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https://www.readbyqxmd.com/read/29679483/prostaglandin-fp-receptor-antagonists-discovery-pharmacological-characterization-and-therapeutic-utility
#1
REVIEW
Najam A Sharif, Peter G Klimko
In contrast to the availability of potent and selective antagonists of several prostaglandin (PG) receptor types (including DP1 , DP2 , EP, and TP receptors), there has been a paucity of well-characterized, selective FP-receptor antagonists. The earliest ones included dimethyl amide and dimethyl amine derivatives of PGF2α , but these have failed to gain prominence. The fluorinated PGF2α analogs, AL-8810 and AL-3138, were subsequently discovered as competitive and non-competitive FP-receptor antagonists, respectively...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679318/engineering-citric-acid-based-porous-scaffolds-for-bone-regeneration
#2
Jacqueline J Masehi-Lano, Eun Ji Chung
Tissue engineering aims to develop scaffolds that are biocompatible and mimic the mechanical and biological properties of the target tissue as closely as possible. Here, we describe the fabrication and characterization of a biodegradable, elastomeric porous scaffold: poly(1,8-octanediol-co-citric acid) (POC) incorporated with nanoscale hydroxyapatite (HA). While this chapter focuses on the scaffold's potential for bone regeneration, POC can also be used in other tissue engineering applications requiring an elastomeric implant...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29677110/dietary-treatment-of-metabolic-acidosis-in-chronic-kidney-disease
#3
REVIEW
Roswitha Siener
Chronic kidney disease and reduced glomerular filtration rate are risk factors for the development of chronic metabolic acidosis. The prevention or correction of chronic metabolic acidosis has been found to slow progression of chronic kidney disease. Dietary composition can strongly affect acid⁻base balance. Major determinants of net endogenous acid production are the generation of large amounts of hydrogen ions, mostly by animal-derived protein, which is counterbalanced by the metabolism of base-producing foods like fruits and vegetables...
April 20, 2018: Nutrients
https://www.readbyqxmd.com/read/29676577/oxidation-of-acid-base-and-amide-side-chain-amino-acid-derivatives-via-hydroxyl-radical
#4
Jon Uranga, Jon I Mujika, Rafael Grande-Aztatzi, Jon M Matxain
Hydroxyl radical (●OH) is known to be highly reactive. Herein, we analyze the oxidation of acid (Asp and Glu), base (Arg and Lys) and amide (Asn and Gln) containing amino acids by the consecutive attack of two ●OH. In this work we study the reaction pathway by means of density functional theory. The oxidation mechanism is divided into two steps: 1) the first ●OH can abstract a H atom or an electron, leading to a radical amino acid derivative, which is the intermediate of the reaction 2) the second ●OH can abstract another H atom or add itself to the formed radical, rendering the final oxidized products...
April 20, 2018: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/29676158/hierarchical-fau-zif-8-hybrid-materials-as-highly-efficient-acid-base-catalysts-for-aldol-condensation
#5
Duangkamon Suttipat, Wannaruedee Wannapakdee, Thittaya Yutthalekha, Somlak Ittisanronnachai, Thasanaporn Ungpittagul, Khamphee Phomphrai, Sareeya Bureekaew, Chularat Wattanakit
The composite of hierarchical faujasite nanosheets and zeolitic imidazolate framework-8 (Hie-FAU/ZIF-8) has been successfully prepared via a stepwise deposition of ZIF-8 on modified zeolite surfaces. Compared to the direct deposition of MOF on zeolite surfaces, ZIF-8 nanospheres were selectively attached to external surfaces of the MOF ligand-grafted FAU crystals because of the enhancing interaction between zeolite and MOF in the composite. In addition, the degree of surface functionalization can be greatly enhanced due to the presence of hierarchical structures...
April 20, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29675709/acid-base-status-and-its-clinical-implications-in-critically-ill-patients-with-cirrhosis-acute-on-chronic-liver-failure-and-without-liver-disease
#6
Andreas Drolz, Thomas Horvatits, Kevin Roedl, Karoline Rutter, Richard Brunner, Christian Zauner, Peter Schellongowski, Gottfried Heinz, Georg-Christian Funk, Michael Trauner, Bruno Schneeweiss, Valentin Fuhrmann
BACKGROUND: Acid-base disturbances are frequently observed in critically ill patients at the intensive care unit. To our knowledge, the acid-base profile of patients with acute-on-chronic liver failure (ACLF) has not been evaluated and compared to critically ill patients without acute or chronic liver disease. RESULTS: One hundred and seventy-eight critically ill patients with liver cirrhosis were compared to 178 matched controls in this post hoc analysis of prospectively collected data...
April 19, 2018: Annals of Intensive Care
https://www.readbyqxmd.com/read/29674965/development-of-matrix-metalloproteinase-2-inhibitors-for-cardioprotection
#7
Péter Bencsik, Krisztina Kupai, Anikó Görbe, Éva Kenyeres, Zoltán V Varga, János Pálóczi, Renáta Gáspár, László Kovács, Lutz Weber, Ferenc Takács, István Hajdú, Gabriella Fabó, Sándor Cseh, László Barna, Tamás Csont, Csaba Csonka, György Dormán, Péter Ferdinandy
The objective of our present study is to develop novel inhibitors for MMP-2 for acute cardioprotection. In a series of pilot studies, novel substituted carboxylic acid derivatives were synthesized based on imidazole and thiazole scaffolds and then tested in a screeening cascade for MMP inhibition. We found that the MMP-inhibiting effects of imidazole and thiazole carboxylic acid-based compounds are superior in efficacy in comparison to the conventional hydroxamic acid derivatives of the same molecules. Based on these results, a 568-membered focused library of imidazole and thiazole compounds was generated in silico and then the library members were docked to the 3D model of MMP-2 followed by an in vitro medium throughput screening (MTS) based on a fluorescent assay employing MMP-2 catalytic domain...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29674823/efficacy-of-new-irrigating-solution-on-smear-layer-removal-in-apical-third-of-root-canal-a-scanning-electron-microscope-study
#8
Priyanka Himmatrao Patil, Meenal Nitin Gulve, Swapnil Janardan Kolhe, Roshan Mathew Samuel, Gayatri Balasaheb Aher
Aims: The aim of this in vitro study is to evaluate and compare the smear layer removal efficacy of etidronic acid-based irrigating solution with others in the apical third of the root canal. Materials and Methods: Forty human single-rooted mandibular premolar teeth were taken and decoronated to standardize the canal length. After biomechanical preparation, teeth were randomly divided into four groups ( n = 10) and the final irrigation was carried out with tested irrigants...
March 2018: Journal of Conservative Dentistry: JCD
https://www.readbyqxmd.com/read/29674624/brain-and-spinal-cord-injury-repair-by-implantation-of-human-neural-progenitor-cells-seeded-onto-polymer-scaffolds
#9
Jeong Eun Shin, Kwangsoo Jung, Miri Kim, Kyujin Hwang, Haejin Lee, Il-Sun Kim, Bae Hwan Lee, Il-Shin Lee, Kook In Park
Hypoxic-ischemic (HI) brain injury and spinal cord injury (SCI) lead to extensive tissue loss and axonal degeneration. The combined application of the polymer scaffold and neural progenitor cells (NPCs) has been reported to enhance neural repair, protection and regeneration through multiple modes of action following neural injury. This study investigated the reparative ability and therapeutic potentials of biological bridges composed of human fetal brain-derived NPCs seeded upon poly(glycolic acid)-based scaffold implanted into the infarction cavity of a neonatal HI brain injury or the hemisection cavity in an adult SCI...
April 20, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29674134/higher-dietary-acid-load-is-associated-with-higher-likelihood-of-peripheral-arterial-disease-among-american-adults
#10
Mohsen Mazidi, Dimitri P Mikhailidis, Maciej Banach
OBJECTIVE: To explore the association between dietary acid load, potential renal acid load (PRAL) and net endogenous acid production (NEAP), and peripheral arterial disease (PAD) in a national representative sample of American adults. METHODS: The National Health and Nutrition Examination Survey (NHANES) database (for 1999-2002) was used. PAD was diagnosed by ankle brachial index assessment. Analysis of covariance was used to examine adjusted mean of different dietary acid load by PAD status; multivariable logistic regression was used to relate dietary acid load with prevalent PAD...
March 9, 2018: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/29671619/how-to-design-non-essential-amino-acid-based-diet-for-rheumatic-heart-disease-patients
#11
Jing Li, Shanshan An, Xiaoxiao Zhang, Lan Ouyang, Qiuyun Liu
No abstract text is available yet for this article.
January 1, 2018: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/29670349/fabrication-of-a-triptolide-loaded-and-poly-%C3%AE-glutamic-acid-based-amphiphilic-nanoparticle-for-the-treatment-of-rheumatoid-arthritis
#12
Li Zhang, Junli Chang, Yongjian Zhao, Hao Xu, Tengteng Wang, Qiang Li, Lianping Xing, Jing Huang, Yongjun Wang, Qianqian Liang
Triptolide (TP) exhibits immunosuppressive, cartilage-protective and anti-inflammatory effects in rheumatoid arthritis. However, the toxicity of TP limits its widespread use. To decrease the toxic effects, we developed a novel nano-drug carrier system containing TP using poly-γ-glutamic acid-grafted di-tert-butyl L-aspartate hydrochloride (PAT). PAT had an average diameter of 79±18 nm, a narrow polydispersity index (0.18), a strong zeta potential (-32 mV) and a high drug encapsulation efficiency (EE1 =48...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29669838/effects-of-adjuvants-on-hiv-1-envelope-glycoprotein-sosip-trimers-in-vitro
#13
Gabriel Ozorowski, Albert Cupo, Michael Golabek, Michelle LoPiccolo, Thomas A Ketas, Matt Cavallary, Christopher A Cottrell, P J Klasse, Andrew B Ward, John P Moore
Native-like, soluble, recombinant SOSIP trimers of various designs and based on several env genes of human immunodeficiency virus type 1 (HIV-1) are being tested as immunogens in different animal models. These experiments almost always involve co-formulating the trimers with an adjuvant to boost the magnitude of the immune responses. One factor relevant to the choice of an adjuvant is that it should not physically damage the immunogen or impede its ability to present relevant epitopes. As examples, an adjuvant formulation that includes harsh detergents could disrupt the structural integrity of a trimer, and any charged compounds in the formulation could bind to counter-charged regions of the trimer and physically occlude nearby epitopes...
April 18, 2018: Journal of Virology
https://www.readbyqxmd.com/read/29669498/an-indian-desert-shrub-hiran-chabba-farsetia-hamiltonii-royle-exhibits-potent-antioxidant-and-hepatoprotective-effect-against-iron-overload-induced-liver-toxicity-in-swiss-albino-mice
#14
Tapasree Basu, Bipul Kumar, Anil Khushalrao Shendge, Sourav Panja, Heerak Chugh, Hemant K Gautam, Nripendranath Mandal
BACKGROUND: Farsetia hamiltonii Royle, also known as Hiran Chabba grows in desert regions. It is widely used as folk medicine to treat joint pains, diarrhea and diabetes. However, its antioxidant and iron chelation abilities both in vitro and in vivo have not yet been investigated. METHODS: The 70% methanolic extract of F.hamiltonii (FHME) was investigated for its free radical scavenging and iron chelation potential, in vitro. An iron-overload situation was established by intraperitoneal injection of iron-dextran in Swiss albino mice, followed by oral administration of FHME...
April 18, 2018: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29669419/dynamic-behavior-of-rna-nanoparticles-analyzed-by-afm-on-a-mica-air-interface
#15
Sameer Sajja, Morgan Chandler, Dmitry Federov, Wojciech K Kasprzak, Alexander Y Lushnikov, Mathias Viard, Ankit Shah, Dylan Dang, Jared Dahl, Beamlak Worku, Marina A Dobrovolskaia, Alexey Krasnoslobodtsev, Bruce A Shapiro, Kirill A Afonin
RNA is an attractive biopolymer for engineering self-assembling materials suitable for biomedical applications. Previously, programmable hexameric RNA rings were developed for the controlled delivery of up to six different functionalities. To increase the potential for functionalization with little impact on nanoparticle topology, we introduce gaps into the double-stranded regions of the RNA rings. Molecular dynamic simulations are used to assess the dynamic behavior and the changes in the flexibility of novel designs...
April 18, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/29668565/the-effects-of-genetic-3-mercaptopyruvate-sulfurtransferase-deficiency-in-murine-traumatic-hemorrhagic-shock
#16
Michael Gröger, Martin Wepler, Ulrich Wachter, Tamara Merz, Oscar McCook, Sandra Kress, Britta Lukaschewski, Sebastian Hafner, Markus Huber-Lang, Enrico Calzia, Michael Georgieff, Noriyuki Nagahara, Csaba Szabó, Peter Radermacher, Clair Hartmann
INTRODUCTION: Hemorrhagic shock is a major cause of death after trauma. An additional blunt chest trauma independently contributes to mortality upon the development of an acute lung injury (ALI) by aggravating pathophysiological consequences of hemorrhagic shock. The maintenance of hydrogen sulfide availability is known to play an important role during hemorrhage and ALI. We therefore tested the impact of a genetic 3-mercaptopyruvate sulfurtransferase mutation (Δ3-MST) in a resuscitated murine model of traumatic-hemorrhagic shock...
April 17, 2018: Shock
https://www.readbyqxmd.com/read/29667915/chronic-lithium-treatment-induces-novel-patterns-of-pendrin-localization-and-expression
#17
Nathaniel J Himmel, Yirong Wang, Daniel A Rodriguez, Michael A Sun, Mitsi A Blount
Prolonged lithium treatment is associated with various renal side effects and is known to induce inner medullary collecting duct (IMCD) remodeling. In animals treated with lithium, the fraction of intercalated cells (ICs), which are responsible for acid-base homeostasis, increases as compared to renal principal cells (PCs). In order to investigate the intricacies of lithium-induced IMCD remodeling, male Sprague Dawley rats were fed a lithium-enriched diet for 0,1, 2, 3, 6, 9, or 12 weeks. Urine osmolality was decreased at 1 week, and from 2-12 weeks, animals were severely polyuric...
April 18, 2018: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29667395/benzothiazole-based-aiegen-with-tunable-excited-state-intramolecular-proton-transfer-esipt-and-restricted-intramolecular-rotation-rir-processes-for-highly-sensitive-physiological-ph-sensing
#18
Kai Li, Qi Feng, Guangle Niu, Weijie Zhang, Yuanyuan Li, Miaomiao Kang, Kui Xu, Juan He, Hongwei Hou, Ben Zhong Tang
In this work, a benzothiazole-based aggregation-induced emission luminogen (AIEgen) of 2-(5-(4-carboxyphenyl)-2-hydroxyphenyl)benzothiazole (3) was designed and synthesized, which exhibited multi-fluorescence emissions in different dispersed or aggregated state based on tunable excited-state intramolecular proton transfer (ESIPT) and restricted intramolecular rotation (RIR) processes. 3 was successfully used as a ratiometric fluorescent chemosensor for the detection of pH, which exhibited reversible acid/base-switched yellow/cyan emission transition...
April 18, 2018: ACS Sensors
https://www.readbyqxmd.com/read/29665554/inhibition-by-non-steroidal-anti-inflammatory-drugs-of-compound-action-potentials-in-frog-sciatic-nerve-fibers
#19
Rika Suzuki, Tsugumi Fujita, Kotaro Mizuta, Eiichi Kumamoto
AIMS: Although antinociception produced by non-steroidal anti-inflammatory drugs (NSAIDs) is partly attributed to nerve conduction inhibition, this has not been thoroughly examined yet. The aim of the present study was to reveal quantitatively how various types of NSAIDs affect compound action potentials (CAPs), a measure of nerve conduction. MAIN METHODS: CAPs were recorded from the frog sciatic nerve by using the air-gap method. KEY FINDINGS: Soaking the sciatic nerve with acetic acid-based NSAIDs (diclofenac and aceclofenac) reduced the peak amplitude of CAP in a concentration-dependent manner; their IC50 values were 0...
April 14, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29664420/controlled-release-of-18-%C3%AE-glycyrrhetic-acid-by-nanodelivery-systems-increases-cytotoxicity-on-oral-carcinoma-cell-line
#20
Ilaria Cacciotti, Laura Chronopoulou, Cleofe Palocci, Adriana Amalfitano, Monica Cantiani, Massimo Cordaro, Carlo Lajolo, Cinzia Callà, Alma Boninsegna, Donatella Lucchetti, Patrizia Gallenzi, Alessandro Sgambato, Giuseppina Nocca, Alessandro Arcovito
The topical treatment for oral mucosal diseases is often based on products optimized for dermatologic applications; consequently, a lower therapeutic effect may be present.
 18-β-Glycyrrhetic Acid (GA) is extracted from Glycirrhiza glabra. The first aim of this study was to test the cytotoxicity of GA on PE/CA-PJ15 cells. The second aim was to propose and test two different delivery systems, i.e. nanoparticles and fibers, to guarantee a controlled release of GA in vitro. We used chitosan and poly(lactic-co-glycolic) acid based nanoparticles and polylactic acid fibers...
April 17, 2018: Nanotechnology
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