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https://www.readbyqxmd.com/read/28231065/exposure-of-children-to-phthalates-and-the-impact-of-consumer-practices-in-slovakia
#1
Miroslava Šidlovská, Ida Petrovičová, Branislav Kolena, Tomáš Pilka, Eva Šovčíková, Tomáš Trnovec
Phthalates are environmental pollutants that can enter the human body by ingestion, inhalation and dermal absorption. Food constitutes the most important source of human exposure to these chemicals. The aim of our study was the biological monitoring of exposure to eight phthalate metabolites in children (n=107), 10-12 years of age, living in eastern Slovakia. Additionally, we analysed some associations between anthropometric measures, questionnaire data (i.e. eating and drinking habits, practice of personal care products) and concentrations of phthalate metabolites...
February 23, 2017: Reviews on Environmental Health
https://www.readbyqxmd.com/read/28230749/design-of-drug-delivery-systems-containing-artemisinin-and-its-derivatives
#2
REVIEW
Blessing Atim Aderibigbe
Artemisinin and its derivatives have been reported to be experimentally effective for the treatment of highly aggressive cancers without developing drug resistance, they are useful for the treatment of malaria, other protozoal infections and they exhibit antiviral activity. However, they are limited pharmacologically by their poor bioavailability, short half-life in vivo, poor water solubility and long term usage results in toxicity. They are also expensive for the treatment of malaria when compared to other antimalarials...
February 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28229138/eawag-soil-in-envipath-a-new-resource-for-exploring-regulatory-pesticide-soil-biodegradation-pathways-and-half-life-data
#3
Diogo A R S Latino, Jörg Wicker, Martin Gütlein, Emanuel Schmid, Stefan Kramer, Kathrin Fenner
Developing models for the prediction of microbial biotransformation pathways and half-lives of trace organic contaminants in different environments requires as training data easily accessible and sufficiently large collections of respective biotransformation data that are annotated with metadata on study conditions. Here, we present the Eawag-Soil package, a public database that has been developed to contain all freely accessible regulatory data on pesticide degradation in laboratory soil simulation studies for pesticides registered in the EU (282 degradation pathways, 1535 reactions, 1619 compounds and 4716 biotransformation half-life values with corresponding metadata on study conditions)...
February 23, 2017: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/28228105/mesenchymal-stromal-cells-as-vehicles-of-tetravalent-bispecific-tandab-cd3-cd19-for-the-treatment-of-b-cell-lymphoma-combined-with-ido-pathway-inhibitor-d-1-methyl-tryptophan
#4
Xiaolong Zhang, Yuanyuan Yang, Leisheng Zhang, Yang Lu, Qing Zhang, Dongmei Fan, Yizhi Zhang, Yanjun Zhang, Zhou Ye, Dongsheng Xiong
BACKGROUND: Although blinatumomab, a bispecific T cell engaging antibody, exhibits high clinical response rates in patients with relapsed or refractory B-precursor acute lymphoblastic leukemia (B-ALL) and B cell non-Hodgkin's lymphoma (B-NHL), it still has some limitations because of its short half-life. Mesenchymal stromal cells (MSCs) represent an attractive approach for delivery of therapeutic agents to cancer sites owing to their tropism towards tumors, but their immunosuppression capabilities, especially induced by indoleamine 2,3-dioxygenase (IDO), should also be taken into consideration...
February 23, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28228077/antioxidant-nanoplatforms-for-dermal-delivery-melatonin
#5
Aroha Belen Sánchez Milán, Ana C Calpena Campmany, Beatriz Clares Naveros
Melatonin (MLT) is emerging as a promising therapeutic agent, mainly due to its role as antioxidant. Substantial evidences show that melatonin is potentially effective on a variety of diseases as cancer, inflammation and neurodegenerative diseases. The excellent antioxidant capacity with pharmacokinetics characteristics and the emerging search for new pharmaceutical nanotechnology based systems, make it particularly attractive to elaborate nanoplatforms based on MLT for biomedical or cosmetic dermal applications...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28225674/inhibiting-plasma-kallikrein-for-hereditary-angioedema-prophylaxis
#6
Aleena Banerji, Paula Busse, Mustafa Shennak, William Lumry, Mark Davis-Lorton, Henry J Wedner, Joshua Jacobs, James Baker, Jonathan A Bernstein, Richard Lockey, H Henry Li, Timothy Craig, Marco Cicardi, Marc Riedl, Ahmad Al-Ghazawi, Carolyn Soo, Ryan Iarrobino, Daniel J Sexton, Christopher TenHoor, Jon A Kenniston, Ryan Faucette, J Gordon Still, Harvey Kushner, Robert Mensah, Chris Stevens, Joseph C Biedenkapp, Yung Chyung, Burt Adelman
Background Hereditary angioedema with C1 inhibitor deficiency is characterized by recurrent, unpredictable swelling episodes caused by uncontrolled plasma kallikrein generation and excessive bradykinin release resulting from cleavage of high-molecular-weight kininogen. Lanadelumab (DX-2930) is a new kallikrein inhibitor with the potential for prophylactic treatment of hereditary angioedema with C1 inhibitor deficiency. Methods We conducted a phase 1b, multicenter, double-blind, placebo-controlled, multiple-ascending-dose trial...
23, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28225020/improved-antitumor-activity-of-trail-fusion-protein-via-formation-of-self-assembling-nanoparticle
#7
Kaizong Huang, Ningjun Duan, Chunmei Zhang, Ran Mo, Zichun Hua
Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) has been known as a promising agent for cancer therapy due to its specific apoptosis-inducing effect on tumor cells rather than most normal cells. However, systemically delivered TRAIL suffers from a rapid clearance from the body with an extremely short half-life. Thermally responsive elastin-like polypeptides (ELPs) are a promising class of temperature sensitive biopolymers based on the structural motif found in mammalian tropoelastin and retain the advantages of polymeric drug delivery systems...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28224326/treatment-with-telmisartan-a-long-acting-angiotensin-ii-receptor-blocker-prevents-migraine-attacks-in-japanese-non-responders-to-lomerizine
#8
Ken Ikeda, Sayori Hanashiro, Yuichi Ishikawa, Masahiro Sawada, Maya Kyuzen, Harumi Morioka, Junya Ebina, Junpei Nagasawa, Masaru Yanagihashi, Ken Miura, Takehisa Hirayama, Takanori Takazawa, Osamu Kano, Kiyokazu Kawabe, Yasuo Iwasaki
Lomerizine, calcium channel blocker, is the most used medication for migraine prophylaxis in Japan. The effectiveness of this drug is reported as 50-75%. Telmisartan is angiotensin II receptor blockers which plasma half-life is 24 h. We examined whether telmisartan has preventative benefits in lomerizine non-responsive migraineurs. Lomerizine non-responders received telmisartan (20 mg/day) for 3 months after the investigation period of 3 months. Blood pressure, frequency of headache days/month, headache severity, and doses of triptans and analgesics were analyzed by Wilcoxon signed rank test...
February 21, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28223717/scale-up-and-pharmacokinetic-study-of-a-novel-mutated-chimeric-tissue-plasminogen-activator-mt-pa-in-rats
#9
Mozhgan Raigani, Mohammad-Reza Rouini, Ali-Akbar Golabchifar, Esmat Mirabzadeh, Behrouz Vaziri, Farzaneh Barkhordari, Fatemeh Davami, Fereidoun Mahboudi
Because of high mortality caused by cardiovascular diseases, various fibrinolytic agents with diverse pharmacokinetic and pharmacodynamic properties have been developed. A novel mutated chimeric tissue plasminogen activator (mt-PA) was developed by the removal of first three domains of t-PA, insertion of GHRP sequence and mutation towards resistance to plasminogen activator inhibitor-1 (PAI-1). Mt-PA protein was expressed in Expi293F cells. The expression level of mt-PA was found to be 5000 IU/mL. Following purification, the pharmacokinetic properties of mt-PA were evaluated in three doses in rats...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28223355/glial-fibrillary-acidic-protein-exhibits-altered-turnover-kinetics-in-a-mouse-model-of-alexander-disease
#10
Laura R Moody, Gregory A Barrett-Wilt, Michael R Sussman, Albee Messing
Mutations in the astrocyte-specific intermediate filament, glial fibrillary acidic protein (GFAP), lead to the rare and fatal disorder, Alexander disease (AxD). A prominent feature of the disease is aberrant accumulation of GFAP. It has been proposed that this accumulation occurs due to an increase in gene transcription coupled with impaired proteasomal degradation, yet this hypothesis remains untested. We therefore sought to directly investigate GFAP turnover in a mouse model of AxD that is heterozygous for a disease-causing point mutation (GfapR236H/+) (and thus expresses both wild-type and mutant protein)...
February 21, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28222395/technetium-99m-radiolabeled-paclitaxel-as-an-imaging-probe-for-breast-cancer-in-vivo
#11
Liziane O F Monteiro, Renata S Fernandes, Luciano C Castro, Valbert N Cardoso, Mônica C Oliveira, Danyelle M Townsend, Alice Ferretti, Domenico Rubello, Elaine A Leite, André L B de Barros
The high incidence and mortality of breast cancer supports efforts to develop innovative imaging probes to effectively diagnose, evaluate the extent of the tumor, and predict the efficacy of tumor treatments while concurrently and selectively delivering anticancer agents to the cancer tissue. In the present study we described the preparation of technetium-99m ((99m)Tc)-labeled paclitaxel (PTX) and evaluated its feasibility as a radiotracer for breast tumors (4T1) in BALB/c mice. Thin Layer Chromatography (TLC) was used to determine the radiochemical purity and in vitro stability of (99m)Tc-PTX...
February 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28222073/a-phase-i-study-of-intravenous-and-oral-rucaparib-in-combination-with-chemotherapy-in-patients-with-advanced-solid-tumours
#12
Richard H Wilson, Tr Jeffry Evans, Mark R Middleton, L Rhoda Molife, James Spicer, Veronique Dieras, Patricia Roxburgh, Heidi Giordano, Sarah Jaw-Tsai, Sandra Goble, Ruth Plummer
BACKGROUND: This study evaluated safety, pharmacokinetics, and clinical activity of intravenous and oral rucaparib, a poly(ADP-ribose) polymerase inhibitor, combined with chemotherapy in patients with advanced solid tumours. METHODS: Initially, patients received escalating doses of intravenous rucaparib combined with carboplatin, carboplatin/paclitaxel, cisplatin/pemetrexed, or epirubicin/cyclophosphamide. Subsequently, the study was amended to focus on oral rucaparib (once daily, days 1-14) combined with carboplatin (day 1) in 21-day cycles...
February 21, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28220555/population-pharmacokinetic-characterization-of-bay-81-8973-a-full-length-recombinant-factor-viii-lessons-learned-importance-of-including-samples-with-factor-viii-levels-below-the-quantitation-limit
#13
D Garmann, S McLeay, A Shah, P Vis, M Maas Enriquez, B A Ploeger
INTRODUCTION: The pharmacokinetics (PK), safety and efficacy of BAY 81-8973, a full-length, unmodified, recombinant human factor VIII (FVIII), were evaluated in the LEOPOLD trials. AIM: The aim of this study was to develop a population PK model based on pooled data from the LEOPOLD trials and to investigate the importance of including samples with FVIII levels below the limit of quantitation (BLQ) to estimate half-life. METHODS: The analysis included 1535 PK observations (measured by the chromogenic assay) from 183 male patients with haemophilia A aged 1-61 years from the 3 LEOPOLD trials...
February 20, 2017: Haemophilia: the Official Journal of the World Federation of Hemophilia
https://www.readbyqxmd.com/read/28220111/identity-abundance-and-reactivation-kinetics-of-thermophilic-fermentative-endospores-in-cold-marine-sediment-and-seawater
#14
Marta Volpi, Bente Aa Lomstein, Andreas Sichert, Hans Røy, Bo B Jørgensen, Kasper U Kjeldsen
Cold marine sediments harbor endospores of fermentative and sulfate-reducing, thermophilic bacteria. These dormant populations of endospores are believed to accumulate in the seabed via passive dispersal by ocean currents followed by sedimentation from the water column. However, the magnitude of this process is poorly understood because the endospores present in seawater were so far not identified, and only the abundance of thermophilic sulfate-reducing endospores in the seabed has been quantified. We investigated the distribution of thermophilic fermentative endospores (TFEs) in water column and sediment of Aarhus Bay, Denmark, to test the role of suspended dispersal and determine the rate of endospore deposition and the endospore abundance in the sediment...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28219473/needham-at-the-crossroads-history-politics-and-international-science-in-wartime-china-1942-1946
#15
Thomas Mougey
In 1946, the British biochemist Joseph Needham returned from a four-year stay in China. Needham scholars have considered this visit as a revelatory period that paved the way for his famous book series Science and Civilization in China (SCC). Surprisingly, however, Needham's actual time in China has remained largely unstudied over the last seventy years. As director of the Sino-British Scientific Cooperation Office, Needham travelled throughout Free China to promote cooperation between British and Chinese scientists to contain the Japanese invasion during the Second World War...
February 21, 2017: British Journal for the History of Science
https://www.readbyqxmd.com/read/28216883/comparative-pharmacokinetic-profiles-of-three-protoberberine-type-alkaloids-from-raw-and-bile-processed-rhizoma-coptidis-in-heat-syndrome-rats
#16
Yuan Zi-Min, Chen Yue, Gao Hui, Lv Jia, Chen Gui-Rong, Jing Wang
BACKGROUND: The Bile-processed Rhizoma coptidis (BRC), which has a colder drug property than Rhizoma coptidis (RC), is widely used for the treatment of heat syndrome. We compared the pharmacokinetics of the protoberberine-type alkaloids in BRC and RC in rats with heat syndrome to elucidate the bile-processing mechanism. MATERIAL AND METHODS: We established a rapid and sensitive method for simultaneously determining three alkaloids: berberine, palmatine, and jatrorrhizine, in rat plasma based on ultra-performance liquid chromatography/tandem mass spectrometry...
January 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28216581/biopharmaceutical-characterization-and-bioavailability-study-of-a-tetrazole-analog-of-clofibric-acid-in-rat
#17
Nancy Vara-Gama, Adriana Valladares-Méndez, Gabriel Navarrete-Vazquez, Samuel Estrada-Soto, Luis Manuel Orozco-Castellanos, Julio César Rivera-Leyva
In the current investigation, the physicochemical, biopharmaceutical and pharmacokinetic characterization of a new clofibric acid analog (Compound 1) was evaluated. Compound 1 showed affinity by lipophilic phase in 1 to 5 pH interval, indicating that this compound would be absorbed favorably in duodenum or jejunum. Also, Compound 1 possess two ionic species, first above of pH 4.43 and, the second one is present over pH 6.08. The apparent permeability in everted sac rat intestine model was 8.73 × 10(-6) cm/s in duodenum and 1...
February 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28216330/-223-ra-dichloride-spectrometric-characterization-searching-for-the-presence-of-long-lived-isotopes-with-radiological-protection-implications
#18
J Sánchez-Jiménez, A López-Montes, L Núñez-Martínez, A Villa-Abaunza, L M Fraile, V Sánchez-Tembleque, J M Udías
(223)Ra-dichloride was approved with the commercial name of Xofigo in 2014 for treatment of metastatic castration-resistant prostate cancer. (223)Ra is obtained by neutron irradiation of (226)Ra yielding (227)Ac, which decays to (227)Th and (223)Fr, both decaying to (223)Ra. Since (223)Ra is predominantly (95.3%) an alpha emitter with a 11.42days long half-life, the radiopharmaceutical, its remnants, the patient, and waste material can be managed and disposed with low radiation protection requirements. (227)Ac is a long-lived (T1/2=21...
February 16, 2017: Physica Medica: PM
https://www.readbyqxmd.com/read/28216314/visual-working-memory-requires-permissive-and-instructive-no-cgmp-signaling-at-presynapses-in-the-drosophila-central-brain
#19
Sara Kuntz, Burkhard Poeck, Roland Strauss
The gaseous second messenger nitric oxide (NO) has been shown to regulate memory formation by activating retrograde signaling cascades from post- to presynapse that involve cyclic guanosine monophosphate (cGMP) production to induce synaptic plasticity and transcriptional changes. In this study, we analyzed the role of NO in the formation of a visual working memory that lasts only a few seconds. This memory is encoded in a subset of ring neurons that form the ellipsoid body in the Drosophila brain. Using genetic and pharmacological manipulations, we show that NO signaling is required for cGMP-mediated CREB activation, leading to the expression of competence factors like the synaptic homer protein...
February 8, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28216260/optimal-expression-of-a-fab-effector-fusion-protein-in-escherichia-coli-by-removing-the-cysteine-residues-responsible-for-an-interchain-disulfide-bond-of-a-fab-molecule
#20
Hyeon-Ju Kang, Hye-Jin Kim, Mun-Sik Jung, Jae-Kyu Han, Sang-Hoon Cha
Development of novel bi-functional or even tri-functional Fab-effector fusion proteins would have a great potential in the biomedical sciences. However, the expression of Fab-effector fusion proteins in Escherichia coli is problematic especially when a eukaryotic effector moiety is genetically linked to a Fab due to the lack of proper chaperone proteins and an inappropriate physicochemical environment intrinsic to the microbial hosts. We previously reported that a human Fab molecule, referred to as SL335, reactive to human serum albumin has a prolonged in vivo serum half-life in rats...
February 16, 2017: Immunology Letters
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