Facile Synthesis of Mill Moth's Sex Pheromone Components

An improved method for the preparation of mill moth's sex pheromone components in high diastereomeric purity is described.     

A quadratic spinor Lagrangian for general relativity

We present a newfinite action for Einstein gravity in which the Lagrangian is quadratic in the covariant derivative of a spinor field. Via a new spinor-curvature identity, it is related to the standard Einstein-Hilbert Lagrangian by a total differential term. The corresponding Hamiltonian, like the one associated with the Witten positive energy proof, is fully 4-covariant. It defines quasi-local energy-momentum and can be reduced to the one in our recent positive energy proof.This essay received the fourth award from the Gravity Research Foundation, 1994—Ed.     

High-performance liquid chromatographic determination of rifapentine in serum using column switching.

A high-performance liquid chromatographic method with column switching has been developed for the determination of rifapentine in serum. The serum samples were injected onto a precolumn packed with Corasil RP C18 (37-50 microns) after simple dilution with an internal standard in a 1% ascorbic acid solution. Polar serum components were washed out using 0.05 M phosphate buffer. After valve switching, the concentrated drugs were eluted in the back-flush mode and separated by a mu Bondapak C18 column with acetonitrile-tetrahydrofuran-0.05 M phosphate buffer (pH 7.0) (42:5:53, v/v/v) as the mobile phase. The method showed excellent precision with good sensitivity and speed, and a detection limit of 0.1 microgram/ml. The total analysis time was less than 25 min and the mean coefficients of variation for intra- and inter-assay were less than 4.8%. The method has been successfully applied to serum samples from dogs after the oral administration of rifapentine.     

Effect of oxygen vacancies in anodic titanium oxide films on the kinetics of the oxygen electrode reaction

The effect of oxygen vacancies in the anodic oxide film on passive titanium on the kinetics of the oxygen electrode reaction has been studied by potentiodynamic polarization and electrochemical impedance spectroscopy (EIS). Oxide films of different donor density were prepared galvanostatically at various current densities until a potential of 20.0 V_SHE was achieved. The semiconductive properties of the oxide films were characterized using EIS and Mott-Schottky analysis, and the thickness was measured using ellipsometry. The film thickness was found to be almost constant at ∼44.7 ± 2.0 nm, but Mott-Schottky analysis of the measured high frequency interracial capacitance showed that the donor (oxygen vacancy) density in the n-type passive film decreased sharply with increasing oxide film formation rate (current density). Passive titanium surfaces covering a wide range of donor density were used as substrates for ascertaining relationships between the rates of oxygen reduction/evolution and the donor density. These studies show that the rates of both reactions are higher for passive films having higher donor densities. Possible explanations include enhancement of the conductivity of the film due to the vacancies facilitating charge transfer and the surface oxygen vacancies acting as catalytic sites for the reactions. The possible involvement of surface oxygen vacancies in the oxygen electrode reaction was explored by determining the kinetic order of the OER with respect to the donor concentration. The kinetic orders were found to be greater than zero, indicating that oxygen vacancies are involved as electrocatalytic reaction centers in both the oxygen evolution and reduction reactions. This paper was submitted in honor of the many contributions to electrochemistry that have been made by Professor Boris Grafov. The article is published in the original.     

"In-gel patch electrophoresis:" a new method for environmental DNA purification

Most of the microorganism species are largely untapped and could represent an interesting reservoir of genes useful for biotechnological applications. Unfortunately, a major difficulty associated with the methods used to isolate environmental DNA is related to the contamination of the extracted material with humic substances. These polyphenolic compounds inhibit the DNA processing reactions and severely impede cloning procedures. In this work, we describe a rapid, simple, and efficient method for the purification of genomic DNA from environmental samples: we added a chromatography step directly embedded into an agarose gel electrophoresis. This strategy enabled the DNA extraction from various environmental samples and it appeared that the purity grade was compatible with digestion by restriction enzymes and polymerase chain reaction (PCR) amplifications.     

CD137 induces adhesion and cytokine production in human monocytic THP-1 cells

CD137, which is expressed on activated T cells, plays a critical role in inflammatory responses. However, the exact role that CD137 plays in monocytes is not fully known. Here we studied the expression and function of CD137 in human monocytic THP-1 cells, which we found constitutively expresses CD137 at the mRNA and protein level. Cross-linking of CD137 increased the secretion of IL-8 and TNF-alpha, promoted the expression of CD54 and CD11b, and increased adhesion to extracellular matrix (ECM) proteins. In particular CD137-induced adhesion of THP-1 cells was inhibited by an inhibitor of mitogen-activated protein kinase kinase (MEK), but not by a p38 kinase inhibitor. Taken together, these results show that the adhesion and cytokine production of THP-1 cells induced by CD137 occur via activation of MEK, which results in the activation of ERK-1/2 signaling pathways. Therefore, this study suggests that CD137 induces an activating and migrating signal during inflammatory processes.     

Determination of uranium,plutonium and selected fission products in the coolant of the KS-150 reactor

The method of monitoring of U, Pu and some fission products (^103,106Ru,^134,137Cs and^141,144Ce) in gaseous CO₂ coolant is described. The method is based on the retention of the radionuclides studied by membrane filters built in by-pass of the burst-cartridge detection (BCD) system. The purpose of the present study was the determination of U, Pu in CO₂ and the verification of the possibility of the indirect monitoring of U and Pu contents in the coolant, using the gamma-spectrometric determination of selected fission products retained by the filter. For calibration of the proposed method after decomposition of the filters, uranium was determined spectrophotometrically using Arsenazo III, plutonium was determined radiometrically after its separation by extraction with 2-thenoyltrifluoracetone and the fission products were determined by gamma-spectrometry. From the results obtained it follows that a correlation exists between the U and Pu content in the coolant and the activity of certain fission products retained on the filter.     

Two-dimensional offsets and medial axis transform

We present a mathematical theory of the two-dimensional offset curves from the viewpoint of medial axis transform. We explore the local geometry of the offset curve in relation with the medial axis transform, culminating in the classification of points on the offset curve. We then study the domain decomposition from the viewpoint of offsets, and in particular introduce the concept of monotonic fundamental domain as a device for detecting the correct topology of offsets as well as for stable numerical computation. The monotonic fundamental domains are joined by peaks or valleys of the medial axis transform, or by what we call the critical horizonal section whose algebro-geometric properties are rigorously treated as well. First author holds joint appointment in the Research Institute of Mathematics, Seoul National University.     

Scaffold Repurposing of In-House Small Molecule Candidates Leads to Discovery of First-in-Class CDK-1/HER-2 Dual Inhibitors: In Vitro and In Silico Screening

Recently, multitargeted drugs are considered a potential approach in treating cancer. In this study, twelve in-house indole-based derivatives were preliminary evaluated for their inhibitory activities over VEGFR-2, CDK-1/cyclin B and HER-2. Compound 15l showed the most inhibitory activities among the tested derivatives over CDK-1/cyclin B and HER-2. Compound 15l was tested for its selectivity in a small kinase panel. It showed dual selectivity for CDK-1/cyclin B and HER-2. Moreover, in vitro cytotoxicity assay was assessed for the selected series against nine NCI cell lines. Compound 15l showed the most potent inhibitory activities among the tested compounds. A deep in silico molecular docking study was conducted for compound 15l to identify the possible binding modes into CDK-1/cyclin B and HER-2. The docking results revealed that compound 15l displayed interesting binding modes with the key amino acids in the binding sites of both kinases. In vitro and in silico studies demonstrate the indole-based derivative 15l as a selective dual CDK-1 and HER-2 inhibitor. This emphasizes a new challenge in drug development strategies and signals a significant milestone for further structural and molecular optimization of these indole-based derivatives in order to achieve a drug-like property.