chang, Hui-Ching Lin, Shiang-Suo Huang, I-Chih Chen, Kai-Wen Chu, Chun-Lien Chih, Yao-Wen Liang, Yi-Chung Lee, You-Yin Chen, Yi-Hsuan Lee, I-Hui Lee
Inhibition and deletion of soluble epoxide hydrolase (sEH) has been suggested to ameliorate infarction in experimental ischemic stroke possibly via vasoactive epoxyeicosatrienoic acids. However, it is unknown whether the neuroprotective mechanisms involve alteration of post-ischemic neuronal transmission and neurotrophic signaling. We used a permanent middle cerebral artery occlusion (MCAO) model in adult wild-type mice with the sEH inhibitor 12-(3-adamantan-1-yl-ureido)dodecanoic acid (AUDA) post-treatment and in sEH knockout (sEH KO) mice...
January 8, 2018: Scientific Reports
Vladimir Burmistrov, Christophe Morisseau, Todd R Harris, Gennady Butov, Bruce D Hammock
Adamantyl groups are widely used in medicinal chemistry. However, metabolism limits their usage. Herein, we report the first systematic study of adamantyl ureas and diureas bearing substituents in bridgehead positions of adamantane and/or spacers between urea groups and adamantane group, and tested their effects on soluble epoxide hydrolase inhibitor potency and metabolic stability. Interestingly, the effect on activity against human and murine sEH varied in opposite ways with each new methyl group introduced into the molecule...
December 30, 2017: Bioorganic Chemistry
Samuel D Lotz, Alex Dickson
Ligand (un)binding kinetics is being recognized as a determinant of drug specificity and efficacy in an increasing number of systems. However, the calculation of kinetics and the simulation of drug unbinding is more difficult than computing thermodynamic quantities, such as binding free energies. Here we present the first full simulations of an unbinding process at pharmacologically relevant time scales (11 min), without the use of biasing forces, detailed prior knowledge, or specialized processors using the weighted ensemble based algorithm, WExplore...
January 5, 2018: Journal of the American Chemical Society
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