Search results for "Biological activity"
showing 10 items of 465 documents
Anti-inflammatory effects of cerebrocrast in a model of rat paw edema and on mononuclear THP-1 cells.
2002
Cerebrocrast (IOS 1.1212; 4-[2-(difluoromethoxy)phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid di(2-propoxyethyl) diester) is a novel derivative of 1,4-dihydropyridine, which does not antagonize Ca(2+) influx in neuronal tissues. Since several classical dihydropyridines possess anti-inflammatory properties, we first studied the effects of cerebrocrast in a model of rat paw edema induced by carrageenan. Cerebrocrast had a preventative effect in this model of inflammation, with maximal activity (32-45% inhibition) in the 0.1-0.25 mg kg(-1) range. It was ineffective when added after the injection of carrageenan. Subsequent in vitro experiments showed that cerebrocrast in the mi…
Insulin-Mimetic Action of Vanadate
2001
Abstract — — The insulin-mimetic effect of vanadate is well established, and vanadate has been shown to improve insulin sensitivity in diabetic rats and humans. Although the exact mechanism(s) remain undefined, we have previously demonstrated a direct relation of intracellular free magnesium (Mg i ) levels to glucose disposal, to insulinemic responses following glucose loading, and to insulin-induced ionic effects. To investigate whether the insulin-mimetic effects of vanadate could similarly be mediated by Mg i , we utilized 31 P-nuclear magnetic resonance spectroscopy to measure Mg i in erythrocytes from normal (NL, n=10) and hypertensive (HTN, n=12) subjects, before and after incubation…
Differential effects of isoliquiritigenin and YC-1 in rat aortic smooth muscle.
1997
We investigated the effects of isoliquiritigenin and YC-1 (3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole) on tension in endothelial-free rat aortic rings precontracted with phenylephrine (3 microM). Both compounds induced a concentration-dependent relaxation (EC50 of YC-1 1.9 microM and of isoliquiritigenin 9.4 microM). The effects developed faster with YC-1 than with isoliquiritigenin, and the effects of YC-1 were potentiated by isoliquiritigenin (10 microM). 1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one (30 microM) inhibited the effect of YC-1, but not of isoliquiritigenin. These results suggest that the effects of YC-1 are due to stimulation of soluble guanylyl cyclase activity, whereas …
Effects of Lycopene, Indole-3-Carbinol, and Luteolin on Nitric Oxide Production and iNOS Expression are Organ-Specific in Rats
2010
Effects of Lycopene, Indole-3-Carbinol, and Luteolin on Nitric Oxide Production and iNOS Expression are Organ-Specific in RatsNatural compounds are known to modify NO content in tissues; however, the biological activity of polyphenol-rich food often does not correspond to the effects of individual polyphenols on NO synthase activity. The aim of this study was to see how natural compounds luteolin, indole-3-carbinol, and lycopene modify NO production in rat tissues and change the expression of the iNOS gene and protein. Indole-3-carbinol produced multiple effects on the NO level; it significantly decreased NO concentration in blood, lungs, and skeletal muscles and increased it in the liver. …
Permissive and suppressive effects of dexamethasone on enzyme induction in hepatocyte co-cultures.
2002
1. Steroids are known to act as permissive factors in hepatocytes. This study shows that dexamethasone (DEX) is a permissive factor for induction of CYP2B1/2, CYP3A1, CYP2A1 and probably also CYP2C11 in cultures with primary rat hepatocytes. 2. The induction factor of phenobarbital (PB)-induced formation of 16beta-hydroxytestosterone (OHT), a testosterone biotransformation product predominantly formed by CYP2B1, is increased 18-fold by the addition of 32 nM DEX to the culture medium. Interestingly, higher concentrations of DEX up to 1000 nM led to a concentration-dependent maximally 5-fold decrease (p = 0.002) of phenobarbital-induced 16beta-OHT formation compared with the effect observed w…
Combination of open field and elevated plus-maze: a suitable test battery to assess strain as well as treatment differences in rat behavior.
1998
Abstract 1. 1. A test battery consisting of a standard open field, an enriched open field and an elevated plus maze was used to study behavior in rats. 2. 2. Male rats of the strains PVG/OlaHsd (PVG) and Sprague-Dawely-Hsd (SPRD) (150–200g body wt) were used to assess interstrain differences as well as handling effects. In a subsequent experiment an other set of male PVG rats (150–200g body wt) treated either with diazepam or zolpidem was used to evaluate the test battery for pharmacological purposes. 3. 3. SPRD rats displayed higher motor activity levels and also higher levels of exploratory behavior than the PVG rats. In contrast plus-maze activity indicated more anxiety of SPRD than PVG …
Naphthalimide imidazolium-based supramolecular hydrogels as bioimaging and theranostic soft materials
2020
1,8-Naphthalimide-based imidazolium salts differing for the alkyl chain length and the nature of the anion were synthesized and characterized to obtain fluorescent probes for bioimaging applications. First, their self-assembly behavior and gelling ability were investigated in water and water/dimethyl sulfoxide binary mixtures. Only salts having longer alkyl chains were able to give supramolecular hydrogels, whose properties were investigated by using a combined approach of fluorescence, resonance light scattering, and rheology measurements. Morphological information was obtained by scanning electron microscopy. In addition, conductive properties of organic salts in solution and gel state we…
Biological activity of the two geometrical isomers of methomyl on maize mitochondria
1983
Abstract Methomyl ( S -methyl- N [(methylcarbamoyl)oxy]thioacetimidate), the active ingredient in lannate insecticide, gave a geometrical isomer after acid
3,5-bis(3'-indolyl)pyrazoles, analogues of marine alkaloid nortopsentin: synthesis and antitumor properties.
2007
A series of 10 bis-indolylpyrazoles of type 9, 10 were obtained by cyclization of diketones 8 using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Derivatives 9a,c,d were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, 9d, the most active compound was effective against all the tested cell lines with a GI(50) mean value of 3.23 microM; TGI and LC(50) values were 14.5 and 58.9 microM having positive response on 91% and 41% of the tested cell lines, respectively.
Effect of triterpenoids on the inflammation induced by protein kinase C activators, neuronally acting irritants and other agents.
2000
In order to establish the mode of the anti-inflammatory activity of triterpenoids, 11 naturally occurring compounds were assayed on mouse ear oedema induced by the protein kinase C activators, mezerein, 12-O-tetradecanoylphorbol-13-acetate (TPA), two 12-deoxyphorbol-13-monoesters (13-tetradecanoate (DPT) and 13-phenylacetate (DPP)) and bryostatin 1, and by resiniferatoxin, xylene and arachidonic acid. The effects on bradykinin-induced paw oedema and on the rat skin inflammation caused by hydrogen peroxide were also examined. The oedema induced by mezerein and DPT was reduced to different extents by the triterpenoids administered epicutaneously (0.5 mg per ear). Against DPT-induced oedema, l…