Search results for "drugs."
showing 10 items of 733 documents
3-Deazaneplanocin A (DZNep), an Inhibitor of the Histone Methyltransferase EZH2, Induces Apoptosis and Reduces Cell Migration in Chondrosarcoma Cells
2014
Objective Growing evidences indicate that the histone methyltransferase EZH2 (enhancer of zeste homolog 2) may be an appropriate therapeutic target in some tumors. Indeed, a high expression of EZH2 is correlated with poor prognosis and metastasis in many cancers. In addition, 3-Deazaneplanocin A (DZNep), an S-adenosyl-L homocysteine hydrolase inhibitor which induces EZH2 protein depletion, leads to cell death in several cancers and tumors. The aim of this study was to determine whether an epigenetic therapy targeting EZH2 with DZNep may be also efficient to treat chondrosarcomas. Methods EZH2 expression was determined by immunohistochemistry and western-blot. Chondrosarcoma cell line CH2879…
LC–MS–MS metodes izstrāde četru pirmās izvēles prettuberkulozes zāļu vielu un to galveno metabolītu noteikšanai cilvēka asins plazmā
2020
Darbā apkopota literatūra par esošajām prettuberkulozes zāļu vielu un to metabolītu LC–MS–MS noteikšanas metodēm, raksturotas paraugu sagatavošanas un hromatogrāfisko metožu pielietošanas iespējas. Darba gaitā eksperimentāli pārbaudītas dažādas paraugu sagatavošanas un hromatogrāfiskās noteikšanas metodes, izstrādāta un validēta metode četru pirmās izvēles prettuberkulozes zāļu vielu un to galveno metabolītu noteikšanai cilvēka asins plazmā. Izstrādātās metodes veiktspēju pārbaudīja, analizējot klīniskos paraugus (n=12).
Calorimetric investigation of the interaction between a macromolecular prodrug of diflunisal and human platelets
1995
The thermal effect due to the interaction between human platelets and α,β poly(N-hydroxy-ethyl)-DL-aspartamide (PHEA) or the PHEA-Diflunisal conjugate was measured by the calorimetric technique at 25°C. The experimental data confirm that PHEA is a biocompatible macromolecule and that its conjugate influences the physiological activity of human platelets.
Macromolecular Prodrugs Based on Synthetic Polyaminoacids: Drug Delivery and Drug Targeting in Antitumor Therapy
2011
In the last twenty years a depth study on potential pharmaceutical applications of synthetic polymers at proteinlike structure as carrier for macromolecular prodrug production has been performed in academia and in industry. In particular α,β-poly(N-2-hydroxyethyl)-DL-aspartamide (PHEA), α,β-polyaspartylhydrazide (PAHy), poly(glutamic acid) (PGA), poly(aspartic acid) (PAA) and polylysine (PLL) have been extensively studied in this field. In the present review, the use of PHEA, PAHy, PGA as starting materials to prepare macromolecular prodrugs is reported and drug delivery and targeting aspects have been considered.
Loss of spatial learning in a patient with topographical disorientation in new environments
2003
The case is described of a patient who, following cerebral hypoxia, developed severe difficulty in orienting himself in new environments in the context of a mild global amnesic syndrome. Some episodes he related suggested that his main difficulty was remembering the spatial/directional value of landmarks he recognised. A neuroradiological examination documented severe bilateral atrophy of the hippocampi associated with atrophic changes in the cerebral hemispheres, most marked in the dorsal regions. Neuropsychological and experimental evaluation showed a severe deficit of spatial learning with substantially preserved ability to learn verbal and visual-object information. He was also virtuall…
Unexpected identification and characterization of a cathinone precursor in the new psychoactive substance market: 3',4'-methylenedioxy-2,2-dibromobut…
2019
Abstract 3′,4′-methylenedioxy-2,2-dibromobutyrophenone has been identified and fully characterized in a sample obtained from an anonymous consumer acquired as ketamine through the Internet market. The substance has been deeply characterized by using standard and high performance analytical techniques such as: attenuated total reflectance-infrared spectroscopy, gas chromatography–mass spectrometry, high-resolution mass spectrometry, elemental analysis, and nuclear magnetic resonance, including 1H, 13C, distortionless enhancement by polarization transfer, two dimensional homonuclear 1H-1H correlation spectroscopy, and 1H-13C heteronuclear single-quantum correlation spectra. 3′,4′-methylenedio…
Synthesis and in vitro studies on a potential dopamine prodrug.
2008
Dopamine delivery to the central nervous system (CNS) undergoes the permeability limitations of blood-brain barrier (BBB) which is a selective interface that excludes most water-soluble molecules from entering the brain. Neutral amino acids permeate the BBB by specific transport systems. Conden- sation of dopamine with neutral amino acids could afford potential prodrugs able to interact with the BBB endogenous transporters and easily enter the brain. The synthesis and characterization of the dopamine derivative 2-amino-N-[2-(3,4-dihydroxy-phenyl)-ethyl]-3-phenyl-propionamide (7) is de- scribed. The chemical and enzymatic stability of 7 was evaluated. The molecular weight (300 Da) and Log P …
Galactosylated micelles for a ribavirin prodrug targeting to hepatocytes.
2013
Polymeric micelles potentially able to carry to hepatocytes a ribavirin (RBV) prodrug, exploiting the presence of carbohydrate receptors, that is, ASGPR, were prepared starting from a galactosylated polylactide-polyaminoacid conjugate. This latter was obtained by chemical reaction of α,β-poly(N-2-hydroxyethyl) (2-aminoethylcarbamate)-dl-aspartamide (PHEA-EDA) with polylactic acid (PLA), and subsequent reaction with lactose, obtaining PHEA-EDA-PLA-GAL copolymer. To enhance the entrapment into obtained nanostructures, a hydrophobic RBV prodrug, that is, RBV tripalmitate, was synthesized and its capability to release RBV in the presence of an adequate enzymatic activity was demonstrated. Liver…
Jenisseensosides C and D, biologically active acylated triterpene saponins from Silene jenisseensis
1997
Abstract We previously reported the isolation and structure elucidation of a new trans - p -methoxycinnamoyl triterpene-saponin along with its cis - p -methoxycinnamoyl isomer as an inseparable mixture from the roots of Silene jenisseensis . In a continuing study on this plant, two additional new acylated triterpene-saponins were obtained as an inseparable mixture. Their structures have been established by chemical means and spectroscopic methods including 1D and 2D homonuclear and heteronuclear correlation NMR spectroscopy as 3- O -[β- d -galactopyranosyl-(1 → 2)-β- d -glucuronopyranosyl]-28- O -[{α- l -rhamnopyranosyl-(1 → 2)}- {4- O - trans - p -methoxycinnamoyl}-β- d -fucopyranosyl] qui…
Real‐world evidence of tisagenlecleucel for the treatment of relapsed or refractory large B‐cell lymphoma
2021
Abstract Tisagenlecleucel (tisa‐cel) is a second‐generation autologous CD19‐targeted chimeric antigen receptor (CAR) T‐cell therapy approved for relapsed/refractory (R/R) large B‐cell lymphoma (LBCL). The approval was based on the results of phase II JULIET trial, with a best overall response rate (ORR) and complete response (CR) rate in infused patients of 52% and 40%, respectively. We report outcomes with tisa‐cel in the standard‐of‐care (SOC) setting for R/R LBCL. Data from all patients with R/R LBCL who underwent leukapheresis from December 2018 until June 2020 with the intent to receive SOC tisa‐cel were retrospectively collected at 10 Spanish institutions. Toxicities were graded accor…