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https://www.readbyqxmd.com/read/28545253/encapsulation-of-the-antioxidant-r-%C3%AE-lipoic-acid-in-permethylated-%C3%AE-and-%C3%AE-cyclodextrins-thermal-and-x-ray-structural-characterization-of-the-1-1-inclusion-complexes
#1
Mino R Caira, Susan A Bourne, Buntubonke Mzondo
The naturally occurring compound α-lipoic acid (ALA) is implicated in manifold critical biological roles and its potent antioxidant properties and potential for treatment of various diseases have led to its widespread use as a dietary supplement. However, shortcomings of poor aqueous solubility and low thermal stability have hampered its development as a medicinal agent, prompting the use of cyclodextrins (CDs) to address these problems. The paucity of published structural data on the nature of the interactions between ALA and CDs motivated the present study, which describes the synthesis and X-ray structural elucidation of crystalline inclusion complexes between the biologically relevant R-(+)-α-lipoic acid (RALA) and the host molecules permethylated α-CD (TMA) and permethylated β-CD (TMB)...
May 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28544982/an-evaluation-of-minor-groove-binders-as-anti-fungal-and-anti-mycobacterial-therapeutics
#2
Fraser J Scott, Ryan J O Nichol, Abedawn I Khalaf, Federica Giordani, Kirsten Gillingwater, Soumya Ramu, Alysha Elliott, Johannes Zuegg, Paula Duffy, Michael-Jon Rosslee, Lerato Hlaka, Santosh Kumar, Mumin Ozturk, Frank Brombacher, Michael Barrett, Reto Guler, Colin J Suckling
This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGBs that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MIC80s of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MIC99s of 3...
May 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28544807/effects-of-teriparatide-on-joint-erosions-in-rheumatoid-arthritis-a-randomized-controlled-trial
#3
D H Solomon, J Kay, J Duryea, B Lu, M B Bolster, R A Yood, R Han, S Ball, C Coleman, E Lo, A Wohlfahrt, M Sury, M Yin, Z Yu, A Zak, E M Gravallese
BACKGROUND: Articular erosions correlate with disability in rheumatoid arthritis (RA). Biologic treatments for RA reduce erosion progression, but erosion healing occurs infrequently. The goal of this study was to assess the effects of the anabolic agent teriparatide on joint erosion volume in RA patients treated with a tumor necrosis factor inhibitor (TNFi). METHODS: We conducted a randomized controlled trial in 24 patients with erosive RA, osteopenia, and disease activity controlled on a TNFi for at least three months...
May 23, 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/28544675/cyclotides-overview-and-biotechnological-applications
#4
REVIEW
Andrew Gould, Julio A Camarero
Cyclotides are globular microproteins with a unique head-to-tail cyclized backbone, stabilized by three disulfide bonds forming a cystine knot. This unique circular backbone topology and knotted arrangement of three disulfide bonds makes them exceptionally stable to chemical, thermal, and biological degradation compared to other peptides of similar size. In addition, cyclotides have been shown to be highly tolerant to sequence variability, aside from the conserved residues forming the cystine knot. Cyclotides can also cross cellular membranes and are able to modulate intracellular protein-protein interactions, both in vitro and in vivo...
May 24, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28544648/effects-of-a-web-based-patient-decision-aid-on-biologic-and-small-molecule-agents-for-rheumatoid-arthritis-answer-2-a-proof-of-concept-study
#5
Linda C Li, Chris Shaw, Diane Lacaille, Elaine Yacyshyn, C Allyson Jones, Cheryl Koehn, Alison M Hoens, Jasmina Geldman, Eric C Sayre, Graham Macdonald, Jenny Leese, Nick Bansback
OBJECTIVES: To assess the extent to which ANSWER-2, an interactive online patient decision aid, reduces patients' decisional conflict and improves their medication-related knowledge and self-management capacity. METHODS: We used a pre-post study design. Eligible participants had a diagnosis of rheumatoid arthritis (RA), had been recommended to start using a biologic or small molecule agent or to switch to a new one, and had Internet access. Access to ANSWER-2 was provided immediately after enrollment...
May 23, 2017: Arthritis Care & Research
https://www.readbyqxmd.com/read/28544643/adaptations-to-endurance-training-depend-on-exercise-induced-oxidative-stress-exploiting-redox-inter-individual-variability
#6
Nikos V Margaritelis, Anastasios A Theodorou, Vassilis Paschalis, Aristidis S Veskoukis, Konstantina Dipla, Andreas Zafeiridis, George Panayiotou, Ioannis S Vrabas, Antonios Kyparos, Michalis G Nikolaidis
AIM: The aim of the present study was to reveal the role of reactive oxygen and nitrogen species (RONS) in exercise adaptations under physiological in vivo conditions and without the interference from other exogenous redox agents (e.g., a pro-oxidant or antioxidant). METHODS: We invented a novel methodological set-up that exploited the large redox inter-individual variability in exercise responses. More specifically, we used exercise-induced oxidative stress as the "classifier" measure (i...
May 24, 2017: Acta Physiologica
https://www.readbyqxmd.com/read/28544497/cell-tracking-using-gold-nanoparticles-and-computed-tomography-imaging
#7
REVIEW
Rinat Meir, Rachela Popovtzer
Cell-based therapies utilize transplantation of living cells with therapeutic traits to alleviate numerous diseases and disorders. The use of such biological agents is an attractive alternative for diseases that existing medicine cannot effectively treat. Although very promising, translating cell therapy to the clinic has proven to be challenging, due to inconsistent results in preclinical and clinical studies. To examine the underlying cause for these inconsistencies, it is crucial to noninvasively monitor the accuracy of cell injection, and cell survival and migration patterns...
May 24, 2017: Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology
https://www.readbyqxmd.com/read/28544494/4-substituted-thieno-2-3-d-pyrimidines-as-potent-antibacterial-agents-rational-design-microwave-assisted-synthesis-biological-evaluation-and-molecular-docking-studies
#8
Rupinder K Gill, Harpreet Singh, Tilak Raj, Anuradha Sharma, Gagandeep Singh, Jitender Bariwal
In an attempt to discover a new class of antibacterial agents with improved efficacy and to overcome the drug resistant problems, some novel 4-substituted thieno[2,3-d]pyrimidines have been synthesized via microwave assisted methodology and evaluated for their in vitro antibacterial activity against various pathogenic bacterial strains. Compounds 12b and 13c showed the promising inhibitory potencies against S. aureus, B. subtilis, P. aeruginosa and E. coli with MICs ranging from 2 to 10 μg/ml. Compound 13c was also found to be highly potent against methicillin resistant S...
May 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28543820/design-synthesis-and-biological-evaluation-of-coumarin-triazole-hybrid-molecules-as-potential-antitumor-and-pancreatic-lipase-agents
#9
Bahittin Kahveci, Fatih Yılmaz, Emre Menteşe, Serdar Ülker
The design, synthesis, and investigation of antitumor and anti-lipase activities of some coumarin-triazole hybrid molecules are reported. The synthesis of these hybrid molecules was performed under microwave irradiation and conventional heating procedures. The newly synthesized hybrid molecules were investigated as inhibitors against four tumor cell lines (BT20 human breast carcinoma, SK-Mel 128 melanoma, DU-145 prostate carcinoma, and A549 lung carcinoma) and porcine pancreatic lipase (PPL). Most of these compounds showed notable antitumor activities against the tested tumor cell lines, and compounds 8i and 8l showed the best anti-lipase activity of 99...
May 22, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28543738/crispr-editing-in-biological-and-biomedical-investigation
#10
Xing-Da Ju, Jing Xu, Zhong Sheng Sun
The CRISPR (clustered regularly interspaced short palindromic repeat)-Cas (CRISPR--associated protein) system, a prokaryotic RNA-based adaptive immune system against viral infection, is emerging as a powerful genome editing tool in broad research areas. To further improve and expand its functionality, various CRISPR delivery strategies have been tested and optimized, and key CRISPR system components such as Cas protein have been engineered with different purposes. Benefiting from more in-depth understanding and further development of CRISPR, versatile CRISPR-based platforms for genome editing have been rapidly developed to advance investigations in biology and biomedicine...
May 20, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28543443/structural-review-of-ppar%C3%AE-in-complex-with-ligands-cartesian-and-dihedral-angle-principal-component-analyses-of-x-ray-crystallographic-data
#11
Åsmund Kaupang, Tuomo Laitinen, Antti Poso, Trond Vidar Hansen
Two decades of research into the ligand-dependent modulation of the activity of the peroxisome proliferator-activated receptor γ (PPARγ) have demonstrated the heterogeneous modes of action of PPARγ ligands, in terms of their interaction surfaces in the ligand-binding pocket, binding stoichiometry and ability to interact with functionally important parts of the receptor, through both direct and allosteric mechanisms. These findings signal the complex mechanistic bases of the distinct biological effects of different classes of PPARγ ligands...
May 24, 2017: Proteins
https://www.readbyqxmd.com/read/28542193/an-agent-based-model-of-leukocyte-transendothelial-migration-during-atherogenesis
#12
Rita Bhui, Heather N Hayenga
A vast amount of work has been dedicated to the effects of hemodynamics and cytokines on leukocyte adhesion and trans-endothelial migration (TEM) and subsequent accumulation of leukocyte-derived foam cells in the artery wall. However, a comprehensive mechanobiological model to capture these spatiotemporal events and predict the growth and remodeling of an atherosclerotic artery is still lacking. Here, we present a multiscale model of leukocyte TEM and plaque evolution in the left anterior descending (LAD) coronary artery...
May 2017: PLoS Computational Biology
https://www.readbyqxmd.com/read/28541831/genotoxicity-and-antigenotoxicity-assessments-of-the-flavonoid-vitexin-by-the-drosophila-melanogaster-somatic-mutation-and-recombination-test
#13
Liliane Menezes Fernandes, Zaira da Rosa Guterres, Igor Vivian Almeida, Veronica Elisa Pimenta Vicentini
Vitexin is a C-glycosylated flavone found in various medicinal plants with several proven biological properties such as anti-inflammatory, antispasmodic, antimicrobial, cytotoxic, and antioxidant activities. Considering that the human population consumes many foods that contain this flavonoid, the objective of this study was to investigate the genotoxic and the antigenotoxic potentials of vitexin by the SMART (Somatic Mutation and Recombination Test) in Drosophila melanogaster wings, in vivo. To evaluate the genotoxic activity, larvae obtained from standard (ST) and high bioactivation (HB) crosses were chronically treated with different concentrations of vitexin (0...
May 25, 2017: Journal of Medicinal Food
https://www.readbyqxmd.com/read/28541488/the-role-of-il-12-23-in-t-cell-related-chronic-inflammation-implications-of-immunodeficiency-and-therapeutic-blockade
#14
Anna Schurich, Charles Raine, Vanessa Morris, Coziana Ciurtin
In this review we discuss the divergent role of two closely related cytokines, IL-12 and IL-23, in shaping immune responses. In light of current therapeutic developments using biologic agents to block these two pathways, a better understanding of the immunological function of these cytokines is pivotal.
May 24, 2017: Rheumatology
https://www.readbyqxmd.com/read/28541144/in-vitro-characterization-of-a-formulation-of-butorphanol-tartrate-in-a-poloxamer-407-base-intended-for-use-as-a-parenterally-administered-slow-release-analgesic-agent
#15
Delphine Laniesse, Dale A Smith, Heather K Knych, Cornelia Mosley, David Sanchez-Migallon Guzman, Hugues Beaufrère
OBJECTIVE To assess rheological properties and in vitro diffusion of poloxamer 407 (P407) and butorphanol-P407 (But-P407) hydrogels and to develop a sustained-release opioid formulation for use in birds. SAMPLE P407 powder and a commercially available injectable butorphanol tartrate formulation (10 mg/mL). PROCEDURES P407 and But-P407 gels were compounded by adding water or butorphanol to P407 powder. Effects of various concentrations of P407 (20%, 25% and 30% [{weight of P407/weight of diluent} × 100]), addition of butorphanol, and sterilization through a microfilter on rheological properties of P407 were measured by use of a rheometer...
June 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28540805/the-in-vivo-performance-of-a-novel-thermal-accelerant-agent-used-for-augmentation-of-microwave-energy-delivery-within-biologic-tissues-during-image-guided-thermal-ablation-a-porcine-study
#16
William Keun Chan Park, Aaron Wilhelm Palmer Maxwell, Victoria Elizabeth Frank, Michael Patrick Primmer, Jarod Brian Paul, Scott Andrew Collins, Kara Anne Lombardo, Shaolei Lu, Tiffany Marie Borjeson, Grayson Luderman Baird, Damian Edward Dupuy
OBJECTIVES: To investigate the effects of a novel caesium-based thermal accelerant (TA) agent on ablation zone volumes following in vivo microwave ablation of porcine liver and skeletal muscle, and to correlate the effects of TA with target organ perfusion. MATERIALS AND METHODS: This prospective study was performed following institutional animal care and use committee approval. Microwave ablation was performed in liver and resting skeletal muscle in eight Sus scrofa domesticus swine following administration of TA at concentrations of 0 mg/mL (control), 100 mg/mL and 250 mg/mL...
April 24, 2017: International Journal of Hyperthermia
https://www.readbyqxmd.com/read/28540751/treatment-of-adult-onset-still-s-disease-up-to-date
#17
Dae Hyun Yoo
Adult onset Still's disease (AOSD) is a systemic inflammatory disorder of unknown etiology, and approximately 60-70% of patients may develop a chronic polyphasic form of the disease or a chronic polyarthritis. Due to rarity of disease, treatment of AOSD is not based on controlled study, but on case based experiences. Recently, the application of anti-cytokine therapy based on pathophysiology has resulted in significant progress in the treatment of AOSD. Here, we review current knowledge of the pathogenesis, disease progression, currently available biomarkers of disease activity, standard therapeutic agents, utility of biologic agents, future perspectives for treatment and treatment of macrophage activation syndrome...
May 25, 2017: Expert Review of Clinical Immunology
https://www.readbyqxmd.com/read/28540646/the-molecular-mechanism-of-glucagon-like-peptide-1-therapy-in-alzheimer-s-disease-based-on-a-mechanistic-target-of-rapamycin-pathway
#18
Lin Li
The mechanistic target of rapamycin (mTOR) is an important molecule that connects aging, lifespan, energy balance, glucose and lipid metabolism, and neurodegeneration. Rapamycin exerts effects in numerous biological activities via its target protein, playing a key role in energy balance, regulation of autophagy, extension of lifespan, immunosuppression, and protection against neurodegeneration. There are many similar pathophysiological processes and molecular pathways between Alzheimer's disease (AD) and type 2 diabetes mellitus (T2DM), and pharmacologic agents used to treat T2DM, including glucagon-like peptide-1 (GLP-1) analogs, seem to be beneficial for AD...
May 24, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28540607/treatment-response-to-etanercept-in-methotrexate-refractory-juvenile-idiopathic-arthritis-an-analysis-of-predictors-and-long-term-outcomes
#19
Yueh Su, Yao-Hsu Yang, Bor-Luen Chiang
The aim of the study is to evaluate the long-term outcomes, predictors, and the role of inflammatory cytokines in methotrexate (MTx) refractory juvenile idiopathic arthritis (JIA) patients. This is a retrospective cohort study. MTx refractory JIA patients who received etanercept as their first biological agent in National Taiwan University Hospital (NTUH) were enrolled. Patients were classified into remission group, non-remission group, relapsing group, and non-relapsing group according to the criteria of disease remission and disease flares defined by Wallace et al...
May 24, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28540590/pediatric-psoriasis
#20
REVIEW
Maria Relvas, Tiago Torres
Psoriasis is a chronic inflammatory systemic disease associated with an important physical and physiological burden. It primarily affects the skin, but it is associated with several serious medical co-morbidities. One third of total psoriatic cases have their onset during the pediatric age, although some of them may not be diagnosed until the patient reaches adulthood. Additionally, in the pediatric age, there is an association with several medical co-morbidities; thus, an early recognition of the disease and a subsequent appropriate approach may delay or even prevent considerable co-morbidities...
May 24, 2017: American Journal of Clinical Dermatology
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