Search results for "Potency"
showing 10 items of 122 documents
The Effect of Fluctuating Temperature on the Stability of Turoctocog Alfa for Hemophilia A
2019
Abstract Background and objective Factor VIII (FVIII) is indicated for the prevention or treatment of bleeding in patients with hemophilia A. FVIII product stability under high and fluctuating temperatures is important, particularly for patients who reside in, or travel to, regions with high ambient temperatures, as they may remove their product from the refrigerator and return it, unused, multiple times. We evaluated the effect of variable temperature storage conditions, including up to 40 °C, on the stability of the recombinant FVIII product, turoctocog alfa. Methods Turoctocog alfa dry powder stability was assessed when moved between storage conditions of 5 °C (ambient humidity) and 40 °…
Cytotoxic Potencial Acetogenins ofAnnonaGenus
2016
Over the centuries, nature has contributed to the basic needs of human beings. In particular, plants have cooperated as a source of drugs for the treatment of a broad spectrum of diseases because of the structural diversity of secondary metabolites. With strict attention to antineoplastic therapy, the search for anticancer drugs has increased in order to meet more specific and selective treatments. The acetogenins (ACGs), a class of secondary metabolites found exclusively in the family Annonaceae, are substances of great importance due to their well-known cytotoxic potency in human tumor cell lines in vitro , which can be exploited in designing anticancer agents. Among the 150 genera of Ann…
Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors
2021
Despite the therapeutic relevance of δ-containing γ-aminobutyric acid type A receptors (GABAARs) and the need for δ-selective compounds, the structural determinants for the mode and molecular site of action of δ-selective positive allosteric modulator imidazo[1,2-a]pyridine DS2 remain elusive. To guide the quest for insight, we synthesized a series of DS2 analogues guided by a structural receptor model. Using a fluorescence-based fluorometric imaging plate reader membrane potential assay, we found that the δ-selectivity and the pharmacological profile are severely affected by substituents in the 5-position of the imidazopyridine core scaffold. Interestingly, the 5-methyl, 5-bromo, and 5-chl…
Getting new bronchodilator compounds from molecular topology.
2003
Abstract Molecular topology has been used to select new lead bronchodilator compounds. The main advantage of this method, as compared to others frequently used, is that it does not require a previous explicit knowledge of the mechanism of action (MOA) of the compounds analyzed. A large database (12,000 chemicals) has been examined in this study to find less than 5% compounds with bronchodilator activity. After removing those compounds already described as bronchodilators, we present here the results for 20 among these compounds, some of them showing other pharmacological activities. Some of the compounds selected in this study showed higher relaxation and higher potency than theophylline, w…
ChemInform Abstract: Tucupentol, a Novel Mono-tetrahydrofuranic Acetogenin from Annona montana, as a Potent Inhibitor of Mitochondrial Complex I.
2009
Ten acetogenins, one of them new, were isolated from leaves and twigs of a Bolivian collection of Annona montana. The new compound that we named tucupentol (1) is a mono-tetrahydrofuran-pentahydroxy-acetogenin. The inhibitory potency of tucupentol (1) on the mitochondrial complex I was evaluated, and this activity was compared with that of the known acetogenins, annonacin-A, cis-annonacin-10-one, aromin, and gigantetronenin, also isolated from this plant material. The mentioned acetogenins acted as selective inhibitors of mitochondrial complex I in the 0.8-5.4-nM range.
Bioactive chromenes from Rhyncholacis penicillata.
1994
Investigation of the aerial parts of Rhyncholacis penicillata afforded the new chromenes, 7-hydroxy-6-(3-methylbutyryl)-5-oxymethyl-chromene (rhynchonin A) and 7-hydroxy-6-(2-methylbutyryl)-6-oxymethylchromene (rhynchonin B). Structures were elucidated by spectroscopic methods and independent synthesis. Rhynchonin A showed broad insecticidal, acaricidal and nematicidal potency including strong biological activity against Heliothis zea.
Pharmacodynamic approach to study the gene transfer process employing non-viral vectors
2000
Abstract In the present work we set out to apply pharmacodynamic concepts derived from dose–response curves (Potency and Efficacy) to characterize the gene transfer efficiency of a vector:DNA complex. We employed two widely used vectors, the cationic lipid DOTAP (N,N,N-trimethyl 1-2-3-bis (1-oxo-9-octa-decenyl)oxy-(Z,Z)-1-propanaminium methyl sulfate) and the cationic polymer PEI (polyethylenimine, 800 kDa) to transfect several constructions of the green fluorescent protein cDNA. The analysis of dose–response curves indicated that in all cases the goodness-of-fit was > 0.99. Potency is a measure that provides information on gene activity per amount of DNA. Efficacy is a measure of maximum g…
Multipotent adult germline stem cells and embryonic stem cells have similar microRNA profiles.
2008
Spermatogonial stem cells (SSCs) isolated from the adult mouse testis and cultured have been shown to respond to culture conditions and become pluripotent, so called multipotent adult germline stem cells (maGSCs). microRNAs (miRNAs) belonging to the 290 and 302 miRNA clusters have been previously classified as embryonic stem cell (ESC) specific. Here, we show that these miRNAs generally characterize pluripotent cells. They are expressed not only in ESCs but also in maGSCs as well as in the F9 embryonic carcinoma cell (ECC) line. In addition, we tested the time-dependent influence of different factors that promote loss of pluripotency on levels of these miRNAs in all three pluripotent cell t…
The role of information and communication technologies in the relationship between group potency and group maintenance outcomes: a longitudinal study
2013
Group potency is one of the major factors influencing work group success. However, little is known about the effects of potency on group maintenance outcomes, especially in virtual teams. The present study examines the moderating role of information and communication technologies ICTs in the relationships between potency and group maintenance outcomes in a longitudinal study. The study involved 44 groups of four members each, working in two communication media: face-to-face F-t-F and computer-mediated communication CMC. The groups developed a project during four weekly sessions over a 1-month period. The results showed that ICTs moderated the relationship between potency and maintenance out…
Modulation of MHC Class II Determinants on Rat Langerhans Cells During Short Term Culture
1993
Epidermal Langerhans cells (LC) are regarded as the most peripheral outpost of the immune system. They play a pivotal role during the onset of an immune response in the skin. One of the principal functions of LC is reflected in their extraordinary potency to present antigen to high activation requiring naive T cells.