Search results for "General Pharmacology"

Subcellular distribution of choline acetyltransferase by immunogold electron microscopy in non-neuronal cells: Placenta, airways and murine embryonic…

2012

Abstract Aims Acetylcholine is synthesized in more or less all mammalian cells. However, little is known about the subcellular location of acetylcholine synthesis. Therefore, in the present experiments the subcellular location of the synthesizing enzyme choline acetyltransferase (ChAT) was investigated by anti-ChAT immunogold electron microscopy in human placenta and airways as well as in a murine embryonic stem cell line (CGR8 cell line). Main methods Human tissue was obtained as so-called surplus tissue (after delivery/surgical removal because of lung tumor); the CGR8 stem cell line was cultured under standard conditions. For human tissue a monoclonal mouse anti-ChAT antibody (ab) was use…

Pectin: A Long-Neglected Broad-Spectrum Antibacterial.

2020

First reported in the late 1930s and first partly explained in 1970, the antibacterial activity of pectin remained almost ignored until the late 1990s. The concomitant emergence of research on natural antibacterials and on new usages of pectin polysaccharides, including those in medicine widely researched in Russia, has led to a renaissance of research in the physiological properties of this uniquely versatile polysaccharide ubiquitous in plants and fruits. Collecting scattered information, this study provides an updated overview on the subtle factors affecting the behaviour of pectin as antimicrobial. Less degraded pectin extracted via acid-free routes, we argue in the conclusions, will so…

Physicochemical stability of cabazitaxel containing premix solution and diluted infusion solutions

2015

Objectives This study was conducted to investigate the extended physicochemical stability of cabazitaxel containing premix solution and diluted infusion solutions in either 0.9% sodium chloride (NaCl) or 5% glucose (G5) vehicle solution. Methods A stability indicating, reverse phase, high performance liquid chromatography assay with ultraviolet detection was developed and validated. Premix solutions of cabazitaxel were prepared in the original vials. Infusion solutions were prepared in prefilled polypropylene/polyethylene (PP/PE) infusion bags (0.9% NaCl, G5) to achieve the recommended minimum and maximum cabazitaxel concentrations (0.1 mg/mL, 0.26 mg/mL). Test solutions were stored refrige…

A recent portrait of bioactive triazoles

2010

Scientists have extensively explored new synthetic routes in order to obtain 1,2,3- and 1,2,4-triazoles as they represent a very interesting class of compounds due to their wide range of biological activities such as antitumor, antiinflammatory, analgesic, antifungal, antibacterial, antiviral, etc. This mini review reports the synthesis and the biological activities of compounds containing a triazole moiety published since 2007. No attempt is made to provide a comprehensive literature overview, our aim is to highlight some more recent examples of synthetic biological active compounds. In particular, we focus on the applications of “click reactions” that allow the regioselective synthesis of…

New Effects of Prebiotics, Probiotics, and Symbiotics

2020

Neuroprotective Effects of Low Intensity and Low Frequency Electromagnetic �in vitro� Stimulation on Glial Cells

2020

Degenerative neurological diseases (senile dementia, Alzheimer`s disease, glaucoma), post-stroke sequelae are increasing as prevalence nowadays, in context of aging in general population, and there are strong evidences that astrocytes may play a significant role in neuroprotection. The study evaluates the effects of low intensity low frequency electromagnetic field (EMF) �in vitro� stimulation (195 mA, 7-8 Hz) on the glial cells, in different conditions, in order to identify the neuroprotective potential. Three cell lines were used for the study: the Clonetics (Lonza) line of normal human astrocytes, U87 glioblastoma tumor cells (ATCC) and L929 murine fibroblasts. The cell cultures were ex…

Synthesis of Triazenoazaindoles: a New Class of Triazenes with Antitumor Activity

2011

Despite improvements in the treatment and prevention of cancer, the number of new diagnoses continues to rise; this has fuelled substantial interest in the development of new and effective chemotherapeutic agents. Compounds of the triazene class, such as dacarbazine, have been used in the clinical management of many cancer types including brain, leukemia, and melanoma. A new compound class bearing a triazenoazaindole scaffold was synthesized with the aim of identifying new antiproliferative agents. Compounds 5 a-g and 6 a-c were screened against a panel of human tumor cell lines, and two of them, 5 e and 5 f, showed cytotoxicity (GI(50) range: 2.2-8.2 μM) in all cell lines. These two compou…

Side effects of oxysterols: cytotoxicity, oxidation, inflammation, and phospholipidosis.

2008

Oxysterols are 27-carbon atom molecules resulting from autoxidation or enzymatic oxidation of cholesterol. They are present in numerous foodstuffs and have been demonstrated to be present at increased levels in the plasma of patients with cardiovascular diseases and in atherosclerotic lesions. Thus, their role in lipid disorders is widely suspected, and they might also be involved in important degenerative diseases such as Alzheimer's disease, osteoporosis, and age-related macular degeneration. Since atherosclerosis is associated with the presence of apoptotic cells and with oxidative and inflammatory processes, the ability of some oxysterols, especially 7-ketocholesterol and 7β-hydrox…

Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead

2013

Novel rhodesain inhibitors were obtained by combining an enantiomerically pure 3-bromoisoxazoline warhead with a specific peptidomimetic recognition moiety. All derivatives behaved as inhibitors of rhodesain, with low micromolar Ki values. Their activity against the enzyme was found to be paralleled by an in vitro antitrypanosomal activity, with IC50 values in the mid-micromolar range. Notably, a preference for parasitic over human proteases, specifically cathepsins B and L, was observed.

Development of Novel Selective Peptidomimetics Containing a Boronic Acid Moiety, Targeting the 20S Proteasome as Anticancer Agents

2014

This paper describes the design, synthesis, and biological evaluation of peptidomimetic boronates as inhibitors of the 20S proteasome, a validated target in the treatment of multiple myeloma. The synthesized compounds showed a good inhibitory profile against the ChT-L activity of 20S proteasome. Compounds bearing a β-alanine residue at the P2 position were the most active, that is, 3-ethylphenylamino and 4-methoxyphenylamino (R)-1-{3-[4-(substituted)-2-oxopyridin-1(2H)-yl]propanamido}-3-methylbutylboronic acids (3 c and 3 d, respectively), and these derivatives showed inhibition constants (Ki ) of 17 and 20 nM, respectively. In addition, they co-inhibited post glutamyl peptide hydrolase act…