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Zhouen Zhang et al.
Journal of labelled compounds & radiopharmaceuticals, 57(8), 540-549 (2014-07-06)
The nucleosides zidovudine (AZT), stavudine (d4T), and telbivudine (LdT) are approved for use in the treatment of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections. To promote positron emission tomography (PET) imaging studies on their pharmacokinetics, pharmacodynamics, and
Youn Gee Seo et al.
Archives of pharmacal research, 38(2), 223-228 (2014-08-20)
The purpose of this study was to develop a novel tacrolimus-loaded solid self-emulsifying drug delivery system (SEDDS) using Labrafac as an oil phase. The ternary phase diagram was plotted with Labrafac, Labrasol and Lauroglycol used as an oil, surfactant and
Minjie Jiang et al.
PloS one, 10(2), e0116010-e0116010 (2015-02-26)
A rapid, sensitive and selective high-performance liquid chromatography-tandem mass spectrometric method (HPLC-MS) was developed and validated to determine the 14-(3-methylbenzyl)matrine (3MBM) and 14-(4-methylbenzyl)matrine (4MBM) levels in rat plasma in the present study. The analytes were separated using a C18 column
Dao-Jin Chen et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 969, 42-52 (2014-08-26)
Folk drug Gynostemma pentaphyllum (Thunb.) Makino contains many biologically active phytochemicals which have been demonstrated to be effective against chronic diseases. As in vivo anti-tumor experiments of G. pentaphyllum extract (GP) show much stronger antitumor activities than in vitro, it
Sara Hosseininasab et al.
Chemical biology & drug design, 84(3), 307-315 (2014-04-02)
Therapeutic proteins and peptides are corresponding to a major area of research in biotechnology companies and current pharmaceutical. Because of their natural instability, the enormous majority of these drugs require parentéral administration. Oral insulin delivery would be a highly attractive
Barbara Chiavarino et al.
Journal of the American Society for Mass Spectrometry, 24(10), 1603-1607 (2013-08-21)
The C - C bond formation activated under negative electrospray ionization of an acetonitrile solution of 1,3,5-trinitrobenzene is reported. The solvent function is to provide a source of cyanide ion, a highly problematic reagent, which is found to attack the
Johannes Bertsch et al.
Journal of bacteriology, 197(9), 1681-1689 (2015-03-04)
The methylenetetrahydrofolate reductase (MTHFR) of acetogenic bacteria catalyzes the reduction of methylene-THF, which is highly exergonic with NADH as the reductant. Therefore, the enzyme was suggested to be involved in energy conservation by reducing ferredoxin via electron bifurcation, followed by
Amit Kumar et al.
Bioconjugate chemistry, 26(4), 782-789 (2015-03-12)
We report a click-chemistry based modular strategy for antibody labeling with (64)Cu (t1/2 = 12.7 h; β(+) 0.656 MeV, 17.4%; β(-) 0.573 MeV, 39%; EC 43%) under ambient condition utilizing a cross-bridged tetraazamacrocyclic (CB-TE2A) analogue, which otherwise requires harsh conditions
Sarah Afshordel et al.
Pharmacological research, 91, 69-77 (2014-12-17)
Alterations in small GTPase mediated signal transduction pathways have emerged as a central step in the molecular pathogenesis of glioblastoma (GBM), the most common malignant brain tumor in adults. Farnesylpyrophosphate (FPP) and geranylgeranylpyrophosphate (GGPP) are derived from mevalonate, whose production
Adam Byron et al.
Nature communications, 6, 6135-6135 (2015-01-23)
Integrin activation, which is regulated by allosteric changes in receptor conformation, enables cellular responses to the chemical, mechanical and topological features of the extracellular microenvironment. A global view of how activation state converts the molecular composition of the region proximal
Giancarlo Vanini et al.
The European journal of neuroscience, 40(1), 2264-2273 (2014-03-29)
The oral part of the pontine reticular formation (PnO) contributes to the regulation of sleep, anesthesia and pain. The role of PnO γ-aminobutyric acid (GABA) in modulating these states remains incompletely understood. The present study used time to loss and
A T Hughes et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 963, 106-112 (2014-06-22)
Alkaptonuria (AKU) is a rare debilitating autosomal recessive disorder of tyrosine metabolism. Deficiency of homogentisate 1,2-dioxygenase results in increased homogentisic acid (HGA) which although excreted in gram quantities in the urine, is deposited as an ochronotic pigment in connective tissues
Tony Antoniou et al.
Antiviral therapy, 19(6), 607-611 (2014-02-13)
We sought to determine the pharmacokinetic disposition of raltegravir in the blood and seminal plasma of HIV-infected men. We conducted a pharmacokinetic study using a staggered sampling approach. A total of 16 HIV-infected men receiving raltegravir-based therapy were recruited into
Yi Huang et al.
Pharmaceutical biology, 52(6), 681-687 (2014-05-16)
Alismatis rhizome (RA) (Water Plantain Family, also called "Zexie" in Chinese), one of the commonly used components of traditional Chinese medicines, is derived from the dried rhizomes of Alisma orientalis (Sam.) Juzep. (Alismataceae). This study explores the RA influences on
Daniel G Beach et al.
Analytical and bioanalytical chemistry, 407(9), 2473-2484 (2015-01-27)
The analysis of paralytic shellfish toxins (PSTs) by liquid chromatography-mass spectrometry remains a challenge because of their high polarity, large number of analogues and the complex matrix in which they occur. Here we investigate the potential utility of high-field asymmetric
Cordula Stillhart et al.
Pharmaceutical research, 31(12), 3426-3444 (2014-06-26)
In vitro lipolysis is widely utilized for predicting in vivo performance of oral lipid-based formulations (LBFs). However, evaluation of LBFs in the absence of an absorption sink may have limited in vivo relevance. This study aimed at employing biopharmaceutical modeling
Weixia Li et al.
Journal of chromatography. A, 1346, 49-56 (2014-05-06)
The compatibility of Angelicae Sinensis Radix (Danggui, DG) and Chuanxiong Rhizoma (Chuanxiong, CX), a famous herb pair Gui-Xiong (GX), can produce synergistic and complementary hematopoiesis. In present study, global metabolic profiling with ultra-high-performance liquid chromatography coupled to quadrupole time-of-flight mass
Naveen K Bejugam et al.
Drug development and industrial pharmacy, 41(2), 333-341 (2013-11-28)
To develop a tablet formulation for an active pharmaceutical ingredient for which sticking and filming problems occurred during tablet punching. Direct compression and dry granulation tableting techniques were evaluated using factorial experimental design. The effects of chrome-coated punch tips, filler
Timothy Paul Wood et al.
Environmental pollution (Barking, Essex : 1987), 199, 235-243 (2015-02-15)
The study and quantification of personal care products, such as pharmaceuticals, in surface water has become popular in recent years; yet very little description of these compounds' presence in South African surface water exists in the literature. Antiretrovirals (ARVs), used
Amy Barone et al.
Oncotarget, 5(20), 9811-9822 (2014-09-23)
Glioblastoma recurrence involves the persistence of a subpopulation of cells with enhanced tumor-initiating capacity (TIC) that reside within the perivascular space, or niche (PVN). Anti-angiogenic therapies may prevent the formation of new PVN but have not prevented recurrence in clinical
Marialetizia Motta et al.
Human molecular genetics, 23(21), 5814-5826 (2014-06-14)
Saposin (Sap) C is an essential cofactor for the lysosomal degradation of glucosylceramide (GC) by glucosylceramidase (GCase) and its functional impairment underlies a rare variant form of Gaucher disease (GD). Sap C promotes rearrangement of lipid organization in lysosomal membranes
Nagender R Panyala et al.
Journal of pharmaceutical and biomedical analysis, 100, 157-166 (2014-08-29)
3,4,3-LI(1,2-HOPO) is a chelating ligand and decorporation agent that can remove radioactive lanthanides and actinides from the body. Identification of trace impurities in drug samples is gaining much interest due to their significant influence on drug activity. In this study
Xiaofeng Xu et al.
Molecular medicine reports, 11(3), 2191-2198 (2014-11-19)
The incidence and mortality rate of biliary tract cancer have been increasing worldwide; however, its diagnosis and prognosis have not improved in recent years. A novel approach, termed 'metabolomics', may have the potential to be developed as an effective diagnostic
Euan R O Allan et al.
Journal of immunology (Baltimore, Md. : 1950), 192(11), 4989-5001 (2014-04-30)
The chemistries within phagosomes of APCs mediate microbial destruction as well as generate peptides for presentation on MHC class II. The antimicrobial effector NADPH oxidase (NOX2), which generates superoxide within maturing phagosomes, has also been shown to regulate activities of
Rachel Morrison et al.
Pharmaceutical research, 31(10), 2904-2917 (2014-05-06)
To design and synthesize chemoembolization particles for the delivery of Ophiobolin A (OphA), a promising fungal-derived chemotherapeutic, directly at the tumour location. To investigate cell death mechanism of OphA on a Rhabdomyosarcoma cancer (RD) cell line. Rhabdomyosarcoma is the most
Jef Stappaerts et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 90, 1-7 (2015-01-17)
The aim of this study was to evaluate the intestinal disposition of abiraterone acetate, an ester prodrug of the anticancer agent abiraterone. Stability of the prodrug and solubility and dissolution characteristics of both abiraterone and abiraterone acetate were monitored in
Joanne D Du et al.
International journal of pharmaceutics, 471(1-2), 358-365 (2014-06-01)
Targeted drug delivery to the buccal mucosa offers distinct advantages over oral delivery to the gastrointestinal tract including by-passing hepatic first-pass metabolism. However, the buccal route is often limited by low bioavailability, low drug loading and reduced residence time due
Paweł Kubica et al.
Analytical and bioanalytical chemistry, 407(5), 1505-1512 (2014-12-05)
The method for the determination of acesulfame-K, saccharine, cyclamate, aspartame, sucralose, alitame, neohesperidin dihydrochalcone, neotame and five common steviol glycosides (rebaudioside A, rebaudioside C, steviol, steviolbioside and stevioside) in soft and alcoholic beverages was developed using high-performance liquid chromatography and
Wei Liu et al.
PloS one, 10(4), e0122366-e0122366 (2015-04-08)
Vasicine (VAS), a potential natural cholinesterase inhibitor, exhibited promising anticholinesterase activity in preclinical models and has been in development for treatment of Alzheimer's disease. This study systematically investigated the in vitro and in vivo metabolism of VAS in rat using
Tae-Kang Kim et al.
Molecular and cellular endocrinology, 404, 1-8 (2014-08-30)
Melatonin and its metabolites including 6-hydroxymelatonin (6(OH)M), N(1)-acetyl-N(2)-formyl-5-methoxykynuramine (AFMK) and 5-methoxytryptamine (5MT) are endogenously produced in human epidermis. This production depends on race, gender and age. The highest melatonin levels are in African-Americans. In each racial group they are highest
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