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https://www.readbyqxmd.com/read/28805879/downregulation-of-hepatic-multi-drug-resistance-protein-1-mdr1-after-copper-exposure
#1
Sara Reinartz Groba, Sarah Guttmann, Christoph Niemietz, Friedrich Bernick, Vanessa Sauer, Oliver Hachmöller, Uwe Karst, Hans Zischka, Andree Zibert, Hartmut H Schmidt
Copper homeostasis is strictly regulated in mammalian cells. We investigated the adaptation of hepatocytes after long-term copper exposure. Copper-resistant hepatoma HepG2 cell lines lacking ATP7B were generated. Growth, copper accumulation, gene expression, and transport were determined. Hepatocyte-like cells derived from a Wilson disease (WD) patient and the liver of a WD animal model were also studied. The rapidly gained copper resistance was found to be stable, as subculturing of cells in the absence of added copper (weaning) did not restore copper sensitivity...
August 14, 2017: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/28799516/antiepileptic-drugs-in-clinical-development-differentiate-or-die
#2
Gaetano Zaccara, D Schmidt
BACKGROUND: Animal models when carefully selected, designed and conducted, are important parts of any translational drug development strategy. However, research of new compounds for patients with drug-resistant epilepsies is still based on animal experiments, mostly in rodents, which are far from being a model of chronic human epilepsy and have failed to differentiate the efficacy of new compounds versus standard drug treatment. Objective The objective was identification and description of compounds in clinical development in 2016...
August 9, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28795912/effects-of-verapamil-on-the-pharmacokinetics-of-dihydromyricetin-in-rats-and-its-potential-mechanism
#3
Yixiang Huang, Junyong Zhao, Wei Jian, Gang Wang
1. This study investigates the effects of verapamil on the pharmacokinetics of dihydromyricetin in rats and clarifies its main mechanism. 2. The pharmacokinetic profiles of oral or intravenous administration of dihydromyricetin in Sprague-Dawley rats with or without pretreatment with verapamil were investigated. In addition, the effects of verapamil on the transport and metabolic stability of dihydromyricetin were investigated using Caco-2 cell transwell model and rat liver microsomes. 3. In oral group, verapamil could significantly increase Cmax, and decrease oral clearance of dihydromyricetin (P < 0...
August 10, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28792461/interaction-of-flavonoids-from-woodwardia-unigemmata-with-bovine-serum-albumin-bsa-application-of-spectroscopic-techniques-and-molecular-modeling-methods
#4
Rui Ma, Hong Pan, Tao Shen, Peng Li, Yanan Chen, Zhenyu Li, Xiaxia Di, Shuqi Wang
Phytochemical investigation on the methanol extract of Woodwardia unigemmata resulted in the isolation of seven flavonoids, including one new flavonol acylglycoside (1). The structures of these compounds were elucidated on the basis of extensive spectroscopic analysis and comparison of literature data. The multidrug resistance (MDR) reversing activity was evaluated for the isolated compounds using doxorubicin-resistant K562/A02 cells model. Compound 6 showed comparable MDR reversing effect to verapamil. Furthermore, the interaction between compounds and bovine serum albumin (BSA) was investigated by spectroscopic methods, including steady-state fluorescence, synchronous fluorescence, circular dichroism (CD) spectroscopies, and molecular docking approach...
August 9, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28782465/pyramidatine-z88-sensitizes-vincristine-resistant-human-oral-cancer-kb-vcr-cells-to-chemotherapeutic-agents-by-inhibition-of-p-glycoprotein
#5
Zulong Liu, Hengrui Zhu, Shijin Qu, Lisha Tang, Lihuan Cao, Wenbo Yu, Xianmei Yang, Songmin Jiang, Dayuan Zhu, Changheng Tan, Long Yu
Multi-drug resistance (MDR) to anticancer drugs remains a major impediment in cancer therapy. A major goal for scientists is to identify more effective compounds that are able to circumvent MDR and simultaneously have minimal adverse side effects. Here, we reported that Pyramidatine (Z88), a cinnamic acid-derived bisamide compound isolated from the leaves of Aglaia perviridis, had potent anti-MDR activity. The average resistant fold (RF) of Z88 is 0.09 and 0.51 in KB/VCR (vincristine-resistant human oral cancer cells) and MCF-7/ADR (adriamycin-resistant human breast adenocarcinoma) cells...
August 3, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28781802/sorafenib-induced-reversible-posterior-leukoencephalopathy-in-patients-with-renal-cell-carcinoma-a-report-of-two-cases
#6
Nobuki Furubayashi, Takahito Negishi, Hidenori Iwai, Kei Nagase, Motonobu Nakamura
Reversible posterior leukoencephalopathy syndrome (RPLS) is a rare clinicoradiological syndrome that is characterized by neurological symptoms, including seizures, headaches, visual abnormalities, confusion and encephalopathy, accompanied by vasogenic edema of the posterior white matter observed on neuroimaging. Sorafenib is an inhibitor of pro-angiogenic receptor tyrosine kinases, such as vascular endothelial growth factor receptor 2, platelet-derived growth factor receptor β, and vascular endothelial growth factor receptor 3...
August 2017: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/28776672/mechanisms-involved-in-the-cytotoxic-action-of-brazilian-propolis-and-caffeic-acid-against-hep-2-cells-and-modulation-of-p-glycoprotein-activity
#7
Lívia M da Silva, Yahima Frión-Herrera, Ariane R Bartolomeu, Carolina Mendonça Gorgulho, José M Sforcin
OBJECTIVES: The effects of propolis and phenolic compounds (caffeic acid - Caf; dihydrocinnamic acid - Cin; p-coumaric acid - Cou) in the same quantity found in our propolis sample were investigated on human laryngeal epidermoid carcinoma (HEp-2) cells. METHODS: Cell viability, apoptosis/necrosis and cell cycle arrest, P53 and CASPASE-3 gene expression, generation of reactive oxygen species (ROS) and the ability of propolis to induce doxorubicin (DOX) efflux using a P-glycoprotein (P-gp) inhibitor (verapamil) were assayed...
August 4, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28773131/study-of-adsorption-and-desorption-performances-of-zr-based-metal-organic-frameworks-using-paper-spray-mass-spectrometry
#8
Xiaoting Wang, Ying Chen, Yajun Zheng, Zhiping Zhang
The dynamic pore systems and high surface areas of flexible metal-organic framework materials make them excellent candidates to be used in different kinds of adsorption processes. However, the adsorption and desorption behaviors of therapeutic drugs on metal-organic frameworks in solution are not fully developed. Here, we systematically investigated the adsorption and desorption behaviors of a typical therapeutic drug, verapamil, over several Zr-based metal-organic frameworks [e.g., Zr-FUM, UiO-66(Zr), UiO-66(Zr)-NH₂ and UiO-66(Zr)-2COOH] as well as ZrO₂ in an acetonitrile solution by using paper spray mass spectrometry...
July 8, 2017: Materials
https://www.readbyqxmd.com/read/28769742/reproducibility-of-quantitative-brain-imaging-using-a-pet-only-and-a-combined-pet-mr-system
#9
Martin L Lassen, Otto Muzik, Thomas Beyer, Marcus Hacker, Claes Nøhr Ladefoged, Jacobo Cal-González, Wolfgang Wadsak, Ivo Rausch, Oliver Langer, Martin Bauer
The purpose of this study was to test the feasibility of migrating a quantitative brain imaging protocol from a positron emission tomography (PET)-only system to an integrated PET/MR system. Potential differences in both absolute radiotracer concentration as well as in the derived kinetic parameters as a function of PET system choice have been investigated. Five healthy volunteers underwent dynamic (R)-[(11)C]verapamil imaging on the same day using a GE-Advance (PET-only) and a Siemens Biograph mMR system (PET/MR)...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28768994/influx-transport-of-cationic-drug-at-the-blood-retinal-barrier-impact-on-the-retinal-delivery-of-neuroprotectants
#10
Yoshiyuki Kubo, Shin-Ichi Akanuma, Ken-Ichi Hosoya
The retina is a tissue essential for vision, and the blood-retina barrier (BRB) helps to maintain an optimal microenvironment for the neural system in the retina. Recent findings concerning the BRB showed the involvement of transporters at the inner and outer BRB in drug and nutrient transport, suggesting their utility in the development of novel drug delivery systems to the retina. An in vitro-in vivo relationship study of permeability suggested the influx transport of verapamil, a cationic drug, across the BRB, and further in vivo and in vitro studies of cationic drugs, such as verapamil, propranolol and clonidine, revealed the involvement of carrier-mediated process in their influx transport at the BRB...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28760606/synthesis-analytical-characterization-and-capillary-electrophoretic-use-of-the-single-isomer-heptakis-6-o-sulfobutyl-beta-cyclodextrin
#11
Milo Malanga, Ida Fejős, Erzsébet Varga, Gábor Benkovics, András Darcsi, Julianna Szemán, Szabolcs Béni
This contribution reports the synthesis, characterization and capillary electrophoretic application of heptakis-(6-O-sulfobutyl-ether)-β-cyclodextrin sodium salt, (6-(SB)7-β-CD). The compound was obtained through a five-steps synthesis and it represents the first example of single-isomer sulfobutylated cyclodextrin that carries the negatively charged functions exclusively on its primary side and it is unmodified on the lower rim. The purity of each intermediate was determined by appropriate liquid chromatographic methods, while the isomeric purity of the final product was established by an ad-hoc developed HPLC method based on a CD-Screen-IEC column...
July 21, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28760594/s-oxiracetam-protect-against-ischemic-stroke-via-alleviating-blood-brain-barrier-dysfunction-in-rats
#12
Liangliang Huang, Erxin Shang, Wenxiang Fan, Xiang Li, Binbin Li, Shucheng He, Yuxin Fu, Yizhi Zhang, Yunman Li, Weirong Fang
The blood brain barrier (BBB) maintains the basic stability of the brain tissue under physiological conditions, while destroys and exaggerates brain edema and inflammatory response after ischemic stroke. In this study, we researched S-oxiracetam (S-ORC), a nootropic drug, alleviates BBB dysfunction and protects against ischemic stroke in rats. Middle cerebral artery occlusion(MCAO)/reperfusion in rats is applied to mimic ischemic stroke. One hour after reperfusion, rats are administered intravenously with different dose (0...
July 29, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28757552/effects-of-p-glycoprotein-on-the-transport-of-dl0410-a-potential-multifunctional-anti-alzheimer-agent
#13
Xiaocong Pang, Lin Wang, De Kang, Ying Zhao, Song Wu, Ai-Lin Liu, Guan-Hua Du
In our study, we attempted to investigate the influences of P-glycoprotein (P-gp) on DL0410, a novel synthetic molecule for Alzheimer's disease (AD) treatment, for intestinal absorption and blood-brain barrier permeability in vitro and related binding mechanisms in silico. Caco-2, MDCK, and MDCK-MDR1 cells were utilized for transport studies, and homology modelling of human P-gp was built for further docking study to uncover the binding mode of DL0410. The results showed that the apparent permeability (Papp) value of DL0410 was approximately 1 × 10(-6) cm/s, indicating the low permeability of DL0410...
July 25, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28755970/differences-of-first-pass-effect-in-the-liver-and-intestine-contribute-to-the-stereoselective-pharmacokinetics-of-rhynchophylline-and-isorhynchophylline-epimers-in-rats
#14
Xin Wang, Mei Zheng, Jia Liu, Zhifeng Huang, Yidan Bai, Zhuoying Ren, Ziwen Wang, Yangli Tian, Zhou Qiao, Wenyuan Liu, Feng Feng
ETHNOPHARMACOLOGICAL RELEVANCE: Uncaria rhynchophylla (Miq.) Miq. ex Havil., is a plant species used in traditional Chinese medicine to treat cardiovascular and central nervous system diseases. Rhynchophylline (RIN) and isorhynchophylline (IRN), a pair of epimers, are major alkaloids isolated from U. rhynchophylla and exhibit diverse pharmacological effects. Our previous study demonstrated that the pharmacokinetics of these epimers existed stereoselectivity after oral administration; however, the specific mechanism remains unknown and merits investigation...
July 26, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28754855/pleiotrophin-promotes-chemoresistance-to-doxorubicin-in-osteosarcoma-by-upregulating-p-glycoprotein
#15
Dapeng Wu, Liguo Liu, Xuebing Yan, Chunyan Wang, Yaling Wang, Kun Han, Shuchen Lin, Zhihua Gan, Daliu Min
Chemoresistance is a major hindrance to successful treatment of osteosarcoma (OS). Pleiotrophin (PTN), a neurotrophic growth factor, has been linked to the malignant characteristics of various cancer types. We retrospectively examined the correlation between PTN expression and chemoresistance in OS in a cohort of 133 OS patients. Immunohistochemistry revealed that PTN expression correlated with the necrosis rate and local OS recurrence. In a prognostic analysis, high PTN expression was associated with poor overall and disease-free survival, and was an independent adverse prognostic factor for disease-free survival...
July 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28754376/characterization-of-mxr-activity-in-the-sea-anemone-bunodosoma-cangicum-exposed-to-copper
#16
Vanessa Abelaira Anjos, Juliana Zomer Sandrini, Cláudia Bueno Reis Martinez, Marta Marques Souza
Transmembrane proteins of the ABC family contribute to a multiple xenobiotic resistance (MXR) phenotype in cells, driving the extrusion of toxic substances. This phenotype promotes a high degree of protection against xenobiotics. The present study provides a better understanding of the MXR activity in the podal disk cells of Bunodosoma cangicum exposed to copper, and further establishes the relationship between protein activity (measured by accumulation of rhodamine-B) and bioaccumulation of copper in these cells...
July 25, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28751069/activity-dependent-brain-derived-neurotrophic-factor-release-is-required-for-the-rapid-antidepressant-actions-of-scopolamine
#17
Sriparna Ghosal, Eunyoung Bang, Wenzhu Yue, Brendan D Hare, Ashley E Lepack, Matthew J Girgenti, Ronald S Duman
BACKGROUND: Brain-derived neurotrophic factor (BDNF) plays a key role in the pathophysiology and treatment of depression. Recent clinical studies demonstrate that scopolamine, a nonselective muscarinic acetylcholine receptor antagonist, produces rapid antidepressant effects in patients with depression. Rodent studies demonstrate that scopolamine increases glutamate transmission and synaptogenesis in the medial prefrontal cortex (mPFC). Here we tested the hypothesis that activity-dependent BDNF release within the mPFC is necessary for the antidepressant actions of scopolamine...
June 23, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28751012/the-j-to-t-peak-interval-as-a-biomarker-in-drug-safety-studies-a-method-of-accuracy-assessment-applied-to-two-algorithms
#18
W Brian Chiu, Johan de Bie, David W Mortara
OBJECTIVES: To evaluate performance of J-to-T-peak (JTP) measurements of 12-lead ECGs, in a five-arm study using drugs with various levels of electrolyte channel block. METHODS: The novel evaluation method distinguishes between different aspects of measurement. "Random noise" is the variability among repeated measurements made without changing the conditions. "Context noise" is the variability of changes in context of the measurement, e.g. T-wave morphology, autonomic nervous system state...
July 12, 2017: Journal of Electrocardiology
https://www.readbyqxmd.com/read/28745128/the-permeability-characteristics-and-interaction-of-main-components-from-si-ni-san-in-a-mdck-epithelial-cell-monolayer-model
#19
Ruonan Chen, Chenlin Shen, Qingqing Xu, Yaru Liu, Bo Li, Cheng Huang, Taotao Ma, Xiaoming Meng, Maomao Wu, Jun Li
1. Si-Ni-San (SNS) possesses extensive therapeutic effects, however, the extent to which main components are absorbed and the mechanisms involved are controversial. 2. In this study, MDCK cell model was used to determine the permeability characteristics and interaction between the major components of Si-Ni-San, including saikosaponin a, paeoniflorin, naringin and glycyrrhizic acid. 3. The transport of the major components was concentration-dependent in both directions. Moreover, the transport of paeoniflorin, naringin and glycyrrhizic acid was significantly reduced at 4°C or in the presence of NaN3...
July 26, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28744308/recent-pathophysiological-aspects-of-peyronie-s-disease-role-of-free-radicals-rationale-and-therapeutic-implications-for-antioxidant-treatment-literature-review
#20
REVIEW
Gianni Paulis, Gennaro Romano, Luca Paulis, Davide Barletta
Peyronie's disease (PD) is a chronic inflammation of tunica albuginea of the corpora cavernosa that causes an inelastic plaque resulting in penis deformation. Although its etiology is not completely known, there is general consensus that PD is genetically transmitted and secondary to penile trauma. In recent years, numerous studies demonstrated the role played by oxidative stress in PD pathogenesis, and other studies have described successful use of antioxidants in PD treatment. Oxidative stress is an integral part of this disease, influencing its progression...
2017: Advances in Urology
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