The Interaction of Procaine with the Nonmyelinated Nerve Axon

1972 ◽  
Vol 50 (2) ◽  
pp. 174-176 ◽  
Author(s):  
Henry Simpkins ◽  
Elaine Panko ◽  
Sin Tay
Keyword(s):  
Conformational Change ◽  
Potent Inhibitor ◽  
Homarus Americanus ◽  
The Other ◽  
Nerve Axon ◽  
Lipid Structure

The interaction of procaine with the nonmyelinated nerve axon from the legs of Homarus americanus was found to produce a conformational change in the lipid structure of the membrane. This conformational change was also observed after treatment of the nerve with acetylcholine bromide but not with any of the following local anesthetics:lidocaine, carbocaine, prilocaine, and nupercaine. It was also found that procaine is a potent inhibitor of acetylcholinesterase whereas the other anesthetics at the same concentration had little effect.

Spatial and Temporal Overlap of the American Lobster (Homarus americanus) and Sea Scallop (Placopecten magellanicus) as Related to the impact of Inshore Scallop Dragging

1992 ◽  
Vol 49 (7) ◽  
pp. 1486-1492 ◽  
Author(s):  
D. L. Roddick ◽  
R. J. Miller
Keyword(s):  
Nova Scotia ◽  
Homarus Americanus ◽  
Fishing Effort ◽  
The Other ◽  
American Lobster ◽  
Placopecten Magellanicus ◽  
Time And Space ◽  
Sea Scallop ◽  
The Impact ◽  
Temporal Overlap

Assessment of the damage of one fishery by another requires knowledge of the overlap, in time and space, of the damaging fishing effort and the abundance of the damaged species, as well as a measure of the rate of damage. This approach was used to measure the impact of inshore scallop dragging on lobsters in Nova Scotia. Areas of reported co-occurrence of lobster and scallop grounds were surveyed by divers to determine the extent of overlap. Only 2 of 52 sites surveyed had lobsters on scallop grounds that could be dragged. Divers surveyed one site six times during 1987 and 1988 and found lobsters most abundant during August and September. Only 2% of the lobsters in the path of scallop drags were either captured or injured. The estimated value of lobsters destroyed by dragging for scallops during periods of peak lobster abundance was minor: $757 at one site and $176 at the other. Restricting dragging to periods of low lobster abundance significantly reduces this cost.

A Bacteriological study on mineral trioxide aggregate and calcium hydroxide as materials against Streptococcus mutans

2021 ◽  
Vol 30 (1) ◽  
pp. 1-7
Author(s):  
Kareman A. Eshra ◽  
Rasha Adel Elkholy ◽  
Arafa Mohamed Khatab ◽  
Radwa Abd Elmotaleb Eissa
Keyword(s):  
Dental Caries ◽  
Calcium Hydroxide ◽  
Streptococcus Mutans ◽  
Potent Inhibitor ◽  
Mineral Trioxide Aggregate ◽  
The Other ◽  
Primary Molars ◽  
Restorative Material ◽  
Bacteriological Study ◽  
Microbiological Parameters

Background: Streptococcus mutans play an important role in occurrence of dental caries objective: to compare the clinical and microbiological antibacterial outcomes of Mineral trioxide aggregate (MTA) and Calcium hydroxide cement Ca(OH)2. Methodology: 20 primary molars in 10 children with year’s 5-9 y .For each child one tooth was treated with Ca(OH)2 and the other with MTA. Finally, all the cavities were restored using compomer restorative material, and then microbiological parameters were recorded. Results: MTA treated teeth did not show any clinical sign or symptoms of failure. While three teeth treated with Ca(OH)2 were excluded because of necrosis. Changes in color and consistency of dentin were nearly the same for both groups. Microbiological evaluation showed a decrease in the count of Str. mutans with calcium hydroxide and complete killing of bacteria with MTA. Conclusion: The treatment showed satisfactory results of MTA as it was more potent inhibitor of bacterial-growth than Ca(OH)2

Thromboxane-Synthetase Inhibitors Could Be “Large Spectrum” Anti-Aggregating Agents

1981 ◽  
Author(s):  
C Bonne ◽  
B Martin
Keyword(s):  
Platelet Aggregation ◽  
Potent Inhibitor ◽  
Platelet Rich Plasma ◽  
Rat Aorta ◽  
The Other ◽  
Vascular Tissues ◽  
Synthetase Inhibitor ◽  
Compound C ◽  
Thromboxane Synthetase ◽  
Dependent Pathway

“Large spectrum”anti-aggregating activity could be only achieved by agents which increased the c AMP content of platelets. Cyclo-oxygenase inhibitors could only block the Thromboxane (Tx)- dependent pathway of platelet aggregation. Conversely, Tx-synthetase inhibitors could deviate the endoperoxides metabolism to anti-aggregating prostaglandins in particular in the presence of vascular tissues. In this study we have investigated the effect of CBS634 (1-(3-hydroxy- 1 - octenyl)-imidazole nicotinic ester, dichlorhydra- teD, a potent inhibitor of T×A2 synthesis, both on the production of anti-aggregating prosta- glandins and on the simultaneous c AMP synthesis in platelets.Rat aorta fragments pretreated with aspirin were incubated with rat platelet rich plasma in the presence or absence of tested compound, c AMP, T×B2, PGE2 and 6-keto-PGFF1α were determined by radioimmunoassays.In the presence of CBS63U (50μM), T×B2 formation was reduced from 17 ± 2 to 0.2 ng/ml/min. In parallel, PGE production in controls was 1.4 ± 0.6 and 8 ± 1 ng/ml/min in the presence of the drug. On the other hand, 6-keto-PGF1α formation, very low in controls, rose to 4 ±1.2 ng/mV min in the presence of CBS63U. Radiochemical assays performed with c14C)-arachidonate confirmed that metabolic deviation. The increased level of c AMP formed in the presence of T×A2-synthetase inhibitor supports the hypothesis that such a drug could present a “large spectrum”antiaggregating activity.

scholarly journals Acetylcholinesterase and Butyrylcholinesterase Inhibitory Compounds from Corydalis Cava (Fumariaceae)

2011 ◽  
Vol 6 (5) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Jakub Chlebek ◽  
Kateřina Macáková ◽  
Lucie Cahlíková ◽  
Milan Kurfürst ◽  
Jiří Kuneš ◽  
...  
Keyword(s):  
Human Blood ◽  
Inhibitory Activity ◽  
Potent Inhibitor ◽  
The Other ◽  
Spectroscopic Techniques ◽  
Dependent Manner ◽  
Isoquinoline Alkaloids ◽  
Chemical Structures ◽  
Inhibitory Compounds ◽  
Dose Dependent

Tubers of Corydalis cava were extracted with ethanol and fractionated using n-hexane, chloroform and ethanol. Repeated column chromatography, preparative TLC and crystallization led to the isolation of fifteen isoquinoline alkaloids. The chemical structures of the isolated compounds were determined on the basis of spectroscopic techniques and by comparison with literature data. All isolated compounds were tested for human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity. (+)-Canadaline inhibited acetylcholinesterase as well as butyrylcholinesterase in a dose-dependent manner with IC50 values of 20.1 ± 1.1 μM and 85.2 ± 3.2 μM, respectively. (+)-Canadine, with an IC50 value of 12.4 ± 0.9 μM, was the most potent inhibitor of acetylcholinesterase, whilst (±)-corycavidine and (+)-bulbocapnine were effective inhibitors of butyrylcholinesterase with IC50 values of 46.2 ± 2.4 uM and 67.0 ± 2.1 μM, respectively. The other isolated alkaloids were considered inactive (IC50 > 100 μM).

scholarly journals Inhibitor of Apoptosis Protein cIAP2 Is Essential for Lipopolysaccharide-Induced Macrophage Survival

2006 ◽  
Vol 26 (2) ◽  
pp. 699-708 ◽  
Author(s):  
Damiano Conte ◽  
Martin Holcik ◽  
Charles A. Lefebvre ◽  
Eric LaCasse ◽  
David J. Picketts ◽  
...  
Keyword(s):  
Inflammatory Response ◽  
Potent Inhibitor ◽  
Nuclear Factor Κb ◽  
Innate Immune ◽  
The Other ◽  
Inhibitor Of Apoptosis ◽  
Nuclear Factor ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptotic Death ◽  
Apoptosis Protein

ABSTRACT The cellular inhibitor of apoptosis 2 (cIAP2/HIAP1) is a potent inhibitor of apoptotic death. In contrast to the other members of the IAP family, cIAP2 is transcriptionally inducible by nuclear factor-κB in response to multiple triggers. We demonstrate here that cIAP2−/− mice exhibit profound resistance to lipopolysaccharide (LPS)-induced sepsis, specifically because of an attenuated inflammatory response. We show that LPS potently upregulates cIAP2 in macrophages and that cIAP2−/− macrophages are highly susceptible to apoptosis in a LPS-induced proinflammatory environment. Hence, cIAP2 is critical in the maintenance of a normal innate immune inflammatory response.

scholarly journals The murine gammaherpesvirus-68 M11 protein inhibits Fas- and TNF- induced apoptosis

1999 ◽  
Vol 80 (10) ◽  
pp. 2737-2740 ◽  
Author(s):  
Guang-Hua Wang ◽  
Tara L. Garvey ◽  
Jeffrey I. Cohen
Keyword(s):  
Hela Cells ◽  
Potent Inhibitor ◽  
Family Members ◽  
The Other ◽  
Inhibitor Of Apoptosis ◽  
Murine Gammaherpesvirus ◽  
Tnf Α ◽  
Gammaherpesvirus 68 ◽  
Induced Apoptosis ◽  
Murine Gammaherpesvirus 68

The murine gammaherpesvirus-68 (MHV-68) M11 gene encodes a protein predicted to have limited homology to the bcl-2 family of proteins. Unlike most of the other viral bcl-2 homologues, which have both BH1 and BH2 domains conserved with respect to bcl-2, the M11 protein has a BH1 domain, but apparently lacks a BH2 domain. Transfection of HeLa cells with an epitope-tagged MHV-68 M11 construct showed that the protein is predominantly located in the cytoplasm of cells. In HeLa cells, M11 inhibited apoptosis induced by anti-Fas antibody and by TNF-α. Thus, despite its limited conservation with respect to other bcl-2 family members, the MHV-68 M11 protein is a potent inhibitor of apoptosis.

Biosynthesis of Trimethylammonium Compounds in Aquatic Animals: III. Choline Metabolism in Marine Crustacea

1962 ◽  
Vol 19 (3) ◽  
pp. 505-510 ◽  
Author(s):  
E. Bilinski
Keyword(s):  
Homarus Americanus ◽  
The Other ◽  
Intramuscular Administration ◽  
Cancer Magister ◽  
Aquatic Animals ◽  
Choline Metabolism ◽  
Trimethylamine Oxide

The incorporation in vivo of radioactivity into phospholipid-bound choline has been studied in lobster (Homarus americanus) following intramuscular administration of Na-formate-C14, glycine-2-C14, DL-serine-3-C14, L-methionine-methyl-C14 and choline-methyl-C14. Choline and methionine were utilized for formation of phospholipid choline at both metabolic periods of 24 and 72 hours, whereas the other compounds gave only a very limited labelling.When choline-methyl-C14 was administered to crab (Cancer magister), after 24 hours 1.9% of the administered radioactivity was found in phospholipid choline and 0.1% in trimethylamine oxide.

scholarly journals Conformational changes induced by binding of bivalent cations to oncomodulin, a paravalbumin-like tumour protein

1984 ◽  
Vol 220 (1) ◽  
pp. 261-268 ◽  
Author(s):  
J P MacManus ◽  
A G Szabo ◽  
R E Williams
Keyword(s):  
Conformational Change ◽  
Conformational Changes ◽  
The Other ◽  
Excitation Spectra ◽  
Fluorescence Excitation ◽  
Protein Protein Interaction ◽  
Tyrosine Fluorescence ◽  
Bivalent Cations ◽  
Fluorescence Excitation Spectra ◽  
Dependent Protein

When Mg2+ was added to rat oncomodulin, a paravalbumin-like tumour protein, changes in the c.d. spectrum and tyrosine fluorescence intensity were observed. The addition of Ca2+ resulted in even greater changes in these spectra. The fluorescence excitation spectra of apo- and Mg-oncomodulin were superimposable, whereas that of Ca-oncomodulin was markedly different. The u.v.-absorption spectrum of the Ca2+ form also showed major differences from those of the other two forms. These observations indicate that Ca2+ induced a significant and specific conformational change in the protein that was not observed on binding Mg2+. In contrast, the conformational change induced by either Mg2+ or Ca2+ was identical in the homologous rat parvalbumin. This Ca2+-specific conformational change may be the basis for oncomodulin's Ca2+-dependent protein/protein interaction.

scholarly journals Specificity of Interaction of INI1/hSNF5 with Retroviral Integrases and Its Functional Significance

2004 ◽  
Vol 78 (5) ◽  
pp. 2222-2231 ◽  
Author(s):  
Eric Yung ◽  
Masha Sorin ◽  
Emilie-Jeanne Wang ◽  
Seena Perumal ◽  
David Ott ◽  
...  
Keyword(s):  
Particle Production ◽  
Potent Inhibitor ◽  
Host Factor ◽  
The Other ◽  
Molar Ratio ◽  
Interaction Domain ◽  
Immunodeficiency Virus ◽  
Integrase Interactor 1 ◽  
Hiv 1

ABSTRACT Integrase interactor 1 (INI1)/hSNF5 is a host factor that directly interacts with human immunodeficiency virus type 1 (HIV-1) integrase and is incorporated into HIV-1 virions. Here, we show that while INI1/hSNF5 is completely absent from purified microvesicular fractions, it is specifically incorporated into HIV-1 virions with an integrase-to-INI1/hSNF5 stoichiometry of approximately 2:1 (molar ratio). In addition, we show that INI1/hSNF5 is not incorporated into related primate lentiviral and murine retroviral particles despite the abundance of the protein in producer cells. We have found that the specificity in incorporation of INI1/hSNF5 into HIV-1 virions is directly correlated with its ability to exclusively interact with HIV-1 integrase but not with other retroviral integrases. This specificity is also reflected in our finding that the transdominant mutant S6, harboring the minimal integrase interaction domain of INI1/hSNF5, blocks HIV-1 particle production but not that of the other retroviruses in 293T cells. Taken together, these results suggest that INI1/hNSF5 is a host factor restricted for HIV-1 and that S6 acts as a highly specific and potent inhibitor of HIV-1 replication.

Mutagenesis-induced conformational change in domain B of a pullulan-hydrolyzing α-amylase TVA I

Amylase ◽  
2018 ◽  
Vol 2 (1) ◽  
pp. 1-10 ◽  
Author(s):  
Takashi Tonozuka ◽  
Takanori Nihira ◽  
Masahiro Mizuno ◽  
Atsushi Nishikawa ◽  
Shigehiro Kamitori
Keyword(s):  
Kinetic Analysis ◽  
Crystal Structures ◽  
Conformational Change ◽  
The Other ◽  
Wild Type ◽  
Other Hand ◽  
Thermoactinomyces Vulgaris ◽  
Catalytic Cleft

Abstract An α-amylase from Thermoactinomyces vulgaris, TVA I, hydrolyzes both α-1,4- and α-1,6-glucosidic linkages. Two variants of TVA I have been previously constructed, one containing a substitution of three residues, Ala357- Gln359-Tyr360, with Val-Asn-Glu (AQY/VNE), and the other bearing a deletion of 11 residues from Ala363 to Asn373 (Del11). The activities of both AQY/VNE and Del11 for the α-1,4-glucosidic linkage of maltotriose were decreased compared to that of wild-type TVA I, while the activities of the two variants for the α-1,6-glucosidic linkage of a trisaccharide, isopanose, were less significantly altered. Here, we determined the crystal structures of AQY/VNE and Del11. The structure of AQY/VNE was almost isomorphous with that of wild-type TVA I. On the other hand, the structure of Del11 showed that a conformational change in domain B was induced by the 11-residue deletion, causing narrowing of the catalytic cleft. Taken together with the results of kinetic analysis, this narrower catalytic cleft is likely responsible for the preference of the TVA I enzyme for the α-1,6-glucosidic linkage.

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