PEGylated bottom-up synthesized graphene nanoribbons loaded with camptothecin as potential drug carriers

This work discusses the potential use of bottom-up synthesized graphene nanoribbons (GNRs) as nano-carriers for drug delivery systems (DDSs). GNRs have a high loading capacity for anticancer drugs due to their high specific surface area and non-covalent adsorption with hydrophobic anticancer drug molecules. Herein, we synthesized GNRs using a bottom-up approach, modified with PEG2000 (GNR-PEG) and PEG2000 carrying folic acid chains (GNR-PEG-FA), and then loaded with camptothecin (CPT). The targeting ability mediated by folic acid of the GNR derivative was evaluated using cellular assays, and the cytotoxicity of GNR systems loaded with CPT was assessed by in vitro studies. They suggest that the functionalization of GNR derivatives with folic acid significantly affects their interaction with cells expressing different levels of folic acid receptors. The authors also explore the possibility to employ GNRs in photothermal therapy (PTT). GNR-PEG and GNR-PEG-FA display minor or no toxicity in standard cell cultures, but they show remarkable thermal response upon NIR irradiation, causing complete loss of cell viability within a few hours of treatment. This work highlights the potential of GNRs as DDSs and emphasizes the importance of further research on their biocompatibility and as a platform for PTT

Structure-guided discovery of cis-hexahydro-pyrido-oxazinones as reversible, drug-like monoacylglycerol lipase inhibitors

Molecular Physiolog

A new fluorescence resonance energy transfer pair and its application to oligonucleotide labeling and fluorescence resonance energy transfer

We describe two new fluorescence resonance energy transfer (FRET) compatible labels, their covalent linkage to oligonucleotides, and their use as donor and acceptor, respectively, in FRET hybridization studies. The dyes belong to the cyanine dyes, and water solubility is imparted by a phosphonate which represents a new solubilizing group in DNA labels. They were linked to amino-modified synthetic oligonucleotides via oxysuccinimide (OSI) esters. The studies performed include binding assays, determinations of molecular distances, homogeneous competitive assays, and limits of detection, which are in the order of 5 pmol/L for a 15-mer

Chameleon Labels for Staining and Quantifying Proteins

Glowing marks: A new class of protein stains, the pyrylium dyes, undergo a strong color change (typically from blue to red, see picture) on covalently binding to proteins. While the free stains are almost nonfluorescent, the protein-conjugated forms are highly fluorescent. The dyes do not alter the charge of a protein, and thus do not change its electrophoretic properties. The stains also can be used in quantitative protein assays

Use of recombinant activated factor VII in severe post-partum haemorrhage: Data from the Italian Registry. A multicentric observational retrospective study

Purpose: To report the Italian real experience in clinical practice about recombinant factor VII activated (rFVIIa) in Post-Partum Haemorrhage (PPH) treatment. Methods: An Italian retrospective survey of severe primary PPH cases treated with rFVIIa was performed. Anamnestic, clinical and haemostatic data about thirty-five patients with PPH, from 2005 to 2007, were collected. Coagulative parameters and transfusion requirements before and after rFVIIa treatment were compared. Results: After rFVIIa administration INR was significantly decreased, while fibrinogen levels were markedly increased. Median of packed red blood cells units, platelets units, fresh frozen plasma, crystalloids and colloids needed, before and after rFVIIa administration, were respectively 6 and 2 units (p < 1.2exp-6), 1.5 and 0 units (p = 0.001), 1250 and 0\ua0mL (p < 4.4exp-5), 3000 and 1250\ua0mL (p < 0,0042). Twenty-nine of 35 patients needed surgical intervention before rFVIIa administration, 9/35 after treatment. Hysterectomies have been performed respectively in 10/35 cases before and in 6/35 cases after rFVIIa infusion. No maternal deaths have been reported. No adverse events or thromboembolic complications were observed. Conclusions: Our clinical and haemostatic data suggest that recombinant activated factor VII may be a safe and helpful adjunctive therapy in the PPH management. \ua9 2009 Elsevier Ltd. All rights reserved

Use of recombinant activated factor VII in severe post-partum haemorrhage: data from the Italian Registry: a multicentric observational retrospective study

none11noPurpose: To report the Italian real experience in clinical practice about recombinant factor VII activated (rFVIIa) in Post-Partum Haemorrhage (PPH) treatment. Methods: An Italian retrospective survey of severe primary PPH cases treated with rFVIIa was performed. Anamnestic, clinical and haemostatic data about thirty-five patients with PPH, from 2005 to 2007, were collected. Coagulative parameters and transfusion requirements before and after rFVIIa treatment were compared. Results: After rFVIIa administration INR was significantly decreased, while fibrinogen levels were markedly increased. Median of packed red blood cells units, platelets units, fresh frozen plasma, crystalloids and colloids needed, before and after rFVIIa administration, were respectively 6 and 2 units (p < 1.2exp-6), 1.5 and 0 units (p = 0.001), 1250 and 0 mL (p < 4.4exp-5), 3000 and 1250 mL (p < 0,0042). Twenty-nine of 35 patients needed surgical intervention before rFVIIa administration, 9/35 after treatment. Hysterectomies have been performed respectively in 10/35 cases before and in 6/35 cases after rFVIIa infusion. No maternal deaths have been reported. No adverse events or thromboembolic complications were observed. Conclusions: Our clinical and haemostatic data suggest that recombinant activated factor VII may be a safe and helpful adjunctive therapy in the PPH management. © 2009 Elsevier Ltd. All rights reserved.openBarillari G.; Frigo M.G.; Casarotto M.; Farnia A.; Masse B.; Wetzl R.; Bianchin A.; Rabi A.; Malacarne P.; Pasca S.; Bigotto E.Barillari, G.; Frigo, M. G.; Casarotto, M.; Farnia, A.; Masse, B.; Wetzl, R.; Bianchin, A.; Rabi, A.; Malacarne, P.; Pasca, S.; Bigotto, E

SDS-PAGE of Proteins Using a Chameleon-Type of Fluorescent Prestain

A new prestaining method for protein SDS-PAGE was developed using the fluorogenic amino-reactive label Py-1. This resulted in one of the fastest, most sensitive, and environmentally friendly protocols available. It is mainly due to the unique optical properties of Py-1, which is blue and virtually nonfluorescent but turns to red and becomes much more strongly fluorescent once it is conjugated to the amino group of a protein. Staining times of 30 min are adequate to visualize subnanogram quantities of proteins because pre-electrophoretic labeling Py-1 does not require the time-consuming steps of washing or fixation of gels. LODs as low as 16 pg of protein are found which is better than the best (commercial) poststains and comparable to the best (commercial) prestains. In addition, prestaining requires marginal amounts of staining solution. The change in electrophoretic mobility and band broadening is at a low level because Py-1 causes a mass shift of 288 Da per bound molecule only. By virtue of the small mass shift it causes, this stain is compatible with mass spectrometric protein analysis even though it acts as a covalent label

Chromogenic Sensing of Biogenic Amines Using a Chameleon Probe and the Red−Green−Blue Readout of Digital Camera Images

We report on sensing spots containing an amine reactive chromogenic probe and a green fluorescent (amine insensitive) reference dye incorporated in a hydrogel matrix on a solid support. Such spots enable rapid and direct determination of primary amines and, especially, biogenic amines (BA). A distinct color change from blue to red occurs on dipping the test spots into a pH 9.0 sample containing primary amines. BAs can be determined in the concentration range from 0.01 to 10 mM within 15 min, enabling rapid, qualitative, and semiquantitative evaluation. In the “photographic” approach, the typically 4−7.5-fold increase in fluorescence intensity of the probe at 620 nm along with the constant green fluorescence at 515 nm of a reference dye are used for quantitation of BAs. The sensing spots are photoexcited with high-power 505 nm light-emitting diodes (LEDs) in a black box. A digital picture is acquired with a commercially available digital camera, and the color information is extracted via red−green−blue (RGB) readout. The ratio of the intensities of the red (signal) channel and the green (reference) channel yields pseudocolor pictures and calibration plots