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https://www.readbyqxmd.com/read/28812524/biologically-important-hydrazide-containing-fused-azaisocytosines-as-antioxidant-agents
#1
Małgorzata Sztanke, Krzysztof Sztanke
OBJECTIVES: Two important classes of hydrazide-containing fused azaisocytosines were evaluated as possible antioxidants and characterised by UV spectroscopy. METHODS: 2,2-Diphenyl-1-picrylhydazyl (DPPH), nitric oxide (NO), hydrogen peroxide (H2O2) scavenging potencies and reducing power of molecules were evaluated. RESULTS: The strongest DPPH scavengers were found to be 9, showing the potency superior to that of butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), propyl gallate (PG) and 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (Trolox) and comparable to that of ascorbic acid (AA), and 6, revealing the antioxidant potency superior to that of BHA, BHT, PG and Trolox...
August 16, 2017: Redox Report: Communications in Free Radical Research
https://www.readbyqxmd.com/read/28812124/clozapine-chlorpromazine-and-risperidone-dose-dependently-reduce-emotional-hyperthermia-a-biological-marker-of-salience
#2
William W Blessing, Esther M Blessing, Mazher Mohammed, Youichirou Ootsuka
RATIONALE: We recently introduced a new rat model of emotional hyperthermia in which a salient stimulus activates brown adipose tissue (BAT) thermogenesis and tail artery constriction. Antipsychotic drugs, both classical and second generation, act to reduce excessive assignment of salience to objects and events in the external environment. The close association between salient occurrences and increases in body temperature suggests that antipsychotic drugs may also reduce emotional hyperthermia...
August 15, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28811755/a-novel-recombined-potato-virus-y-isolate-in-china
#3
Shuxin Han, Yanling Gao, Guoquan Fan, Wei Zhang, Cailing Qiu, Shu Zhang, Yanju Bai, Junhua Zhang, Carl Spetz
This study reports the findings of a distinct Potato virus Y (PVY) isolate found in Northeast China. One hundred and ten samples (leaves and tubers) were collected from potato plants showing mosaic symptoms around the city of Harbin in Heilongjiang province of China. The collected tubers were planted and let to grow in a greenhouse. New potato plants generated from these tubers showed similar symptoms, except for one plant. Subsequent serological analyses revealed PVY as the causing agent of the disease. A novel PVY isolate (referred to as HLJ-C-44 in this study) was isolated from this sample showing unique mild mosaic and crisped leaf margin symptoms...
August 2017: Plant Pathology Journal
https://www.readbyqxmd.com/read/28811659/identification-synthesis-and-biological-activity-of-alkyl-guanidine-oligomers-as-potent-antibacterial-agents
#4
C Zamperini, G Maccari, D Deodato, C Pasero, I D'Agostino, F Orofino, F De Luca, E Dreassi, J D Docquier, M Botta
In the last two decades, the repertoire of clinically effective antibacterials is shrinking due to the rapidly increasing of multi-drug-resistant pathogenic bacteria. New chemical classes with innovative mode of action are required to prevent a return to the pre-antibiotic era. We have recently reported the identification of a series of linear guanidine derivatives and their antibacterial properties. A batch of a promising candidate for optimization studies (compound 1) turned out to be a mixture containing two unknown species with a better biological activity than the pure compound...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811504/complementarity-among-natural-enemies-enhances-pest-suppression
#5
Matteo Dainese, Gudrun Schneider, Jochen Krauss, Ingolf Steffan-Dewenter
Natural enemies have been shown to be effective agents for controlling insect pests in crops. However, it remains unclear how different natural enemy guilds contribute to the regulation of pests and how this might be modulated by landscape context. In a field exclusion experiment in oilseed rape (OSR), we found that parasitoids and ground-dwelling predators acted in a complementary way to suppress pollen beetles, suggesting that pest control by multiple enemies attacking a pest during different periods of its occurrence in the field improves biological control efficacy...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811134/a-new-chemotype-inhibitor-for-the-human-organic-cation-transporter-3-hoct3
#6
Xiaolei Pan, Kavita A Iyer, Hebing Liu, Douglas H Sweet, Małgorzata Dukat
Human organic cation transporters (OCTs) represent an understudied neurotransmitter uptake mechanism for which no selective agents have yet been identified. Several neurotransmitters (e.g. serotonin, norepinephrine) are low-affinity substrates for these transporters, but possess higher affinity for other transporters (e.g. the serotonin or norepinephrine transporters; SERT and NET, respectively). We have identified a new class of OCT inhibitors with a phenylguanidine structural scaffold. Here, we examine the actions of a series of such compounds and report preliminary structure-activity relationships (SARs) - the first dedicated SAR study of OCT3 action...
August 5, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28811071/biological-evaluation-of-2-pyrazolinyl-1-carbothioamide-derivatives-against-hct116-human-colorectal-cancer-cell-lines-and-elucidation-on-qsar-and-molecular-binding-modes
#7
Beom Soo Kim, Soon Young Shin, Seunghyun Ahn, Dongsoo Koh, Young Han Lee, Yoongho Lim
In the search of compounds exhibiting anticancer activity, 37 derivatives of 2-pyrazolinyl-1-carbothioamide were designed and synthesized. Clonogenic cell survival assays were adapted to measure the cytotoxicities of the synthetic derivatives against HCT116 human colon cancer cell lines. Half-maximal cell growth inhibitory concentrations (GI50) ranged from 0.49 to 41.22µM. The compound with the lowest GI50 value, 3-(2-hydroxy-4,5-dimethoxyphenyl)-5-(naphthalen-1-yl)-N-(3,4,5-trimethoxyphenyl)-pyrazolinyl-1-carbothioamide, was subjected to further biological studies, including cell viability and apoptosis assays to examine levels of annexin-V in the outer plasma membrane layer and poly ADP-ribose polymerase cleavage...
August 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28810954/the-use-of-apremilast-to-treat-psoriasis-during-deployment
#8
Alexandra Rosenberg, Jon Meyerle
Psoriasis is a chronic immune-mediated dermatologic disorder affecting approximately 2% of the general population. Under current U.S. Army regulation, the diagnosis of psoriasis is a bar to enlistment or appointment and, if poorly controlled, is grounds for referral to a Medical Evaluation Board and potential discharge from military service, according to Army Regulation 40-501. However, between 2008 and 2015, over 3,600 soldiers sought care for psoriasis while deployed to combat theaters, indicating that psoriasis remains a significant medical concern in the U...
July 2017: Military Medicine
https://www.readbyqxmd.com/read/28810739/a-hexa-rhodium-metallopeptide-catalyst-for-site-specific-functionalization-of-natural-antibodies
#9
Jun Ohata, Zachary T Ball
Preparation of antibody-drug conjugates (ADCs), an emerging class of targeted biological hybrid agents, necessitates precise control of conjugation reactivity. Antibodies have complex multi-stranded architectures, and specific modification of natu-ral antibodies has proven quite challenging. Here, we demonstrate that cooperative activity of a multi-metallic metallopeptide enables efficient site-specific antibody functionalization, based on molecular recognition of the constant Fc region. This interplay of multiple metal centers enables introduction of an orthogonal alkyne handle into monoclonal or polyclonal antibodies from different species...
August 16, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28810197/photochemical-formation-of-chitosan-stabilized-near-infrared-absorbing-silver-nanoworms-a-green-synthetic-strategy-and-activity-on-gram-negative-pathogenic-bacteria
#10
Sreekar Marpu, Samar S Kolailat, Daniel Korir, Brian L Kamras, Ratnesh Chaturvedi, Abel Joseph, Christopher M Smith, Misael C Palma, Jyoti Shah, Mohammad A Omary
A facile, single-step, non-seeded photochemical protocol for producing a new type of anisotropic silver nanostructure, "nanoworms", with curved longer dimensions and smooth, rounded edges. The nanoworms exhibit surface plasmon resonance (SPR) absorption in the near-infrared window (NIRW) region and are stabilized using biocompatible polymer chitosan, rendering biocompatibility and amplified safety for biological utility of the composition. Both NIRW-absorbing nanoworms and visible-absorbing nanospheres herein are attained exclusively by employing green chemistry principles...
August 4, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28810190/design-synthesis-and-biological-evaluation-of-novel-2-methoxyestradiol-analogs-as-dual-selective-estrogen-receptor-modulators-serms-and-antiangiogenic-agents
#11
Kejing Lao, Yejun Wang, Mingqi Chen, Jingjing Zhang, Qidong You, Hua Xiang
2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-proliferative activities against 5 different cell lines. The results indicated that most compounds exhibited good activities, in which compound 24c and 30c showed the best activity with low micromolar IC50 (2.73 μM -7...
August 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28810001/deferoxamine-synergizes-with-transforming-growth-factor-%C3%AE-signaling-in-chondrogenesis
#12
Zheng Huang, Guangxu He, Yanke Huang
Osteoarthritis, also known as degenerative arthritis or degenerative joint disease, is an epidemic disease that affects millions of people worldwide. Despite extensive recent work on the cellular biology of osteoarthritis, the precise mechanisms involved are still poorly understood and there is no effective treatment for this disease. The role of transforming growth factor-beta (TGF-β) in promoting chondrogenesis and inducing the expression of cartilage-specific extracellular matrix molecules to form cartilage is well-established...
August 14, 2017: Genetics and Molecular Biology
https://www.readbyqxmd.com/read/28809847/genome-wide-expression-datasets-of-anti-vegf-and-dexamethasone-treatment-of-angiogenesis-in-the-rat-cornea
#13
Anthony Mukwaya, Pierfrancesco Mirabelli, Anton Lennikov, Maria Xeroudaki, Mira Schaupper, Beatrice Peebo, Neil Lagali
Therapeutics against pathologic new blood vessel growth, particularly those targeting vascular endothelial growth factor (VEGF) are of enormous clinical interest. In the eye, where anti-VEGF agents are in widespread clinical use for treating retinal and corneal blindness, only partial or transient efficacy and resistance to anti-VEGF agents are among the major drawbacks. Conversely, corticosteroids have long been used in ophthalmology for their potency in suppressing inflammation and angiogenesis, but their broad biological activity can give rise to side effects such as glaucoma and cataract...
August 15, 2017: Scientific Data
https://www.readbyqxmd.com/read/28809799/update-on-monoterpenes-as-antimicrobial-agents-a-particular-focus-on-p-cymene
#14
REVIEW
Anna Marchese, Carla Renata Arciola, Ramona Barbieri, Ana Sanches Silva, Seyed Fazel Nabavi, Arold Jorel Tsetegho Sokeng, Morteza Izadi, Nematollah Jonaidi Jafari, Ipek Suntar, Maria Daglia, Seyed Mohammad Nabavi
p-Cymene [1-methyl-4-(1-methylethyl)-benzene] is a monoterpene found in over 100 plant species used for medicine and food purposes. It shows a range of biological activity including antioxidant, anti-inflammatory, antinociceptive, anxiolytic, anticancer and antimicrobial effects. This last property has been widely investigated due to the urgent need for new substances with antimicrobial properties, to be used to treat communicable diseases whose diffusion in developed countries has been facilitated by globalization and the evolution of antimicrobial resistance...
August 15, 2017: Materials
https://www.readbyqxmd.com/read/28809545/plasmonic-nanoprobe-of-gold-triangular-nanoprism-core-polyaniline-shell-for-real-time-three-dimensional-ph-imaging-of-anterior-chamber
#15
Peijun Tang, Xueqin Jiang, Yangyang Wang, Huanjun Chen, Yu Shrike Zhang, Panpan Gao, Hao Wang, Xuemeng Li, Jianhua Zhou
Three-dimensional (3D) molecular imaging enables the study of biological processes in both living and nonviable systems at the molecular level and has a high potential on early diagnosis. In conjunction with specific molecular probes, optical coherent tomography (OCT) is a promising imaging modality to provide 3D molecular features at the tissue level. In this study, we introduced (gold-triangular-nanoprism-core)/(polyaniline-shell nanoparticles) (GTNPs@PANI) as an OCT contrast agent and pH-responsive nanoprobe for 3D imaging of pH distribution...
August 15, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28809479/natural-seminal-amyloids-as-targets-for-development-of-synthetic-inhibitors-of-hiv-transmission
#16
Daniel A Sheik, Stephen Dewhurst, Jerry Yang
Amyloids refer to a class of protein or peptide aggregates that are heterogeneous in size, morphology, and composition, and are implicated to play a central role in many neurodegenerative and systemic diseases. The strong correlation between biological activity and extent of aggregation of amyloidogenic proteins and peptides has led to an explosion of research efforts to target these materials with synthetic molecules or engineered antibodies to try to attenuate their function in disease pathology. Although many of these efforts to attenuate amyloid function have shown great promise in laboratory settings, the vast majority of work has been focused on targeting amyloids associated with neurologic diseases, which has been met with significant additional challenges that preclude clinical evaluation...
August 15, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28809473/aie-materials-with-different-electric-charges-as-artificial-tongue-design-construction-and-assembly-with-various-pathogenic-bacteria-for-effective-bacterial-imaging-and-discrimination
#17
Guang-Jian Liu, Sheng-Nan Tian, Cui-Yun Li, Guo-Wen Xing, Lei Zhou
Imaging-based total bacterial count and type identification of bacteria play crucial rules in clinical diagnostics, public health, biological and medical science, environmental protection. Herein, we designed and synthesized a series of tetraphenylethenes (TPEs) functionalized with one or two aldehyde, carboxylic acid and quaternary ammonium groups, which were successfully used as fluorescent materials for rapid and efficient staining of 8 kinds of representative bacterial species, including pathogenic bacteria Vibrio cholera, Klebsiella pneumoniae, Listeria monocytogenes and potential bioterrorism agent Yersinia pestis...
August 15, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28809098/interfacially-engineered-pyridinium-pseudo-gemini-surfactants-as-versatile-and-efficient-supramolecular-delivery-systems-for-dna-sirna-and-mrna
#18
Uttam Satyal, Bogdan Draghici, Lisa L Dragic, Qiangnan Zhang, Kyle Norris, Muniswamy Madesh, Eugen Brailoiu, Marc A Ilies
The article presents the synthesis, self-assembling and biological activity as transfection agents for pDNA, siRNA and mRNA of novel pyridinium pseudo-gemini surfactants, interfacially-engineered from the most efficient gemini surfactants and lipids generated in our amphiphile research program. Formulation of novel amphiphiles in water revealed supramolecular properties very similar to gemini surfactants, despite their lipid-like charge/mass ratio. This dual character was found to also enhance endosomal escape and significantly increase the transfection efficiency...
August 15, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28808810/interactions-of-cisplatin-analogues-with-lysozyme-a-comparative-analysis
#19
Giarita Ferraro, Ilaria De Benedictis, Annamaria Malfitano, Giancarlo Morelli, Ettore Novellino, Daniela Marasco
The biophysical characterization of drug binding to proteins plays a key role in structural biology and in the discovery and optimization of drug discovery processes. The search for optimal combinations of biophysical techniques that can correctly and efficiently identify and quantify binding of metal-based drugs to their final target is challenging, due to the physicochemical properties of these agents. Different cisplatin derivatives have shown different citotoxicities in most common cancer lines, suggesting that they exert their biological activity via different mechanisms of action...
August 14, 2017: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/28808592/a-case-of-fulminant-meningococcemia-it-is-all-in-the-complement
#20
Kellie L Hawkins, Mariah Hoffman, Sonia Okuyama, Sarah E Rowan
Eculizumab is a novel monoclonal antibody that inhibits complement-mediated hemolysis in patients with paroxysmal nocturnal hemoglobinuria (PNH). Complement deficiency is a well-known risk factor for meningococcal infection. We describe a case of a young patient with PNH treated with eculizumab who presented with a life-threatening case of nongroupable meningococcemia. As this new biologic agent becomes more widely prescribed, providers should be aware of the increased risk of meningococcemia. In addition to vaccination, providers may consider the use of oral penicillin for antibiotic prophylaxis against Neisseria meningitidis in these cases of functional complement deficiency...
2017: Case Reports in Infectious Diseases
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