Effect of vitamin A deprivation on the cholesterol side-chain cleavage enzyme activity of testes and ovaries of rats (Short Communication)

The cholesterol side-chain cleavage enzyme activity is decreased considerably at the mild stage of vitamin A deficiency in rat testes and ovaries and the decrease in activity becomes more pronounced with progress of deficiency. Supplementation of the deficient rats with retinyl acetate, but not retinoic acid, restores the enzyme activity to normal values. The cholesterol side-chain cleavage enzyme of adrenals is not affected by any of the above treatments.

Mesospheric temperature response to variations in geomagnetic activity

Temperature data collected over several years from rocket grenade and other experiments at Point Barrow (Alaska), Fort Churchill (Canada) and Wallops Island (Virginia) have been analysed to determine the effect of geomagnetic activity on the neutral temperature in the mesosphere and to study the latitudinal variation of this effect. An analysis carried out has revealed almost certainly significant correlations between the temperature and the geomagnetic indicies Kp and Ap at Fort Churchill and marginally significant correlations at Barrow and Wallops. This has also been substantiated by a linear regression analysis. The results indicate two types of interdependence between mesospheric temperature and geomagnetic field variations. The first type is the direct heating effect, during a geomagnetic disturbance, which has been observed in the present analysis with a time lag of 3–15 hr at the high latitudes and 36 hr at the middle latitudes. The magnitude of this heating effect has been found to decrease at the lower altitudes. The second type of interrelation which has been observed is temperature perturbations preceding geomagnetic field variations, both presumably caused by a disturbance in atmospheric circulation at these levels.

The effect of solar activity on temperatures in the equatorial mesosphere

A study of the response of neutral temperatures in the equatorial mesosphere to variations in solar activity has been carried out by investigating the correlation between the 10.7 cm solar radio flux and temperatures obtained from a series of 51 rocket soundings conducted over Thumba, India (8°N, 77°E) during the period December 1970–December 1971. A strong positive correlation between these two parameters has been obtained, indicating mesospheric heating effects caused by day-to-day variations in solar EUV emission. The correlation analysis indicates that this response persists over several days and that the peak correlation between the temperatures and the F10.7 index occurs with a time lag of less than 24 hr.

Alk (en) ylresorcinol concentrations in'Kensington Pride'mango peel and antifungal activity against Colletotrichum gloeosporioides

Two preformed alk(en)ylresorcinols, 5-n-heptadecenylresorcinol and 5-n-pentadecylresorcinol, were identified in ‘Kensington Pride’ mango fruit peel. The alk(en)ylresorcinols had antifungal activity against C. gloeosporioides, as determined from thin layer chromatography bioassays. Soil-applied activators of plant defence (Acibenzolar at 150 mg L-1, and soluble potassium silicate at 200 and 1000 mg L-1) did not influence concentrations of 5-n-heptadecenylresorcinol or 5-n-pentadecyl¬resorcinol in mango peel when applied 2 months after fruit set and one month later. Concentrations of both alk(en)ylresorcinols were high 2 months after fruit set but levels declined by 50% within 1 month (2 months before commercial harvest) and did not change significantly from commercial harvest until eating-ripe.

Synthesis, Reactivity and Biological Activity of 17β-HSD1 Inhibitors Based on a Thieno[2,3-d]pryrimidin-4(3H)-one Core

Breast cancer is the most common cancer in women in Western countries. In the early stages of development most breast cancers are hormone-dependent, and estrogens, especially estradiol, have a pivotal role in their development and progression. One approach to the treatment of hormone-dependent breast cancers is to block the formation of the active estrogens by inhibiting the action of the steroid metabolising enzymes. 17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) is a key enzyme in the biosynthesis of estradiol, the most potent female sex hormone. The 17beta-HSD1 enzyme catalyses the final step and converts estrone into the biologically active estradiol. Blocking 17beta-HSD1 activity with a specific enzyme inhibitor could provide a means to reduce circulating and tumour estradiol levels and thus promote tumour regression. In recent years 17beta-HSD1 has been recognised as an important drug target. Some inhibitors of 17beta-HSD1 have been reported, however, there are no inhibitors on the market nor have clinical trials been announced. The majority of known 17beta-HSD1 inhibitors are based on steroidal structures, while relatively little has been reported on non-steroidal inhibitors. As compared with 17beta-HSD1 inhibitors based on steroidal structures, non-steroidal compounds could have advantages of synthetic accessibility, drug-likeness, selectivity and non-estrogenicity. This study describes the synthesis of large group of novel 17beta-HSD1 inhibitors based on a non-steroidal thieno[2,3-d]pyrimidin-4(3H)-one core. An efficient synthesis route was developed for the lead compound and subsequently employed in the synthesis of thieno[2,3-d]pyrimidin-4(3H)-one based molecule library. The biological activities and binding of these inhibitors to 17beta-HSD1 and, finally, the quantitative structure activity relationship (QSAR) model are also reported. In this study, several potent and selective 17beta-HSD1 inhibitors without estrogenic activity were identified. This establishment of a novel class of inhibitors is a progressive achievement in 17beta-HSD1 inhibitor development. Furthermore, the 3D-QSAR model, constructed on the basis of this study, offers a powerful tool for future 17beta-HSD1 inhibitor development. As part of the fundamental science underpinning this research, the chemical reactivity of fused (di)cycloalkeno thieno[2,3-d]pyrimidin-4(3H)-ones with electrophilic reagents, i.e. Vilsmeier reagent and dimethylformamide dimethylacetal, was investigated. These findings resulted in a revision of the reaction mechanism of Vilsmeier haloformylation and further contributed to understanding the chemical reactivity of this compound class. This study revealed that the reactivity is dependent upon a stereoelectronic effect arising from different ring conformations.

Information flow, trading activity and commodity futures volatility

Based on unique news data relating to gold and crude oil, we investigate how news volume and sentiment, shocks in trading activity, market depth and trader positions unrelated to information flow covary with realized volatility. Positive shocks to the rate of news arrival, and negative shocks to news sentiment exhibit the largest effects. After controlling for the level of news flow and cross-correlations, net trader positions play only a minor role. These findings are at odds with those of [Wang (2002a). The Journal of Futures Markets, 22, 427–450; Wang (2002b). The Financial Review, 37, 295–316], but are consistent with the previous literature which doesn't find a strong link between volatility and trader positions.

Novel Biginelli dihydropyrimidines with potential anticancer activity: A parallel synthesis and CoMSIA study

Novel Biginelli dihydropyrimidines of biological interest were prepared using p-toluene sulphonic acid as an efficient catalyst. All the thirty-two synthesised dihydropyrimidines were evaluated for their in vitro antioxidant activity using DPPH method. Only, compounds 28 and 29 exhibited reasonably good antioxidant activity. Furthermore, the synthesised Biginelli compounds were subjected for their in vitro anticancer activity against MCF-7 human breast cancer cells. The title compounds were tested at the concentration of 10 μg. Compounds exhibited activity ranging from weak to moderate and, from moderate to high in terms of percentage cytotoxicity. Among them, compounds 10 and 11 exhibited significant anticancer activity. In order to elucidate the three-dimensional structure–activity relationships (3D QSAR) towards their anticancer activity, we subjected them for comparative molecular similarity indices analysis (CoMSIA). Illustration regarding their synthesis, analysis, antioxidant activity, anticancer activity and 3D QSAR study is described.

Infrared spectroscopy as a rapid tool to detect methylglyoxal and antibacterial activity in Australian honeys

Methylglyoxal (2-oxopropanal) is a compound known to contribute to the non-peroxide antimicrobial activity of honeys. The feasibility of using infrared spectroscopy as a predictive tool for honey antibacterial activity and methylglyoxal content was assessed. A linear relationship was found between methylglyoxal content (279–1755 mg/kg) in Leptospermum polygalifolium honeys and bacterial inhibition for Escherichiacoli (R2 = 0.80) and Staphylococcusaureus (R2 = 0.64). A good prediction of methylglyoxal (R2 0.75) content in honey was achieved using spectroscopic data from the mid infrared (MIR) range in combination with partial least squares regression. These results indicate that robust predictive equations could be developed using MIR for commercial application where the prediction of bacterial inhibition is needed to ‘value’ honeys with methylglyoxal contents in excess of 200 mg/kg.

Patient preferences for receiving remote communication support for lifestyle physical activity behaviour change: The perspective of patients with musculoskeletal disorders from three hospital services

This study examined patients’ preference ratings for receiving support via remote communication to increase their lifestyle physical activity. Methods People with musculoskeletal disorders ( n=221 of 296 eligible) accessing one of three clinics provided preference ratings for “how much” they wanted to receive physical activity support via five potential communication modalities. The five ratings were generated on a horizontal analogue rating scale (0 represented “not at all”; 10 represented “very much”). Results Most (n=155, 70%) desired referral to a physical activity promoting intervention. “Print and post” communications had the highest median preference rating (7/10), followed by email and telephone (both 5/10), text messaging (1/10), and private Internet-based social network messages (0/10). Desire to be referred was associated with higher preference for printed materials (coefficient = 2.739, p<0.001), telephone calls (coefficient = 3.000, p<0.001), and email (coefficient = 2.059, p=0.02). Older age was associated with lower preference for email (coefficient = −0.100, p<0.001), texting (coefficient = −0.096, p<0.001), and social network messages (coefficient = −0.065, p<0.001). Conclusion Patients desiring support to be physically active indicated preferences for interventions with communication via print, email, or telephone calls.

Promoting and maintaining physical activity in the transition to retirement: A systematic review of interventions for adults around retirement age

It has been argued that transition points in life, such as the approach towards, and early years of retirement present key opportunities for interventions to improve the health of the population. Research has also highlighted inequalities in health status in the retired population and in response to interventions which should be addressed. We aimed to conduct a systematic review to synthesise international evidence on the types and effectiveness of interventions to increase physical activity among people around the time of retirement. A systematic review of literature was carried out between February 2014 and April 2015. Searches were not limited by language or location, but were restricted by date to studies published from 1990 onwards. Methods for identification of relevant studies included electronic database searching, reference list checking, and citation searching. Systematic search of the literature identified 104 papers which described study populations as being older adults. However, we found only one paper which specifically referred to their participants as being around the time of retirement. The intervention approaches for older adults encompassed: training of health care professionals; counselling and advice giving; group sessions; individual training sessions; in-home exercise programmes; in-home computer-delivered programmes; in-home telephone support; in-home diet and exercise programmes; and community-wide initiatives. The majority of papers reported some intervention effect, with evidence of positive outcomes for all types of programmes. A wide range of different measures were used to evaluate effectiveness, many were self-reported and few studies included evaluation of sedentary time. While the retirement transition is considered a significant point of life change, little research has been conducted to assess whether physical activity interventions at this time may be effective in promoting or maintaining activity, or reducing health inequalities. We were unable to find any evidence that the transition to retirement period was, or was not a significant point for intervention. Studies in older adults more generally indicated that a range of interventions might be effective for people around retirement age.

Using UHF proximity loggers to quantify male–female interactions: A scoping study of estrous activity in cattle

Reproductive efficiency is an important determinant of profitable cattle breeding systems and the success of assisted reproductive techniques (ART) in wildlife conservation programs. Methods of estrous detection used in intensive beef and dairy cattle systems lack accuracy and remain the single biggest issue for improvement of reproductive rates and such methods are not practical for either large-scale extensive beef cattle enterprises or free-living mammalian species. Recent developments in UHF (ultra high frequency) proximity logger telemetry devices have been used to provide a continuous pair-wise measure of associations between individual animals for both livestock and wildlife. The objective of this study was to explore the potential of using UHF telemetry to identify the reproductive cycle phenotype in terms of intensity and duration of estrus. The study was conducted using Belmont Red (interbred Africander Brahman Hereford–Shorthorn) cattle grazing irrigated pasture on Belmont Research Station, northeastern Australia. The cow-bull associations from three groups of cows each with one bull were recorded over a 7-week breeding season and the stage of estrus was identified using ultrasonography. Telemetry data from bull and cows, collected over 4 8-day logger deployments, were log transformed and analyzed by ANOVA. Both the number and duration of bull-cow affiliations were significantly (P < 0.001) greater in estrous cows compared to anestrus cows. These results support the development of the UHF technology as a hands-off and noninvasive means of gathering socio-sexual information on both wildlife and livestock for reproductive management.

Electrophysiological activity of the Sirex noctilio ovipositor: You know the drill?

Sirex woodwasp (Sirex noctilio F: Hymenoptera: Siricidae) is a major worldwide pest of pine (Pinus) species. The female woodwasp undertakes exploratory drills with the ovipositor prior to egg-laying to assess tree suitability. Previous work has shown that this behaviour is associated with assessing the osmotic pressure of the tree. Here we show that, in addition, the ovipositor is electrophysiologically active and capable of detecting ethanol and chemical components of solvent extracts of pine needles and bark. Scanning electron micrographs of the ovipositor show the presence of structures which may have a chemoreceptive function. Our research expands our knowledge of the role that the Sirex ovipositor plays in egg-laying site selection.

Cytorhabdovirus phosphoprotein shows RNA silencing suppressor activity in plants, but not in insect cells

RNA silencing in plants and insects provides an antiviral defense and as a countermeasure most viruses encode RNA silencing suppressors (RSS). For the family Rhabdoviridae, no detailed functional RSS studies have been reported in plant hosts and insect vectors. In agroinfiltrated Nicotiana benthamiana leaves we show for the first time for a cytorhabdovirus, lettuce necrotic yellows virus (LNYV), that one of the nucleocapsid core proteins, phosphoprotein (P) has relatively weak local RSS activity and delays systemic silencing of a GFP reporter. Analysis of GFP small RNAs indicated that the P protein did not prevent siRNA accumulation. To explore RSS activity in insects, we used a Flock House virus replicon system in Drosophila S2 cells. In contrast to the plant host, LNYV P protein did not exhibit RSS activity in the insect cells. Taken together our results suggest that P protein may target plant-specific components of RNA silencing post siRNA biogenesis.