Indanones As High‐Potency Reversible Inhibitors of Monoamine Oxidase

Recent reports document that α‐tetralone (3,4‐dihydro‐2H‐naphthalen‐1‐one) is an appropriate scaffold for the design of high‐potency monoamine oxidase (MAO) inhibitors. Based on the structural similarity between α‐tetralone and 1‐indanone, the present study involved synthesis of 34 1‐indanone and related indane derivatives as potential inhibitors of recombinant human MAO‐A and MAO‐B. The results show that C6‐substituted indanones are particularly potent and selective MAO‐B inhibitors, with IC₅₀ values ranging from 0.001 to 0.030 μM . C5‐Substituted indanone and indane derivatives are comparatively weaker MAO‐B inhibitors. Although the 1‐indanone and indane derivatives are selective inhibitors of the MAO‐B isoform, a number of homologues are also potent MAO‐A inhibitors, with three homologues possessing IC₅₀ values <0.1 μM . Dialysis of enzyme–inhibitor mixtures further established a selected 1‐indanone as a reversible MAO inhibitor with a competitive mode of inhibition. It may be concluded that 1‐indanones are promising leads for the design of therapies for neurodegenerative and neuropsychiatric disorders such as Parkinson’s disease and depression.     

Boiling points of the propylene glycol + glycerol system at 1 atmosphere pressure: 188.6–292 °C without and with added water or nicotine

Abstract

In electronic cigarettes (“electronic nicotine delivery systems”, ENDS), mixtures of propylene glycol (PG) and/or glycerol (GL; aka “vegetable glycerin”, VG) with nicotine are vaporized to create a nicotine-containing aerosol. For a given composition, the temperature required to boil the liquid at 1 atmosphere must be at least somewhat greater than the boiling point (BP). The use of ENDS is increasing rapidly worldwide, yet the BP characteristics of the PG?+?GL system have been characterized as the mixtures; here we re-do this, but significantly, also study the effects of added water and nicotine. BP values at 1 atmosphere pressure were measured over the full binary composition range. Fits based on the Gibbs–Konovalov theorem provide BP as a function of composition (by mole-percent, by weight-percent, and by volume-percent). BPs of PG?+?GL mixtures were then tested in the presence of additives such as water (2.5 and 5?mol% added) and nicotine (3?mol%). Water was found to decrease the BP of PG?+?GL mixtures significantly at all compositions tested, and nicotine was found to decrease the BP of PG?+?GL mixtures containing ～75 GL: 25?PG (by moles) or more. The effect of added water (5, 10, and 15?mol% added) on electronic cigarette degradation production (some aldehydes and formaldehyde hemiacetals) was examined and found to have no significant impact on solvent (PG or GL) degradation for the particular device used.     

Effects of seabird vectors on the fate, partitioning, and signatures of contaminants in a High Arctic ecosystem

Seabirds bioaccumulate contaminants from prey, transport them to their nesting sites, and deposit them in their excreta and carcasses, thereby focusing marine-derived contaminants into remote, terrestrial receptor sites. In the case of organochlorine chemicals transported by northern fulmars (Fulmarus glacialis) to a High Arctic seabird colony on Devon Island, Nunavut, Canada (76°13'N, 89°14'W), this contaminant pathway dominates all others. In freshwater ponds below the nesting cliffs, concentrations of organochlorine contaminants characteristic of fulmar input were 2- to 45-fold higher in sediments and water (depending on seabird input to the particular pond) than in ponds remote from the colony. Air-water fugacity quotients for the ponds decreased with seabird input, indicating that fulmar contaminant input shifts air-water partitioning to increasingly favor volatilization to air. Although contaminant evasion from water was favored, direct evidence of it was not detected in air samples. For PCBs, congener profiles of pond sediments or water became more similar to seabird sources as seabird input increased, and less similar to air profiles. Based on measurements of contaminants in fulmars and other local environmental media, this study presents the first application of fugacities and multivariate source apportionment statistics to resolve seabird biological vectors.     

Ellagic acid promoted biomimetic synthesis of shape-controlled silver nanochains

In this work, ellagic acid (EA), a naturally occurring plant polyphenol, was utilized for the biomimetic synthesis of silver (Ag) nanoparticles, which over a period of time formed extended branched nanochains of hexagonal-shaped silver nanoparticles. It was found that EA not only has the capability of reducing silver ions, resulting in the formation of Ag nanoparticles, due to its extended polyphenolic system, but also appears to recognize and affect the Ag nanocrystal growth on the (111) face, leading to the formation of hexagon-shaped Ag nanocrystals. Initially, various Ag nanocrystal shapes were observed; however, over a longer period of time, a majority of hexagonal-shaped nanocrystals were formed. Although the exact mechanism of formation of the nanocrystals is not known, it appears that EA attaches to the silver nuclei, leading to lower surface energy of the (111) face. Further, the nanocrystals fuse together, forming interfaces among the aggregates, and, with time, those interfaces become lesser, and the nanoparticles merge together and share the same single crystallographic orientation, which leads to the formation of long elongated chains of hexagonal nanoparticles. This biomimetic approach may be developed as a green synthetic method to prepare building blocks with tunable properties for the development of nanodevices. Further, we explored the antibacterial properties and found that the tandem of EA-Ag nanochains substantially enhanced the antibacterial properties of both gram-positive and gram-negative bacteria compared to silver nanoparticles or EA alone. Additionally, the materials were also utilized for imaging of mammalian NRK (normal rat kidney) cells.     

Two-year-olds' search strategies and visual tracking in a hidden displacement task.

Children younger than 3 years have difficulty with search tasks that involve hidden displacement. Partial visual information was provided about a ball's path as it moved toward a hiding place. Children (2.0 and 2.5 years old) saw a ball rolling down a ramp placed behind a transparent screen with 4 opaque doors. A wall, placed on the ramp and directly behind 1 of the doors, protruded above the screen and stopped the ball. Children were asked to find the ball. The transparency of the screen permitted visual tracking of the ball between the doors, but its final resting place was obscured. Both age groups were equally proficient at tracking the ball as it rolled behind the screen, but the 2.5-year-olds were more likely to reach to the correct door. Looking behavior was related to errors in the younger group in that tracking that stopped short or continued past the correct door was associated with incorrect choices. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

The abrasive wear of metals

A quite general relationship exists between abrasive wear and the ploughing contribution to friction. Tensile stresses are developed in the material displaced by the ploughing indenter and these give rise to wear particles.     

Productivity and maximal oxygen consumption in sugar cane cutters

Vo2max and daily productivity (metric tons/day) have been measured in 46 sugar cane cutters 18 to 34 years of age. A multiple regression analysis demonstrated that productivity was simultaneously related to VO2max, height and body fat (r=0.685;P less than 0.001). The multiple regression equation was: productivity (tons/day)=0.81 VO2max-0.14 percent fat +0.03 height -1.96. The data indicate that productivity is affected indirectly by nutritional status through the influence of the latter on height, fat content and VO2max. The decrease in VO2max that occurs with age was similar to that reported in the literature. Evidence is presented that, as the worker ages, a higher percent VO2max has to be utilized to maintain productivity.     

Distinct roles for the mammalian A-type cyclins during oogenesis

There are two A-type cyclins in higher vertebrates, cyclin A1 and A2. Targeted mutagenesis has shown that cyclin A2 is essential for early embryonic development while cyclin A1 is required only for male meiosis. The embryonic lethality of cyclin A2 knockout mice has obviated understanding its role in other aspects of mammalian development, including the germ line. We reported previously that cyclin A2 expression in the male germ line is consistent with a role in both mitotic and meiotic cell cycles. Using in situ hybridization and immunohistochemistry, we now observe high levels of cyclin A2 in granulosa cells and less-abundant but readily detectable expression in ovarian and ovulated oocytes. A decrease in cyclin A2 protein was observed in oocytes from embryonic stages to post-natal and adult ovaries. Interestingly, cyclin A2 protein was nuclear in oocytes from embryonic day 13.5 to 15.5, changing to largely cytoplasmic in oocytes from embryonic day 16.5 to post-natal and adults. Readily detectable expression of the cyclin-dependent kinases Cdk1 and Cdk2, two common partners for the A-type cyclins, was observed in granulosa cells and oocytes at all stages of folliculogenesis. Cdk1 was predominantly cytoplasmic, whereas Cdk2 was both cytoplasmic and nuclear in oocytes. No cyclin A1 expression, at either the mRNA level or the protein level was detected in either embryonic or adult ovaries, consistent with the full fertility observed in female cyclin A1-deficient mice. These results suggest that in the female germ line, cyclin A2 but not cyclin A1 has distinct roles in both mitosis and meiosis.     

Development of an optimised papaya pulp nectar using a combination of irradiation and mild heat

Papaya does not sufficiently maintain desired fresh fruit quality when shipped long distances due to an easily bruised soft skin and a short shelf life. This leads to both a large supply of pulp from unsightly fruit that is never shipped and low sales due to blemished fruit. Unfortunately, traditional preservation methods (pasteurisation) negatively alter papaya’s fresh flavour. Thus to effectively utilise available papaya pulp, processing requires an approach that enables retention of papaya’s natural flavours without excessive heat. Papaya fruit (Carica papaya L., var.’s Rainbow (yellow-fleshed) and SunUp (red-fleshed)) were pulped, diluted, and processed with mild heat (80 °C, 5 min), irradiation (5 kGy or 7.5 kGy) or combinations of both. Irradiation resulted in a significant reduction in ascorbic acid content. Mild heat treatment significantly reduced pectinesterase activity and microbiological viability. Irradiation followed by heat further enhanced destruction of Listeria innocua and Clostridium sporogenes and retained the flavour and a nutritional profile closest to untreated controls. The product was microbiologically safe with acceptable enzyme levels and would be shippable under refrigeration.