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Biochemical Pharmacology

Binbin Sun, Zeyu Zhong, Fan Wang, Jiong Xu, Feng Xu, Weimin Kong, Zhaoli Ling, Nan Shu, Ying Li, Tong Wu, Mian Zhang, Liang Zhu, Xiaodong Liu, Li Liu
Skeletal muscle accounts for approximately 75% of glucose disposal in body and statins impair glucose metabolism. We aimed to investigate the effect of atorvastatin on glucose metabolism in C2C12 cells. Glucose metabolism and expression of glucose transporter 4 (GLUT4) and hexokinase II (HXKII) were measured following incubation with atorvastatin or pravastatin. Roles of cholesterol in atorvastatin-induced glucose metabolism impairment were investigated via adding cholesterol or mevalonic acid and confirmed by cholesterol depletion with methyl-β-cyclodextrin...
January 12, 2018: Biochemical Pharmacology
Liang Shi, Zhanxia Hao, Shaobo Zhang, Mengjuan Wei, Bin Lu, Zhengtao Wang, Lili Ji
Acetaminophen (APAP)-induced hepatotoxicity is the main cause of drug-induced liver injury. This study investigated the protection of baicalin and its aglycone baicalein against APAP-induced hepatotoxicity and its mechanism. Baicalein and baicalin alleviated APAP-induced hepatotoxicity both in vitro and in vivo. Moreover, baicalin-provided this protection was not diminished in hepatocytes or mice treated with β-glucuronidase inhibitor. Results of liver glutathione (GSH) and reactive oxygen species (ROS) formation demonstrated the alleviation of baicalein and baicalin on APAP-induced liver oxidative stress injury...
January 12, 2018: Biochemical Pharmacology
Muadh Hussain, Vanessa Zimmermann, Sjoerd J L van Wijk, Simone Fulda
Mouse embryonic fibroblasts (MEFs) have extensively been used to study necroptosis, a recently identified form of programmed cell death. However, very little is yet known about the role of necroptosis and its regulation by reactive oxygen species (ROS) in cell types naturally exposed to high oxygen levels such as mouse lung fibroblasts (MLFs). Here, we discover that MLFs are highly susceptible to undergo necroptosis in a ROS-dependent manner upon exposure to a prototypic death receptor-mediated necroptotic stimulus, i...
January 11, 2018: Biochemical Pharmacology
Md Habibur Rahman, Anup Bhusal, Won-Ha Lee, In-Kyu Lee, Kyoungho Suk
Preclinical studies have suggested that chronic inflammation in the brain might be associated with multiple metabolic disorders, including obesity and diabetes. In particular, hypothalamic inflammation interferes with the endocrine system and modulates nutritional homeostasis, leading to metabolic alterations and consequent pathologies. With regard to the mechanisms underlying molecular and cellular pathogenesis, neurons, non-neuronal cells, and the crosstalk between them have gained particular attention. Specifically, malfunctioning glia have recently been implicated as an important component of pathological hypothalamic inflammation...
January 11, 2018: Biochemical Pharmacology
Michael F Jarvis, S J Enna
No abstract text is available yet for this article.
January 10, 2018: Biochemical Pharmacology
(no author information available yet)
No abstract text is available yet for this article.
January 10, 2018: Biochemical Pharmacology
Akihiko S Kato, Jeffrey M Witkin
The need for improved medications for psychiatric and neurological disorders is clear. Difficulties in finding such drugs demands that all strategic means be utilized for their invention. The discovery of forebrain specific AMPA receptor antagonists, which selectively block the specific combinations of principal and auxiliary subunits present in forebrain regions but spare targets in the cerebellum, was recently disclosed. This discovery raised the possibility that other auxiliary protein systems could be utilized to help identify new medicines...
January 9, 2018: Biochemical Pharmacology
Sevda Gheibi, Sajad Jeddi, Khosrow Kashfi, Asghar Ghasemi
Nitric oxide (NO) and hydrogen sulfide (H2S) are two gasotransmitters that are produced in the vasculature and contribute to the regulation of vascular tone. NO and H2S are synthesized in both vascular smooth muscle and endothelial cells; NO functions primarily through the sGC/cGMP pathway, and H2S mainly through activation of the ATP-dependent potassium channels; both leading to relaxation of vascular smooth muscle cells. A deficit in the NO/H2S homeostasis is involved in the pathogenesis of various cardiovascular diseases, especially hypertension...
January 9, 2018: Biochemical Pharmacology
Daniel P Radin, Yong-Xin Li, Gary Rogers, Richard Purcell, Arnold Lippa
It was previously reported that Stargazin (STG) enhances the surface expression of AMPA receptors, controls receptor gating and slows channel desensitization as an auxiliary subunit of the receptors. Ampakines are a class of AMPA receptor positive allosteric modulators that modify rates of transmitter binding, channel activity and desensitization parameters. As such, they have shown efficacy in animal models of neurodegenerative diseases, where excitatory synaptic transmission is compromised. Given the functional similarities between STG and ampakines, the current study sought to probe interactions between STG and ampakine gating properties...
January 9, 2018: Biochemical Pharmacology
Christopher J Draper-Joyce, Mayako Michino, Ravi Kumar Verma, Carmen Klein Herenbrink, Jeremy Shonberg, Anitha Kopinathan, Peter J Scammells, Ben Capuano, David M Thal, Jonathan A Javitch, Arthur Christopoulos, Lei Shi, J Robert Lane
SB269652 is a negative allosteric modulator of the dopamine D2 receptor (D2R) yet possesses structural similarity to ligands with a competitive mode of interaction. In this study, we aimed to understand the ligand-receptor interactions that confer its allosteric action. We combined site-directed mutagenesis with molecular dynamics simulations using both SB269652 and derivatives from our previous structure activity studies. We identify residues within the conserved orthosteric binding site (OBS) and a secondary binding pocket (SBP) that determine affinity and cooperativity...
January 8, 2018: Biochemical Pharmacology
Ana Lia Mazzeti, Lívia de F Diniz, Karolina R Gonçalves, Alvaro F S Nascimento, Pollyanna A F Spósito, Vanessa C F Mosqueira, George L L Machado-Coelho, Isabela Ribeiro, Maria T Bahia
Benznidazole and nifurtimox-treatments regimens currently used in human are supported by very limited experimental data. This study was designed to evaluate the time and dose dependence for efficacy of the most important nitroheterocyclic drugs in use for Chagas disease. In order to evaluate time dependence, Y strain-infected mice received benznidazole for a total of 1, 3, 7, 10, 20, and 40 days. Treatment courses of 3 to 10-day were effective in clearing parasitaemia and suppressing mortality, but parasitological cure was not achieved...
January 5, 2018: Biochemical Pharmacology
Xiao-Tong Zhang, Xue-Qiang Sun, Chen Wu, Jun-Liang Chen, Jia-Jia Yuan, Qing-Feng Pang, Zhi-Ping Wang
Althoughmethylene blue (MB) has showed strong antioxidant effect, its effect related with heme oxygenase-1(HO-1) is still unclear. Thus, we investigated the effects of MB on HO-1 protein content and enzyme activity, and its protective effect against hydrogen peroxide (H2O2)- induced oxidative damage in RAW264.7 macrophage. The cellviability and the release of lactate dehydrogenase of RAW264.7 were determined. The mitochondrial functions were valuated through these indexes: content of adenosine triphosphate, superoxide dismutase, concentration of reactive oxygen species and mitochondrial membrane potential...
January 5, 2018: Biochemical Pharmacology
Jolien Storme, Annelies Cannaert, Kathleen Van Craenenbroeck, Christophe P Stove
Besides classical G protein coupling, G protein-coupled receptors (GPCRs) are nowadays well known to show significant signalling via other adaptor proteins, such as β-arrestin2 (βarr2). The elucidation of the molecular mechanism of the GPCR-βarr2 interaction is a prerequisite for the structure-activity based design of biased ligands, which introduces a new chapter in drug discovery. The general mechanism of the interaction is believed to rely on phosphorylation sites, exposed upon agonist binding. However, it is not known whether this mechanism is universal throughout the GPCR family or if GPCR-specific patterns are involved...
January 5, 2018: Biochemical Pharmacology
Yuanyuan Ge, Yi Li, Qin Chen, Weiming Zhu, Lugen Zuo, Zhen Guo, Jianfeng Gong, Lei Cao, Lili Gu, Jieshou Li
Both mesenteric adipose tissue (MAT) and lymphatic vessels (LVs) play important roles in the pathogenesis of Crohn's disease (CD), and adipokines have been implicated in the crosstalk between MAT and LVs. Apelin, a newly identified adipokine, has been demonstrated to be crucial in the development and stabilization of LVs. We aimed to identify the expression of apelin in MAT of CD patients and explore whether apelin influences the disease course in murine colitis and determine its contributions to LVs. Expression of apelin in MAT specimens from patients with CD (n=24) and without CD (control, n=12) was detected...
January 5, 2018: Biochemical Pharmacology
Jeannette M Osterloh, Kevin Mullane
Biomedical research is being transformed by the discovery and use of human pluripotent stem cells (hPSCs). Remarkable progress has been made, and assorted clinical trials are underway related to the application of stem cell therapy, including transplantation of hPSC-derived cells, in situ reprogramming or transdifferentiation, and utilization of targets and compounds identified from patient-derived stem cells. However, the pace of discovery is overwhelming efforts to replicate the work of others, prompting a concern over validity and reproducibility...
January 5, 2018: Biochemical Pharmacology
Sébastien Rigali, Sinaeda Anderssen, Aymeric Naômé, Gilles P van Wezel
The World Health Organization (WHO) describes antibiotic resistance as "one of the biggest threats to global health, food security, and development today", as the number of multi- and pan-resistant bacteria is rising dangerously. Acquired resistance phenomena also impair antifungals, antivirals, anti-cancer drug therapy, while herbicide resistance in weeds threatens the crop industry. On the positive side, it is likely that the chemical space of natural products goes far beyond what has currently been discovered...
January 5, 2018: Biochemical Pharmacology
Fatemeh Hassani-Nezhad-Gashti, Jaana Rysä, Outi Kummu, Juha Näpänkangas, Marcin Buler, Mikko Karpale, Janne Hukkanen, Jukka Hakkola
Pregnane X receptor (PXR) is a nuclear receptor that senses chemical environment and is activated by numerous clinically used drugs and environmental contaminants. Previous studies have indicated that several drugs known to activate PXR appear to induce glucose intolerance. We now aimed to reveal the role of PXR in drug-induced glucose intolerance and characterize the mechanisms involved. We used PXR knockout mice model to investigate the significance of this nuclear receptor in the regulation of glucose tolerance...
January 5, 2018: Biochemical Pharmacology
Rou-Ling Cho, Wei-Ning Lin, Chen-Yu Wang, Chien-Chung Yang, Li-Der Hsiao, Chih-Chung Lin, Chuen-Mao Yang
HO-1 (heme oxygenase-1), an antioxidant enzyme, induced by rosiglitazone (PPAR ligands) can be a potential treatment of inflammation. However, the mechanisms of rosiglitazone-induced HO-1 expression in human pulmonary alveolar epithelial cells (HPAEpiCs) remain largely unknown. In this study, we found that upregulation of HO-1 in vitro or in vivo by rosiglitazone attenuated VCAM-1 gene expression and monocyte adhesion to HPAEpiCs challenged with lipopolysaccharide (LPS). The inhibitory effects of rosiglitazone on LPS-mediated responses were reversed by transfection with HO-1 siRNA...
January 5, 2018: Biochemical Pharmacology
Vladimir Pliska, Guido Jutz
The oil immersion method suggested earlier by Kalsner and Nickerson for analysing actions of sympathomimetic drugs in smooth muscle tissues was applied to isometric preparations of rat myometrium stimulated by oxytocin and deaminooxytocin. An exchange of the aqueous medium by mineral oil allows monitoring the displacement of the peptides from their receptor compartment in absence of free diffusion transport between tissue and organ medium. Exponential analysis of the data from the uterotonic decay phase allows several inferences to be drawn: 1) Transport rate constants (roughly equal for the two peptides) are higher than rate constants of (irreversible) elimination from the receptor compartment...
January 5, 2018: Biochemical Pharmacology
Ankita Misra, Prem Prakash, Hobby Aggarwal, Priyanka Dhankani, Sachin Kumar, Chandra Prakash Pandey, Nicholas Pugh, Dominique Bihan, Manoj Kumar Barthwal, Richard W Farndale, Dinesh Kumar Dikshit, Madhu Dikshit
Pharmacological inhibition of platelet collagen interaction is a promising therapeutic strategy to treat intra-vascular thrombosis. S007-867 is a novel synthetic inhibitor of collagen-induced platelet aggregation. It has shown better antithrombotic protection than aspirin and clopidogrel with minimal bleeding tendency in mice. The present study is aimed to systematically investigate the antithrombotic efficacy of S007-867 in comparison to aspirin and clopidogrel in vivo and to delineate its mechanism of action in vitro...
January 5, 2018: Biochemical Pharmacology
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