transition state analogues of enzymatic reaction as potential drugs

... release of drug was studied also in plasma and in PBS after addition of glutaraldehyde Pravastatin assay by UPLC A reversed phase UPLC method was developed and used throughout the study for pravastatin ... fragility was studied for each drug concentration In vitro releasing study The release of pravastatin as well as hemoglobin from carrier erythrocytes were determined as following, ml of packed ... using glutaraldehyde as a membrane stabilizer Also the figure shows the hemoglobin release The releasing curves of pravastatin show release phases, the first is rapid release phase and the second...

Ngày tải lên: 25/10/2012, 11:10

... gastrointestinal tract tolerance test Simulated gastric fluid tolerance test A pH of was selected as the critical point to detect the survival of spores in simulated gastric fluid Simulated gastric ... control (P=0.05) It has been previously reported that use of Bacillus strains as probiotics significantly increased the counts of gastrointestinal lactobacilli and decreased the counts of E coli (Adami ... 2004) Incubation of the spores in gastric juice with a pH of 2.0 for h was an attempt to mimic the conditions that a probiotic would have to survive as it passes through the stomach of a pig The...

Ngày tải lên: 07/07/2014, 19:20

... SYNTHESIS OF GUANIDINO ANALOGUES AS POTENTIAL NITRIC OXIDE SYNTHASE INHIBITORS BONG YONG KOY 2004 SYNTHESIS OF GUANIDINO ANALOGUES AS POTENTIAL NITRIC OXIDE SYNTHASE INHIBITORS BONG ... Oxide Synthase (NOS) Isoforms of Nitric Oxide Synthase Physiological Roles of NO and Pathology of NO Overproduction Inhibition of Nitric Oxide Synthase X-Ray Crystallographic Structure of NOS Molecular ... N1,N2-dialkylguanidines Part II 76 Dehydration of Urea in Solution Phase Reaction Dehydration of Urea in Solid Phase Reaction Optimisation of Dehydration of Urea by TosylCl Optimising Post-Cleavage...

Ngày tải lên: 16/09/2015, 17:13

... luminescence for ATP detection was assessed using a MicroBeta Trilux (PerkinElmer) A standard curve was used to determine the amount of ATP in mg of protein measured from the number of cells per well After ... depolarization, as measured by FRET, was calculated As shown in Figure 3, a statistically significant linear relation between the changes in membrane potential and the transport activity of the cells was ... Fluorescence emission was recorded at 460 and 580 nm After a 20 sec baseline reading, 0.1 ml of PBS containing 10 µM of the compound investigated was added, and the fluorescence signal was recorder for...

Ngày tải lên: 26/10/2012, 10:04

... between [96] Enzymatic hydrolysis of cellulose microfibrils to release glucose involves synergistic action of three enzymes: endo-glucanase, exo-glucanase and β-glucosidase Endo-and exo-glucanases are ... particle size and 10 of reaction time) was supplemented with xylanase preparation during enzymatic hydrolysis [103].Pectin has similar steric effect on enzymatic hydrolysis of cellulose as hemicellulose ... [96]) Enzymatic saccharification of cellulose takes place at optimum temperature of 45-50ºC and pH of 5.0 Cellulase loading range of 10-15 FPU/g dry substrate and b-glucosidase loading of 10-15...

Ngày tải lên: 05/09/2013, 15:28

... (2003) Synthesis and biological evaluation of substrate-based inhibitors of 6-phosphogluconate dehydrogenase as potential drugs against African trypanosomiasis Bioorg Med Chem 11, 3205–3214 Dardonville ... least-squares fit of 468 Ca atoms of LlPDH with TbPDH and ˚ OaPDH results in an rmsd of 1.2 A in both cases (not shown) These values indicate a level of structural conservation similar to that of ... formation Whereas LlPDH and OaPDH have a ˚ buried surface area of  5500 A2, TbPDH has a larger ˚ interface surface area of 6200 A The cofactor-binding site The cofactor binds on the periphery of domain...

Ngày tải lên: 19/02/2014, 05:20

... the steady state kinetics of the glutaminase reaction of CTP synthase from L lactis in order to distinguish between the effects of GTP on the glutaminase reaction and the CTP synthesis reaction ... Furthermore, it was shown that the fold activation of the glutaminase activity by GTP was similar to that of the overall CTP synthesis reaction It was concluded that the effect of GTP was mainly to ... USA) The steady -state heat evolvement from successive injections of glutamine or GTP was recorded as a displacement of the baseline as illustrated in Fig 1A The power value of the baseline and its...

Ngày tải lên: 21/02/2014, 15:20

... pocket Addition of millimolar concentrations of NADPH to cytosol fractions of rat liver has been reported to increase the rate of GSNO disappearance [38] NADPH could indeed be utilized as coenzyme, ... & Jornvall, H (1994) ¨ Alcohol dehydrogenase class III contrasted to class I Characterization of the cyclostome enzyme, the existence of multiple forms as for the human enzyme, and distant cross-species ... Human ADH3 was found to readily reduce GSNO with NADH as coenzyme yielding a kcat/Km of 90 000 min)1ÆmM)1 Reductive capacity for GSNO was drastically reduced by the substitution of Arg115 for...

Ngày tải lên: 31/03/2014, 07:20

... the behaviour of MR when increasing force production is simulated as a combined increase of firing rate and number of MUs Both aMR and eMR increase with simulated force The increase is less for ... first set, the influence of the determinants of MR (number of MUs, firing rate and a combination of both) was investigated while the second set was directed at the influence of parameters, related ... In case the number of MUs was not varied (simulations 2, 4–7), it was set to 5, 10 or 15 The default value of SNR was set to 1000 dB, resembling a signal without noise The default number of fibres...

Ngày tải lên: 19/06/2014, 10:20

... activity was measured daily by the modified method of Anson (Anson 1938) using casein as substrate One activity unit (U) was defined as the amount of enzyme that catalyzed the release of μmol of tyrosine ... U.mg-1) was defined as the activity per milligram of total protein, which was determined by the Lowry protein assay (Lowry 1951) Purification of P excavatus proteases The autolysate was centrifuged ... (U) on these substrates was defined as the amount of enzyme that released of μmol of p-nitroaniline under the given conditions Fibrinolysis was performed on a fibrin plate as described by (Choi...

Ngày tải lên: 20/06/2014, 23:20

... extrahepatic diseases, as well as determining the patency of the portal vein and the origin and branching patterns of the hepatic arterial system Accurate knowledge of the hepatic parenchymal and vascular ... kVp, 20 mAs) was initiated four seconds after contrast material injection Contrast material enhancement was automatically calculated by placing the region of interest cursor over the vessel of interest ... micropigs as measured by multi-detector row computed tomography No Sex Weight (Kg) Volume of liver (ml) Volume of Rt lobe liver (ml) Diameter of *CHA (mm) Diameter of *PHA (mm) Diameter of *PV (mm)...

Ngày tải lên: 07/08/2014, 23:22

... major proportion of the osteoinductive potential of bone extracts [7–9] The BMP-2 promoter has been characterized, and based on the properties of BMP-2, this promoter was utilized as a target to ... In vitro effects Simvastatin, mevastatin and atorvastatin (but not pravastatin) were found to have identical effects to those seen with lovastatin Cerivastatin, however, was 10–100-fold more potent ... Fibroblast growth factor has been previously shown to stimulate bone formation in vivo and was used as a positive control The anabolic effect of statins was confirmed with significant increases...

Ngày tải lên: 09/08/2014, 03:24

... panels of kinases [23,24] SB-203580 has good selectivity for p38α and β over the majority of kinases in a panel of over 300 kinases but does inhibit some MAPKs such as JNK with an IC50 of about ... of cytokine release by the addition of LPS (1 μg/ml) The amount of TNF-α and IL-1β released was measured 18 h later by ELISA (R&D Systems, Minneapolis, MN) The viability of the human PBMCs was ... of cytokine release by the addition of lipopolysaccharide (LPS, μg/ml, E coli 055:B5, Sigma/Aldrich, St Louis, MO, < 3% protein impurities by Lowry assay) The amount of TNF-α released was measured...

Ngày tải lên: 11/08/2014, 08:22

... 11 of 14 Figure Correlation between disease activities of RA and miRNAs in plasma or synovial fluid TJC correlated with plasma miRNAs (A) or SF/PB ratio of miRNA (B) DAS28 correlated with plasma ... the condition of joint space Plasma miRNAs differentiated RA and OA from HC Plasma miRNAs have been expected as biomarkers of malignant tumors [14,17] To determine whether plasma miRNAs can be clinical ... relative expression of synovial fluid miRNAs compared to plasma miRNAs would more reflect the condition of joint of RA than absolute concentration of synovial fluid miRNAs Dot plots of TJC and SF/PB...

Ngày tải lên: 12/08/2014, 12:20

... use of poisoned patients and those with a history of drug abuse as potential organ donors, although there was not complete agreement among all heart surgeons on the suitability of the hearts offered ... only to the specific poison involved Summaries of the scenarios are as follows (see Appendix for full case scenarios) Case 1: Case 2: Case 3: Case 4: deliberate methanol ingestion, presenting ... diagnosis of brain stem death [15], this document states that it is important to exclude the presence of sedative drugs as a cause of central nervous system depression before the diagnosis of brain...

Ngày tải lên: 12/08/2014, 19:22

... inhibition of viral load (Figure 3) Furthermore, HCV viral load was significantly decreased up to 84% with combinations of siRNAs due to the silencing of siCD81+siLDLR gene and siLDLR+SRBI as compared ... inhibition of Figure Combined effect of specific siRNA silencing of HCV receptors on viral titer in Huh-7 cells Huh-7 cells were treated with scrambled siRNAs (Sc) or combinations of siRNAs (siCD81-B ... expression of HCV envelop protein Similarly, western blotting results indicate the significant inhibition of expression of LDLR and SR-B1 when a combination of siRNAs (SR-B1 +siLDLR) was used compared...

Ngày tải lên: 14/08/2014, 19:23

... of effective interface potential as a function of film thickness Line (1) denotes the stable case, line (2) the unstable case and line (3) the metastable case.21 In contrast to polymer which dewets ... Sketch of a liquid drop at solid substrate … Figure 1.2: Sketch of effective interface potential as a function of film thickness Line (1) denotes the stable case, line (2) the unstable case ... lack of precision in location Bottom-up synthesis for nanoparticle arrays is usually categorized into gas (vapor) phase fabrication and liquid phase fabrication Gas phase fabrication, such as pyrolysis...

Ngày tải lên: 09/09/2015, 11:26

... activity of serum creatine kinase and lactate dehydrogenase, contents of serum free fatty acid and lipid peroxide, as well as increase the activity of serum SOD In addition, myocardial blood flow was ... using both cell-based in vitro bioassays and biochemical reactions The selection of assays to screen the fractions was based on current understanding of the pathophysiology of neuronal injury ... (rtPA), urokinase, streptokinase, reteplase, tenecteplase, desmoteplase Anticoagulants heparin, warfarin Cyclo-oxygenase inhibitor: aspirin To restore the blood supply Antiplatelet drugs Indirect...

Ngày tải lên: 11/09/2015, 10:06

... 42 Number of open states as a function of total energy on transition state dividing surface in even parity (dashed line) and odd parity (solid line) 3.6 43 The minimum potential ... initial transition state wave packet contributions as a function of energy 71 List of Figures 4.4 vi Comparison of 7D (solid line) and 8D (dashed line) cumulative reaction ... f as Fig.5.9 with real time from to 4000 a.u 99 List of Figures vii 5.11 Cf s as a function of real time t for the ground transition state by using both the exact transition state...

Ngày tải lên: 13/09/2015, 19:53

... Program (Office of Life Science) and National University of Singapore for providing me the research scholarship I will also like to thank Dr Gigi Chiu (Department of Pharmacy), A/Prof Prof Yao ... supervisor A/Prof Chui Wai Keung, who has guided and supported me throughout my PhD study whilst allowing me the room to work in my own way Thanks to A/Prof Chan Sui Yung, Head of Department of Pharmacy, ... (Department of Chemistry and Biological Sciences) and Prof Bay Boon Huat (Department of Anatomy) for their guidance and precious opinion in our collaboration works I am grateful to have Dr Ma Xiang as...

Ngày tải lên: 14/09/2015, 08:50