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Reversal agents

Hongkang Wang, Jinkai Wang, Sanmu Xie, Wenxing Liu, Chunming Niu
To address the volume change-induced pulverization problem of tin-based anodes, a concept using hollow carbon nanoballs (HCNBs) as buffering supports is herein proposed. HCNBs with hollow interior, flexibility and graphitic crystallization are first prepared by a combined method of chemical vapor deposition (CVD) and template-synthesis using CH4 as the carbon source and CaCO3 as the conformal template. The ultrafine SnO2 nanoparticles are loaded onto the HCNBs (denoted as SnO2@HCNBs) via pyrolysis of tin(ii) 2-ethylhexanoate at 300 °C in air...
March 21, 2018: Nanoscale
Opute M Yvette, Sarel F Malan, Dale Taylor, Erika Kapp, Jacques Joubert
Previously we have shown that pentacycloundecylamine-chloroquinoline (PCU-CQ) conjugates possess significant chemosensitizing abilities and can circumvent the resistance associated with chloroquine (CQ) resistant plasmodia. In order to further explore structurally related polycyclic compounds as reversed CQ agents we synthesized a series of eight aza-adamantanol (1-4) and adamantane-imine (5-8) CQ conjugates. All conjugates showed limited cytotoxicity against CHO cells (IC50  > 37 µM). Compounds 1, 2 and 5 were highly active (K1 IC50  < 100 nM) exhibiting a 3-4-fold increase in antiplasmodial activity against CQ resistant strain K1 compared to CQ...
March 12, 2018: Bioorganic & Medicinal Chemistry Letters
Zhenjing Jin, Siqi Liu, Qian Zhang, Xue Shao, Jingting Ma, Liulan Pan
BACKGROUND: Hepatic fibrosis is a reversible pathological process. Inflammatory responses are the prevailing reactions during hepatic fibrosis. Decoy receptor 3 (DcR3) has been reported to have an anti-inflammatory effect. OBJECTIVES: The aim of the study was to investigate the preventive effects of DcR3 on hepatic fibrosis. MATERIAL AND METHODS: Hepatic fibrosis was induced in rats by administering intraperitoneally (ip.) 1% dimethylnitrosamine (DMN)...
March 20, 2018: Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University
Xinshen Li, Jianhua Peng, Jinwei Pang, Yue Wu, Xueping Huang, Yong Li, Jian Zhou, Long Gu, Xiaochuan Sun, Ligang Chen, Michael P Vitek, Yong Jiang
COG1410, a mimetic peptide derived from the apolipoprotein E (apoE) receptor binding region, exerts positive effect on neurological deficits in early brain injury (EBI) after experimental subarachnoid hemorrhage (SAH). Currently the neuroprotective effect of COG1410 includes inhibiting BBB disruption, reducing neuronal apoptosis, and neuroinflammation. However, the effect and mechanism of COG1410 to subcellular organelles disorder have not been fully investigated. As the main pathway for recycling long-lived proteins and damaged organelles, neuronal autophagy is activated in SAH and exhibits neuroprotective effects by reducing the insults of EBI...
2018: Frontiers in Neuroscience
M Yolanda Cobo-Nuñez, Mariam El Assar, Pedro Cuevas, Alberto Sánchez-Ferrer, Jennifer Martínez-González, Leocadio Rodríguez-Mañas, Javier Angulo
Etamsylate is indicated for several anti-hemorrhagic indications in human and veterinary medicine. However, etamsylate has been shown to be effective only in specific haemorrhagic situations. Furthermore, mechanism of action of etamsylate is not known but recent research has shown its ability to inhibit heparin binding to several growth factors. We have evaluated the ability of etamsylate to interfere with the activities of heparin. Effects of etamsylate on vasodilatory activity of heparin were evaluated in rat aortic segments...
March 16, 2018: European Journal of Pharmacology
Wei Jiang, Xiaojing He, Huiying Fang, Xue Zhou, Haitao Ran, Dajing Guo
The early diagnosis of prostate cancer (PCa) is particularly important for reducing its high mortality rate. With the development of molecular magnetic resonance imaging (MRI), early diagnosis via non-invasive imaging has become possible. In this study, gadopentetic acid (GA)-doped silica (Gd@SiO2 ) was first synthesized by a reverse microemulsion method, and amino and carboxyl groups were then successively introduced onto the surface of Gd@SiO2 . After these steps, a monoclonal antibody (YPSMA-1) to prostate-specific membrane antigen (PSMA) was conjugated with carboxyl-modified Gd@SiO2 (Gd@SiO2 -COOH) nanoparticles (NPs) by the carbodiimide method...
March 16, 2018: Biochemical and Biophysical Research Communications
Ming Hu, Zhenhui Zhang, Bin Liu, Shuangwei Zhang, Renjie Chai, Xiaohua Chen, Tianyu Kong, Fangcheng Zhang, Jingzhi Zhang, Shiming Liu, Ningning Liu
BACKGROUND/AIMS: Cardiac hypertrophy is a major outcome and compensatory response of the cardiovascular system to hemodynamic and additional stress responses that ultimately lead to heart failure. Auranofin (Aur) has been used for treating rheumatic arthritis for several decades. Aur is a 19S proteasome-associated deubiquitinase inhibitor, and inhibition of the proteasome is speculated to reverse cardiac hypertrophy. However, the role of the deubiquitinases, especially 19S proteasome-associated deubiquitinases, in the regulation of cardiac remodeling remains poorly understood...
March 15, 2018: Cellular Physiology and Biochemistry
M S da Silva, S Silveira, V S Caron, A C S Mósena, M N Weber, S P Cibulski, A A R Medeiros, G S Silva, L G Corbellini, R Klein, L C Kreutz, R Frandoloso, C W Canal
Background: Hepatitis E virus (HEV) is the causative agent of acute hepatitis worldwide. There is no seroprevalence study in backyard farms, which are characterized by suboptimal hygienic conditions in Brazil. We aimed to determine the seroprevalence and genetic diversity of HEV in backyard pigs in Brazil. Methods: Swine serum samples collected in 2012 (n=731) and 2014 (n=713) were analysed. The presence of anti-HEV immunoglobulin G in pig serum was evaluated by indirect enzyme-linked immunosorbent assay...
March 15, 2018: Transactions of the Royal Society of Tropical Medicine and Hygiene
A M Illias, A C Gist, H Zhang, A K Kosturakis, P M Dougherty
Activation of innate immune mechanisms within the dorsal root ganglion (DRG) and spinal dorsal horn has been shown to play a key role in the development of neuropathic pain including paclitaxel-related chemotherapy-induced peripheral neuropathy (CIPN). Here we tested whether similar mechanisms are generalizable to oxaliplatin-induced CIPN. After a single intraperitoneal injection of 3mg/kg oxaliplatin, mechanical withdrawal threshold and the expression of C-C chemokine ligand 2 (CCL2) and its receptor, CCR2 in the DRG were measured by behavioral testing and immunohistochemical (IHC) staining, respectively...
March 15, 2018: Pain
Ding Shi, Yongpan Liu, Dong Wu, Xujun Hu
Helicobacter pylori , the primary causative agent of stomach cancer, is known to affect gastric mucin expression. However, the underlying molecular mechanisms mediating this H. pylori -dependent effect remain unknown. In the present study, the effect of exogenous expression of the H. pylori virulence factor, CagA, on mucin 5AC oligomeric muscus/gel-forming (MUC5AC) expression was investigated using an in vitro model of the gastric mucosa. AGS cells were either untreated or transfected by a vector control (pCDNA3...
April 2018: Oncology Letters
Long Cui, Juan Zhao, Jingjing Liu
BACKGROUND: Aberrant Wnt/β-catenin activation has been shown to play essential roles in cancer, including renal cell carcinoma (RCC). In this work, we demonstrate that Wnt/β-catenin inhibition by a Food and Drug Administration-approved drug, pyrvinium, effectively targets clear cell RCC and enhances chemotherapy agent's efficacy. MATERIALS AND METHODS: We performed in vitro cell culture assays and in vivo xenograft tumor model to evaluate the effects of pyrvinium alone and its combination with paclitaxel, and analyzed the underlying mechanism(s) of pyrvinium's action in RCC...
March 2018: American Journal of the Medical Sciences
Maryam Sohrabi, Mahdi Alahgholi-Hajibehzad, Zahra Gholami Mahmoodian, Sayed Ali Hosseini Siyar, Alireza Zamani
BACKGROUND: Studies have indicated that extraweight and obesity induce chronic inflammation, which can lead to other diseases such as cancers. OBJECTIVE: To evaluate the effects of two weight-lowering and anti-inflammatory agents including cinnamon, and turmeric, on serum levels of interleukin-17 (IL-17) as a pro-inflammatory cytokine. METHODS: In this study, 64 rats were designated in eight groups. The control group received normal diet. The other groups were fed with normal diet plus high cinnamon (3 mg/ml), high turmeric (3 mg/ml), high-fructose solution (30%), fructose solution with low (0...
March 2018: Iranian Journal of Immunology: IJI
Benneth Ben-Azu, Adegbuyi Oladele Aderibigbe, Abayomi Mayowa Ajayi, Aya-Ebi Okubo Eneni, Solomon Umukoro, Ezekiel O Iwalewa
GABAergic (Gamma-aminobutyric acid) and neurotrophic derangements have important implication in schizophrenia, a neuropsychiatric disease. Previous studies have shown that nicotinamide adenine dinucleotide phosphate oxidase (NADPH-oxidase) alters GABAergic and neurotrophic activities via inflammatory and oxidative pathways. Thus, it has been proposed that agents with anti-oxidant and anti-inflammatory properties might be beneficial for the treatment of the disease. Morin is neuroactive bioflavonoid compound, which has been reported to demonstrate antipsychotic and anti-oxidant/anti-inflammatory activities...
March 13, 2018: Brain Research Bulletin
N Haber
Respiratory syncytial virus (RSV) is a major cause of severe lower respiratory tract infections in infants and young children. Reinfections are common throughout adult life with more severe presentations occurring in immunocompromised individuals, subjects with underlying high-risk cardiopulmonary diseases, and in the elderly. There is now a significant body of literature indicating that the impact of RSV in elderly adults is similar to that of non-pandemic influenza, both in the community and in nursing homes...
March 13, 2018: Médecine et Maladies Infectieuses
Yukihiro Itoh, Miki Suzuki
Ubiquitin-activating enzyme (E1), which catalyzes the activation of ubiquitin in the initial step of the ubiquitination cascade, is a potential therapeutic target in multiple myeloma and breast cancer treatment. However, only a few E1 inhibitors have been reported to date. Moreover, there has been little medicinal chemistry research on the three-dimensional structure of E1. Therefore, in the present study, we attempted to identify novel E1 inhibitors using structure-based drug design. Following the rational design, synthesis, and in vitro biological evaluation of several such compounds, we identified a reversible E1 inhibitor (4b)...
March 3, 2018: Bioorganic & Medicinal Chemistry Letters
Xiulin Fan, Jie Yue, Fudong Han, Ji Chen, Tao Deng, Xiuquan Zhou, Singyuk Hou, Chunsheng Wang
Room temperature all solid-state Na-S batteries (ASNSBs) using sulfide solid electrolytes are a promising next-generation battery technology due to the high energy, enhanced safety, and earth abundant resources of both sodium and sulfur. Currently, the sulfide electrolyte ASNSBs are fabricated by simple cold-pressing process leaving with high residential stress. Even worse, the large volume change of S/Na2S during charge/discharge cycles induces additional stress, seriously weakening the less-contacted interfaces among the solid electrolyte, active materials and the electron conductive agent that are formed in the cold-pressing process...
March 16, 2018: ACS Nano
Paula V Monje
This chapter describes protocols to establish simplified in vitro assays of Schwann cell (SC) differentiation in the absence of neurons. The assays are based on the capacity of isolated primary SCs to increase or decrease the expression of myelination-associated genes in response to the presence or absence of cell permeable analogs of cyclic adenosine monophosphate (cAMP). No special conditions of media or substrates beyond the administration or removal of cAMP analogs are required to obtain a synchronous response on differentiation and dedifferentiation...
2018: Methods in Molecular Biology
C Lavanya, Manjunatha M Venkataswamy, M K Sibin, M M Srinivas Bharath, G K Chetan
Increased telomerase activity can be blocked by targeting the hTERT activity at both RNA and catalytic subunits. Various inhibitors had been used to regulate hTERT activity in glioblastoma cell lines and showed promising results. The present study hypothesized that the telomerase specific inhibitor BIBR1532 can effectively down-regulate the telomerase activity in LN18 glioblastoma cell line. LN18 glioblastoma cell line was treated with various concentrations of BIBR1532 at different time intervals. MTT assay was performed to determine cell viability after BIBR1532 treatment...
March 15, 2018: Cytotechnology
Caterina Musolino, Giacomo Oteri, Alessandro Allegra, Manuela Mania, Angela D'Ascola, Angela Avenoso, Vanessa Innao, Andrea Gaetano Allegra, Salvatore Campo
Bisphosphonates are formidable inhibitors of osteoclast-mediated bone resorption employed for therapy of multiple myeloma (MM) subjects with osteolytic lesions. Osteonecrosis of the jaw (ONJ) is an uncommon drug-induced adverse event of these agents. MicroRNAs (miRNAs) are a group of small, noncoding RNAs nucleotides, which are essential post-transcriptional controllers of gene expression. They have a central role in the normal bone development. The goal of our study was to investigate 18 miRNAs, whose targets were previously validated and described in MM subjects without ONJ, in peripheral lymphocytes of MM subjects with bisphosphonate-induced ONJ...
March 15, 2018: Annals of Hematology
Vivek Murthy, Janna Minehart, Daniel H Sterman
Modern cancer immunotherapies represent a major shift in paradigm with respect to how we understand innate and adaptive responses to malignancy. Successful tumors co-opt normal immunosurveillance mechanisms by potent interactions between the tumor and local draining lymph nodes. Tumor cells mediate a complex and dynamic immunoediting procedure that results in increased vascular efflux into the draining lymphatics, an immunosuppressive microenvironment rich in regulatory T-lymphocytes, dysfunctional antigen presentation, and downregulation of normal effector lymphocyte responses...
December 1, 2017: Journal of the National Cancer Institute
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