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https://www.readbyqxmd.com/read/28922345/tilianin-post-conditioning-attenuates-myocardial-ischemia-reperfusion-injury-via-mitochondrial-protection-and-inhibition-of-apoptosis
#1
Yangyang Wang, Yong Yuan, Xinchun Wang, Yanfang Wang, Jiang Cheng, Li Tian, Xinhong Guo, Dongmei Qin, Wenjiang Cao
BACKGROUND The aim of this study was to investigate the role of tilianin in modulating mitochondrial functions and mitochondria-mediated apoptosis during cardio-protection. MATERIAL AND METHODS Myocardial ischemia/reperfusion (I/R) injury was induced by 30 minutes coronary occlusion followed by two hours reperfusion in Sprague-Dawley rats. To investigate the cardio-protective effects of tilianin, apoptosis was evaluated by TUNEL. Mitochondrial ultrastructure and function were assessed by transmission electron microscopy, dynamics of mitochondrial permeability transition pore (mPTP) opening and ATP production in the myocardium; Ca2+ content and reactive oxygen species (ROS) were measured to evaluated the level of damage factors in the mitochondria...
September 18, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28922251/shank3-regulates-intestinal-barrier-function-through-modulating-zo-1-expression-through-the-pkc%C3%AE%C2%B5-dependent-pathway
#2
Shu-Chen Wei, Hsin-Fang Yang-Yen, Po-Nien Tsao, Meng-Tzu Weng, Chien-Chih Tung, Linda C H Yu, Liang-Chuan Lai, Jen-Hao Hsiao, Eric Y Chuang, Chia-Tung Shun, Yen-Hsuan Ni, Ramnik J Xavier, Daniel K Podolsky, Jeffery J Y Yen, Jau-Min Wong
BACKGROUND: The integrity of the gut barrier in patients with inflammatory bowel disease is known to be impaired but the exact mechanisms remain mostly unknown. SHANK3 mutations are associated with autism, and patients with autism are known to have higher proportions of inflammatory bowel disease. Here, we explore the role of SHANK3 in inflammatory bowel disease, both in vivo and in vitro. METHODS: Dextran sulfate sodium colitis was induced in SHANK3 knockout mice...
August 23, 2017: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/28921848/interconversion-rates-between-conformational-states-as-rationale-for-the-membrane-permeability-of-cyclosporines
#3
Jagna Witek, Max Mühlbauer, Bettina G Keller, Markus Blatter, Axel Meissner, Trixie Wagner, Sereina Riniker
Cyclic peptides have regained interest as potential inhibitors of challenging targets, but have often a low bioavailability. The natural product cyclosporine A (CsA) is the textbook exception. Despite its size and polar backbone it is able to passively cross membranes. This ability is hypothesized to be due to a conformational change from the low-energy conformation in water to a "congruent" conformation that is populated both in water and inside the membrane. Here, we use a combination of NMR measurements and kinetic models based on molecular dynamics simulations to rationalize the difference in the membrane permeability of cyclosporine E (CsE) and CsA...
September 17, 2017: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
https://www.readbyqxmd.com/read/28921719/inflammation-alters-ampa-stimulated-calcium-responses-in-dorsal-striatal-d2-but-not-d1-spiny-projection-neurons
#4
Carissa D Winland, Nora Welsh, Alberto Sepulveda-Rodriguez, Stefano Vicini, Kathleen A Maguire-Zeiss
Neuroinflammation precedes neuronal loss in striatal neurodegenerative diseases and can be exacerbated by the release of proinflammatory molecules by microglia. These molecules can affect trafficking of AMPARs. The preferential trafficking of calcium-permeable versus impermeable AMPARs can result in disruptions of [Ca(2+) ]i and alter cellular functions. In striatal neurodegenerative diseases, changes in [Ca(2+) ]i and L-type voltage-gated calcium channels (VGCCs) have been reported. Therefore, the present study sought to determine whether a proinflammatory environment alters AMPA-stimulated [Ca(2+) ]i through calcium-permeable AMPARs and/or L-type VGCCs in dopamine-2 and dopamine-1 expressing striatal spiny projection neurons (D2 and D1 SPNs) in the dorsal striatum...
September 16, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28921713/chebulinic-acid-isolated-from-the-fruits-of-terminalia-chebula-specifically-induces-apoptosis-in-acute-myeloid-leukemia-cells
#5
Stuti Chhabra, Tripti Mishra, Yogesh Kumar, Gatha Thacker, Sanjeev Kanojiya, Naibedya Chattopadhyay, Tadigoppula Narender, Arun Kumar Trivedi
Chebulinic acid, an ellagitannin found in the fruits of Terminalia chebula, has been extensively used in traditional Indian system of medicine. It has shown to have various biological activities including antitumor activity. The present study aims to investigate the cytotoxic potential of chebulinic acid in human myeloid leukemia cells. Interestingly, chebulinic acid caused apoptosis of acute promyelocytic leukemia HL-60 and NB4 cells but not K562 cells. In vitro antitumor effects of chebulinic acid were investigated by using various acute myeloid leukemia cell lines...
September 18, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28921467/mir-155-dysregulation-and-therapeutic-intervention-in-multiple-sclerosis
#6
Claire E McCoy
microRNAs play a fundamental role in the immune system. One particular microRNA, miR-155 plays a critical role in hematopoietic cell development and tightly regulates innate and adaptive immune responses in response to infection. However, its dysregulation, more specifically its overexpression, is closely associated with various inflammatory disorders. The purpose of this review is to consolidate how miR-155 underpins a variety of processes that contribute to the pathology of multiple sclerosis (MS). In particular, the impact of miR-155 is discussed with respect to human pathology and animal models...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28921048/antibacterial-and-antitumor-activity-of-bogorol-b-jx-isolated-from-brevibacillus-laterosporus-jx-5
#7
Hongxia Jiang, Chao Ji, Junkang Sui, Rongbo Sa, Xiaohui Wang, Xunli Liu, Tai L Guo
Antimicrobial peptides are promising anti-infective agent candidates because they have a broad antimicrobial spectrum and bioactivity and are unlikely to elicit antibiotic resistance. The bogorols represent a new cationic antibiotic peptide and possess great therapeutic potential because of their bioactivity and precise mode of action. Here, we report that Bogorol B-JX (BBJX), a peptide previously isolated from Brevibacillus laterosporus JX-5 by us, has significant antibacterial and antitumor activities in vitro...
September 18, 2017: World Journal of Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28920862/enhanced-endothelium-epithelial-sodium-channel-signaling-prompts-left-ventricular-diastolic-dysfunction-in-obese-female-mice
#8
Guanghong Jia, Javad Habibi, Annayya R Aroor, Michael A Hill, Vincent G DeMarco, Li E Lee, Lixin Ma, Brady J Barron, Adam Whaley-Connell, James R Sowers
OBJECTIVE: Enhanced activation of cell specific mineralocorticoid receptors (MRs) in obesity plays a key role in the development of cardiovascular disease including cardiac diastolic dysfunction as a critical prognosticator. Our previous investigations demonstrated that selective endothelium MR activation promotes a maladaptive inflammatory response and fibrosis in cardiovascular tissue in female mice fed a western diet (WD), and this was associated with expression and activation of the epithelial sodium channel on the surface of endothelial cells (EnNaC)...
September 8, 2017: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/28920690/regional-intestinal-permeability-in-rats-a-comparison-of-methods
#9
Carl Roos, David Dahlgren, E Sjögren, Christer Tannergren, Bertil Abrahamsson, H Lennernas
Currently, the screening of new drug candidates for intestinal permeation is typically based on in vitro models which give no information regarding regional differences along the gut. When evaluation of intestinal permeability by region is undertaken, two preclinical rat models are commonly used, the Ussing chamber method and single-pass intestinal perfusion (SPIP). To investigate the robustness of in vivo predictions of human intestinal permeability, a set of four model compounds was systematically investigated in both these models, using tissue specimens and segments from the jejunum, ileum, and colon of rats from the same genetic strain...
September 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28920595/a-unique-rectilinearly-%C3%AF-extended-rhodamine-dye-with-large-stokes-shift-and-near-infrared-fluorescence-for-bioimaging
#10
Chang Liu, Xiaojie Jiao, Qing Wang, Kun Huang, Song He, Liancheng Zhao, Xianshun Zeng
The synthesis of a novel rectilinearly π-extended rhodamine dye (TJ730) has been described. It exhibits NIR fluorescence emission with a Stokes shift of >110 nm. TJ730 and its ester derivative are cell permeable, have low cytotoxicity, are biocompatible, and can be directly used as NIR tracers for lysosome staining. Using TJ730 as a precursor, two probes have been prepared for Cu(2+).
September 18, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28920575/the-p2x7-receptor-forms-a-dye-permeable-pore-independent-of-its-intracellular-domain-but-dependent-on-membrane-lipid-composition
#11
Akira Karasawa, Kevin Michalski, Polina Mikhelzon, Toshimitsu Kawate
The P2X7 receptor mediates extracellular-ATP signaling implicated in the development of devastating diseases such as chronic pain and cancer. Activation of the P2X7 receptor leads to opening of the characteristic dye-permeable membrane pore for molecules up to ~900 Da. However, it remains controversial what constitutes this peculiar pore and how it opens. Here we show that the panda P2X7 receptor, when purified and reconstituted into liposomes, forms an intrinsic dye-permeable pore in the absence of other cellular components...
September 18, 2017: ELife
https://www.readbyqxmd.com/read/28920426/methotrexate-camptothecin-prodrug-nanoassemblies-as-a-versatile-nanoplatform-for-biomodal-imaging-guided-self-active-targeted-and-synergistic-chemotherapy
#12
Yang Li, Jinyan Lin, Jinyuan Ma, Liang Song, Huirong Lin, Bowen Tang, Dengyue Chen, Guanghao Su, Shefang Ye, Xuan Zhu, Fang-Hong Luo, Zhenqing Hou
"All-in-one" carrier-free-based nano-multi-drug self-delivery system could combine triple advantages of small molecules, nanoscale characteristics, and synergistic combination therapy together. Researches have showed that dual-acting small molecular methotrexate (MTX) could target and kill the folate receptors-overexpressing cancer cells. Inspired by this mechanism, a novel collaborative "early-phase tumor-selective targeting and late-phase synergistic anticancer" approach was developed for the self-assembly of chemotherapeutic drug-drug conjugate, which showed various advantages of more simplicity, efficiency, and flexibility over the conventional approach that was only based on single or combination cancer chemotherapy...
September 18, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28920425/a-far-red-emitting-fluorescence-probe-for-sensitive-and-selective-detection-of-peroxynitrite-in-live-cells-and-tissues
#13
Di Wu, Jae-Chan Ryu, Youn Wook Chung, Dayoung Lee, Ji-Hwan Ryu, Joo Heon Yoon, Juyoung Yoon
In this study, the far-red emitting fluorescence probe 1, containing a rhodamine derivative and a hydrazide reactive group, was developed for peroxynitrite detection and imaging. This probe, which is cell permeable and shows high sensitivity and selectivity in fluorometric detection of peroxynitrite over other ROS/RNS, was successfully utilized to detect exogenous and endogenous peroxynitrite in HeLa and RAW 264.7 cells, respectively. More importantly, 1 can also be used to detect endogenous peroxynitrite generated in Pseudomonas aeruginosa (PAO1) infected mouse bone marrow-derived neutrophils...
September 18, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28920186/investigation-of-cis-trans-isomer-dependent-dermatotoxicokinetics-of-uv-filter-ethylhexyl-methoxycinnamate-through-stratum-corneum-in-vivo
#14
Anežka Sharma, Katarína Bányiová, Branislav Vrana, Ivan Justan, Pavel Čupr
2-Ethylhexyl methoxycinnamate (EHMC) is one of the most used ultraviolet filters in personal care products. It undergoes cis/trans isomerization in sunlight, and there is limited toxicological understanding of the effects of the cis-isomer. It is known that two geometric isomers of one compound can have different physico-chemical properties and effects. However, there are no studies focusing on toxicokinetics of EHMC isomerization products to compare their potential difference in dermal exposure to cis-EHMC and trans-EHMC due to the difference in their dermatotoxicokinetics...
September 17, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28919790/exploring-bacterial-outer-membrane-barrier-to-combat-bad-bugs
#15
REVIEW
Ishan Ghai, Shashank Ghai
One of the main fundamental mechanisms of antibiotic resistance in Gram-negative bacteria comprises an effective change in the membrane permeability to antibiotics. The Gram-negative bacterial complex cell envelope comprises an outer membrane that delimits the periplasm from the exterior environment. The outer membrane contains numerous protein channels, termed as porins or nanopores, which are mainly involved in the influx of hydrophilic compounds, including antibiotics. Bacterial adaptation to reduce influx through these outer membrane proteins (Omps) is one of the crucial mechanisms behind antibiotic resistance...
2017: Infection and Drug Resistance
https://www.readbyqxmd.com/read/28919709/puerarin-transport-across-rat-nasal-epithelial-cells-and-the-influence-of-compatibility-with-peoniflorin-and-menthol
#16
Lin Zhang, Shou-Ying Du, Yang Lu, Chang Liu, Hui-Chao Wu, Zhi-Hao Tian, Min Wang, Chang Yang
Nose-to-brain transport can provide an excellent pathway for drugs of the central nervous system. Consequently, how to make full use of this pathway in practical applications has become a focus of drug design. However, many aspects affecting drug delivery from the nose to the brain remain unclear. This study aimed to more deeply investigate the transport of puerarin and to explore the mechanism underlying the influence of compatible drugs on puerarin permeability in a primary cell model simulating the nasal mucosa...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28919470/preparation-and-characterization-of-amorphous-ciprofloxacin-amino-acid-salts
#17
Hanah Mesallati, Daryl Conroy, Sarah Hudson, Lidia Tajber
The amorphization of the poorly soluble drug ciprofloxacin (CIP) may be facilitated by the use of a suitable stabilizer. In this study seven amino acids, with various side chain properties, were evaluated in this regard. Solid dispersions were prepared by ball milling 1:1 molar ratios of CIP with the amino acids, and their solid-state and pharmaceutical properties were then examined. Fully X-ray amorphous solid dispersions were obtained with aspartic acid, glutamic acid, cysteine and arginine. In each case, evidence of salt formation between the drug and amino acids was found via Fourier transform infrared spectroscopy and solid-state nuclear magnetic resonance...
September 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28919384/the-combination-of-gis-and-biphasic-to-better-predict-in-vivo-dissolution-of-bcs-class-iib-drugs-ketoconazole-and-raloxifene
#18
Yasuhiro Tsume, Naoto Igawa, Adam J Drelich, Gregory E Amidon, Gordon L Amidon
The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the human gastrointestinal (GI) tract. Since the GI environment influences the drug dissolution of BCS class II drugs, the human GI characteristics should be incorporated into the in vitro dissolution system to predict bioperformance of BCS class II drugs. An absorptive compartment may be important in dissolution apparatus for BCS class II drugs, especially for bases (BCS IIb) because of high permeability, precipitation and supersaturation...
September 14, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28919383/prediction-of-air-entrapment-in-tableting-an-approximate-solution
#19
Antonios Zavaliangos, Jeffrey M Katz, Dominick Daurio, Michael Johnson, Armen Pirjanian, Fernando Alvarez-Nunez
Αn approximate solution is presented for the prediction of air entrapment during tableting. Assuming weak coupling of the deformation of the solid phase, the flow of interstitial air and a set of reasonable additional geometric assumptions, the general problem is reduced to one dimension. Experimental values of air permeability through tablet specimens of commonly used pharmaceutical excipients were obtained using a 3D printed test cell outfitted to a powder rheometer. Using these values, combined with a numerical solution of the governing partial differential equation, parametric studies are presented that demonstrate the importance of permeability, compaction speed, tablet size, and punch-die tolerance on air entrapment...
September 14, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28919099/development-of-an-abiraterone-acetate-formulation-with-improved-oral-bioavailability-guided-by-absorption-modeling-based-on-in-vitro-dissolution-and-permeability-measurements
#20
Tamás Solymosi, Zsolt Ötvös, Réka Angi, Betti Ordasi, Tamás Jordán, Sándor Semsey, László Molnár, Soma Ránky, Genovéva Filipcsei, Gábor Heltovics, Hristos Glavinas
Particle size reduction of drug crystals in the presence of surfactants (often called "top-down" production methods) is a standard approach used in the pharmaceutical industry to improve bioavailability of poorly soluble drugs. Based on the mathematical model used to predict the fraction dose absorbed this formulation approach is successful when dissolution rate is the main rate limiting factor of oral absorption. In case compound solubility is also a major factor this approach might not result in an adequate improvement in bioavailability...
September 15, 2017: International Journal of Pharmaceutics
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