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https://www.readbyqxmd.com/read/28431385/a-method-for-evaluating-the-pharmaceutical-deconjugation-potential-in-river-water-environments
#1
Takashi Azuma, Mao Ishida, Kanae Hisamatsu, Ayami Yunoki, Kana Otomo, Mari Kunitou, Mai Shimizu, Kaori Hosomaru, Shiori Mikata, Yoshiki Mino
A new enzymatic assay method that uses deconjugation enzymes was developed to evaluate the presence and extent of conjugated pharmaceuticals in the form of glucuronide conjugates or sulphate conjugates in river environments. First, acetaminophen glucuronide (Ace Glu) and acetaminophen sulphate (Ace Sul) were used as model conjugated pharmaceuticals to determine the appropriate combination of deconjugation enzymes and reaction conditions, including temperature, duration and pH. Next, we applied the defined method to 19 pharmaceuticals grouped into nine therapeutic classes that were chosen based on previously detected levels and frequencies in sewage and river water...
April 10, 2017: Chemosphere
https://www.readbyqxmd.com/read/28431354/first-example-of-peptides-targeting-the-dimer-interface-of-leishmania-infantum-trypanothione-reductase-with-potent-in%C3%A2-vitro-antileishmanial-activity
#2
Marta Ruiz-Santaquiteria, Pedro A Sánchez-Murcia, Miguel A Toro, Héctor de Lucio, Kilian Jesús Gutiérrez, Sonia de Castro, Filipa A C Carneiro, Federico Gago, Antonio Jiménez-Ruiz, María-José Camarasa, Sonsoles Velázquez
A series of 9-mer and 13-mer amide-bridged cyclic peptides derived from the linear prototype Ac-PKIIQSVGIS-Nle-K-Nle-NH2 (Toro et al. ChemBioChem2013) has been designed and synthesized by introduction of the lactam between amino acid side chains that are separated by one helical turn (i, i+4). All of these compounds were tested in vitro as both dimerization and enzyme inhibitors of Leishmania infantum trypanothione reductase (Li-TryR). Three of the 13-mer cyclic peptide derivatives (3, 4 and 6) inhibited the oxidoreductase activity of Li-TryR in the low micromolar range and they also disrupted enzyme dimerization...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431329/stealth-recombinant-human-serum-albumin-nanoparticles-conjugating-5-fluorouracil-augmented-drug-delivery-and-cytotoxicity-in-human-colon-cancer-ht-29-cells
#3
Ankita Sharma, Amanpreet Kaur, Upendra Kumar Jain, Ramesh Chandra, Jitender Madan
BACKGROUND AND OBJECTIVE: 5-Fluorouracil (5-FU) is a first-line chemotherapeutic drug in colorectal cancer. However, intravenous administration of 5-FU at the dose of 7-12mg/kg exhibits curbs like short half-life (20min) and toxic side-effects on bone marrow cells. Therefore, in present investigation, 5-FU was conjugated to poly (ethylene glycol) anchored recombinant human serum albumin nanoparticles (5-FU-rHSA-PEG-NPs) to improve the pharmacokinetic and therapeutic profiles. METHODS AND RESULTS: The mean particle size of 5-FU-rHSA-NPs was measured to be 44...
April 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28431327/dendrimer-conjugated-iron-oxide-nanoparticles-as-stimuli-responsive-drug-carriers-for-thermally-activated-chemotherapy-of-cancer
#4
Saumya Nigam, Dhirendra Bahadur
In recent years, functional nanomaterials have found an appreciable place in the understanding and treatment of cancer. This work demonstrates the fabrication and characterization of a new class of cationic, biocompatible, peptide dendrimers, which were then used for stabilizing and functionalizing magnetite nanoparticles for combinatorial therapy of cancer. The synthesized peptide dendrimers have an edge over the widely used PAMAM dendrimers due to better biocompatibility and negligible cytotoxicity of their degradation products...
April 13, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28431285/two-benzoyl-coumarin-amide-fluorescence-chemosensors-for-cyanide-anions
#5
Zian Wang, Qianqian Wu, Jiale Li, Shuang Qiu, Duxia Cao, Yongxiao Xu, Zhiqiang Liu, Xueying Yu, Yatong Sun
Two new benzoyl coumarin amide derivatives with ortho hydroxyl benzoyl as terminal group have been synthesized. Their photophysical properties and recognition properties for cyanide anions in acetonitrile have also been examined. The influence of electron donating diethylamino group in coumarin ring and hydroxyl in benzoyl group on recognition properties was explored. The results indicate that the compounds can recognize cyanide anions with obvious absorption and fluorescence spectral change and high sensitivity...
April 13, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28431209/drug-delivery-systems-based-on-hydroxyethyl-starch
#6
Constantinos M Paleos, Zili Sideratou, Dimitris Tsiourvas
Τhe advantageous biological properties of hydroxyethyl starch (HES) triggered research interest towards design and synthesis of Drug Delivery Systems (DDSs) based on this polysaccharide. Convenient reaction schemes, including one-step reactions, led to the synthesis of HES conjugates with selected anticancer molecules or therapeutic proteins. Nanocapsules and hydrogels based on HES were also prepared and studied as prospective drug delivery systems. Formulations originating from these drug conjugates and also from nanocapsules and hydrogels loaded with drugs were characterized, highlighting on the extension of their half-life in plasma which is a critical property as far as their efficacy is concerned...
April 21, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28430776/aminoazo-dye-protein-adduct-enhances-inhibitory-effect-on-digestibility-and-damages-to-gastro-duodenal-hepatic-axis
#7
Li-Yun Lin, Chiung-Chi Peng, Yeh Chen, Boa-Chan Huang, Chun Chao Chang, Robert Y Peng
4-Dimethylaminoazobenzene (DAB, methyl yellow, or butter yellow), a human carcinogen, has been banned for use in foods since 1988. In 2014, DAB adulteration in Tofu occurred in Taiwan. We hypothesize that DAB can form [DAB•SBP]adduct adduct with soybean protein (SBP) which could damage Gastro-Duodenal-Hepatic axis. Sprague-Dawley rats gavage fed [DAB•SBP]adduct adduct revealed severely reduced body weight and damaged duodenum, liver, hepatic mitochondria, and spleen. Hepatic levels of glutathione and ATP were severely reduced...
2017: PloS One
https://www.readbyqxmd.com/read/28430714/ultrasound-molecular-imaging-of-inflammation-in-mouse-abdominal-aorta
#8
Shiying Wang, Sunil Unnikrishnan, Elizabeth B Herbst, Alexander L Klibanov, Frank William Mauldin, John A Hossack
OBJECTIVES: The aim of this study was to demonstrate a new clinically translatable ultrasound molecular imaging approach, modulated acoustic radiation force-based imaging, which is capable of rapid and reliable detection of inflammation as validated in mouse abdominal aorta. MATERIALS AND METHODS: Animal studies were approved by the Institutional Animal Care and Use Committee at the University of Virginia. C57BL/6 mice stimulated with tumor necrosis factor α, or fed with a high-fat diet, were used as inflammation (MInflammation) and diet-induced obesity (DIO) (MDIO) models, respectively...
April 20, 2017: Investigative Radiology
https://www.readbyqxmd.com/read/28430651/doxorubicin-loaded-platelets-conjugated-with-anti-cd22-mabs-a-novel-targeted-delivery-system-for-lymphoma-treatment-with-cardiopulmonary-avoidance
#9
Peipei Xu, Huaqin Zuo, Rongfu Zhou, Fan Wang, Xu Liu, Jian Ouyang, Bing Chen
B-cell lymphoma accounts for approximately 85% of all adult non-Hodgkin's lymphoma cases. Doxorubicin (DOX) is an indispensable drug for the treatment of non-Hodgkin's lymphoma. However, DOX causes severe cardiotoxicity, which limits its use in conventional treatment strategies. In this study, we developed a novel drug delivery system for lymphoma treatment: DOX-loaded platelets that were conjugated with anti-CD22 monoclonal antibodies (mAbs) (DOX-platelet-CD22). Platelets are bio- and immune-compatible drug carriers that can prolong the circulation time of drugs...
April 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28430648/radioimmunotherapy-for-cd133-colonic-cancer-stem-cells-inhibits-tumor-development-in-nude-mice
#10
Dinghu Weng, Xueyan Jin, Saimei Qin, Xiaoli Lan, Chong Chen, Xun Sun, Xianliang She, Changling Dong, Rui An
Accumulating evidence indicates that cancer stem cells (CSCs) are the cause of tumor drug/radio-resistance or distant metastasis; therefore, it is essential to eliminate CSCs to cure cancer completely. The purpose of this study was to utilize radioimmunotherapy (RIT) to target CD133(+) colonic CSCs and observe whether this prevented tumor development, by assessing the maximum tolerated dose (MTD) of HCT116 tumor-bearing nude mice with escalating doses of 131I-AC133.1 monoclonal antibody (mAb), and determining the therapeutic efficacy of RIT with 131I-AC133...
April 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28430439/molecular-organization-of-2-1-3-benzothiadiazoles-in-the-solid-state
#11
Sophie Langis-Barsetti, Thierry Maris, James D Wuest
Derivatives of 2,1,3-benzothiadiazole (1) are widely used in many areas of science and are particularly valuable as components of active layers in various thin-film optoelectronic devices. Even more effective benzothiadiazoles are likely to result if a deeper understanding of their preferred patterns of molecular association can be acquired. To provide new insight, we have analyzed the structures of compounds in which multiple benzothiadiazole units are attached to well-defined planar and nonplanar molecular cores...
April 21, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28430413/bioimaging-with-macromolecular-probes-incorporating-multiple-bodipy-fluorophores
#12
Ek Raj Thapaliya, Yang Zhang, Pravat Dhakal, Adrienne S Brown, James N Wilson, Kevin Collins, Françisco M Raymo
Seven macromolecular constructs incorporating multiple borondipyrromethene (BODIPY) fluorophores along a common poly(methacrylate) backbone with decyl and oligo(ethylene glycol) side chains were synthesized. The hydrophilic oligo(ethylene glycol) components impose solubility in aqueous environment on the overall assembly. The hydrophobic decyl chains insulate effectively the fluorophores from each other to prevent detrimental interchromophoric interactions and preserve their photophysical properties. As a result, the brightness of these multicomponent assemblies is approximately three times greater than that of a model BODIPY monomer...
April 21, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28430366/cyclic-rgd-penta-peptides-crgdyk-derivatized-with-cyclopentadienyl-complexes-of-technetium-and-rhenium-as-radiopharmaceutical-probes
#13
Qaisar Nadeem, Yunjun Shen, Muhammad Farooq Warsi, Gulfam Nasar, Muhammad Abdul Qadir, Roger Alberto
The present study reports the syntheses of half-sandwich complexes of the type [M(η(5) -C5 H4 CONH-R)(CO)3 ] (M = Re,(99m) Tc;R = cyclic RGD peptide (cRGDyK) for potential imaging of αv β3 integrin expression. The (99m) Tc complex was prepared directly from the reaction of [(99m) Tc(OH2 )3 (CO)3 ](+) with cRGDyK, doubly conjugated to Thiele's acid [(C5 H5 COOH)2 ] in water. This approach extends the viability of metal-mediated retro Diels-Alder reactions for the preparation of small molecules such as linear tripeptides to a more complex cyclic peptide carrying a [(η(5) -C5 H4 )(99m) Tc(CO)3 ] tag...
April 21, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28430266/machine-learning-approach-to-oam-beam-demultiplexing-via-convolutional-neural-networks
#14
Timothy Doster, Abbie T Watnik
Orbital angular momentum (OAM) beams allow for increased channel capacity in free-space optical communication. Conventionally, these OAM beams are multiplexed together at a transmitter and then propagated through the atmosphere to a receiver where, due to their orthogonality properties, they are demultiplexed. We propose a technique to demultiplex these OAM-carrying beams by capturing an image of the unique multiplexing intensity pattern and training a convolutional neural network (CNN) as a classifier. This CNN-based demultiplexing method allows for simplicity of operation as alignment is unnecessary, orthogonality constraints are loosened, and costly optical hardware is not required...
April 20, 2017: Applied Optics
https://www.readbyqxmd.com/read/28430247/precise-calibration-of-pupil-images-in-pyramid-wavefront-sensor
#15
Yong Liu, Quanquan Mu, Zhaoliang Cao, Lifa Hu, Chengliang Yang, Li Xuan
The pyramid wavefront sensor (PWFS) is a novel wavefront sensor with several inspiring advantages compared with Shack-Hartmann wavefront sensors. The PWFS uses four pupil images to calculate the local tilt of the incoming wavefront. Pupil images are conjugated with a telescope pupil so that each pixel in the pupil image is diffraction-limited by the telescope pupil diameter, thus the sensing error of the PWFS is much lower than that of the Shack-Hartmann sensor and is related to the extraction and alignment accuracy of pupil images...
April 20, 2017: Applied Optics
https://www.readbyqxmd.com/read/28430150/synthesis-and-self-assembly-of-shape-amphiphiles-based-on-poss-dendron-conjugates
#16
Yu Shao, Minyuan Ding, Yujie Xu, Fangjia Zhao, Hui Dai, Xia-Ran Miao, Shuguang Yang, Hui Li
Shape has been increasingly recognized as an important factor for self-assembly. In this paper, a series of shape amphiphiles have been built by linking polyhedral oligomeric silsesquioxane (POSS) and a dendron via linkers of different lengths. Three conjugates of octahedral silsesquioxanes (T₈-POSS) and dendron are designed and synthesized and are referred to as isobutyl T₈-POSS gallic acid derivatives (BPOSS-GAD-1, BPOSS-GAD-2, BPOSS-GAD-3). These samples have been fully characterized by ¹H-NMR, (13)C-NMR, Fourier transform infrared (FT-IR) spectroscopy and matrix-assisted laser desorption/ionization time of flight (MALDI-TOF) mass spectrometry to establish their chemical identity and purity...
April 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28429938/high-resolution-accurate-mass-mass-spectrometry-enables-in-depth-characterization-of-in-vivo-biotransformations-for-intact-antibody-drug-conjugates
#17
Jintang He, Dian Su, Carl K Ng, Luna Liu, Shang-Fan Yu, Thomas H Pillow, Geoffrey Del Rosario, Martine Darwish, Byoung-Chul Lee, Rachana Ohri, Hongxiang Zhou, Xueji Wang, Jiawei Lu, Surinder Kaur, Keyang Xu
Antibody-drug conjugates (ADCs) represent a promising class of therapeutics for the targeted delivery of highly potent cytotoxic drugs to tumor cells to improve bioactivity while minimizing side effects. ADCs are composed of both small and large molecules, and therefore have complex molecular structures. In vivo biotransformations may further increase the complexity of ADCs, representing a unique challenge for bioanalytical assays. Quadrupole time-of-flight mass spectrometry (Q-TOF MS) with electrospray ionization has been widely used for characterization of intact ADCs...
April 21, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28429896/production-of-a-conjugate-between-the-rk346-antigen-from-leishmania-infantum-and-the-horseradish-peroxidase-c-for-the-detection-of-rk346-antibodies
#18
Juan Rengifo-González, Yollyseth Medina-Mora, Sasha Silva-Barrios, María Elizabeth Márquez-Contreras, María Tibisay Ruiz, Ana J Cáceres, Juan Luis Concepción, Wilfredo Quiñones
It was designed and characterized a reporter system to be captured by an- tibodies bound to ELISA plates. The system was designed with the rK346 from Leishmania infantum, a highly antigenic and specific protein. The rK346 was coupled to the horseradish peroxidase C (HRPc) from Armoracia rusticana using glutaraldehyde or sulfo-SMCC. Gluta- raldehyde conjugation was performed in two steps. Separation of conjugates was carried out using a Sepharose S-200 in size exclusion chromatography (SEC); fractions were analyzed via HRPc activity and through ELISA plates sensitized with polyclonal anti-rK346 IgG puri- fied from rabbit serum...
June 2016: Investigación Clínica
https://www.readbyqxmd.com/read/28429891/comparison-of-immunization-rates-of-adults-ages-65-years-and-older-managed-within-two-nurse-practitioner-owned-clinics-with-national-immunization-rates
#19
Wendy L Wright, Elise Morrell, Jennie Lee, Norma Graciela Cuellar, Patricia White
BACKGROUND AND PURPOSE: Adults ages ≥65 years are at increased risk for infectious diseases. Ensuring these individuals are fully vaccinated is imperative. The purpose of this study was to assess the immunization rates of adults ages ≥65 years managed by nurse practitioners (NPs) and compare the results with national immunization rates and Healthy People 2020 goals. METHODS: A convenience sample of adults ages ≥65 years was obtained from two NP-managed clinics...
April 21, 2017: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/28429813/rh-catalyzed-direct-arylation-of-a-polyhedral-oligomeric-silsesquioxane
#20
Hiroaki Imoto, Satoshi Wada, Kensuke Naka
The electronic properties of polyhedral oligomeric silsesquioxanes (POSS) have recently been subjected to study. Although theoretical calculations have predicted that POSS can work as an acceptor for π-conjugated organic units, an effective reaction to incorporate aryl groups into a POSS backbone remains to be established. In this work, Rh-catalyzed direct arylation has been developed. Heptaisobutyl-POSS with a Si-H group was reacted with various aryl halides to form aryl-substitued POSSs.
April 21, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
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