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Nopphasul Sirijant, Rasana W Sermswan, Surasakdi Wongratanacheewin
Burkholderia pseudomallei, the causative agent of melioidosis, has been found to increase its resistance to antibiotics when growing as a biofilm. The resistances are related to several mechanisms. One of the possible mechanisms is the efflux pump. Using bioinformatics analysis, it was found that BPSL1661, BPSL1664 and BPSL1665 were orthologous genes of the efflux transporter encoding genes for biofilm related antibiotic resistance PA1874-PA1877 genes in Pseudomonas aeruginosa strain PAO1. Expressions of selected encoding genes for the efflux transporter system during biofilm formation were investigated...
September 30, 2016: Journal of Medical Microbiology
Babita Kumari, Karthikeyan Kesavan
Clotrimazole (CTZ) is a broad spectrum antimycotic agent known to be very effective locally for the treatment of fungal skin infections. The aim of this study was to study the effect of chitosan-coated microemulsion (CME) for topical delivery of CTZ and also evaluate its in-vitro antifungal efficacy, Ex-vivo permeation and retention ability on the skin surface. The pseudo-ternary phase diagrams were developed using clove oil as oil phase, Tween 80 and propylene glycol as surfactant and co-surfactant, respectively and distilled water as aqueous phase...
August 30, 2016: Pharmaceutical Development and Technology
Lúcia de Fátima Almeida de Deus Moura, Marina de Deus Moura de Lima, Cacilda Castelo Branco Lima, Jessa Iashmin Alcobaça Gomes Machado, Marcoeli Silva de Moura, Paulo Vasconcelos de Carvalho
OBJECTIVE: This study presents 38 cases of primary molars with necrotic pulps treated with antibiotics-based paste. CASE REPORT: The technique consisted of necrotic tissue removal of the pulp chamber, using spoons excavators and low speed drills. Pulp cavity was washed with saline solution and dried with sterile cotton balls. Then an antibiotic paste composed of chloramphenicol, tetracycline, zinc oxide and eugenol - CTZ paste - was inserted at the entrance of root canals...
2016: Journal of Clinical Pediatric Dentistry
Ryo Nishihara, Daniel Citterio, Koji Suzuki
The development of coelenterazine (CTZ) derivatives resulting in superior optical characteristics is an efficient method to extend the range of its possible applications. Here, we describe the synthesis of three C-6 substituted CTZ derivatives retaining the recognition by Renilla luciferase (RLuc) and its derivatives. The novel derivatives are useful as bright blue-shifted CTZ derivatives, which can be used as an alternative to hitherto reported compound DeepBlueC™.
2016: Methods in Molecular Biology
Legna Colina-Vegas, Jocely Lucena Dutra, Wilmer Villarreal, João Honorato de A Neto, Marcia Regina Cominetti, Fernando Pavan, Maribel Navarro, Alzir A Batista
Three ruthenium complexes [RuCl(CTZ)(bipy)(P-P)]PF6 [P-P=1,2-bis(diphenylphosphino)ethane (dppe-1), 1,4-bis(diphenylphosphino)butane (dppb-2) and 1,1'-bis(diphenylphosphino)ferrocene (dppf-3), bipy=2,2'-bipiridine and clotrimazole (CTZ) 1-[(2-chlorophenyl)diphenylmethyl]-1H-imidazole] were synthesized. These complexes were characterized by a combination of elemental analysis, molar conductivity, infrared and UV-vis spectroscopy, (1)H, (13)C{(1)H} and (31)P{(1)H} nuclear magnetic resonance techniques, cyclic voltammetry and mass spectroscopy...
June 25, 2016: Journal of Inorganic Biochemistry
Alberto Batticciotto, Roberto Ravasio, Marta Riva, Piercarlo Sarzi-Puttini
INTRODUCTION: Only limited information is available on cost efficacy of the various biological agents used to treat patients with rheumatoid arthritis with intolerance or for whom it would be inappropriate to continue treatment with conventional agents. We estimated the efficacy and treatment costs of monotherapy with biological agents in the treatment of this group of patients. METHODS: Data from two previous meta-analyses in the treatment of patients who are intolerant to methotrexate (MTX), or for whom it would be inappropriate to continue treatment with MTX was used...
August 2016: Advances in Therapy
Takeru Shimizu, Robert M Dietz, Ivelisse Cruz-Torres, Frank Strnad, Ana K Garske, Myriam Moreno, Venugopal R Venna, Nidia Quillinan, Paco S Herson
INTRODUCTION: TRPM2 channels have been suggested to play a role in ischemic neuronal injury, specifically in males. A major hindrance to TRPM2 research has been the lack of specific TRPM2 inhibitors. The current study characterized the specificity and neuroprotective efficacy of a novel TRPM2 inhibitor. METHODS: Fluorescent calcium imaging (Fluo5F) was used to determine inhibitor efficacy of the TRPM2 peptide inhibitor (tat-M2NX) in HEK293 cells stably expressing hTRPM2...
September 2016: Experimental Neurology
Bradley J Gardiner, Yoav Golan
Avibactam, a novel β-lactamase inhibitor, has recently been co-formulated with ceftazidime and approved for use in patients with complicated intra-abdominal and urinary tract infections, where no better treatment alternative exists. The basis for its FDA approval has been the extensive clinical experience with ceftazidime and the demonstration in vitro and in animal models that the addition of avibactam reverses resistance to ceftazidime in extended-spectrum β-lactamase and some carbapenemase-producing Enterobacteriaceae...
2016: Expert Review of Anti-infective Therapy
Tianyu Jiang, Lupei Du, Minyong Li
Bioluminescence-based techniques, such as bioluminescence imaging, BRET and dual-luciferase reporter assay systems, have been widely used to examine a myriad of biological processes. Coelenterazine (CTZ), a luciferin or light-producing compound found in bioluminescent organisms, has sparked great curiosity and interest in searching for analogues with improved photochemical properties. This review summarizes the current development of coelenterazine analogues, their bioluminescence properties, and the rational design of caged coelenterazine towards biotargets, as well as their applications in bioassays...
April 2016: Photochemical & Photobiological Sciences
Khalid Mohamed El-Say
This study was aimed at developing a controlled-release cetirizine hydrochloride (CTZ)-loaded polymethacrylate microsphere by optimization technique using software-based response surface methodology. The emulsion solvent evaporation method was utilized in the preparation of microspheres. Four process variables were selected, namely, Eudragit RLPO loading percentage in total polymer, the emulsifier hydrophilic lipophilic balance (HLB), the antitacking percentage, and the dispersed phase volume. The desired responses were particle size, angle of repose, production yield, encapsulation efficiency, loading capacity, initial drug release, and the time for 85% of drug release from the microspheres...
2016: Drug Design, Development and Therapy
Yoshie Hasegawa, Hirokazu Tanino, Jun Horiguchi, Daishu Miura, Takashi Ishikawa, Mitsuhiro Hayashi, Shintaro Takao, Seung Jin Kim, Kazuhiko Yamagami, Masaru Miyashita, Muneharu Konishi, Yasushi Shigeoka, Masato Suzuki, Tetsuya Taguchi, Tomoyuki Kubota, Kouhei Akazawa, Norio Kohno
PURPOSE: Zoledronic acid (ZOL) is a nitrogen-containing bisphosphonate that induces osteoclast apoptosis and inhibits bone resorption by inhibiting the mevalonate pathway. Its benefit for the prevention of skeletal complications due to bone metastases has been established. However, the antitumor efficacy of ZOL, although suggested by multiple preclinical and clinical studies, has not yet been clinically proven. We performed the present randomized Phase 2 trial to investigate the antitumor effect of ZOL with chemotherapy (CT)...
2015: PloS One
Masahito Nagashima, Yuka Yamagishi, Hiroshige Mikamo
There have been the current Japanese data on susceptibility testing for Candida isolates from vaginal candidiasis. The in vitro activities of therapeutic antifungal drugs for vulvovaginal candidiasis (VVC); miconazole (MCZ), itraconazole (ITCZ), fluconazole (FLCZ), clotrimazole (CTZ), oxiconazole (OCZ), isoconazole (ICZ) and bifonazole (BFZ) against vaginal isolates. Fifty-four strains Candida albicans and 19 strains of Candida glabrata were evaluated using a broth microdilution method specified by Clinical Laboratories Standard Institute (CLSI) document M27-A3...
February 2016: Journal of Infection and Chemotherapy: Official Journal of the Japan Society of Chemotherapy
Chien-Te Lee, Hwee-Yeong Ng, Yueh-Ting Lee, Li-Wen Lai, Yeong-Hau H Lien
Calbindin-D28k (CBD-28k) is a calcium binding protein located in the distal convoluted tubule (DCT) and plays an important role in active calcium transport in the kidney. Loop and thiazide diuretics affect renal Ca and Mg handling: both cause Mg wasting, but have opposite effects on Ca excretion as loop diuretics increase, but thiazides decrease, Ca excretion. To understand the role of CBD-28k in renal Ca and Mg handling in response to diuretics treatment, we investigated renal Ca and Mg excretion and gene expression of DCT Ca and Mg transport molecules in wild-type (WT) and CBD-28k knockout (KO) mice...
February 1, 2016: American Journal of Physiology. Renal Physiology
Francesco Caso, Ennio Lubrano, Antonio Del Puente, Paolo Caso, Rosario Peluso, Francesca Foglia, Carolina Benigno, Nicolò Girolimetto, Paolo Bottiglieri, Raffaele Scarpa, Luisa Costa
The improved recognition of pathogenetic molecular mechanisms has led to the use of drugs targeting cytokines in different inflammatory arthropathies as well psoriatic arthritis (PsA). In particular, the progress in knowledge on tumor necrosis factor (TNF)-α in the pathogenesis of PsA has changed the therapeutic approach by use of direct and receptor cytokine antagonists. Currently, infliximab (IFX), adalimumab, etanercept, golimumab and certolizumab pegol represent the five anti-TNF-α available for the treatment of PsA...
2016: Expert Review of Clinical Immunology
Nidia Quillinan, Himmat Grewal, Jelena Klawitter, Paco S Herson
Calcium-permeable transient receptor potential M2 (TRPM2) ion channel activation contributes to cerebral ischemic injury specifically in males. In male mice, circulating androgens are required for TRPM2 inhibition with clotrimazole (CTZ) to provide protection following experimental stroke. Sufficient levels of circulating androgens are necessary to support ischemia-induced activation of poly ADP ribose polymerase (PARP) and consequent activation of TRPM2 channels. In this study, we tested whether differences in sex steroids contribute to the lack of CTZ neuroprotection in females...
November 2014: ENeuro
Sung Bae Kim, Simon Miller, Nobuhiro Suzuki, Toshiya Senda, Ryo Nishihara, Koji Suzuki
The present study demonstrates cation-driven optical properties of artificial luciferases (ALucs) from copepod luciferases, as an optical readout for bioanalysis. An assignment of the supersecondary structure code (SSC) of ALucs revealed that ALucs carry a helix-loop-helix structure, which appears at the same sites of the EF-hands of typical Ca(2+)-binding proteins. A mutagenesis study shows that the EF-hand-like structure is a pivotal site for enzymatic activity. The effects of 20 kinds of mono- and multivalent cations on ALuc activities were estimated with column-purified ALuc16...
2015: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
G B Christiansen, B Harbak, S E Hede, A H Gouliaev, L Olsen, K Frydenvang, J Egebjerg, J S Kastrup, M M Holm
Positive allosteric modulators (PAMs) of 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptors receive increasing interest as therapeutic drugs and have long served as important experimental tools in the study of the molecular mechanisms underlying glutamate-mediated neurotransmission. The aim of this study was to investigate functional and structural aspects of a novel analog of the AMPA receptor PAM cyclothiazide (CTZ) on recombinant and native glutamate receptors. We expressed rat GluA4flip and flop in Xenopus oocytes and characterized NS1376 and CTZ under two-electrode voltage-clamp...
December 3, 2015: Neuroscience
Michael E El-Kommos, Samia M El-Gizawy, Noha N Atia, Noha M Hosny
A validated simple, novel, and rapid spectrofluorimetric method was developed for the determination of some non-sedating antihistamines (NSAs); namely cetirizine (CTZ), ebastine (EBS), fexofenadine (FXD), and loratadine (LOR). The method is based on measuring the native fluorescence of the cited drugs after protonation in acidic media and studying their quantitative fluorescence intensity - structure relationships. There was a linear relationship between the relative fluorescence intensity and the concentration of the investigated drug...
November 2015: Journal of Fluorescence
Joana Galvao, Filipe Elvas, Tiago Martins, M Francesca Cordeiro, António Francisco Ambrósio, Ana Raquel Santiago
Death of retinal neural cells, namely retinal ganglion cells (RGCs), is a characteristic of several retinal neurodegenerative diseases. Although the role of adenosine A3 receptor (A3R) in neuroprotection is controversial, A3R activation has been reported to afford protection against several brain insults, with few studies in the retina. In vitro models (retinal neural and organotypic cultures) and animal models [ischemia-reperfusion (I-R) and partial optic nerve transection (pONT)] were used to study the neuroprotective properties of A3R activation against retinal neurodegeneration...
November 2015: Experimental Eye Research
Takamitsu Hosoya, Rie Iimori, Suguru Yoshida, Yuto Sumida, Yuiko Sahara-Miura, Jun-ichi Sato, Satoshi Inouye
A novel synthetic method for v-coelenterazine (v-CTZ), which is a vinylene-bridged analog of native CTZ with a large red-shifted luminescence property, is described. The synthesis was achieved in a concise way through the use of three sequential cross-coupling reactions and ring-closing metathesis (RCM). A newly synthesized C2-modified trifluoromethyl analog cf3-v-CTZ showed slightly more red-shifted luminescence than v-CTZ when it was used as a substrate for Renilla luciferases.
August 7, 2015: Organic Letters
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