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https://www.readbyqxmd.com/read/29453982/glucagon-like-peptide-1-contributes-to-increases-abca1-expression-by-downregulating-mir-758-to-regulate-cholesterol-homeostasis
#1
Yue Yao, Qiang Li, Ping Gao, Wei Wang, Lili Chen, Jinchao Zhang, Yi Xu
Abnormal regulation of lipid metabolism is associated with type 2 diabetes mellitus (T2DM). GLP-1 as a new treatment for T2DM, has unique effects in modulating cholesterol homeostasis. However, the mechanism of this effect is largely missing. The aim of this study was to determine the effects of GLP-1 on cholesterol-induced lipotoxicity in hepatocytes and examine the underlying mechanisms. The cell viability was determined, and caspase-3 was used to detect the effects of GLP-1 on cholesterol-induced apoptosis...
February 14, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29453250/retinal-chitosan-conjugates-effectively-deliver-active-chromophores-to-retinal-photoreceptor-cells-in-blind-mice-and-dogs
#2
Songqi Gao, Shirin Kahremany, Jianye Zhang, Beata Jastrzebska, Janice Querubin, Simon M Petersen-Jones, Krzysztof Palczewski
The retinoid (visual) cycle consists of a series of biochemical reactions needed to regenerate the visual chromophore, 11-cis-retinal and sustain vision. Genetic or environmental factors affecting chromophore production can lead to blindness. Using animal models that mimic human retinal diseases, we previously demonstrated that mechanism-based pharmacological interventions can maintain vision in otherwise incurable genetic diseases of the retina. Here, we report that after 9-cis-retinal administration to lecithin:retinol acyltransferase-deficient (Lrat-/-) mice, the drug was rapidly absorbed and then cleared within 1-2 h...
February 16, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29453199/simultaneous-assessment-of-clearance-metabolism-induction-and-drug-drug-interaction-potential-using-a-long-term-in-vitro-liver-model-for-a-novel-hepatitis-b-virus-inhibitor
#3
Nicole A Kratochwil, Miriam Triyatni, Martina B Mueller, Florian Klammers, Brian Leonard, Dan Turley, Josephine Schmaler, Aynur Ekiciler, Birgit Molitor, Isabelle Walter, Pierre-Alexis Gonsard, Charles A Tournillac, Alexandre Durrwell, Michaela Marschmann, Russell Jones, Mohammed Ullah, Franziska Boess, Giorgio Ottaviani, Yuyan Yin, Neil J Parrott, Stephen Fowler
Long-term in vitro liver models are now widely explored for human hepatic metabolic clearance prediction, enzyme phenotyping, cross species metabolism, comparison of low clearance drugs as well as induction studies. Here, we present studies using a long-term liver model which show how metabolism and active transport, drug-drug interactions and enzyme induction in healthy and diseased states, e.g. hepatitis B virus (HBV) infection, may be assessed in a single test system to enable effective data integration for PBPK modeling...
February 16, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29453102/preparation-of-plga-rose-bengal-colloidal-particles-by-double-emulsion-and-layer-by-layer-for-breast-cancer-treatment
#4
María F Loya-Castro, Mariana Sánchez-Mejía, Dante R Sánchez-Ramírez, Rossina Domínguez-Ríos, Noé Escareño, Paola E Oceguera-Basurto, Édgar B Figueroa-Ochoa, Antonio Quintero, Alicia Del Toro-Arreola, Antonio Topete, Adrián Daneri-Navarro
The use of colloidal particles (CPs) in the transport of drugs is developing rapidly thanks to its effectiveness and biosafety, especially in the treatment of various types of cancer. In this study Rose Bengal/PLGA CPs synthesized by double emulsion (W/O/W) and by electrostatic adsorption (layer-by-layer), were characterized and evaluated as potential breast cancer treatment. CPs were evaluated in terms of size, zeta potential, drug release kinetics and cell viability inhibition efficacy with the triple negative breast cancer cell line HCC70...
February 7, 2018: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29453086/pegylated-polyaminoacid-capped-mesoporous-silica-nanoparticles-for-mitochondria-targeted-delivery-of-celastrol-in-solid-tumors
#5
Ju Yeon Choi, Biki Gupta, Thiruganesh Ramasamy, Jee-Heon Jeong, Sung Giu Jin, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
The major goal of cancer chemotherapy is to maximize the therapeutic efficacy of anticancer drugs, while minimizing their associated side effects. Celastrol (CST), which is extracted from the traditional Chinese medicinal plant Tripterygium wilfordii, has been reported to exhibit significant anticancer effects in various in vitro and in vivo cancer models. Nanoparticulate drug delivery systems could be employed to preserve and enhance the pharmacological effects of CST in cancer cells. Among these, mesoporous silica nanoparticles (MSNs) are one of the most promising drug delivery systems...
February 11, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29453043/understanding-of-human-atp-binding-cassette-superfamily-and-novel-multidrug-resistance-modulators-to-overcome-mdr
#6
REVIEW
Imran Shair Mohammad, Wei He, Lifang Yin
Indeed, multi-drug resistance (MDR) is a significant obstacle to effective chemotherapy. The overexpression of ATP-binding cassette (ABC) membrane transporters is a principal cause of enhanced cytotoxic drug efflux and treatment failure in various types of cancers. At cellular level, the pumps of ABC family regulate the transportation of numerous substances including drugs in and out of the cells. In past, the overexpression of ABC pumps suggested a well-known mechanism of drug resistance in cancers as well as infectious diseases...
February 13, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29452210/computer-simulations-for-bioequivalence-trials-selection-of-analyte-in-bcs-class-ii-and-iv-drugs-with-first-pass-metabolism-two-metabolic-pathways-and-intestinal-efflux-transporter
#7
V Mangas-Sanjuan, C Navarro-Fontestad, A García-Arieta, I F Trocóniz, M Bermejo
A semi-physiological two compartment pharmacokinetic model with two active metabolites (primary (PM) and secondary metabolites (SM)) with saturable and non-saturable pre-systemic efflux transporter, intestinal and hepatic metabolism has been developed. The aim of this work is to explore in several scenarios which analyte (parent drug or any of the metabolites) is the most sensitive to changes in drug product performance (i.e. differences in in vivo dissolution) and to make recommendations based on the simulations outcome...
February 13, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29451681/verification-of-a-physiologically-based-pharmacokinetic-model-of-ritonavir-to-estimate-drug-drug-interaction-potential-of-cyp3a4-substrates
#8
Ken-Ichi Umehara, Felix Huth, Christina S Won, Tycho Heimbach, Handan He
Ritonavir is one of several ketoconazole alternatives used to evaluate strong CYP3A4 inhibition potential in clinical drug-drug interaction (DDI) studies. In this study, four physiologically-based pharmacokinetic (PBPK) models of ritonavir as an in vivo time-dependent inhibitor of CYP3A4 were created and verified for the oral doses of 20, 50, 100 and 200 mg using fraction absorbed (Fa) and oral clearance (CLoral) values reported in the literature, as transporter and CYP enzyme reaction phenotyping data were not available...
February 16, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29451352/chronic-exposure-of-mice-to-low-doses-of-imazalil-induces-hepatotoxicity-at-the-physiological-biochemical-and-transcriptomic-levels
#9
Cuiyuan Jin, Ting Luo, Zhengwei Fu, Yuanxiang Jin
Imazalil (IMZ), which is a widely used fungicide, can accumulate in the body and threaten an animal's health. However, this fungicide has adverse effects on aquatic organisms and ultimately affects human health when it leaches into the environment. Our research tried to determine that if IMZ might cause liver damage and its potential to cause-related diseases. In this study, male adult C57BL/6 mice were exposed to 0.1, 0.5, or 2.5 mg/kg body weight IMZ in drinking water for 15 weeks. Then, we evaluated the liver damage at the physiological, biochemical, and transcriptome levels in mice after chronic IMZ exposure...
February 16, 2018: Environmental Toxicology
https://www.readbyqxmd.com/read/29451287/computational-identification-of-the-binding-mechanism-of-a-triple-reuptake-inhibitor-amitifadine-for-the-treatment-of-major-depressive-disorder
#10
Weiwei Xue, Panpan Wang, Gao Tu, Fengyuan Yang, Guoxun Zheng, Xiaofeng Li, Xiaoxu Li, Yuzong Chen, Xiaojun Yao, Feng Zhu
Amitifadine, the only drug ever clinically tested in Phase 3 for treating depression, is a triple reuptake inhibitor (TRI) that simultaneously interacts with human monoamine transporters (MATs) including hSERT, hNET and hDAT. This novel multi-target strategy improves drug efficacy and reduces the toxic side effects of drugs. However, the binding modes accounting for amitifadine's polypharmacological mode of action are still elusive, and extensive exploration of the amitifadine-target interactions between amitifadine and MATs is urgently needed...
February 16, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29450934/imaging-proton-transport-in-giant-vesicles-through-cyclic-peptide-polymer-conjugate-nanotube-transmembrane-ion-channels
#11
Jason G Binfield, Johannes C Brendel, Neil R Cameron, Ahmed M Eissa, Sébastien Perrier
Since their discovery in 1993, interest in various aspects of cyclic peptides (CPs) has expanded rapidly. Of particular note is their potential to form artificial ion channels in lipid membranes, an attractive characteristic in supramolecular chemistry and biological research. The design and synthesis of cyclic peptide-polymer conjugates (CPPCs) that can self-assemble within lipid bilayers into nanotubes, mimicking naturally occurring membrane channels and pores, has been reported. However, methods that allow direct detection of the transport process with high levels of certainty are still lacking...
February 16, 2018: Macromolecular Rapid Communications
https://www.readbyqxmd.com/read/29450829/artificial-lipid-membrane-permeability-method-for-predicting-intestinal-drug-transport-probing-the-determining-step-in-the-oral-absorption-of-sulfadiazine-influence-of-the-formation-of-binary-and-ternary-complexes-with-cyclodextrins
#12
Alicia Delrivo, Carolina Aloisio, Marcela R Longhi, Gladys Granero
We propose an in vitro permeability assay by using a modified lipid membrane to predict the in vivo intestinal passive permeability of drugs. Two conditions were tested, one with a gradient pH (pH 5.5 donor/pH 7.4 receptor) and the other with an iso-pH 7.4. The predictability of the method was established by correlating the obtained apparent intestinal permeability coefficients (P app ) and the oral dose fraction absorbed in humans (f a ) of 16 drugs with different absorption properties. The P app values correlated well with the absorption rates under the two conditions, and the method showed high predictability and good reproducibility...
February 15, 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29450657/in-silico-identification-of-small-molecules-as-novel-lxr-agonists-for-the-treatment-of-cardiovascular-disease-and-cancer
#13
Xin Wang, Kaimin Lu, Hao Luo, Danfeng Liang, Xin Long, Yuan Yuan, Chuanfang Wu, Jinku Bao
Liver X receptor (LXR), a member of the nuclear receptor superfamily, mainly serves as a reverse cholesterol transporter in lipid metabolism. It has been demonstrated that LXR is a promising target for the treatment of cardiovascular diseases. LXR is also involved in cancer metabolism, glucose homeostasis, immunity, and various physiological processes. The antitumor function of LXR has become of great interest to researchers in recent years. However, while it is believed that activating LXR with small molecules could be a promising approach to cancer treatment, effective drugs that target LXR are yet to be reported...
February 15, 2018: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/29449184/relation-of-overactive-bladder-with-motor-symptoms-and-dopamine-transporter-imaging-in-drug-na%C3%A3-ve-parkinson-s-disease
#14
Yasunori Mito, Ichiro Yabe, Hiroaki Yaguchi, Toshiki Takei, Satoshi Terae, Yasutaka Tajima
OBJECTIVES: The aim of the present study was to determine the relation of urinary dysfunction with motor symptoms and nigrostriatal neuron loss in drug-naïve patients with Parkinson's disease (PD). We therefore examined the relation of overactive bladder (OAB) symptoms with motor symptoms and striatal dopamine transporter (DAT) binding measured by [123-Iodine]-fluoropropyl-2beta-carbomethoxy-3beta-(4-iodophenylnortropane) dopamine transporter single-photon emission computed tomography ( 123 I-FP-CIT SPECT)...
February 9, 2018: Parkinsonism & related Disorders
https://www.readbyqxmd.com/read/29449138/driving-with-drug-resistant-and-controlled-seizures-from-a-patient-s-perspective-assessment-of-attitudes-and-practices
#15
Lakshman Arcot Jayagopal, Kaeli K Samson, Olga Taraschenko
BACKGROUND: Driving restrictions in epilepsy are intended to safeguard public and personal safety; however, these limitations inhibit socialization, restrict employment, and reduce self-esteem in patients with seizures. A large proportion of patients with seizures continue to drive, and factors leading to noncompliance with driving regulations are poorly understood. Thus, the patients' perspective on driving safety is not incorporated into the existing counseling tools on driving safety in epilepsy...
February 12, 2018: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/29449054/second-generation-antipsychotic-induced-mitochondrial-alterations-implications-for-increased-risk-of-metabolic-syndrome-in-patients-with-schizophrenia
#16
Giselli Scaini, João Quevedo, Dawn Velligan, David L Roberts, Henriette Raventos, Consuelo Walss-Bass
Metabolic syndrome (MetS) is seen more frequently in persons with schizophrenia than in the general population, and these metabolic abnormalities are further aggravated by second generation antipsychotic (SGA) drugs. Although the underlying mechanisms responsible for the increased prevalence of MetS among patients under SGA treatment are not well understood, alterations in mitochondria function have been implicated. We performed a comprehensive evaluation of the role of mitochondrial dysfunction in the pathophysiology of drug-induced MetS in schizophrenia...
February 12, 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29448871/interactions-of-organophosphorus-pesticides-with-solute-carrier-slc-drug-transporters
#17
Lisa Chedik, Arnaud Bruyere, Olivier Fardel
1. Organophosphorus pesticides (OPs) are known to interact with human ATP-binding cassette drug efflux pumps. The present study was designed to determine whether they can also target activities of human solute carrier (SLC) drug transporters. 2. The interactions of thirteen OPs with SLC transporters involved in drug disposition, such as organic cation transporters (OCTs), multidrug and toxin extrusion proteins (MATEs), organic anion transporters (OATs) and organic anion transporting polypeptides (OATPs), were mainly investigated using transporter-overexpressing cell clones and fluorescent or radiolabeled reference substrates...
February 16, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29448866/multifunctional-mesoporous-silica-nanoparticles-as-efficient-transporters-of-doxorubicin-and-chlorin-e6-for-chemo-photodynamic-combinatorial-cancer-therapy
#18
Jing-Hua Sun, Wei Zhang, Dong-Yang Zhang, Jianliang Shen, Cai-Ping Tan, Liang-Nian Ji, Zong-Wan Mao
A multimodal nanocarrier based on mesoporous silica nanoparticles (MSNs) is developed to co-delivery photosensitizer chlorin e6 (Ce6) and chemotherapeutic agent doxorubicin (Dox) for cancer combination therapy. Ce6 was covalently conjugated with mesoporous silica nanoparticles, which could increase the loading efficiency, and allowed for photodynamic therapy. Doxorubicin was loaded into the pores of mesoporous silica nanoparticles to afford the dual drug delivery system Dox@MSNs-Ce6. These hybrid nanoparticles have an average diameter of about 100 nm and slightly negative charge of about -17 mV...
January 1, 2018: Journal of Biomaterials Applications
https://www.readbyqxmd.com/read/29446631/mechanistic-investigation-and-multiplexing-of-liposome-assisted-metabolic-glycan-labeling
#19
Yuting Sun, Senlian Hong, Ran Xie, Rongbing Huang, Ruoxing Lei, Bo Cheng, Deen Sun, Yifei Du, Corwin M Nycholat, James C Paulson, Xing Chen
Metabolic labeling of glycans with bioorthogonal reporters has been widely used for glycan imaging and glycoproteomic profiling. One of the intrinsic limitations of metabolic glycan labeling is the lack of cell-type selectivity. The recently developed liposome-assisted bioorthogonal reporter (LABOR) strategy provides a promising means to overcome this limitation, but the mechanism of LABOR has not been investigated in detail. In this work, we performed a mechanistic study on LABOR and explored its multiplexing capability...
February 15, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29446432/serum-albumin-hydrogels-in-broad-ph-and-temperature-ranges-characterization-of-their-self-assembled-structures-and-nanoscopic-and-macroscopic-properties
#20
S Hamidreza Arabi, Behdad Aghelnejad, Christian Schwieger, Annette Meister, Andreas Kerth, Dariush Hinderberger
We report extended pH- and temperature-induced preparation procedures and explore the materials and molecular properties of different types of hydrogels made from human and bovine serum albumin, the major transport protein in the blood of mammals. We describe the diverse range of properties of these hydrogels at three levels: (1) their viscoelastic (macroscopic) behavior, (2) protein secondary structure changes during the gelation process (via ATR-FTIR spectroscopy), and (3) the hydrogel fatty acid (FA) binding capacity and derive from this the generalized tertiary structure through CW EPR spectroscopy...
February 15, 2018: Biomaterials Science
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