Binding Mode Identification for 7-keto-8-Aminopelargonic Acid Synthase (AtKAPAS) Inhibitors

In this study, we determined the 3D structure of Arabidopsis thaliana KAPAS by homology modeling. We then investigated the binding mode of compounds obtained from the in-house library using computational docking methods. From the flexible docking study, we achieved high dock scores for the active compounds denoted in this study as compound 3 and compound 4. Thus, we highlight the flexibility of specific residues, Lys 312 and Phe 172, when used in active sites

Flavonol glycosides from the aerial parts of Aceriphyllum rossii and their antioxidant activities

The methanol extract obtained from the aerial parts ofAceriphyllum rossii (Saxifragaceae) was fractionated into ethyl acetate (EtOAc),n-BuOH and H2O layers through solvent fractionation. Repeated silica gel column chromatography of EtOAc andn-BuOH layers afforded six flavonol glycosides. They were identified as kaempferol 3-O-β-D-glucopyranoside (astragalin,1), quercetin 3-O-β-D-glucopyranoside (isoquercitrin,2), kaempferol 3-O-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside (3), quercetin 3-O-α-L-rhamnopyranosyl (1→6)-β-D-glucopyrano-side (rutin,4), kaempferol 3-O-[α-L-rhamnopyranosyl (1→4)-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside] (5) and quercetin 3-O-[α-L-rhamnopyranosyl (1→4)-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside] (6) on the basis of several spectral data. The antioxidant activity of the six compounds was investigated using two free radicals such as the ABTS free radical and superoxide anion radical. Compound1 exhibited the highest antioxidant activity in the ABTS2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging method. 100 mg/L of compound1 was equivalent to 72.1±1.4 mg/L of vitamin C, and those of compounds3 and5 were equivalent to 62.7±0.5 mg/L and 54.3±1.3 mg/L of vitamin C, respectively. And in the superoxide anion radical scavenging method, compound5 exhibited the highest activity with an IC50 value of 17.6 ± 0.3 μM. In addition, some physical and spectral data of the flavonoids were confirme

Comparison of total body irradiation-based or non-total body irradiation-based conditioning regimens for allogeneic stem cell transplantation in pediatric leukemia patients

Purpose : This study aims to compare the outcome of total body irradiation (TBI)- or non-TBI-containing conditioning regimens for leukemia in children. Methods : We retrospectively evaluated 77 children conditioned with TBI (n=40) or non-TBI (n=37) regimens, transplanted at Chonnam National University Hospital between January 1996 and December 2007. The type of transplantation, disease status at the time of transplant, conditioning regimen, engraftment kinetics, development of graft-versus-host disease (GVHD), complications, cause of deaths, overall survival (OS), and event-free survival (EFS) were compared between the 2 groups. Results : Among 34 patients with acute lymphoblastic leukemia (ALL), 28 (82.4%) were in the TBI group, while 72.7% (24/33) of patients with myeloid leukemia were in the non-TBI group. Although the 5-year EFS of the 2 groups was similar for all patients (62% vs 63%), the TBI group showed a better 5-year EFS than the non-TBI group when only ALL patients were analyzed (65% vs 17%&#59; P =0.005). In acute myelogenous leukemia patients, the non-TBI group had better survival tendency (73% vs 38%&#59; P=0.089). The incidence of GVHD, engraftment, survival, cause of death, and late complications was not different between the 2 groups. Conclusion : The TBI and non-TBI groups showed comparable results, but the TBI group showed a significantly higher 5-year EFS than the non-TBI group in ALL patients. Further prospective, randomized controlled studies involving larger number of patients are needed to assess the late-onset complications and to compare the socioeconomic quality of life

Preparation, characterization, and cytotoxicity of CPT/Fe2O3-embedded PLGA ultrafine composite fibers: a synergistic approach to develop promising anticancer material

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Gaussian Quantum Illumination via Monotone Metrics

Quantum illumination is to discern the presence or absence of a low reflectivity target, where the error probability decays exponentially in the number of copies used. When the target reflectivity is small so that it is hard to distinguish target presence or absence, the exponential decay constant falls into a class of objects called monotone metrics. We evaluate monotone metrics restricted to Gaussian states in terms of first-order moments and covariance matrix. Under the assumption of a low reflectivity target, we explicitly derive analytic formulae for decay constant of an arbitrary Gaussian input state. Especially, in the limit of large background noise and low reflectivity, there is no need of symplectic diagonalization which usually complicates the computation of decay constants. First, we show that two-mode squeezed vacuum (TMSV) states are the optimal probe among pure Gaussian states with fixed signal mean photon number. Second, as an alternative to preparing TMSV states with high mean photon number, we show that preparing a TMSV state with low mean photon number and displacing the signal mode is a more experimentally feasible setup without degrading the performance that much. Third, we show that it is of utmost importance to prepare an efficient idler memory to beat coherent states and provide analytic bounds on the idler memory transmittivity in terms of signal power, background noise, and idler memory noise. Finally, we identify the region of physically possible correlations between the signal and idler modes that can beat coherent states.Comment: 16 pages, 6 figure

Treatment of Fingertip Amputation in Adults by Palmar Pocketing of the Amputated Part

BackgroundFirst suggested by Brent in 1979, the pocket principle is an alternative method for patients for whom a microsurgical replantation is not feasible. We report the successful results of a modified palmar pocket method in adults.MethodsBetween 2004 and 2008, we treated 10 patients by nonmicrosurgical replantation using palmar pocketing. All patients were adults who sustained a complete fingertip amputation from the tip to lunula in a digits. In all of these patients, the amputation occurred due to a crush or avulsion-type injury, and a microsurgical replantation was not feasible. We used the palmar pocketing method following a composite graft in these patients and prepared the pocket in the subcutaneous layer of the ipsilateral palm.ResultsOf a total of 10 cases, nine had complete survival of the replantation and one had 20% partial necrosis. All of the cases were managed to conserve the fingernails, which led to acceptable cosmetic results.ConclusionsA composite graft and palmar pocketing in adult cases of fingertip injury constitute a simple, reliable operation for digital amputation extending from the tip to the lunula. These methods had satisfactory results

Substitution of Specific Amino Acids in Insulin-like Growth Factor (IGF) Binding Protein 5 Alters Heparin Binding and Its Change in Affinity for IGF-I in Response to Heparin

Heparin binding to insulin-like growth factor (IGF)-binding protein 5 (IGFBP-5) leads to a 17-fold decrease in its affinity for IGF-I, and a region that contains several basic amino acids (Arg201-Arg218) may be involved in this affinity shift. In the present study, mutagenesis was used to analyze the effect of substitutions for basic amino acids in the Arg201-Arg218 region of IGFBP-5 on heparin-binding and the heparin-induced affinity shift. Nine mutant forms were prepared. Their association constants (Ka) for IGF-I were similar to native IGFBP-5. When 10 microg/ml of heparin was added, the Ka of native IGFBP-5 decreased 17-fold, and the Ka of the K134A/R136A mutant decreased 16-fold. In contrast, substitutions for specific basic amino acids in the Arg2O1-Arg218 region decrease the affinity shift to 1.1-3.2-fold. Lys 211 was especially important. When a mutant containing that single substitution was tested, heparin caused only a 2.5-fold reduction in IGF-I affinity. Affinity cross-linking studies showed that heparin was equipotent in inhibiting the formation of 125I-IGF-I-K134A/Rl36A mutant complexes compared to native IGFBP-5. In contrast, heparin had minimal effects on the formation of complexes between 125I-IGF-I and the other mutants. The heparin-binding activity of each mutant was determined. Four mutants, R201A/K202N, K202A/K206A/R207A, R201A/K202N/K206N/K208N, and K211N/R214A/K217A/R218A, had reduced heparin binding compared to native IGFBP-5. The other five mutants, including the K21IN mutant, showed no change in heparin binding. The four mutants with reduced heparin binding could be dissociated from heparin-Sepharose with much lower NaCl concentrations, indicating that they had reduced affinity. These findings suggest that Arg201 Lys202, LysS206, and Arg214 are important for heparin binding. In contrast, LyS211 is not important for the binding of IGFBP-5 to heparin, but substitution for it reduced the heparin-induced affinity shift