Some Monohydroxy Tetradecanoic Acid Isomers as Novel Urease and Elastase Inhibitors and as New Antioxidants

A series of some 3-,6-,7-,9-,12- monohydroxy tetradecanoic acids were evaluated for their antiurease, antielastase and antioxidant activities for the first time in this study. All the test compounds exhibited antioxidant, antielastase and antiurease activities. The relationship between the position of the hydroxy group and the enzyme inhibition effect is studied in this work. The mentioned biological activities are depending on the position of hydroxy group of tetradecanoic acid isomers. The results obtained in this work are indicating that 3-,6-,7-,9-,12-monohydroxy tetradecanoic acid isomers can be used in agriculture, pharmacy and cosmetic industries due to their excellent antielastase, antiurease and antioxidant activities.     

Rapid Homogenous Time-Resolved Fluorescence (HTRF) Immunoassay for Anthrax Detection

Infection with Bacillus anthracsis spores induces an acute anthrax disease that can cause casualties and death in untreated cases. Thus rapid diagnosis of anthrax at early stage of the disease is essential to allow an effective treatment. Here we present the development of rapid and sensitive homogenous time-resolved fluorescence (HTRF) immunoassays based on the energy transfer process of europium cryptate (EuK) donor to AlexaFluor647 acceptor. The energy transfer process is limited to d?<?10 nm, making the HTRF an ideal assay for examination of homogenous and complex samples, since only mutual binding of the donor and acceptor antibodies to the analyte would result in positive signal. HTRF assay was developed for the detection of the bacterial Protective Antigen (PA) toxin, a serological marker that correlates with bacteremia in infected hosts, using two monoclonal anti-PA antibodies that specifically recognize two different epitopes on the PA molecule. The assay was sensitive enabling detection of 2 ng/ml PA in the serum of B. anthracsis-infected rabbits in only 15 min assay. Additionally, HTRF assay was developed for the detection of bacterial spores using polyclonal anti-spore antibodies that recognize many epitopes on the bacterial surface. The assay enabled the detection of 2?×?10⁶ spores/ml in 30 min assay and was specific, showing no cross reactivity with closely related non-virulent bacillus cereus strain. This study describes the use of the HTRF assay for the detection of both singled-epitope (proteins) and multi-epitope (particles) as rapid, simple and sensitive method that can be used at the time that fast results are needed to allow an effective medical care.     

A multigrid solver to the Helmholtz equation with a point source based on travel time and amplitude

The Helmholtz equation arises when modeling wave propagation in the frequency domain. The equation is discretized as an indefinite linear system, which is difficult to solve at high wave numbers. In many applications, the solution of the Helmholtz equation is required for a point source. In this case, it is possible to reformulate the equation as two separate equations: one for the travel time of the wave and one for its amplitude. The travel time is obtained by a solution of the factored eikonal equation, and the amplitude is obtained by solving a complex‐valued advection–diffusion–reaction equation. The reformulated equation is equivalent to the original Helmholtz equation, and the differences between the numerical solutions of these equations arise only from discretization errors. We develop an efficient multigrid solver for obtaining the amplitude given the travel time, which can be efficiently computed. This approach is advantageous because the amplitude is typically smooth in this case and, hence, more suitable for multigrid solvers than the standard Helmholtz discretization. We demonstrate that our second‐order advection–diffusion–reaction discretization is more accurate than the standard second‐order discretization at high wave numbers, as long as there are no reflections or caustics. Moreover, we show that using our approach, the problem can be solved more efficiently than using the common shifted Laplacian multigrid approach.     

Localized In Vivo Activation of a Photoactivatable Doxorubicin Prodrug in Deep Tumor Tissue

Sparing sensitive healthy tissue from chemotherapy exposure is a critical challenge in the treatment of cancer. The work described here demonstrates the localized in vivo photoactivation of a new chemotherapy prodrug of doxorubicin (DOX). The DOX prodrug (DOX‐PCB) was 200 times less toxic than DOX and was designed to release pure DOX when exposed to 365 nm light. This wavelength was chosen because it had good tissue penetration through a 1 cm diameter tumor, but had very low skin penetration, due to melanin absorption, preventing uncontrolled activation from outside sources. The light was delivered specifically to the tumor tissue using a specialized fiber‐optic LED system. Pharmacokinetic studies showed that DOX‐PCB had an α circulation half‐life of 10 min which was comparable to that of DOX at 20 min. DOX‐PCB demonstrated resistance to metabolic cleavage ensuring that exposure to 365 nm light was the main mode of in vivo activation. Tissue extractions from tumors exposed to 365 nm light in vivo showed the presence of DOX‐PCB as well as activated DOX. The exposed tumors had six times more DOX concentration than nearby unexposed control tumors. This in vivo proof of concept demonstrates the first preferential activation of a photocleavable prodrug in deep tumor tissue.     

Isotopic Exchange Between Barium Oxalate and Barium Ion in Aqueous Solution

The heterogeneous isotopic exchange reaction of precipitated barium oxalate in barium chloride solution has been studied using Ba-133 as tracer. The effect of barium chloride concentration on the rate of isotopic exchange reaction has been studied. It was found that the rate was controlled by surface mass reaction and particle diffusion process in the solid particle. The result also indicate that the effect of recrystallization can be neglected.     

MAX CUT in cubic graphs

We present an improved semidefinite programming based approximation algorithm for the MAX CUT problem in graphs of maximum degree at most 3. The approximation ratio of the new algorithm is at least 0.9326. This improves, and also somewhat simplifies, a result of Feige, Karpinski and Langberg. We also observe that results of Hopkins and Staton and of Bondy and Locke yield a simple combinatorial 4/5-approximation algorithm for the problem. Finally, we present a combinatorial 22/27-approximation algorithm for the MAX CUT problem for regular cubic graphs.     

A quantum mechanical approach to electrochemical behavior of spirochromics

Fully optimized semiempirical quantum‐chemical calculations of photochromic spiropyrans are presented. The vertical ionization potentials are calculated and their variation with substitutions are correlated to experimental oxidation potentials. The effects of the substitutions are studied and the partial charges on indoline and pyran components generated by HOMO are found to be responsible for the variations. The deactivating groups on the indoline ring system and deactivating groups on the pyran system increase the ionization potential and, consecutively, the oxidation potential. ©1999 John Wiley & Sons, Inc. Int J Quant Chem 75: 111–117, 1999     

Carbon nanofiber based CuO nanorod counter electrode for enhanced solar cell performance and adsorptive photocatalytic activity

Journal of Nanoparticle Research - A comprehensive study of the antibacterial (bacteriostatic and bactericidal) properties of non-doped carbon nanodots (CNDs), nitrogen-doped (N-doped), and...     

Ring opening process of some spirochromenes by photoproduced HCl in poly(N-vinyl carbazole)

The coloration reaction of some spirochromenes (SP) has been investigated in the case of a free radical photosensitive system composed of a poly(N-vinylcarbazole) matrix (PVCz) in dichloromethane containing carbon tetrachloride as an activator at average ratios of 5:1:0.1 for PVCz, CCl₄ and SP, respectively. In this system, photoproduced HCl leads to the formation of the colored forms of SP. Acidification and irradiation of the variety of spirochromene solutions in the presence and absence of PVCz were also investigated and compared with the effect of photoproduced HCl on the reversibility of the ring opening process. The opened forms of the compounds were characterized by UV–visible spectra, pH and conductivity measurements. The effect of solvent and the substituent of SP were investigated. Decoloration reactions of the opened forms of SP at 50°C were followed using UV–visible spectroscopy, pH and conductivity measurements. © 1997 John Wiley & Sons, Ltd.     

Synthesis and Crystal Structure of Dimethyl-7-oxabicyclo[2.2.1]hept-5-ene exo,exo-2,3-dicarboxylate

Dimethyl-7-oxabicyclo[2.2.1]hept-5-ene exo,exo-2,3-dicarboxylate (1) was prepared by Fisher esterification of 7-oxabicyclo[2.2.1]-hept-5-ene exo-2,3-dicarboxylic anhydride (2) in methanol. The colorless plates obtained were characterized by FT-IR, ¹H- and ¹³C-NMR, TGA-DSC, and single crystal X-ray diffraction. The material crystallizes in space group P2₁/c, with a = 9.2375(14) Å, b = 12.8757(18) Å, c = 9.4608(15) Å, β = 115.327(3)°, V = 1017.1(3) Å³, and Z = 4. Chains of hydrogen-bonded molecules along the c-axis interact in the b direction to form layers parallel to the bc plane.