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https://www.readbyqxmd.com/read/28538688/in-silico-study-and-bioprospection-of-the-antibacterial-and-antioxidant-effects-of-flavone-and-its-hydroxylated-derivatives
#1
Camila de Albuquerque Montenegro, Gregório Fernandes Gonçalves, Abrahão Alves de Oliveira Filho, Andressa Brito Lira, Thays Thyara Mendes Cassiano, Natanael Teles Ramos de Lima, José Maria Barbosa-Filho, Margareth de Fátima Formiga Melo Diniz, Hilzeth Luna Freire Pessôa
Flavonoid compounds are widely used as natural protective species, which can act as anti-inflammatory, antioxidant, anticoagulant, antihypertensive and antitumor agents. This study set out to investigate the probable pharmacological activities, along with the antibacterial and antioxidant effects, of flavone and its hydroxy derivatives: 3-hydroxyflavone, 5-hydroxyflavone and 6-hydroxyflavone. To do so, we investigated their pharmacological characteristics, using in silico tests that indicate likelihood of activity or inactivity, with the PASS online software, and the antimicrobial potential against Gram positive and Gram negative bacteria was also analyzed, including bacteria of clinical importance...
May 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28538152/apoptotic-bax-at-oxidatively-stressed-mitochondrial-membranes-lipid-dynamics-and-permeabilization
#2
Artur Peter Günther Dingeldein, Šárka Pokorná, Martin Lidman, Tobias Sparrman, Radek Šachl, Martin Hof, Gerhard Gröbner
Mitochondria are crucial compartments of eukaryotic cells because they function as the cellular power plant and play a central role in the early stages of programmed cell death (apoptosis). To avoid undesired cell death, this apoptotic pathway is tightly regulated by members of the Bcl-2 protein family, which interact on the external surface of the mitochondria, i.e., the mitochondrial outer membrane (MOM), and modulate its permeability to apoptotic factors, controlling their release into the cytosol. A growing body of evidence suggests that the MOM lipids play active roles in this permeabilization process...
May 23, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28537927/wx-132-18b-a-novel-microtubule-inhibitor-exhibits-promising-anti-tumor-effects
#3
Fang Guan, Rui Ding, Qi Zhang, Wei Chen, Feifei Li, Long Long, Wei Li, Linna Li, Dexuan Yang, Lan Xie, Shoujun Yuan, Lili Wang
Cancer drug researchers have been seeking microtubule-inhibiting agents (MIAs) with higher bioactivity and lower toxicity than currently marketed drugs. WX-132-18B, a novel structural compound synthesized at our institute, specifically bound to the colchicine-binding site on tubulin rather than the vinblastine site, and concentration-dependently reduced microtubule content via depolymerization. It exhibited the same cellular phenotypic profiles as the classic MIAs (colchicine, vincristine, and taxol), including inducing cell cycle arrest at the G2/M phase, triggering tumor cell apoptosis, promoting nuclear membrane permeability, reducing mitochondrial membrane potential, and disrupting the redox system balance...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28535500/transient-receptor-potential-vanilloid-5-mediates-ca2-influx-and-inhibits-chondrocyte-autophagy-in-a-rat-osteoarthritis-model
#4
Yingliang Wei, Yanfang Wang, Yutong Wang, Lunhao Bai
BACKGROUND: Autophagy, a self-protective mechanism of chondrocytes, has become a promising target to impede the progress of osteoarthritis (OA). Autophagy is regulated by cytosolic Ca2+ activity and may thus be modified by the Ca2+ permeable transient receptor potential channel vanilloid 5 (TRPV5). Therefore, we investigated the potential role of TRPV5 in mediating Ca2+ influx and in inhibiting chondrocyte autophagy in a rat OA model. METHODS: The rat OA model was assessed by macroscopic and histological analyses...
May 25, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28535433/a-highly-selective-surface-coating-for-enhanced-membrane-rejection-of-endocrine-disrupting-compounds-mechanistic-insights-and-implications
#5
Hao Guo, Yu Deng, Zhikan Yao, Zhe Yang, Jianqiang Wang, Chuner Lin, Tong Zhang, Baoku Zhu, Chuyang Y Tang
We designed a highly selective surface coating to achieve enhanced rejection of endocrine disrupting compounds (EDCs) by nanofiltration membranes. A commercial NF90 membrane was first coated with polydopamine (PDA) followed by in situ immobilization of silver nanoparticles (AgNPs). This PDA/AgNPs coating greatly improved EDC rejection at the expense of slight water permeability loss (4-10%). This improvement in rejection can be attributed to a combination of enhanced size exclusion and suppressed hydrophobic interaction...
May 18, 2017: Water Research
https://www.readbyqxmd.com/read/28535336/transport-of-the-glucosamine-derived-browning-product-fructosazine-polyhydroxyalkylpyrazine-across-the-human-intestinal-caco-2-cell-monolayer-role-of-the-hexose-transporters
#6
Abhishek Bhattacherjee, Yuliya Hrynets, Mirko Betti
The transport mechanism of fructosazine, a glucosamine self-condensation product, was investigated using a Caco-2 cell model. Fructosazine transport was assessed by measuring the bidirectional permeability coefficient across Caco-2 cells. The mechanism of transport was evaluated using phlorizin, an inhibitor of sodium-dependent glucose cotransporters (SGLT) 1 and 2, phloretin and quercetin, an inhibitors of glucose transporters (GLUT) 1 and 2, transcytosis inhibitor wortmannin, and gap junction disruptor cytochalasin D...
May 23, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28535125/preparation-and-characterization-of-adefovir-dipivoxil-stearic-acid-cocrystal-with-enhanced-physicochemical-properties
#7
Jeong-Woong Seo, Kyu-Min Hwang, Sung-Hoon Lee, Dong-Wook Kim, Eun-Seok Park
The objectives of this study were to prepare cocrystal composed of adefovir dipivoxil (AD) and stearic acid (SA) and to investigate the enhanced properties of the cocrystal. The cocrystal was prepared by antisolvent precipitation and characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC). The enhanced properties were evaluated by dissolution testing, permeability studies, and powder rheology analysis...
May 23, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28535068/a-conformal-lithium-fluoride-protection-layer-on-three-dimensional-lithium-by-non-hazardous-gaseous-reagent-freon
#8
Dingchang Lin, Yayuan Liu, Wei Chen, Guangmin Zhou, Kai Liu, Bruce S Dunn, Yi Cui
Research on lithium (Li) metal chemistry has been rapidly gaining momentum nowadays not only because of the appealing high theoretical capacity, but also its indispensable role in the next-generation Li-S and Li-air batteries. However, two root problems of Li metal, namely high reactivity and infinite relative volume change during cycling, bring about numerous other challenges that impede its practical applications. In the past, extensive studies have targeted these two root causes by either improving interfacial stability or constructing a stable host...
May 23, 2017: Nano Letters
https://www.readbyqxmd.com/read/28535030/sulfonated-holey-graphene-oxide-shgo-filled-sulfonated-poly-ether-ether-ketone-membrane-the-role-of-holes-in-the-shgo-in-improving-its-performance-as-proton-exchange-membrane-for-direct-methanol-fuel-cells
#9
Zhong-Jie Jiang, Zhongqing Jiang, Xiaoning Na Tian, Lijuan Luo, Meilin Liu
Sulfonated holey graphene oxides (SHGOs) have synthesized by the etching of sulfonated graphene oxides with concentrated HNO3 under the assistance of ultrasonication. These SHGOs could be used as the fillers for the sulfonated aromatic poly(ether ether ketone) (SPEEK) membrane. The obtained SHGO incorporated SPEEK membrane has a uniform and dense structure, exhibiting the higher performance as proton exchange membranes (PEMs), for instance, higher proton conductivity, lower activation energy for proton conduction, and comparable methanol permeability, as compared to Nafion® 112...
May 23, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28534850/exploration-of-the-esophageal-mucosal-barrier-in-non-erosive-reflux-disease
#10
Nicolaas F Rinsma, Ricard Farré, Fred J Troost, Montserrat Elizalde, Daniel Keszthelyi, Zsuzsanna Helyes, Ad A Masclee, José M Conchillo
In the absence of visible mucosal damage, it is hypothesized that the esophageal mucosal barrier is functionally impaired in patients with non-erosive reflux disease (NERD). The aim of the present study was to perform an exploratory analysis of the mucosal barrier in NERD compared to erosive esophagitis (EE) and controls. A second aim was to explore TRPV1 gene transcription in relation to the mucosal barrier function and heartburn symptoms. In this prospective study, 10 NERD patients, 11 patients with active erosive esophagitis and 10 healthy volunteers were included...
May 19, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28534826/atp-driven-contraction-of-phage-t3-capsids-with-dna-incompletely-packaged-in-vivo
#11
Philip Serwer, Elena T Wright
Adenosine triphosphate (ATP) cleavage powers packaging of a double-stranded DNA (dsDNA) molecule in a pre-assembled capsid of phages that include T3. Several observations constitute a challenge to the conventional view that the shell of the capsid is energetically inert during packaging. Here, we test this challenge by analyzing the in vitro effects of ATP on the shells of capsids generated by DNA packaging in vivo. These capsids retain incompletely packaged DNA (ipDNA) and are called ipDNA-capsids; the ipDNA-capsids are assumed to be products of premature genome maturation-cleavage...
May 19, 2017: Viruses
https://www.readbyqxmd.com/read/28534662/neuroprotection-of-brain-permeable-iron-chelator-vk-28-against-intracerebral-hemorrhage-in-mice
#12
Qian Li, Jieru Wan, Xi Lan, Xiaoning Han, Zhongyu Wang, Jian Wang
Iron overload plays a key role in the secondary brain damage that develops after intracerebral hemorrhage (ICH). The significant increase in iron deposition is associated with the generation of reactive oxygen species (ROS), which leads to oxidative brain damage. In this study, we examined the protective effects of VK-28, a brain-permeable iron chelator, against hemoglobin toxicity in an ex vivo organotypic hippocampal slice culture (OHSC) model and in middle-aged mice subjected to an in vivo, collagenase-induced ICH model...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/28534300/formulation-and-evaluation-of-naringenin-nanosuspensions-for-bioavailability-enhancement
#13
Sonia Gera, Sreekanth Talluri, Nagarjun Rangaraj, Sunitha Sampathi
The clinical potential of naringenin (NRG) is compromised due to its poor aqueous solubility and low oral bioavailability. The study is aimed at addressing these issues by means of naringenin nanosuspensions (NRG-NS) formulated using polyvinylpyrrolidone (PVP K-90) as stabiliser via antisolvent sonoprecipitation method. Optimisation of sonication time, drug concentration and stabilisers was done based on particle size. Characterisation of pure NRG and NRG-NS was carried out by scanning electron microscopy, differential scanning calorimetry (DSC), x-ray powder diffractometry (XRD) and Fourier transform infrared spectroscopy (FTIR)...
May 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28534288/physicochemical-and-biological-characterization-of-sustained-isopropyl-unoprostone-release-device-made-of-poly-ethyleneglycol-dimethacrylates
#14
Nobuhiro Nagai, Yasuko Izumida, Yoshimasa Yamazaki, Hirokazu Kaji, Junichi Kawasaki, Matsuhiko Nishizawa, Toshiaki Abe
Transscleral drug delivery is becoming increasingly popular to manage posterior eye diseases. To evaluate the clinical application of a transscleral, sustained, unoprostone (UNO)-release device (URD) constructed of photopolymerized tri(ethyleneglycol) dimethacrylate and poly(ethyleneglycol) dimethacrylate, we evaluated physicochemical and biological properties of this device. The URD consists of a drug-impermeable reservoir and a semi-permeable cover. The in vitro release rate of UNO from the URD increased with increasing temperatures from 20 to 45 °C...
July 2017: Journal of Materials Science. Materials in Medicine
https://www.readbyqxmd.com/read/28534140/protective-effects-of-neural-crest-derived-stem-cell-conditioned-media-against-ischemia-reperfusion-induced-lung-injury-in-rats
#15
Chung-Kan Peng, Shu-Yu Wu, Shih-En Tang, Min-Hui Li, Shih-Shiuan Lin, Shi-Jye Chu, Kun-Lun Huang
Current treatments for ischemia-reperfusion (IR)-induced acute lung injury are limited. Mesenchymal stem cell-conditioned medium (CM) has been reported to attenuate lung injury. Neural crest stem cells (NCSCs), a type of multipotent stem cells, are more easily obtained than mesenchymal stem cells. We hypothesize that NCSC-CM has anti-inflammatory properties that could protect against IR-induced lung injury in rats. In this study, NCSC-CM was derived from rat NCSCs. Typical acute lung injury was induced by 30-min ischemia followed by 90-min reperfusion in adult male Sprague-Dawley rats...
May 23, 2017: Inflammation
https://www.readbyqxmd.com/read/28534026/how-cells-can-control-their-size-by-pumping-ions
#16
Alan R Kay
The ability of all cells to set and regulate their size is a fundamental aspect of cellular physiology. It has been known for sometime but not widely so, that size stability in animal cells is dependent upon the operation of the sodium pump, through the so-called pump-leak mechanism (Tosteson and Hoffman, 1960). Impermeant molecules in cells establish an unstable osmotic condition, the Donnan effect, which is counteracted by the operation of the sodium pump, creating an asymmetry in the distribution of Na(+) and K(+) staving off water inundation...
2017: Frontiers in Cell and Developmental Biology
https://www.readbyqxmd.com/read/28533987/exoskeleton-may-influence-the-internal-body-temperatures-of-neotropical-dung-beetles-col-scarabaeinae
#17
Valentina Amore, Malva I M Hernández, Luis M Carrascal, Jorge M Lobo
The insect exoskeleton is a multifunctional coat with a continuum of mechanical and structural properties constituting the barrier between electromagnetic waves and the internal body parts. This paper examines the ability of beetle exoskeleton to regulate internal body temperature considering its thermal permeability or isolation to simulated solar irradiance and infrared radiation. Seven Neotropical species of dung beetles (Coleoptera, Scarabaeinae) differing in colour, surface sculptures, size, sexual dimorphism, period of activity, guild category and altitudinal distribution were studied...
2017: PeerJ
https://www.readbyqxmd.com/read/28533908/ascites-refractory-ascites-and-hyponatremia-in-cirrhosis
#18
Brett Fortune, Andres Cardenas
Ascites is the most common complication related to cirrhosis and is associated with increased morbidity and mortality. Ascites is a consequence of the loss of compensatory mechanisms to maintain the overall effective arterial blood volume due to worsening splanchnic arterial vasodilation as a result of clinically significant portal hypertension. In order to maintain effective arterial blood volume, vasoconstrictor and antinatriuretic pathways are activated, which increase overall sodium and fluid retention...
May 2017: Gastroenterology Report
https://www.readbyqxmd.com/read/28533680/preparation-characterization-and-in-vitro-vivo-studies-of-oleanolic-acid-loaded-lactoferrin-nanoparticles
#19
Xiaojing Xia, Haowei Liu, Huixia Lv, Jing Zhang, Jianping Zhou, Zhiying Zhao
Oleanolic acid (OA), a pentacyclic triterpene, is used to safely and economically treat hepatopathy. However, OA, a Biopharmaceutics Classification System IV category drug, has low bioavailability owing to low solubility (<1 μg/mL) and biomembrane permeability. We developed a novel OA nanoparticle (OA-NP)-loaded lactoferrin (Lf) nanodelivery system with enhanced in vitro OA dissolution and improved oral absorption and bioavailability. The OA-NPs were prepared using NP albumin-bound technology and characterized using dynamic light scattering, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro dissolution test...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28533410/correction-for-lucotte-et-al-direct-visualization-of-the-arterial-wall-water-permeability-barrier-using-cars-microscopy
#20
(no author information available yet)
No abstract text is available yet for this article.
May 22, 2017: Proceedings of the National Academy of Sciences of the United States of America
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