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Inhibitor Activity (inhibitor + activity)
Kinds of Inhibitor Activity Selected AbstractsVegetative Storage Protein with Trypsin Inhibitor Activity Occurs in Sapindus mukorassi, a Sapindaceae Deciduous TreeJOURNAL OF INTEGRATIVE PLANT BIOLOGY, Issue 4 2009Shi-Biao Liu Abstract A vegetative storage protein (VSP) with trypsin inhibitor activity in a deciduous tree, Sapindus mukorassi, was characterized by means of sodium dodecyl sulfate-polyacrylamide gel electrophoresis, Western-blot, immuno-histochemical localization, light- and electro-microscopy, together with analysis of proteinase inhibitor activity of the purified VSP in vitro. There were two proteins with molecular masses of about 23 and 27 kDa in a relatively high content in the bark tissues of terminal branches of S. mukorassi in leafless periods. The proteins decreased markedly during young shoot development, indicating their role in seasonal nitrogen storage. Immuno-histochemical localization with the polyclonal antibodies raised against the 23 kDa protein demonstrated that the 23 kDa protein was the major component of protein inclusions in protein-storing cells. The protein inclusions were identified by protein-specific staining and should correspond to the electron-dense materials in different forms in the vacuoles of phloem parenchyma cells and phloem ray parenchyma cells under an electron microscope. So, the 23 kDa protein was a typical VSP in S. mukorassi. The 23 and 27 kDa proteins shared no immuno-relatedness, whereas the 23 kDa protein was immuno-related with the 22 kDa VSP in lychee and possessed trypsin inhibitor activity. The 23 kDa protein may confer dual functions: nitrogen storage and defense. [source] Modeling the Inhibitor Activity and Relative Binding Affinities in Enzyme-Inhibitor-Protein Systems: Application to Developmental Regulation in a PG-PGIP SystemBIOTECHNOLOGY PROGRESS, Issue 3 2004Wayne W. Fish Within a number of classes of hydrolytic enzymes are certain enzymes whose activity is modulated by a specific inhibitor-protein that binds to the enzyme and forms an inactive complex. One unit of a specific inhibitor-protein activity is often defined as the amount necessary to inhibit one unit of its target enzyme by 50 %. No objective quantitative means is available to determine this point of 50 % inhibition in crude systems such as those encountered during purification. Two models were derived: the first model is based on an irreversible binding approximation, and the second, or equilibrium, model is based on reversible binding. The two models were validated using the inhibition data for the polygalacturonase-polygalacturonase-inhibiting protein (PG-PGIP) system. Theory and experimental results indicate that the first model can be used for inhibitor protein activity determination and the second model can be used for inhibitor protein activity determination as well as for comparison of association constants among enzymes and their inhibitor-proteins from multiple sources. The models were used to identify and further clarify the nature of a differential regulation of expression of polygalacturonase-inhibiting protein in developing cantaloupe fruit. These are the first relations that provide for an objective and quantitative determination of inhibitor-protein activity in both pure and crude systems. Application of these models should prove valuable in gaining insights into regulatory mechanisms and enzyme-inhibitor-protein interactions. [source] Changes in the biochemical and functional properties of the extruded hard-to-cook cowpea (Vigna unguiculata L. Walp)INTERNATIONAL JOURNAL OF FOOD SCIENCE & TECHNOLOGY, Issue 4 2010Karla A. Batista Summary Changes in the biochemical and functional properties of the hard-to-cook cowpea bean after treatment by the extrusion process are reported. The extrusion was carried out at 150 °C, with a compression ratio screw of 3:1, a 5-mm die, and a screw speed of 150 r.p.m. The extrusion caused the complete inactivation of the ,-amylase and lectin and it also reduced the trypsin inhibitor activity (38.2%) and phytic acid content (33.2%). The functional properties were also modified by the process, an increase of 2.5 times in the water absorption index and 3.1% in the water solubility were observed. The digestibility of the hard-to-cook flour of the cowpea bean was improved after the extrusion, with a 55.9% increase in protein digestibility and a 5.9% increase in starch digestibility. [source] A heat-stable trypsin inhibitor in adzuki bean (Vigna angularis): effect of extraction media, purification and biochemical characteristicsINTERNATIONAL JOURNAL OF FOOD SCIENCE & TECHNOLOGY, Issue 1 2010Sappasith Klomklao Summary Trypsin inhibitor from adzuki bean (Vigna angularis) seed was isolated and characterised. Extraction of seed with NaCl at the concentration of 0.15 m showed a higher recovery of trypsin inhibitor than other solvents tested (P < 0.05). Optimal extraction time for the recovery trypsin inhibitor from adzuki bean seed was 30 min (P < 0.05). Purification of inhibitor was achieved by heat-treatment at 90 °C for 10 min, followed by ammonium sulphate precipitation with 30,65% saturation and size exclusion chromatography on Sephacryl S-200, presenting a yield and purification of 53.9% and 10.91-fold, respectively. The apparent molecular weight of trypsin inhibitor was estimated to be 14 kDa based on SDS-PAGE and inhibitor activity of zones separated by electrophoresis. The purified inhibitor was stable over a broad pH range and retained high inhibitory activity toward trypsin after incubation at 90 °C for 60 min. NaCl, at 0,3% concentration, did not affect the inhibitory activity of purified trypsin inhibitor, however, the activity was lost when sample was treated with ,-mercaptoethanol prior to electrophoresis. [source] Quality attributes of vegetable soybean as a function of boiling time and conditionINTERNATIONAL JOURNAL OF FOOD SCIENCE & TECHNOLOGY, Issue 11 2009Leandro A. Mozzoni Summary Vegetable soybeans are marketed fresh or frozen, either shelled or in pods. The objective of this research was to characterise the change in quality attributes of vegetable soybean with boiling time (0,20 min), and presence/absence of pods, using an electrical-resistance stove or a steam-jacketed kettle. Trypsin inhibitor activity (TIA), texture, colour, soluble sugars, nitrogen, calcium and iron content were analysed. Blanching using a steam-jacketed kettle for approximately 2 min rendered 80% inactivation of TIA, and resulted in high colour, texture and sucrose. There were no differences between blanching in pods or shelled for TIA, colour and texture; however, blanching in pods prevented losses of sucrose. Blanching did not affect iron, mono- and oligosaccharide levels, but increased nitrogen and calcium content. Additionally, we observed that all traits decreased linearly with cooking time when using an electrical-resistance stove, except for calcium and nitrogen that increased, and oligosaccharides that remained constant. [source] ISOLATION AND CHARACTERIZATION OF TRYPSIN INHIBITORS FROM SOME THAI LEGUME SEEDSJOURNAL OF FOOD BIOCHEMISTRY, Issue 2 2000SOOTTAWAT BENJAKUL ABSTRACT Trypsin inhibitors from cultivars of cowpea (Vigna unguiculata (L.) Wasp.), pigeon pea (Cajanus cajan (L.) Millsp.) and bambara groundnuts (Voandzeia subterranea (L.) Thou) grown in Thailand were isolated and characterized. Extraction of seeds with NaCl rendered a higher recovery of trypsin inhibitor than other solvents tested (P<0.05). The extraction time affected the inhibitor recovery (P<0.05). The extraction time of 3 h was optimum for the recovery of trypsin inhibitor from pigeon and bambara groundnuts, whereas 1 h was optimum for cowpea. Based cn inhibitor activity of zones separated by electrophoresis, the molecular mass of the inhibitor from bambara groundnuts was 13 kDa. Two inhibitory bands were observed for cowpea (10 and 18 kDa) and pigeon pea (15 and 25 kDa). Partial purification of inhibitors was achieved by heat-treatment at 90C for 10 min, followed by ammonium sulfate precipitation with 30,65% saturation. The partially purified inhibitors from four seeds were heat stable up to 30 min at 90C at pH 7.0. The activities were also retained over a wide pH range at 25C but were lost when samples were treated with ,-mercaptoethanol prior to electrophoresis. [source] Quality Characteristics of Spaghetti as Affected by Green and Yellow Pea, Lentil, and Chickpea FloursJOURNAL OF FOOD SCIENCE, Issue 6 2005Yonghuan H. Zhao ABSTRACT Spaghetti was made from semolina, containing 5% to 30% milled flours of green pea, yellow pea, chickpea, and lentil, respectively. Physical-chemical characteristics and descriptive sensory and consumer acceptance characteristics were measured. Spaghetti containing legume flours darkened the spaghetti (P < 0.05) but did not affect the cooked weight significantly. Cooking loss and firmness increased with an increase in legume flour content. Trypsin inhibitor activity (TIA/g) was significantly reduced after cooking. Descriptive intensity analysis showed that the firmness, pulse flavor, and color intensity of the pasta products increased with the increase in the percentages of legume flour fortification up to 30%, whereas the intensity of the shiny appearance, elasticity, and overall quality decreased. Consumers preferred control spaghetti (without legume additives) more than the spaghetti containing legume flours and they slightly liked the spaghetti with 15% lentil or green pea and the spaghetti with 20% chickpea or yellow pea. [source] Vegetative Storage Protein with Trypsin Inhibitor Activity Occurs in Sapindus mukorassi, a Sapindaceae Deciduous TreeJOURNAL OF INTEGRATIVE PLANT BIOLOGY, Issue 4 2009Shi-Biao Liu Abstract A vegetative storage protein (VSP) with trypsin inhibitor activity in a deciduous tree, Sapindus mukorassi, was characterized by means of sodium dodecyl sulfate-polyacrylamide gel electrophoresis, Western-blot, immuno-histochemical localization, light- and electro-microscopy, together with analysis of proteinase inhibitor activity of the purified VSP in vitro. There were two proteins with molecular masses of about 23 and 27 kDa in a relatively high content in the bark tissues of terminal branches of S. mukorassi in leafless periods. The proteins decreased markedly during young shoot development, indicating their role in seasonal nitrogen storage. Immuno-histochemical localization with the polyclonal antibodies raised against the 23 kDa protein demonstrated that the 23 kDa protein was the major component of protein inclusions in protein-storing cells. The protein inclusions were identified by protein-specific staining and should correspond to the electron-dense materials in different forms in the vacuoles of phloem parenchyma cells and phloem ray parenchyma cells under an electron microscope. So, the 23 kDa protein was a typical VSP in S. mukorassi. The 23 and 27 kDa proteins shared no immuno-relatedness, whereas the 23 kDa protein was immuno-related with the 22 kDa VSP in lychee and possessed trypsin inhibitor activity. The 23 kDa protein may confer dual functions: nitrogen storage and defense. [source] Regulation of glial development by cystatin CJOURNAL OF NEUROCHEMISTRY, Issue 1 2007Akiko Hasegawa Abstract Cystatin C (CysC) is an endogenous cysteine proteases inhibitor produced by mature astrocytes in the adult brain. Previously we isolated CysC as a factor activating the glial fibrillary acidic protein (GFAP) promoter, and showed that CysC is expressed in astrocyte progenitors during development. Here we show that protease inhibitor activity increased daily in conditioned medium, and that this activity was mainly a result of CysC released from primary cultured cells. Human CysC added to the culture medium of primary brain cells increased the number of GFAP-positive and nestin-positive cells. Human CysC also increased the number of neurospheres formed from embryonic brain, and thus it increases the number of neural stem/precursor cells in a manner similar to glycosylated rat CysC. The addition of a neutralizing antibody, on the other hand, greatly decreased the number of GFAP and glutamate aspartate transporter (GLAST)-positive astrocytes. This decrease was reversed by the addition of CysC but not by another cysteine protease inhibitor. Thus, the promotion of astrocyte development by CysC appears to be independent of its protease inhibitor activity. The antibody increased the number of oligodendrocytes and their precursors. Therefore, CysC modifies glial development in addition to its activity against neural stem/precursor cells. [source] Nutritional value of African yambean (Sphenostylis stenocarpa L): improvement by lactic acid fermentationJOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, Issue 6 2005Marshall A Azeke Abstract Tropical African yambean (Sphenostylis stenocarpa L) is an under-utilised hardy, protein-rich legume. Antinutrients and the excessively long cooking time (4,6 h), among other factors, limit the food use of African yambean seeds. To reduce these limitations, non-traditional, less energy-consuming processing methods are required. Seeds of different varieties were (i) examined for ingredients and (ii) fermented with Lactobacillus plantarum. Comparisons with traditionally cooked beans were made. Protein content and in vitro protein digestibility were increased slightly by fermentation or cooking. Reductions in trypsin and ,-amylase inhibitor activity and tannin ranged from significant to complete. The contents of potentially very toxic cyanogenic glycosides and flatulence-causing ,-galactosides were high in raw beans. Reduction by fermentation (by 85%) was clearly more effective than by traditional cooking (10,20%). The results demonstrate (i) that fermentation can substantially improve the nutritional quality and (ii) that the energy requirement to produce a basic consumable fermented food from African yambean is only 10% of that of traditional cooking. On these grounds, widespread application of lactic acid fermentation by individuals or small-scale industries would be advantageous in the context of small-household economy, environmental protection, health and long-term sustainable agriculture in Nigeria. Copyright © 2005 Society of Chemical Industry [source] Aprotinin in orthotopic liver transplantation: Evidence for a prohemostatic, but not a prothrombotic, effectLIVER TRANSPLANTATION, Issue 10 2001I. Quintus Molenaar Aprotinin reduces blood transfusion requirements in orthotopic liver transplantation (OLT). Concern has been voiced about the potential risk for thrombotic complications when aprotinin is used. The aim of this study is to evaluate the effects of aprotinin on the two components of the hemostatic system (coagulation and fibrinolysis) in patients undergoing OLT. As part of a larger, randomized, double-blind, placebo-controlled study, we compared coagulation (fibrinogen level, activated partial thromboplastin time [aPTT], prothrombin time, and platelet count) and fibrinolytic variables (tissue-type plasminogen activator [tPA] antigen and activity, plasminogen activator inhibitor activity, and D-dimer), as well as thromboelastography (reaction time [r], clot formation time, and maximum amplitude) in 27 patients administered either high-dose aprotinin (2 × 106 kallikrein inhibitor units [KIU] at induction, continuous infusion of 1 × 106 KIU/h, and 1 × 106 KIU before reperfusion; n = 10), regular-dose aprotinin (2 × 106 KIU at induction and continuous infusion of 0.5 × 106 KIU/h; n = 8), or placebo (n = 9) during OLT. Blood samples were drawn at seven standardized intraoperative times. Baseline characteristics were similar for the three groups. During the anhepatic and postreperfusion periods, fibrinolytic activity (plasma D-dimer and tPA antigen levels) was significantly lower in aprotinin-treated patients compared with the placebo group. Interestingly, coagulation times (aPTT and r) were significantly more prolonged in aprotinin-treated patients than the placebo group. No difference was seen in the incidence of perioperative thrombotic complications in the entire study population (n = 137). Aprotinin has an anticoagulant rather than a procoagulant effect. Its blood-sparing (prohemostatic) effect appears to be the overall result of a strong antifibrinolytic and a weaker anticoagulant effect. These findings argue against a prothrombotic effect of aprotinin in patients undergoing OLT. [source] Defense mechanisms against grazing: a study of trypsin inhibitor responses to simulated grazing in the sedge Carex bigelowiiOIKOS, Issue 9 2007Åsa Lindgren Trypsin inhibitors have been suggested to constitute an inducible defense in the sedge Carex bigelowii, and some former studies suggest that this might be a cause for the cyclic population dynamics in many alpine and arctic small mammals, for example lemmings (Lemmus lemmus). We investigated this further by using a method of simulated grazing (clipping) at different intensities, in three different habitats with varying resource availability, with different harvest times (hours after clipping), and two different stages of ramets (reproductive/vegetative) in a study from the Swedish mountain range. Our results do not indicate that C. bigelowii has an inducible defense constituted by an increase in trypsin inhibitor activity (TIA), but rather that the amount of soluble plant proteins (SPP) is lowered in wounded plants. The responses were somewhat different in the three habitats, with ramets growing in the marsh showing the highest ratio of TIA to SPP, due to low amounts of SPP. We did not find any significant effects of harvest time, or of the stage of the ramet that could support the hypothesis of an inducible defense. To conclude, we could not find any evidence for an inducible defense consisting of trypsin inhibitors in Carex bigelowii ramets, but we did find variations in the amount of SPP that may have nutritional consequences for herbivores. [source] Intraclonal variation in defence substances and palatability: a study on Carex and lemmingsOIKOS, Issue 3 2004Kari Anne Bråthen Clonal sedges consist of integrated ramets at different development stages. Many of these sedges are important food for herbivores, yet differences in herbivore preferences and defence allocation between ramet development stages have not previously been evaluated. In this study we investigated intraclonal ramet variation in level of plant defence and nutrient compounds and intraclonal ramet preferences by lemmings (Lemmus trimucronatus) in field samples of a rhizomatous sedge (Carex stans). Plant defence was measured as the level of proteinase inhibitor activity (PIA) and the ratio of PIA to soluble plant proteins (SPP), whereas plant nutrients were measured as the level of soluble plant sugars (SPS) and SPP. Flowering ramets generally had a higher content of defence compared to vegetative ramets, which is consistent with the optimal defence theory predicting that defence compounds are allocated to the ramet stage of the highest fitness value. Compared to vegetative ramets, the flowering ramets had a lower content of SPP and a higher content of SPS. The lemmings showed preference differences between the ramet development stages, and to a large extent the ramet content of defence compounds and nutrient compounds covaried with these preferences in the predicted way. This study shows that defence allocation between ramet development stages of the clonal sedge Carex conforms to predictions of the optimal defence theory. [source] Thrombin activatable fibrinolysis inhibitor activity, thrombin-antithrombin complex and D-dimer levels in preterm neonates with early respiratory distress syndromeAMERICAN JOURNAL OF HEMATOLOGY, Issue 1 2008Tugba Gursoy Intraalveolar fibrin deposition found in neonates with respiratory distress syndrome (RDS) is explained by the activation of the coagulation system and inefficient fibrinolysis. However, thrombin activatable fibrinolysis inhibitor activity (TAFIa), an inhibitor of fibrinolysis, and the ratio of D-dimer to thrombin,antithrombin complex (D-dimer/TAT), an index of fibrinolytic activity, have not been reported previously in neonatal RDS. Aim of this study is to evaluate the influence of plasma TAFIa levels on the fibrinolytic state in neonatal RDS. The RDS group (Group 1) consisted of 29 neonates, and 18 neonates served as the control group (Group 2). Plasma TAFIa levels and D-dimer/TAT ratios were evaluated in all neonates in the first 6 hr of life. Neonates in the RDS group were further divided into two subgroups; Group 1a consisted of 12 neonates with evidence of mild asphyxia (Apgar score at 5 min <7 and cord pH <7.26), and Group 1b consisted of 17 nonasphyxiated neonates. No significant difference was found in TAFIa levels and D-dimer/TAT ratios between Groups 1 and 2 [214% (56.2,361%) and 124.3 (4.4,3,921) in Group 1 and 201% (60.3,381%) and 147 (5.9,1,426) in Group 2]. There were negative correlations between cord pH and TAFIa levels in both groups. Increased TAFIa levels and decreased D-dimer/TAT ratios and platelet counts were detected in mildly asphyxiated neonates when compared with nonasphyxiated ones. TAFIa is not responsible for the hypofibrinolytic state reported in RDS. However, asphyxia influences TAFIa levels and increased TAFIa levels depress fibrinolysis. Am. J. Hematol., 2008. © 2007 Wiley-Liss, Inc. [source] Insect growth inhibitor activity of arjunolic acid isolated from Cornus capitataPHYTOTHERAPY RESEARCH, Issue S1 2002R. S. Bhakuni Abstract Arjunolic acid (a pentacyclictrihydroxytriterpenic acid) isolated from the stem of Cornus capitata (Cornaceae) exhibited significant inhibitory activity towards 4th instar larvae of Spilarctia obliqua. A dose dependent relationship of both activities was observed. The effective concentration (EC50) to reduce feeding and growth of the larvae of S. obliqua was found to be 617.8 and 666.9,ppm, respectively. Copyright © 2002 John Wiley & Sons, Ltd. [source] Analysis of inhibitor binding in influenza virus neuraminidasePROTEIN SCIENCE, Issue 4 2001Brian J. Smith Abstract 2,3-didehydro-2-deoxy- N -acetylneuraminic acid (DANA) is a transition state analog inhibitor of influenza virus neuraminidase (NA). Replacement of the hydroxyl at the C9 position in DANA and 4-amino-DANA with an amine group, with the intention of taking advantage of an increased electrostatic interaction with a conserved acidic group in the active site to improve inhibitor binding, significantly reduces the inhibitor activity of both compounds. The three-dimensional X-ray structure of the complexes of these ligands and NA was obtained to 1.4 Å resolution and showed that both ligands bind isosterically to DANA. Analysis of the geometry of the ammonium at the C4 position indicates that Glu119 may be neutral when these ligands bind. A computational analysis of the binding energies indicates that the substitution is successful in increasing the energy of interaction; however, the gains that are made are not sufficient to overcome the energy that is required to desolvate that part of the ligand that comes in contact with the protein. [source] Angiotensin I-converting enzyme is expressed by erythropoietic cells of normal and myeloproliferative bone marrowBRITISH JOURNAL OF HAEMATOLOGY, Issue 3 2003Maruska Marusic-Vrsalovic Summary. It is proposed that a locally active, intrinsic renin,angiotensin system (RAS) exists in the bone marrow (BM) and plays a role in regulating haematopoiesis. Angiotensin II type I receptor has been detected on erythroid burst-forming unit-derived cells; its antagonist losartan and angiotensin I-converting enzyme (ACE) inhibitors can suppress erythropoiesis. The possible role of ACE/RAS in BM was investigated by evaluating ACE expression in normal BM, several myeloproliferative disorders and myelodysplasia. Immunohistochemical studies showed that erythroid elements expressed ACE protein in both normal and disturbed haematopoiesis. The presence of ACE in erythroid cells suggests another mechanism for direct ACE inhibitor activity in erythropoiesis. [source] Computational analysis of the cathepsin B inhibitors activities through LR-MMPBSA binding affinity calculation based on docked complexJOURNAL OF COMPUTATIONAL CHEMISTRY, Issue 14 2009Zhigang Zhou Abstract Cathepsin B, a ubiquitous lysosomal cysteine protease, is involved in many biological processes related to several human diseases. Inhibitors targeting the enzyme have been investigated as possible diseases treatments. A set of 37 compounds were recently found active in a high throughput screening assay to inhibit the catalytic activity of Cathepsin B, with chemical structures and biological test results available to the public in the PubChem BioAssay Database (AID 820). In this study, we compare these experimental activities to the results of theoretical predictions from binding affinity calculation with a LR-MM-PNSA approach based on docked complexes. Strong correlations (r2 = 0.919 and q2 = 0.887 for the best) are observed between the theoretical predictions and experimental biological activity. The models are cross-validated by four independent predictive experiments with randomly split compounds into training and test sets. Our results also show that the results based on protein dimer show better correlations with experimental activity when compared to results based on monomer in the in silico calculations. © 2009 Wiley Periodicals, Inc. J Comput Chem, 2009 [source] | ||||||||||||||||