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https://www.readbyqxmd.com/read/28231521/therapeutic-journey-of-2-4-thiazolidinediones-as-a-versatile-scaffold-an-insight-into-structure-activity-relationship
#1
REVIEW
Mohd Javed Naim, Md Jahangir Alam, Shujauddin Ahmad, Farah Nawaz, Neelima Shrivastava, Meeta Sahu, Ozair Alam
Thiazolidinedione is an important heterocyclic ring system, a pharmacophore and a privileged scaffold in medicinal chemistry; is a derivative of thiazolidine ring which came into existence for its role as antihyperglycemic agent and a specific ligand of PPAR's (Peroxisome proliferator activated receptor). Exhaustive research has led to determination of its vast biological profile with wide range of therapeutic applications. This review covers recent pharmacological advancements of thiazolidinedione moiety along with structure activity relationship so as to provide better correlation among different structures and their receptor interactions...
February 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28231264/precision-engineering-for-prrsv-resistance-in-pigs-macrophages-from-genome-edited-pigs-lacking-cd163-srcr5-domain-are-fully-resistant-to-both-prrsv-genotypes-while-maintaining-biological-function
#2
Christine Burkard, Simon G Lillico, Elizabeth Reid, Ben Jackson, Alan J Mileham, Tahar Ait-Ali, C Bruce A Whitelaw, Alan L Archibald
Porcine Reproductive and Respiratory Syndrome (PRRS) is a panzootic infectious disease of pigs, causing major economic losses to the world-wide pig industry. PRRS manifests differently in pigs of all ages but primarily causes late-term abortions and stillbirths in sows and respiratory disease in piglets. The causative agent of the disease is the positive-strand RNA PRRS virus (PRRSV). PRRSV has a narrow host cell tropism, limited to cells of the monocyte/macrophage lineage. CD163 has been described as a fusion receptor for PRRSV, whereby the scavenger receptor cysteine-rich domain 5 (SRCR5) region was shown to be an interaction site for the virus in vitro...
February 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28230915/a-singlet-oxygen-generating-agent-by-chirality-dependent-plasmonic-shell-satellite-nanoassembly
#3
Fengli Gao, Maozhong Sun, Wei Ma, Xiaoling Wu, Liqiang Liu, Hua Kuang, Chuanlai Xu
Photodynamic therapy (PDT) agent, which generates singlet oxygen ((1) O2 ) under light, has attracted significant attention for its broad biological and medical applications. Here, DNA-driven shell-satellite (SS) gold assemblies as chiral photosensitizers are first fabricated. The chiral plasmonic nanostructure, coupling with cysteine enantiomers on its surface, exhibits intense chiroplasmonic activities (-40.2 ± 2.6 mdeg) in the visible region. These chiral SS nanoassemblies have high reactive oxygen species generating efficiency under circular polarized light illumination, resulting in a (1) O2 quantum yield of 1...
February 23, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28230870/colloidal-capsules-nano-and-microcapsules-with-colloidal-particle-shells
#4
REVIEW
Tobias Bollhorst, Kurosch Rezwan, Michael Maas
Utilizing colloidal particles for the assembly of the shell of nano- and microcapsules holds great promise for the tailor-made design of new functional materials. Increasing research efforts are devoted to the synthesis of such colloidal capsules, by which the integration of modular building blocks with distinct physical, chemical, or morphological characteristics in a capsule's shell can result in novel properties, not present in previous encapsulation structures. This review will provide a comprehensive overview of the synthesis strategies and the progress made so far of bringing nano- and microcapsules with shells of densely packed colloidal particles closer to application in fields such as chemical engineering, materials science, or pharmaceutical and life science...
February 23, 2017: Chemical Society Reviews
https://www.readbyqxmd.com/read/28230744/s-allylmercaptocysteine%C3%A2-attenuates%C3%A2-cisplatin-induced%C3%A2-nephrotoxicity%C3%A2-through%C3%A2-suppression%C3%A2-of%C3%A2-apoptosis-%C3%A2-oxidative%C3%A2-stress-%C3%A2-and%C3%A2-inflammation
#5
Xiaosong Zhu, Xiaoyan Jiang, Ang Li, Zhongxi Zhao, Siying Li
Cisplatin is a potent chemotherapeutic agent, but its clinical usage is limited by nephrotoxicity. S-allylmercaptocysteine (SAMC), one of the water-soluble organosulfur garlic derivatives, has antioxidant and anti-inflammatory properties and plays an important role in protecting cells from apoptosis. This study aims to examine the protective effects of SAMC on cisplatin nephrotoxicity and to explore the mechanism of its renoprotection. Rats were treated with cisplatin with or without pre-treatment with SAMC...
February 20, 2017: Nutrients
https://www.readbyqxmd.com/read/28230558/risk-for-overall-infection-with-anti-tnf-and-anti-integrin-agents-used-in-ibd-a-systematic-review-and-meta-analysis
#6
Eric D Shah, Jeremy P Farida, Corey A Siegel, Kelly Chong, Gil Y Melmed
BACKGROUND: The overall risk for infection with contemporary biological agents in treating Crohn's disease (CD) and ulcerative colitis (UC) has not been systematically assessed. METHODS: We performed a PubMed and Cochrane database literature search to evaluate randomized, placebo-controlled trials of biologics in treating UC and CD. Meta-analysis was performed using a DerSimonian and Laird random effects model. We determined relative risk (RR) of harm against placebo; number needed to harm (NNH) was reported when appropriate...
February 22, 2017: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/28229433/adalimumab-a-review-in-non-infectious-non-anterior-uveitis
#7
Sheridan M Hoy
Adalimumab (Humira(®)) is a tumour necrosis factor (TNF)-α inhibitor available in various countries worldwide, including the USA, Japan and those of the EU, for the treatment of non-infectious intermediate, posterior and panuveitis in adults. It is the first biological agent approved for this indication. In two multinational, phase III studies in adults with active and inactive disease, subcutaneous adalimumab significantly reduced the risk of treatment failure relative to placebo following the tapered withdrawal of corticosteroid therapy...
February 22, 2017: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
https://www.readbyqxmd.com/read/28228735/the-potential-use-of-pharmacological-agents-to-modulate-orthodontic-tooth-movement-otm
#8
REVIEW
Thaleia Kouskoura, Christos Katsaros, Stephan von Gunten
The biological processes that come into play during orthodontic tooth movement (OTM) have been shown to be influenced by a variety of pharmacological agents. The effects of such agents are of particular relevance to the clinician as the rate of tooth movement can be accelerated or reduced as a result. This review aims to provide an overview of recent insights into drug-mediated effects and the potential use of drugs to influence the rate of tooth movement during orthodontic treatment. The limitations of current experimental models and the need for well-designed clinical and pre-clinical studies are also discussed...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28228687/reproductive-biology-and-variation-of-nuclear-ribosomal-its-and-ets-sequences-in-the-calligonum-mongolicum-complex-polygonaceae
#9
Wei Shi, Jun Wen, Yanfeng Zhao, Gabriel Johnson, Borong Pan
To explore the biosystematics of the Calligonum mongolicum complex (Polygonaceae), the flowering phenological period, breeding and pollination characters and seed set of the complex (Calligonum Mongolicum Turze, Calligonum chinense A. Los., Calligonum gobicum A. Los., Calligonum pumilum A. Los. and Calligonum zaidamense A. Los.) were documented in the Turpan Eremophyte Botanical Garden, China. The sequences of the nuclear ribosomal ITS and ETS region were employed to differentiate the Calligonum mongolicum complex and other species in sect...
2017: PhytoKeys
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#10
Golla Madhava, Katla Venkata Ramana, Saddala Madhu Sudhana, Devineni Subba Rao, Kuntrapakam Hema Kumar, Valluru Lokanatha, Asupatri Usha Rani, Chamarthi Naga Raju
BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory dynamic agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards the synthesis of anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, and evaluated their anti-inflammatory activity in both methods in vitro and in vivo, and molecular docking study on COX-2 enzyme will be discussed in this study...
February 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28228075/challenges-in-dermal-delivery-of-therapeutic-antimicrobial-protein-and-peptides
#11
Rohan Aminbhai Lalani, Ambikanandan Misra, Jitendra Amrutiya, Hinal Patel, Priyanka Bhatt, Vivek Patel
BACKGROUND: Protein and peptides in biological system form an important part of innate immune system and are being explored for potential use in various diseases as therapeutics. Importance of proteins and peptides as a new class of antimicrobial agents have boosted research in the field of biotechnology as potential alternative to antibiotic agents. OBJECTIVE: Protein and peptides antimicrobial as a therapeutics class are structurally diverse and exhibit potent activity against microbes by various mechanisms...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228073/principal-physicochemical-methods-used-to-characterize-dendrimer-molecule-complexes-used-as-genetic-therapy-agents-nanovaccines-or-drug-carriers
#12
Rodríguez Fonseca Rolando Alberto, Rodrigues Joao, Muñoz-Fernández María de Los Angeles, Martínez Muñoz Alberto, Fragoso Vázquez Manuel Jonathan, Correa Basurto José
Nanomedicine is the application of nanotechnology to medicine. This field is related to the study of nanodevices and nanomaterials applied to various medical uses, such as in improving the pharmacological properties of different molecules. Dendrimers are synthetic nanoparticles whose physicochemical properties vary according to their chemical structure. These molecules have been extensively investigated as drug nanocarriers to improve drug solubility and as sustained-release systems. New therapies such as gene therapy and the development of nanovaccines can be improved by the use of dendrimers...
February 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28227910/development-of-a-three-dimensional-lattice-free-multiscale-model-of-the-mammary-terminal-end-bud
#13
Joseph D Butner, Vittorio Cristini, Zhihui Wang, Joseph D Butner, Vittorio Cristini, Zhihui Wang, Vittorio Cristini, Joseph D Butner, Zhihui Wang
The terminal end bud (TEB) is a bulbous structure composed of highly proliferative cells that is responsible for mammary gland development during the pubertal stage. This is a highly organized process, involving cellular differentiation hierarchies regulated by endocrine and paracrine signaling. Here, we present development of a lattice-free, three dimensional multiscale agent based model of the TEB to study the effects of cellular phenotypic hierarchies, endocrine and paracrine signaling, and proliferation demographics on pubertal mammary gland development...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28225210/prophylactic-drug-management-for-febrile-seizures-in-children
#14
REVIEW
Martin Offringa, Richard Newton, Martinus A Cozijnsen, Sarah J Nevitt
BACKGROUND: Febrile seizures occurring in a child older than one month during an episode of fever affect 2% to 4% of children in Great Britain and the United States and recur in 30%. Rapid-acting antiepileptics and antipyretics given during subsequent fever episodes have been used to avoid the adverse effects of continuous antiepileptic drugs. OBJECTIVES: To evaluate primarily the effectiveness and safety of antiepileptic and antipyretic drugs used prophylactically to treat children with febrile seizures; but also to evaluate any other drug intervention where there was a sound biological rationale for its use...
February 22, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28224391/development-and-evaluation-of-a-nanoemulsion-containing-ursolic-acid-a-promising-trypanocidal-agent-nanoemulsion-with-ursolic-acid-against-t-cruzi
#15
Erika Cristina Vargas de Oliveira, Zumira Aparecida Carneiro, Sérgio de Albuquerque, Juliana Maldonado Marchetti
Over a hundred years after the discovery of Chagas disease, this ailment continues to affect thousands of people. For more than 40 years, only two drugs have been available to treat it. Ursolic acid is a naturally occurring terpene that has shown a good trypanocidal action. However, the hydrophobicity of this compound presents a challenge for the development of proper delivery systems. Nanostructured systems are a prominent in delivering lipophilic drugs. Thus, a nanoemulsion containing ursolic acid was developed and had its trypanocidal activity and cytotoxicity evaluated...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28223863/design-synthesis-molecular-modeling-and-biological-evaluation-of-novel-diaryl-heterocyclic-analogs-as-potential-selective-cyclooxygenase-2-cox-2-inhibitors
#16
Deema A Al-Turki, Mohamed A Al-Omar, Laila A Abou-Zeid, Ihsan A Shehata, Mohammed S Al-Awady
New series of 3,4-diaryl-2-thioxoimidazolidin-4-ones and 3-alkylthio-4,5-diaryl-4H-1,2,4-triazoles were designed, synthesized and evaluated for their activity as anti-inflammatory agents. Compounds 20, 21, 23 and 34 are highly selective inhibitors of COX-2 enzyme at a concentration of 100 mM relative to celecoxib, the standard reference. (±)-3-(4-Phenoxy-phenyl)-5-phenyl-2-thioxoimidazolidin-4-ones 23 exhibited the most active anti-inflammatory agent.
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28223859/histatin-peptides-pharmacological-functions-and-their-applications-in-dentistry
#17
REVIEW
Zohaib Khurshid, Shariq Najeeb, Maria Mali, Syed Faraz Moin, Syed Qasim Raza, Sana Zohaib, Farshid Sefat, Muhammad Sohail Zafar
There are many human oral antimicrobial peptides responsible for playing important roles including maintenance, repairing of oral tissues (hard or soft) and defense against oral microbes. In this review we have highlighted the biochemistry, physiology and proteomics of human oral histatin peptides, secreted from parotid and submandibular salivary glands in human. The significance of these peptides includes capability for ionic binding that can kill fungal Candida albicans. They have histidine rich amino acid sequences (7-12 family members; corresponding to residues 12-24, 13-24, 12-25, 13-25, 5-11, and 5-12, respectively) for Histatin-3...
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28223857/erythrocyte-nanovesicles-biogenesis-biological-roles-and-therapeutic-approach-erythrocyte-nanovesicles
#18
REVIEW
Gamaleldin I Harisa, Mohamed M Badran, Fars K Alanazi
Nanovesicles (NVs) represent a novel transporter for cell signals to modify functions of target cells. Therefore, NVs play many roles in both physiological and pathological processes. This report highlights biogenesis, composition and biological roles of erythrocytes derived nanovesicles (EDNVs). Furthermore, we address utilization of EDNVs as novel drug delivery cargo as well as therapeutic target. EDNVs are lipid bilayer vesicles rich in phospholipids, proteins, lipid raft, and hemoglobin. In vivo EDNVs biogenesis is triggered by an increase of intracellular calcium levels, ATP depletion and under effect of oxidative stress conditions...
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28223802/fe3o4-based-plga-nanoparticles-as-mr-contrast-agents-for-the-detection-of-thrombosis
#19
Jia Liu, Jie Xu, Jun Zhou, Yu Zhang, Dajing Guo, Zhigang Wang
Thrombotic disease is a great threat to human health, and early detection is particularly important. Magnetic resonance (MR) molecular imaging provides noninvasive imaging with the potential for early disease diagnosis. In this study, we developed Fe3O4-based poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) surface-modified with a cyclic Arg-Gly-Asp (cRGD) peptide as an MR contrast agent for the detection of thrombosis. The physical and chemical characteristics, biological toxicity, ability to target thrombi, and biodistribution of the NPs were studied...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28223691/cellular-glycosylation-affects-herceptin-binding-and-sensitivity-of-breast-cancer-cells-to-doxorubicin-and-growth-factors
#20
Diluka Peiris, Alexander F Spector, Hannah Lomax-Browne, Tayebeh Azimi, Bala Ramesh, Marilena Loizidou, Hazel Welch, Miriam V Dwek
Alterations in protein glycosylation are a key feature of oncogenesis and have been shown to affect cancer cell behaviour perturbing cell adhesion, favouring cell migration and metastasis. This study investigated the effect of N-linked glycosylation on the binding of Herceptin to HER2 protein in breast cancer and on the sensitivity of cancer cells to the chemotherapeutic agent doxorubicin (DXR) and growth factors (EGF and IGF-1). The interaction between Herceptin and recombinant HER2 protein and cancer cell surfaces (on-rate/off-rate) was assessed using a quartz crystal microbalance biosensor revealing an increase in the accessibility of HER2 to Herceptin following deglycosylation of cell membrane proteins (deglycosylated cells Bmax: 6...
February 22, 2017: Scientific Reports
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