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Evdokimov N.M.,New Mexico Institute of Mining and Technology | Lamoral-Theys D.,Laboratoire Of Chimie Analytique | Mathieu V.,Free University of Colombia | Andolfi A.,University of Naples Federico II | And 7 more authors.
Bioorganic and Medicinal Chemistry | Year: 2011

As a continuation of our studies aimed at the development of a new cytostatic agent derived from an Amaryllidaceae alkaloid lycorine, we synthesized 32 analogues of this natural product. This set of synthetic analogues included compounds incorporating selective derivatization of the C1 versus C2 hydroxyl groups, aromatized ring C, lactamized N6 nitrogen, dihydroxylated C3-C3a olefin functionality, transposed olefin from C3-C3a to C2-C3 or C3a-C4, and C1 long-chain fatty esters. All synthesized compounds were evaluated for antiproliferative activities in vitro in a panel of tumor cell lines including those exhibiting resistance to proapoptotic stimuli and representing solid cancers associated with dismal prognoses, such as melanoma, glioblastoma, and non-small-cell lung cancer. Most active analogues were not discriminatory between cancer cells displaying resistance or sensitivity to apoptosis, indicating that these compounds are thus able to overcome the intrinsic resistance of cancer cells to pro-apoptotic stimuli. 1,2-Di-O-allyllycorine was identified as a lycorine analogue, which is 100 times more potent against a U373 human glioblastoma model than the parent natural product. Furthermore, a number of synthetic analogues were identified as promising for the forthcoming in vivo studies. © 2011 Elsevier Ltd. All rights reserved. Source

Balde E.S.,Laboratoire Of Toxicologie | Andolfi A.,University of Naples Federico II | Bruyere C.,Laboratoire Of Toxicologie | Cimmino A.,University of Naples Federico II | And 7 more authors.
Journal of Natural Products | Year: 2010

Fourteen metabolites, isolated from phytopathogenic and toxigenic fungi, were evaluated for their in vitro antigrowth activity for six distinct cancer cell lines, using the MTT colorimetric assay. Bislongiquinolide (1) and dihydrotrichodimerol (5), which belong to the bisorbicillinoid structural class, displayed significant growth inhibitory activity against the six cancer cell lines studied, while the remaining compounds displayed weak or no activity. The data show that 1 and 5 have similar growth inhibitory activities with respect to those cancer cell lines that display certain levels of resistance to pro-apoptotic stimuli or those that are sensitive to apoptosis. Quantitative videomicroscopy analysis revealed that 1 and 5 exert their antiproliferative effect through cytostatic and not cytotoxic activity. The preliminary results from the current study have stimulated further structure-activity investigations with respect to the growth inhibitory activity of compounds belonging to the bisorbicillinoid group. © 2010 The American Chemical Society and American Society of Pharmacognosy. Source

Blackman J.,Charles Sturt University | Rutledge D.N.,Laboratoire Of Chimie Analytique | Tesic D.,Charles Sturt University | Saliba A.,Charles Sturt University | Scollary G.R.,University of Melbourne
Analytica Chimica Acta | Year: 2010

The application of a multi-block statistical analysis method, known as Common Components and Specific Weight Analysis, to the determination of connections between sensory descriptors and analytical data for Hunter Valley Semillon is described. Sixteen wines were used in the data analysis with 15 sensory descriptors and 10 analytical measurements available for each wine. The multi-block analysis simplifies the comparison between the data sets and allows relationships between the sensory and analytical parameters to be readily ascertained, more effectively than a linear regression approach. A sweetness zone established the connections between several sensory descriptors and analytical measurements based on fructose. Glucose was not part of the sweetness connections, although glycerol was connected to the sensory sweetness descriptors. Sensory assessment of acidity was positively related to the titratable acidity and pH was negatively related. The malic acid concentration was also negatively related to sensory acidity and the possible reasons for this are described. Several sensory descriptors including toast, honey and kerosene were found to be in opposition to the sweetness sensory parameters and not connected to any analytical parameters. The outcomes of this multi-block treatment indicate the potential for using analytical measurements as a surrogate for sensory analysis. © 2009 Elsevier B.V. All rights reserved. Source

Hagege A.A.,University of Paris Descartes | Caudron E.,Laboratoire Of Chimie Analytique | Damy T.,Center Dinvestigation Clinique And Plateforme Of Ressources Biologiques | Jabbour F.,Laboratoire Of Biochimie | And 4 more authors.
Heart | Year: 2011

Background: Patients with Fabry disease (FD) show left ventricular hypertrophy (LVH) mimicking hypertrophic cardiomyopathy (HCM) of sarcomeric origin and might benefit, if detected early, from specific enzyme replacement therapy. The prevalence of FD in patients with LVH of 13 mm or greater, screened using the leucocyte alpha-galactosidase A (α-gal A) activity test, a technique that is difficult to apply routinely, ranged from 0% to 6%. Objective: To screen systematically for FD in patients with a diagnosis of HCM (LVH ≥15 mm) in primary cardiology practice, a validated, physician-friendly α-gal A assay was used on dried blood spots using a filter paper test. Design and patients: A cohort of 392 adults (278 men) followed for HCM were screened for FD. A standard blood test was used for confirmation in nine men in whom the α-gal A result was 40% or less. Results: Four men (1.5%; 1.8% of men ≥40 years vs 0% <40 years; all with α-gal A <30%), but no women, were diagnosed with FD. Index cases presented with diffuse but asymmetric LVH, with severe obstruction in one case and frequent high-grade atrioventricular conduction block necessitating a pacemaker in three cases. Family screening identified eight additional cases. Genotyping was performed successfully on DNA extracted from the filter papers. Conclusion: In male patients diagnosed as having HCM, pure FD cardiac variants are not exceptional and can be specifically identified using a simple filter-paper test. The sensitivity of this test is low in female patients. Source

Lipka E.,Laboratoire Of Chimie Analytique | Danel C.,Laboratoire Of Chimie Analytique | Yous S.,University of Lille Nord de France | Bonte J.-P.,Laboratoire Of Chimie Analytique | Vaccher C.,Laboratoire Of Chimie Analytique
Electrophoresis | Year: 2010

In this study, baseline separation of the stereoisomers of six tetrahydronaphthalenic derivatives (agonists and antagonists for the melatonin (N-acetyl-5-methoxytryptamin) binding sites) was successfully achieved using CE and CDs as chiral selectors. The method for the simultaneous chiral separation of the four stereoisomers uses a capillary dynamically coated with polyethylene oxide and a dual CD system. Optimisation was performed first upon the constituents of the CD system, by varying neutral and anionic CD type, size and concentration, at first in mono-CD systems and subsequently in dual neutral/anionic CD systems. Once these characteristics of the dual CD system were established, operational parameters such as voltage and temperature were then optimised. Under the optimal conditions (i.e. 1.5% w/v of highly S-β-CD and 10mM of γ-CD in 25mM phosphate buffer (pH 2.5) as the BGE, separation voltage 20 kV and a temperature of 25°C), complete resolution of the six molecules was accomplished. Preliminary results for repeatability and the migration order of the optimised method are described. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA. Source

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