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https://www.readbyqxmd.com/read/28335566/profiling-and-preparation-of-metabolites-from-pyragrel-in-human-urine-by-online-solid-phase-extraction-coupled-with-high-performance-liquid-chromatography-tandem-mass-spectrometry-followed-by-a-macroporous-resin-based-purification-approach
#1
Xin Zhao, Jingjing Jiang, Guang Yang, Jie Huang, Guoping Yang, Guangwei He, Zhaoxing Chu, Taijun Hang, Guorong Fan
Pyragrel, a new anticoagulant drug, is derived from the molecular combination of ligustrazine and ferulic acid. Pyragrel showed significant inhibitory activity against platelet aggregation induced by adenosine diphosphate (ADP), and had been approved for a phase I clinical trial by CFDA. To characterize the metabolites of Pyragrel in human urine after intravenous administration, a reliable online solid-phase extraction couple with high performance liquid chromatography tandem mass spectrometry (online SPE-HPLC-MS(n)) method was conceived and applied...
March 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335525/the-history-of-clotting-factor-concentrates-pharmacokinetics
#2
REVIEW
Massimo Morfini
Clotting factor concentrates (CFCs) underwent tremendous modifications during the last forty years. Plasma-derived concentrates made the replacement therapy feasible not only in the hospital but also at patients' home by on-demand or prophylactic regimen. Virucidal methods, implemented soon after hepatitis and AIDS outbreak, and purification by Mabs made the plasma-derived concentrates safer and purer. CFCs were considered equivalent to the other drugs and general rules and methods of pharmacokinetics (PK) were applied to their study...
March 20, 2017: Journal of Clinical Medicine
https://www.readbyqxmd.com/read/28335470/design-of-new-benzo-h-chromene-derivatives-antitumor-activities-and-structure-activity-relationships-of-the-2-3-positions-and-fused-rings-at-the-2-3-positions
#3
Rawda M Okasha, Fawzia F Alblewi, Tarek H Afifi, Arshi Naqvi, Ahmed M Fouda, Al-Anood M Al-Dies, Ahmed M El-Agrody
A series of novel 4H-benzo[h]chromenes 4, 6-11, 13, 14; 7H-benzo[h]chromeno[2,3-d]pyrimidines 15-18, 20, and 14H-benzo[h]chromeno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 19a-e, 24 was prepared. The structures of the synthesized compounds were characterized on the basis of their spectral data. Some of the target compounds were examined for their antiproliferative activity against three cell lines; breast carcinoma (MCF-7), human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2). The cytotoxic behavior has been tested using MTT assay and the inhibitory activity was referenced to three standard anticancer drugs: vinblastine, colchicine and doxorubicin...
March 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335462/therapeutic-potentials-of-microalgae-in-the-treatment-of-alzheimer-s-disease
#4
REVIEW
Tosin A Olasehinde, Ademola O Olaniran, Anthony I Okoh
Current research is geared towards the discovery of new compounds with strong neuroprotective potential and few or no side effects compared to synthetic drugs. This review focuses on the potentials of extracts and biologically active compounds derived from microalgal biomass for the treatment and management of Alzheimer's disease (AD). Microalgal research has gained much attention recently due to its contribution to the production of renewable fuels and the ability of alga cells to produce several secondary metabolites such as carotenoids, polyphenols, sterols, polyunsaturated fatty acids and polysaccharides...
March 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335253/soft-interaction-in-liposome-nanocarriers-for-therapeutic-drug-delivery
#5
REVIEW
Domenico Lombardo, Pietro Calandra, Davide Barreca, Salvatore Magazù, Mikhail A Kiselev
The development of smart nanocarriers for the delivery of therapeutic drugs has experienced considerable expansion in recent decades, with the development of new medicines devoted to cancer treatment. In this respect a wide range of strategies can be developed by employing liposome nanocarriers with desired physico-chemical properties that, by exploiting a combination of a number of suitable soft interactions, can facilitate the transit through the biological barriers from the point of administration up to the site of drug action...
June 25, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335215/rapamycin-loaded-solid-lipid-nanoparticles-as-a-new-tool-to-deliver-mtor-inhibitors-formulation-and-in-vitro-characterization
#6
Alice Polchi, Alessandro Magini, Jarosław Mazuryk, Brunella Tancini, Jacek Gapiński, Adam Patkowski, Stefano Giovagnoli, Carla Emiliani
Recently, the use of mammalian target of rapamycin (mTOR) inhibitors, in particular rapamycin (Rp), has been suggested to improve the treatment of neurodegenerative diseases. However, as Rp is a strong immunosuppressant, specific delivery to the brain has been postulated to avoid systemic exposure. In this work, we fabricated new Rp loaded solid lipid nanoparticles (Rp-SLN) stabilized with polysorbate 80 (PS80), comparing two different methods and lipids. The formulations were characterized by differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), wide angle X-ray scattering (WAXS), cryo-transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS) and particle tracking...
May 9, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335197/cationic-nanoparticles-assembled-from-natural-based-steroid-lipid-for-improved-intracellular-transport-of-sirna-and-pdna
#7
Ruilong Sheng, Xiaoqing Zhuang, Zhao Wang, Amin Cao, Kaili Lin, Julian X X Zhu
Developing new functional biomaterials from biocompatible natural-based resources for gene/drug delivery has attracted increasing attention in recent years. In this work, we prepared a series of cationic nanoparticles (Diosarg-DOPE NPs) by assembly of a natural steroid diosgenin-based cationic lipid (Diosarg) with commercially-available helper lipid 1,2-dioleoyl-sn-glycero-3-phosphorethanolamine (DOPE). These cationic Diosarg-DOPE NPs were able to efficiently bind siRNA and plasmid DNA (pDNA) via electrostatic interactions to form stable, nano-sized cationic lipid nanoparticles instead of lamellar vesicles in aqueous solution...
April 13, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335102/efficacy-of-a-multiplex-paclitaxel-emission-stent-using-a-pluronic-%C3%A2-mixture-membrane-versus-a-covered-metal-stent-in-malignant-biliary-obstruction-a-prospective-randomized-comparative-study
#8
Sung Ill Jang, Se Joon Lee, Seok Jeong, Don Haeng Lee, Myung-Hwan Kim, Hong Jin Yoon, Dong Ki Lee
Background/Aims: A drug-eluting stent for unresectable malignant biliary obstruction was developed to increase stent patency by preventing tumor ingrowth. The safety and efficacy of a new generation of metallic stents covered with a paclitaxel-incorporated membrane using a Pluronic(®) mixture (MSCPM-II) were compared prospectively with those of covered metal stents (CMSs) in patients with malignant biliary obstructions. Methods: This study was initially designed as a prospective randomized trial but was closed early because of a high incidence of early occlusion...
March 24, 2017: Gut and Liver
https://www.readbyqxmd.com/read/28334884/improvement-in-the-prognosis-of-ovarian-cancer-in-the-era-before-addition-of-molecular-targeting-therapy
#9
Takako Shimada, Toshiaki Saito, Mototsugu Shimokawa, Kumi Shimamoto, Shuhei Matsushita, Shinichiro Yamaguchi, Kazuya Ariyoshi, Masao Okadome
Objective: The prognosis of ovarian cancer has improved because of platinum- and taxane-containing chemotherapy. We investigated the 5-year disease-specific overall survival and prognostic factors of patients with advanced ovarian cancer to elucidate the change in clinical course of ovarian cancer with the advance of chemotherapy for patients who developed relapse in the era before the addition of molecular targeting therapy. Methods: We reviewed the clinical course of 134 patients with advanced ovarian cancer (FIGO Stage III and IV) treated in the past 11 years (1999-2010)...
February 24, 2017: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28334805/hair-testing-for-drugs-of-abuse-and-new-psychoactive-substances-in-a-high-risk-population
#10
Alberto Salomone, Joseph J Palamar, Enrico Gerace, Daniele Di Corcia, Marco Vincenti
Hundreds of new psychoactive substances (NPS) have emerged in the drug market over the last decade. Few drug surveys in the USA, however, ask about use of NPS, so prevalence and correlates of use are largely unknown. A large portion of NPS use is unintentional or unknown as NPS are common adulterants in drugs like ecstasy/Molly, and most NPS are rapidly eliminated from the body, limiting efficacy of urine, blood and saliva testing. We utilized a novel method of examining prevalence of NPS use in a high-risk population utilizing hair-testing...
March 4, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28334739/hiv-treatment-as-prevention-implications-for-health-promotion
#11
Sean Slavin
Evidence has been accumulating in recent years that individuals with HIV who are effectively treated with antiretroviral drugs are highly unlikely to transmit the virus to their sexual partners. This approach has great potential to contribute to ongoing prevention efforts and has been termed 'treatment as prevention'. International political momentum has been building in recent years to attempt to significantly reduce new HIV infections globally and end the epidemic by 2030. In pursuit of such aims a number of local health authorities and communities have adopted intensified 'test and treat' strategies to quickly diagnose infections and reduce the risk of onward transmission through an immediate offer of treatment...
October 8, 2016: Health Promotion International
https://www.readbyqxmd.com/read/28334702/in-vitro-antibacterial-activity-of-7-substituted-6-fluoroquinolone-and-7-substituted-6-8-difluoroquinolone-derivatives
#12
Socorro Leyva-Ramos, Denisse de Loera, Jaime Cardoso-Ortiz
BACKGROUND: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. METHODS: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method...
March 24, 2017: Chemotherapy
https://www.readbyqxmd.com/read/28334544/-antiplatelet-thromboprophylaxis-of-arterial-vascular-diseases-and-organovascular-ischemic-diseases
#13
Peter Gavorník, Andrej Dukát, Ľudovít Gašpar, Eva Gavorníková, Naďa Hučková, Anna Petrášová, Gabriela Gubo, Iveta Gašparová, Lujza Sabolová
Antiplatelet therapy by acetylsalicylic acid (ASA, aspirin) provided pivotal advances in the prevention and treatment of organovascular (angiovascular, cardiovascular, cerebrovascular, extremitovascular, renovascular, genitovascular, mesenteriointestinokolonovascular, bronchopulmovascular, oculovascular, otovascular and other) arterial ischemic diseases. Currently available antiplatelet drugs have some limitations which might be overcomed by improved dosing regimens, use of combination of agents affecting different platelet functions and, in particular, by the new antiplatelet drugs (new arterial antithrombotics) with distinct pharmacodynamic properties offering new advantages, including faster onset of action, greater potency, and reversibility of effects...
2017: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/28334507/comparative-study-of-cytotoxicity-and-genotoxicity-of-commercial-jeffamines%C3%A2-and-polyethylenimine-in-cho-k1-cells
#14
Leniher Castan, Cristiano José da Silva, Eduardo Ferreira Molina, Raquel Alves Dos Santos
Jeffamines(®) are a family of polymers containing primary amine groups attached to the extremities of polyether backbone which can be used as biomaterials. They have been used in combination with polyethylenimine (PEI) to improve biocompatibility in drug and gene delivery systems. Despite these facts, very few studies have been done on cytotoxicity and genotoxicity of pure Jeffamines(®) or compared with PEI. The present study aimed to evaluate and compare the cytotoxic and genotoxic effects of Jeffamines(®) and PEI in CHO-K1 cells...
March 23, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
https://www.readbyqxmd.com/read/28334468/supporting-the-aboriginal-alcohol-and-other-drug-workforce-in-new-south-wales-australia
#15
K S Kylie Lee, Bradley Freeburn, Steve Ella, Scott Wilson, Kristie Harrison, Monique McEwan, Katherine M Conigrave
No abstract text is available yet for this article.
March 23, 2017: Drug and Alcohol Review
https://www.readbyqxmd.com/read/28334457/a-bibliometric-review-of-drug-and-alcohol-research-focused-on-indigenous-peoples-of-australia-new-zealand-canada-and-the-united-states
#16
REVIEW
Anton Clifford, Anthony Shakeshaft
ISSUES: Indigenous peoples of Australia, New Zealand, Canada and the United States experience a disproportionately high burden of harms from substance misuse. Research is therefore required to improve our understanding of substance use in Indigenous populations and provide evidence on strategies effective for reducing harmful use. APPROACH: A search of 13 electronic databases for peer-reviewed articles published between 1993 and 2014 focusing on substance use and Indigenous peoples of Australia, New Zealand, Canada and the United States...
March 23, 2017: Drug and Alcohol Review
https://www.readbyqxmd.com/read/28334417/pharmacovigilance-database-search-discloses-clc-k-channels-as-a-novel-target-of-the-at1-receptor-blockers-valsartan-and-olmesartan
#17
Paola Imbrici, Domenico Tricarico, Giuseppe Felice Mangiatordi, Orazio Nicolotti, Marcello Diego Lograno, Diana Conte, Antonella Liantonio
BACKGROUND AND PURPOSE: Human ClC-K chloride channels are highly attractive targets for drug discovery for their physiological role and association with genetic disorders. These channels are pivotal in the kidney as they control chloride reabsorption and water diuresis. In addition, loss-of-function mutations of CLCKNB and BSND genes cause Bartter's syndrome (BS), whereas CLCNKA and CLCKNB gain-of-function polymorphisms predispose to a rare form of salt sensitive hypertension. Both disorders lack a personalized therapy that is in most cases only symptomatic...
March 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28334324/understanding-the-genetic-landscape-of-small-cell-carcinoma-of-the-urinary-bladder-and-implications-for-diagnosis-prognosis-and-treatment-a-review
#18
Erik J Kouba, Liang Cheng
Importance: Small cell carcinoma of the urinary bladder is a rare and aggressive neuroendocrine tumor of the urinary bladder. Although research has been performed since the first case was reported in 1981, most of our understanding of the disease treatments has been extrapolated from small cell carcinoma of the lung. However, current data on patient survival have been stagnant. Observations: With the advent of advanced molecular diagnostic methods, a new potential for understanding the origin and treatment of small cell carcinoma of the urinary bladder has become evident...
March 23, 2017: JAMA Oncology
https://www.readbyqxmd.com/read/28333950/drug-resistant-hiv-behaviors-and-characteristics-among-los-angeles-men-who-have-sex-with-men-with-new-hiv-diagnosis
#19
Pamina M Gorbach, Marjan Javanbakht, Lorelei Bornfleth, Robert K Bolan, Martha Lewis Blum
Epidemiology of drug resistant HIV has focused on trends and less attention has been given to identification of factors, especially behaviors including substance use, in acquisition of drug-resistant HIV. From 2009 to 2012 The Metromates Study enrolled and followed for one year men who have sex with men (MSM) seeking testing for HIV in a community clinic in Los Angeles assessing those testing positive for acute and recent HIV infection. Behavioral data were collected via Computer-Assisted Self-Interview from 125 classified as newly HIV infected and 91 as chronically infected (newly HIV-diagnosed); specimens were available and viable for resistance testing for 154 of the 216 HIV positives with new diagnoses...
2017: PloS One
https://www.readbyqxmd.com/read/28333738/diabetes-drug-receives-new-indication
#20
Diane S Aschenbrenner
No abstract text is available yet for this article.
April 2017: American Journal of Nursing
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