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Antagonistic Properties (antagonistic + property)
Selected AbstractsA Mechanism of Vasodilatory Action of Polyamines and Acetylpolyamines: Possible Involvement of their Ca2+ Antagonistic PropertiesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2000CHANG-SEON MYUNG Polyamines, a class of low-molecular weight organic polycations, have been shown to produce relaxing effects in vascular smooth muscles, although the mechanism has not been carefully examined. In this study, the mechanism of vascular action of polyamines and their metabolites, acetylpolyamines, was pharmacologically examined in the rabbit isolated thoracic aorta focusing on an endothelium-dependent component of vasodilatation and Ca2+ influx through plasma membrane channels. Both polyamines and acetylpolyamines (except N1 -acetylputrescine, which produced no response or very slight contraction) caused concentration-dependent relaxation in pre-constricted aortic rings containing an intact endothelium. Aortic rings denuded of endothelium were also responsive to both polyamines and acetylpolyamines. Inhibitors of nitric oxide (reduced haemoglobin and N, -nitro- l -arginine methyl ester), vasodilator prostaglandins (indomethacin) and guanylyl cyclase (methylene blue) did not affect the relaxation induced by both polyamines and acetylpolyamines in either endothelium-intact or -denuded aortic rings. Both polyamines and acetylpolyamines inhibited the concentration-dependent contraction for phenylephrine and K+. The Ca2+ agonist Bay K 8644 induced concentration-dependent contraction in segments of rabbit aorta partially depolarized with 15 mm KCl, and both polyamines and acetylpolyamines relaxed the Bay K 8644-induced contraction in a concentration-dependent manner. Interestingly, both polyamines and acetylpolyamines also decreased contractions evoked by the Ca2+ ionophore A23187. The concentration-response curve to exogenous Ca2+ in K+ -depolarization medium (K+ = 120 mm) was shifted to the right by both polyamines and acetylpolyamines. The response elicited by Ca2+ was increased by Bay K 8644 (10,6m), and this potentiation was also inhibited by both polyamines and acetylpolyamines. The results indicate that both polyamines and acetylpolyamines can induce vasorelaxation of rabbit thoracic aorta by an endothelium-independent mechanism in-vitro and relax vascular smooth muscle by acting at the plasma membrane level, decreasing the influx of Ca2+. Therefore, polyamines and acetylpolyamines may have Ca2+ antagonistic properties which may, in part, be involved in the mechanism of rabbit aortic vascular smooth muscle relaxation. [source] Two similar enhanced root-colonizing Pseudomonas strains differ largely in their colonization strategies of avocado roots and Rosellinia necatrix hyphaeENVIRONMENTAL MICROBIOLOGY, Issue 12 2008Clara Pliego Summary Pseudomonas alcaligenes AVO73 and Pseudomonas pseudoalcaligenes AVO110 were selected previously as efficient avocado root tip colonizers, displaying in vitro antagonism towards Rosellinia necatrix, causal agent of avocado white root rot. Despite the higher number of antagonistic properties shown in vitro by AVO73, only AVO110 demonstrated significant protection against avocado white root rot. As both strains are enhanced root colonizers, and as colonization is crucial for the most likely biocontrol mechanisms used by these strains, namely production of non-antibiotic antifungal compounds and competition for nutrients and niches, we decided to compare the interactions of the bacterial strains with avocado roots as well as with R. necatrix hyphae. The results indicate that strain AVO110 is superior in biocontrol trait swimming motility and establishes on the root tip of avocado plants faster than AVO73. Visualization studies, using Gfp-labelled derivatives of these strains, showed that AVO110, in contrast to AVO73, colonizes intercellular crevices between neighbouring plant root epidermal cells, a microhabitat of enhanced exudation. Moreover, AVO110, but not AVO73, also colonizes root wounds, described to be preferential penetration sites for R. necatrix infection. This result strongly suggests that AVO110 meets, and can attack, the pathogen on the root. Finally, when co-inoculated with the pathogen, AVO110 utilizes hyphal exudates more efficiently for proliferation than AVO73 does, and colonizes the hyphae more abundantly than AVO73. We conclude that the differences between the strains in colonization levels and strategies are likely to contribute to, and even can explain, the difference in disease-controlling abilities between the strains. This is the first report that shows that two similar bacterial strains, selected by their ability to colonize avocado root, use strongly different root colonization strategies and suggests that in addition to the total bacterial root colonization level, the sites occupied on the root are important for biocontrol. [source] Yeasts as antagonists against fireblightEPPO BULLETIN, Issue 3 2004A. Seibold Yeasts are potential antagonists of microorganisms in the phyllosphere. Due to their osmotolerance, they should also be able to colonize apple flowers. In field experiments, we applied yeast agents against fireblight at two different sites in the southern part of Germany. They showed efficiencies 0,20% below Plantomycin (streptomycin). Co-culture experiments in liquid basal media with synthetic nectar resulted in suppression of Erwinia amylovora by yeast. This effect could not be confirmed with population studies of yeasts and E. amylovora in flower clusters. Field and laboratory experiments indicated that yeasts have antagonistic properties against fireblight but further research is needed to investigate this potential. [source] Identification of a human estrogen receptor ,-derived antiestrogenic peptide that adopts a polyproline II conformationJOURNAL OF PEPTIDE SCIENCE, Issue 7 2009Josef Kapitán Abstract Polyproline II (PPII) helix is an extended secondary structure present in a number of proteins. PPII-containing sequences mediate specific protein,protein interactions with partners containing appropriate cognate domains called PPII-recognizing domains (PRDs) and are involved in the activation of intracellular signaling pathways. Thus, the identification of PPII structures in proteins is of great interest, not only to explore molecular and physiological mechanisms, but also to elaborate new potential drugs. By revisiting X-ray crystal structures of liganded ,-type human estrogen receptor (ER,), we have identified an 11-residue PPII-helical sequence (D321AEPPILYSEY331) in the ligand-binding domain of the receptor. The data recorded by far-ultraviolet circular dichroism (far-UV CD), vibrational Raman optical activity (ROA) and differential scanning calorimetry (DSC) show that the corresponding peptide (Ac-DAEPPILYSEY-NH2) is particularly well structured in PPII, with the same proportion of PPII as observed from X-ray structures (,85%). In addition, studies carried out on ER,-negative Evsa-T breast cancer cells transiently co-transfected with a pcDNA3-ER, plasmid and a Vit-tk-Luc reporter gene revealed that the peptide antagonizes the estradiol-induced transcription providing perspectives for researching new molecules with antagonistic properties. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd. [source] Molecular dynamics simulation of human neurohypophyseal hormone receptors complexed with oxytocin,modeling of an activated stateJOURNAL OF PEPTIDE SCIENCE, Issue 3 2006Magdalena J., lusarz Abstract The neurohypophyseal hormone oxytocin (CYIQNCPLG-NH2, OT) is involved in the control of labor, secretion of milk and many social and behavioral functions via interaction with its receptors (OTR) located in the uterus, mammary glands and peripheral tissues, respectively. In this paper we propose the interactions responsible for OT binding and selectivity to OTR versus vasopressin ([F3,R8]OT, AVP) receptors: V1aR and V2R, all three belonging to the Class A G protein-coupled receptors (GPCRs). Three-dimensional models of the activated receptors were constructed using a multiple sequence alignment and the activated rhodopsin,transducin (MII,Gt) prototype [,lusarz and Ciarkowski, 2004] as a template. The 1 ns unconstrained molecular dynamics (MD) of three pairs of receptor,OT complexes (two complexes per each receptor) immersed in the fully hydrated 1-palmitoyl-2-oleoyl- sn -glycero-3-phosphatidylcholine (POPC) lipid bilayer was conducted in the AMBER 7.0 force field. The relaxed models of ligand,receptor complexes were used to identify the putative binding sites of OT. The stabilizing interactions with conserved Gln residues in all complexes were identified. The nonconserved hydrophobic residues were proposed as responsible for OTR,OT selectivity and ligand recognition. These results provide guidelines for experimental site-directed mutagenesis and if confirmed, they may be helpful in designing new selective OT analogs with both agonistic or antagonistic properties. Copyright © 2005 European Peptide Society and John Wiley & Sons, Ltd. [source] A Mechanism of Vasodilatory Action of Polyamines and Acetylpolyamines: Possible Involvement of their Ca2+ Antagonistic PropertiesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2000CHANG-SEON MYUNG Polyamines, a class of low-molecular weight organic polycations, have been shown to produce relaxing effects in vascular smooth muscles, although the mechanism has not been carefully examined. In this study, the mechanism of vascular action of polyamines and their metabolites, acetylpolyamines, was pharmacologically examined in the rabbit isolated thoracic aorta focusing on an endothelium-dependent component of vasodilatation and Ca2+ influx through plasma membrane channels. Both polyamines and acetylpolyamines (except N1 -acetylputrescine, which produced no response or very slight contraction) caused concentration-dependent relaxation in pre-constricted aortic rings containing an intact endothelium. Aortic rings denuded of endothelium were also responsive to both polyamines and acetylpolyamines. Inhibitors of nitric oxide (reduced haemoglobin and N, -nitro- l -arginine methyl ester), vasodilator prostaglandins (indomethacin) and guanylyl cyclase (methylene blue) did not affect the relaxation induced by both polyamines and acetylpolyamines in either endothelium-intact or -denuded aortic rings. Both polyamines and acetylpolyamines inhibited the concentration-dependent contraction for phenylephrine and K+. The Ca2+ agonist Bay K 8644 induced concentration-dependent contraction in segments of rabbit aorta partially depolarized with 15 mm KCl, and both polyamines and acetylpolyamines relaxed the Bay K 8644-induced contraction in a concentration-dependent manner. Interestingly, both polyamines and acetylpolyamines also decreased contractions evoked by the Ca2+ ionophore A23187. The concentration-response curve to exogenous Ca2+ in K+ -depolarization medium (K+ = 120 mm) was shifted to the right by both polyamines and acetylpolyamines. The response elicited by Ca2+ was increased by Bay K 8644 (10,6m), and this potentiation was also inhibited by both polyamines and acetylpolyamines. The results indicate that both polyamines and acetylpolyamines can induce vasorelaxation of rabbit thoracic aorta by an endothelium-independent mechanism in-vitro and relax vascular smooth muscle by acting at the plasma membrane level, decreasing the influx of Ca2+. Therefore, polyamines and acetylpolyamines may have Ca2+ antagonistic properties which may, in part, be involved in the mechanism of rabbit aortic vascular smooth muscle relaxation. [source] Riluzole prolongs survival time and alters nuclear inclusion formation in a transgenic mouse model of Huntington's diseaseMOVEMENT DISORDERS, Issue 4 2002Johannes Schiefer MD Abstract Glutamate excitotoxicity has been suggested to contribute to the pathogenesis of Huntington's disease (HD). Riluzole is a substance with glutamate antagonistic properties that is used for neuroprotective treatment in amyotrophic lateral sclerosis and which is currently tested in clinical trials for treatment of HD. R6/2 transgenic mice, which express exon 1 of the human HD gene with an expanded CAG triplet repeat, serve as a well-characterized mouse model for HD with progressing neurological abnormalities and limited survival. We treated R6/2 HD transgenic mice with riluzole orally beginning at a presymptomatic stage until death to investigate its potential neuroprotective effects in this mouse model and found that survival time in the riluzole group was significantly increased in comparison to placebo-treated transgenic controls. Additionally, the progressive weight loss was delayed and significantly reduced by riluzole treatment; behavioral testing of motor coordination and spontaneous locomotor activity, however, showed no statistically significant differences. We also examined the formation of the HD characteristic neuronal intranuclear inclusions (NII) immunohistologically. At a late disease stage, striatal NII from riluzole-treated transgenic mice showed profound changes in ubiquitination, i.e., NII were less ubiquitinated and surrounded by ubiquitinated micro-aggregates. Staining with antibodies directed against the mutated huntingtin revealed no significant difference in this component of NII. Taken together, these data suggest that riluzole is a promising candidate for neuroprotective treatment in human HD. © 2002 Movement Disorder Society [source] Interactions between Fusarium species from sugarcane and the stalk borer, Eldana saccharina (Lepidoptera: Pyralidae)ANNALS OF APPLIED BIOLOGY, Issue 3 2009S.A. McFarlane Abstract In this study, beneficial relationships between Fusarium species in sugarcane and the stalk borer, Eldana saccharina (Lepidoptera: Pyralidae) were demonstrated in vitro. In addition, Fusarium species with antagonistic properties were found to inhabit sugarcane. Attenuated Fusarium isolates from sugarcane stalks collected across the South African sugar industry were incorporated into diet formulated to mass rear E. saccharina. Of the over 200 Fusarium isolates obtained, 10 that significantly improved the survival and development of E. saccharina larvae and considered to be beneficial were selected for further study, as were 10 that were detrimental or antagonistic to the stalk borer. Twelve of the selected isolates were identified as F. sacchari by direct sequencing of translation elongation factor-1, fragments, eight of which resulted in reduced numbers of surviving larvae and significantly lower larval masses. F. proliferatum isolates resulted in increased survival and mass of E. saccharina and three of the five isolates assigned to the F. pseudonygamai group enhanced E. saccharina development. Results from olfactory choice experiments suggested the production of attractive and repellent metabolites by certain isolates. Findings from this study may offer additional or alternative strategies for managing E. saccharina infestation of sugarcane. [source] Estrogenic agonism and antagonism of the soy isoflavone genistein in uterus, bone and lymphopoiesis in mice,APMIS, Issue 5 2005M. C. ERLANDSSON The isoflavone genistein (Gen) is a naturally occurring phytoestrogen found in high concentrations in soy. The biological effects of Gen have been extensively studied. The immunomodulating properties of Gen are, however, less well investigated and the results are contradictory. Our aim was to study possible estrogen agonistic and antagonistic properties of Gen in uterus, bone, lymphopoiesis and B-cell function by comparing effects in castrated and intact female mice, respectively. Oophorectomized (OVX) and sham-operated mice were treated with s.c. doses of 17,-estradiol (E2) (0.16 mg/kg), Gen (50 mg/kg), or vehicle (olive oil) as control. Effects on bone mineral density (BMD) were studied using peripheral quantitative computerized tomography, uterine and thymus weights were examined, lymphopoiesis in thymus and bone marrow was analyzed using flow cytometry, and the frequency of immunoglobulin-producing B cells in bone marrow and spleen was studied using an ELISPOT assay. Gen was clearly antagonizing endogenous estrogen in sham-operated female mice as shown by inhibiting the uterine weight and by increasing the frequency of B lymphopoietic cells in bone marrow. The only agonistic effect of Gen was shown by increased BMD in OVX mice. Our results are discussed in the context of estrogen receptor biology. [source] Penaeus monodon larvae can be protected from Vibrio harveyi infection by pre-emptive treatment of a rearing system with antagonistic or non-antagonistic bacterial probioticsAQUACULTURE RESEARCH, Issue 6 2010Srinivas Somnath Pai Abstract This study shows that the disease resistance and survival rate of Penaeus monodon in a larval rearing systems can be enhanced by supplementing with antagonistic or non-antagonistic probiotics. The antagonistic mode of action of Pseudomonas MCCB 102 and MCCB 103 against vibrios was demonstrated in larval mesocosm with cultures having sufficient concentration of antagonistic compounds in their culture supernatant. Investigations on the antagonistic properties of Bacillus MCCB 101, Pseudomonas MCCB 102 and MCCB 103 and Arthrobacter MCCB 104 against Vibrio harveyi MCCB 111 under in vitro conditions revealed that Pseudomonas MCCB 102 and MCCB 103 were inhibitory to the pathogen. These inhibitory properties were further confirmed in the larval rearing systems of P. monodon. All these four probionts significantly improved larval survival in long-term treatments as well as when challenged with a pathogenic strain of V. harveyi MCCB 111. We could demonstrate that Pseudomonas MCCB 102 and MCCB 103 accorded disease resistance and a higher survival rate in P. monodon larval rearing systems through active antagonism of vibrios, whereas Bacillus MCCB 101 and Arthrobacter MCCB 104 functioned as probiotics through immunostimulatory and digestive enzyme-supporting modes of action. [source] Cardiovascular Properties of Yangambin, a Lignan Isolated from Brazilian PlantsCARDIOVASCULAR THERAPEUTICS, Issue 4 2001Eduardo Tibiriçá ABSTRACT Yangambin was initially selected from a number of lignans isolated from Brazilian plants for its ability to antagonize Platelet-Activating Factor (PAF, 1- O -hexadecyl-2-acetyl-sn-glyceryl-3-phosphorylcholine)-induced biological effects. Subsequently it was shown that, besides its antagonistic properties at PAF receptors, yangambin also prevents the cardiovascular collapse observed during anaphylactic and endotoxic/septic shocks, as well as the vascular and cardiac hyporesponsiveness to catecholamines in endotoxic shock. It is suggested that this naturally occurring compound could be of potential interest in the adjunctive management of the above mentioned pathologies. In the present article, we review the main studies investigating the pharmacological properties of yangambin related to the cardiovascular function. [source] | |||||||||||||