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Basic & Clinical Pharmacology & Toxicology

Ali Kermanizadeh, Klaus Villadsen, Ragnhild G Østrem, Knud J Jensen, Peter Møller, Steffen Loft
Utilisation of functionalized liposomes as the means of targeted delivery of therapeutics may enhance specific transport of biologically active drugs to target tissues, while avoiding or reducing undesired side effects. In the present investigation, peptide-conjugated cationic liposomes were constructed with the aim of targeting integrins (i.e. vitronectin and/or fibronectin receptors) on activated endothelial cells. The peptide-conjugated liposomes induced only cytotoxicity at the highest concentration in non-activated or activated endothelial cells, as well as in co-culture of endothelial cells and macrophages...
October 21, 2016: Basic & Clinical Pharmacology & Toxicology
Maria Zhivagui, Michael Korenjak, Jiri Zavadil
Mutation spectra in cancer genomes provide information on the disease aetiology and the causality underlying the evolution and progression of cancer. Genome-wide mutation patterns reflect the effects of mutagenic insults and can thus reveal past carcinogen-specific exposures and inform hypotheses on the causative factors for specific cancer types. In order to identify mutation profiles in human cancers, single genes studies were first employed, focusing mainly on the tumour suppressor gene TP53. Furthermore, experimental studies had been developed in model organisms...
October 18, 2016: Basic & Clinical Pharmacology & Toxicology
Leanne Stannard, Shareen H Doak, Ann Doherty, Gareth J Jenkins
Humans are exposed to carcinogens through air, water, food and tobacco smoke. Nickel chloride (NiCl2 ) is a toxic and carcinogenic environmental and occupational pollutant, which was previously classified as a non-genotoxic carcinogen, and thought to not directly alter the DNA. Non-genotoxic carcinogens like NiCl2 are difficult to detect in vitro, hence a heavy reliance on animal studies exists. NiCl2 has previously been classified as a non-genotoxic carcinogen (NGTC); however, after studying the effect of NiCl2 on many mechanistic endpoints, it has become clear that NiCl2 behaves more like a genotoxic carcinogen...
October 17, 2016: Basic & Clinical Pharmacology & Toxicology
Yaping Zhang, Wei Zhang, Lars Edvinsson, Cang-Bao Xu
Abnormal contraction of vessels termed "vasospasm" is associated with various cardiovascular diseases. Smoking is a well-known risk factor that increases vasospasm. However, the molecular mechanisms by which smoking leads to vasospasm and cardiovascular disease are not fully understood. The present study was designed to examine if DMSO-extracted cigarette smoke particles (DSP) could induce up-regulation of vascular endothelin type A (ETA ) receptors, and if ETA receptor is up-regulated through activation of extracellular regulated protein kinase 1 and 2 (ERK1/2) signal pathways...
October 12, 2016: Basic & Clinical Pharmacology & Toxicology
Hongwen Cao, Yigeng Feng, Lei Chen
As the main component of realgar, arsenic sulfide (As4 S4 ) contains anti-tumour activity by repressing cancer cell proliferation and migration in many tumours. However, the detailed mechanism of these processes is not clear yet. MicroRNAs (miRNAs) can function as tumour suppressor or oncogene based on their target mRNAs in different tumour tissues. Here, we found that As4 S4 could repress the over-expression of microRNA-372 (miR-372) in two prostate cancer cell lines and its over-expression promoted cell proliferation and migration...
October 12, 2016: Basic & Clinical Pharmacology & Toxicology
Yang Quan-Jun, Zhang Jian-Ping, Zhang Jian-Hua, Han Yong-Long, Xin Bo, Zhang Jing-Xian, Dai Bona, Zhang Yuan, Guo Cheng
Inhaled budesonide and salbutamol represent the most important and frequently used drugs in asthmatic children during acute exacerbation. However, there is still no consensus about their resulting metabolic derangements; thus, the present study was conducted to determine the distinct metabolic profiles of these two drugs. A total of 69 children with asthma during acute exacerbation were included, and their serum and urine were investigated using high-resolution nuclear magnetic resonance (NMR). A metabolomics analysis was performed using a principal component analysis and orthogonal signal correction-partial least squares using SIMCA-P...
October 12, 2016: Basic & Clinical Pharmacology & Toxicology
Kylie Mueller, Nijole Bernaitis, Tony Badrick, Shailendra Anoopkumar-Dukie
The HAS-BLED model is widely utilised to assess patients' bleed risk prior to anticoagulant therapy including warfarin. Some of the variables assessed in the model are also known to influence warfarin control, commonly measured by time in therapeutic range (TTR). The aim of the study was to determine if the HAS-BLED risk tool is a good predictor of bleed risk and warfarin control in deep vein thrombosis (DVT) patients. Retrospective data were collected for DVT warfarin care patients at Sullivan Nicolaides Pathology...
October 8, 2016: Basic & Clinical Pharmacology & Toxicology
Solveig Sakshaug, Marte Handal, Vidar Hjellvik, Christian Berg, Åse Ripel, Ingebjørg Gustavsen, Jørg Mørland, Svetlana Skurtveit
Benzodiazepine-like drugs (z-hypnotics) are the most commonly used drugs for treatment of insomnia in Norway. Z-hypnotics are recommended for short-term treatment not exceeding 4 weeks. We aimed to study the use of z-hypnotics in the adult population in Norway with focus on recurrent use in new users, treatment intensity and co-medication with benzodiazepines and opioids in long-term users. Data were obtained from the Norwegian Prescription Database. New users in 2009 were followed through 2013. Recurrent z-hypnotic use was defined as new fillings at least once in each of the four 365-day follow-up periods...
October 7, 2016: Basic & Clinical Pharmacology & Toxicology
Gustavo H Oliveira-Paula, Marcelo R Luizon, Riccardo Lacchini, Vanessa Fontana, Pamela S Silva, Celso Biagi, E Tanus-Santos
Protein kinase C (PKC) signaling is critically involved in the control of blood pressure. Angiotensin-converting enzyme inhibitors (ACEi) affect PKC expression and activity, which are partially associated with thel responses to ACEi. We examined whether PRKCA (Protein Kinase C, Alpha) polymorphisms (rs887797 C>T, rs1010544 T>C, and rs16960228 G>A), or haplotypes, and gene-gene interactions within the ACEi pathway affect the antihypertensive responses in 104 hypertensive patients treated with enalapril as monotherapy...
October 1, 2016: Basic & Clinical Pharmacology & Toxicology
Kim Brøsen, Stig Ejdrup Andersen, Jeanett Borregaard, Hanne Rolighed Christensen, Palle Mark Christensen, Kim Peder Dalhoff, Per Damkier, Jesper Hallas, Jens Heisterberg, Niels Jessen, Gesche Jürgens, Jens Peter Konnerup Kampmann, Britt Elmedal Laursen, Torben Laursen, Lars Peter Nielsen, Birgitte Klindt Poulsen, Henrik Enghusen Poulsen, Ljubica Vukelic Andersen, Thomas Senderovitz, Jesper Sonne
The Danish Society of Clinical Pharmacology was founded in 1976, and mainly thanks to the persistent efforts of the Society, clinical pharmacology became an independent medical speciality in Denmark in 1996. Since then, clinical pharmacology has gone from strength to strength. In the Danish health care system, clinical pharmacology has established itself as an indispensible part of the efforts to promote the rational, safe and economic use of drugs. Clinical pharmacologists are active in drug committees in both hospitals and in the primary sector...
September 29, 2016: Basic & Clinical Pharmacology & Toxicology
Junfang Zhao, Zhiyang Zeng, Jialiang Sun, Yuanjin Zhang, Dali Li, Xueli Zhang, Mingyao Liu, Xin Wang
P-glycoprotein (P-gp), an important efflux transporter in intestine, regulates the bioavailability of orally taken drugs. To develop an in vitro model that preferably mimics the physiological microenvironment of human intestine, we employed the three-dimensionally (3D) cultured organoids from human normal small intestinal epithelium. It was observed that the intestinal crypts could efficiently form cystic organoid structure with the extension of culture time. Furthermore, the physiological express of ABCB1 was detected at both mRNA and protein levels in cultured organoids...
September 22, 2016: Basic & Clinical Pharmacology & Toxicology
Raul Hernandes Bortolin, Francisco Paulo Freire Neto, Carlos Alberto Arcaro Filho, João Felipe Bezerra, Flávio Santos da Silva, Marcela Abott Galvão Ururahy, Karla Simone da Costa Souza, Valeria Morgiana Gualberto Duarte Moreira Lima, André Ducati Luchessi, Francisco Pignataro Lima, Marcus Vinicius Lia Fook, Bartolomeu Jorge da Silva, Maria das Graças Almeida, Bento João Abreu, Luciana Augusto de Rezende, Adriana Augusto de Rezende
Type 1 diabetes mellitus (T1DM) is associated with several skeletal alterations, particularly in conditions of poor glycaemic control. Insulin therapy is the major conservative treatment for T1DM; however, the effects of this hormone on bone markers of T1DM rats are limited, and the regulatory mechanisms remain elusive. Therefore, the evaluation of molecular and non-molecular parameters in a chronic animal model of T1DM-induced bone loss, treated with and without insulin, may help in elucidating insulin mechanisms...
September 21, 2016: Basic & Clinical Pharmacology & Toxicology
Yuanchao Cao, Xinsheng Wang, Shenqian Li, Hongqiang Wang, Lei Yu, Peitao Wang
In order to explore the possibility of L-carnitine (LC) as a protector of male fertility in chemotherapy, we observed the damage of cyclophosphamide (CTX) to Sertoli cells and the protective effect of LC on the testis Sertoli cells from such damage in this study. Healthy adult male mice were divided into three groups. Chemotherapy group were injected intraperitoneally with the CTX; Protective agent group were injected both LC and CTX; Control group mice were injected only with isochoric physiological saline; all once a day for 5 days...
September 21, 2016: Basic & Clinical Pharmacology & Toxicology
Tim Schutte, Jelle Tichelaar, Prabath Nanayakkara, Milan Richir, Michiel van Agtmael
Given the increasing healthcare costs of an ageing population, there is growing interest in rational prescribing, which takes costs of medication into account. We aimed to gain insight into the attitude to and knowledge of medication costs of medical students and doctors in daily practice. This was a cross-sectional electronic survey among medical students (bachelor/master) and doctors (consultants/registrars). Attitude to costs was evaluated using a cost-consciousness scale. In open questions, the participants estimated the cost of commonly prescribed (generic/non-generic) drugs (including separate pharmacy dispensing costs)...
September 17, 2016: Basic & Clinical Pharmacology & Toxicology
Jinju Guk, Hankil Son, Dong Woo Chae, Kyungsoo Park
Megestrol acetate, an appetite stimulant with low bioavailability, shows increased bioavailability when taken together with food. However, the pharmacokinetic characteristics of megestrol acetate and its relation with food are not well understood. This study aimed to investigate the food effect on the pharmacokinetics (PK) of the recently developed nano-crystallized megestrol acetate (NCMA), using a model-based approach. Data were obtained from an NCMA PK study consisting of a single dose in fasting (39 individuals) and fed conditions (40 individuals)...
September 17, 2016: Basic & Clinical Pharmacology & Toxicology
Cristina Lemini, María Estela Avila, Martha Medina, Carlos Sánchez, Alejandra Figueroa, Juana García-Mondragón, Arsenio Vargas-Vázquez, Alejandro Jiménez-Orozco
The 17β-aminoestrogens (AEs) prolame, butolame and pentolame are weakly oestrogenic in rodents and display anticoagulant properties in contrast to oestradiol (E2 ) which presents procoagulant effects, potentially thrombogenic. They possess anti-anxiety and anti-depressive properties, being good candidates for menopausal hormone therapy. Their capability to induce proliferation of MCF-7 human breast cancer cells, which proliferative rate depends on oestrogens, has not been explored; thus, the aim of this work was to characterize it...
September 16, 2016: Basic & Clinical Pharmacology & Toxicology
Wan-Su Park, Seunghoon Han, Jongtae Lee, Taegon Hong, Jonghwa Won, Yangmi Lim, Kyuhyun Lee, Han Yeul Byun, Dong-Seok Yim
GC1118 is an anti-epidermal growth factor receptor (EGFR) monoclonal antibody that is currently under clinical development. In this study, the pharmacokinetics (PK) of GC1118 were modelled in monkeys to predict human PK and receptor occupancy (RO) profiles. The serum concentrations of GC1118 and its comparator (cetuximab) were assessed in monkeys with a non-compartmental analysis and a target-mediated drug disposition (TMDD) model following intravenous infusion (3-25 mg/kg) of these drugs. The scaling exponent of the EGFR synthesis rate was determined using a sensitivity analysis...
September 16, 2016: Basic & Clinical Pharmacology & Toxicology
Fabien Cusin, Liliana Fernandes Azevedo, Pierre Bonnaventure, Jules Desmeules, Youssef Daali, Catherine M Pastor
Peroperative imaging with indocyanin green (ICG) is developing to increase safety in dissecting anatomical structures during hepatobiliary surgery. Images obtained with the fluorescence camera rely on concentrations measured in liver regions of interest. However, how ICG sinusoidal uptake and hepatocyte elimination rates generate ICG hepatocyte concentrations is largely unknown. To investigate such issue and better understand the role of membrane transporters in generating ICG hepatocyte concentrations, we perfused ICG in livers isolated from normal livers...
September 14, 2016: Basic & Clinical Pharmacology & Toxicology
Filip Rendel, Christina Fjaeraa Alfredsson, Carl-Gustaf Bornehag, Birgitta E Sundström, Eewa Nånberg
Neuropeptide Y (NPY) is an abundant neuropeptide in the mammalian brain important for behavioural consequences of stress and energy metabolism. We have addressed possible effects of the phthalate DiNP on NPY expression in human SH-SY5Y cells, a neuronal in vitro differentiation model. Pico- to nanomolar doses of DiNP and its metabolite MiNP resulted in decreased NPY mRNA and peptide expression in retinoid-differentiated cells. Thus, dys-regulated NPY may be an adverse outcome for exposure to low doses of DiNP in human beings...
September 13, 2016: Basic & Clinical Pharmacology & Toxicology
Ricardo Basto Souza, Annyta Fernandes Frota, Rayane Siqueira Sousa, Nayara Araújo Cezario, Tarcizio Brito Santos, Luziana Mara Frota Souza, Chistiane Oliveira Coura, Valdécio Silvano Monteiro, Gerardo Cristino Filho, Silvânia Maria Mendes Vasconcelos, Rodrigo Maranguape Silva da Cunha, Lissiana Magna Vasconcelos Aguiar, Norma Maria Barros Benevides
Parkinson's disease (PD) is a multifactorial disease associated with the degeneration of dopaminergic neurons and behavioural alterations. Natural bioactive compounds may provide new therapeutic alternatives for neurodegenerative disorders, such as PD. The sulphated polysaccharides isolated from marine algae are heterogenic molecules that show different biological activities. The red marine alga Gracilaria cornea has a sulphated polysaccharide (SA-Gc) with structure and anti-inflammatory and antinociceptive activities reported in the literature...
September 9, 2016: Basic & Clinical Pharmacology & Toxicology
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