Interaction of dinotefuran and its analogues with nicotinic acetylcholine receptors of cockroach nerve cords

To investigate the action of dinotefuran (MTI-446, 1-methyl-2-nitro-3-(tetrahydro-3-furylmethyl)guanidine), a recently developed insecticide, on insect nicotinic acetylcholine receptors (nAChRs), we determined the potencies of the compound and 15 analogues in inhibiting the specific binding of [3H]epibatidine (EPI), a nAChR agonist, and [3H]alpha-bungarotoxin (alpha-BGT), a competitive nAChR antagonist, to the nerve cord membranes of American cockroaches (Periplaneta americana). Racemic dinotefuran inhibited [3H]EPI binding with an IC50 of 890 nM and [3H]alpha-BGT binding with an IC50 of 36.1 microM. Scatchard analysis indicated that the dinotefuran inhibition of [3H]EPI binding was a competitive one. Slight structural modification caused a drastic reduction in potency; only four analogues were found to be equipotent to or more potent than dinotefuran. Chloropyridinyl and chlorothiazolyl neonicotinoid insecticides displayed two or three orders of magnitude higher potency than dinotefuran. There was a good correlation between the IC50 values of tested compounds obtained with [3H]EPI and those obtained with [3H]alpha-BGT. A better correlation was observed between 3-h knockdown activities (KD50) against German cockroaches (Blattella germanica) and IC50 values obtained from [3H]EPI assays than between 24-h lethal activities (LD50) and IC50 values. While the results indicate that dinotefuran and its analogues interact with the ACh-binding site in cockroach nAChRs, it remains to be elucidated why they displayed lower potencies than those expected based on their insecticidal activities.     

Seasonal stream habitat of adult Sakhalin taimen,Parahucho perryi,in the Bekanbeushi River system,eastern Hokkaido,Japan

Behavioural tracking of endangered adult Sakhalin taimen (Parahucho perryi) by acoustic telemetry was conducted in the Bekanbeushi River system that flows through eastern Hokkaido in 2008–2010. A total of 39 tracked P. perryi showed extensive use of the river system, both upstream and downstream, regardless of the month or year. No tracked adult P. perryi stayed in the ocean for more than 1 day. Some of the fish (20%) dwelled in upstream habitat consistently from spring to autumn, while 40% of individuals showed wide utilisation of the entire upstream and downstream systems. Although 39.4% of tracked fish utilised two or more primary tributaries to the main river, 6.1% used only the main river system. Distinct variability was observed between individuals based on the proportion of time spent in each stream reach (up‐, mid‐, and downstream). A trend was observed in 2008 and 2010 showing that tracked fish moved to the upper stream reaches when water temperatures downstream increased. This trend was not observed in 2009 when the summer water temperature downstream was more than 2 °C below average when compared to 2008 and 2010. Our results suggest that adult P. perryi in the Bekanbeushi River system exhibit high behavioural plasticity, that is, the fish can select habitats based on their own individual requirements. Our results also demonstrate the importance of physical continuity among river reaches both upstream and downstream such that P. perryi does not experience barriers in moving to optimal habitats.     

Effect of intermittent heat treatment on crystallinity in wood cellulose

The effect of intermittent heat treatment on cellulose crystallites in wood was studied to evaluate quantitatively the changes of crystallinity induced by intermittent and continuous heating. The changes in crystallinity were found to be strongly affected by the intermittent heat treatment. The increased crystallinity, the width of the crystals, and the piezoelectric properties were the same for the first intermittent heating as for continuous heating. Further intermittent heating for the same time duration and temperature had no effect on the above properties, probably due to the stopping of the thermal reaction during the interval. Our results suggested that intermittent heat treatment has certain critical cooling temperatures that stop the thermal reaction and are closely related to the duration of the interval. Samples once exposed to a certain duration of heat treatment and then cooled need more time, about twice that of the first duration of intermittent heating compared with continuous heating, to reach maximum crystallinity in wood cellulose.     

The therapeutic effects of SET/I2PP2A inhibitors on canine melanoma

Canine melanoma is one of the most important diseases in small animal medicine. Protein phosphatase 2A (PP2A), a well conserved serine/threonine phosphatase, plays a critical role as a tumor suppressor. SET/I2PP2A is an endogenous inhibitor for PP2A, which directly binds to PP2A and suppresses its phosphatase activity. Elevated SET protein levels have been reported to exacerbate human tumor progression. The role of SET in canine melanoma, however, has not been understood. Here, we investigated the potential therapeutic role for SET inhibitors in canine melanoma. The expression of SET protein was observed in 6 canine melanoma cell lines. We used CMeC-1 cells (primary origin) and CMeC-2 cells (metastatic origin) to generate cell lines stably expressing SET-targeting shRNAs. Knockdown of SET expression in CMeC-2, but not in CMeC-1, leads to decreased cell proliferation, invasion and colony formation. Phosphorylation level of p70 S6 kinase was decreased by SET knockdown in CMeC-2, suggesting the involvement of mTOR (mammalian target of rapamycin)/p70 S6 kinase signaling. The SET inhibitors, OP449 and FTY720, more effectively killed CMeC-2 than CMeC-1. We observed PP2A activation in CMeC-2 treated with OP449 and FTY720. These results demonstrated the potential therapeutic application of SET inhibitors for canine melanoma.     

Does future climate change facilitate expansion of evergreen broad-leaved tree species in the human-disturbed landscape of the Korean Peninsula? Implication for monitoring design of the impact assessment

To quantitatively assess future change of evergreen broad-leaved tree species’ distributions in human-disturbed landscapes of the Korean Peninsula under climate change, potential habitats (PHs) were projected for four important evergreen broad-leaved tree species (Quercus acuta, Castanopsis sieboldii, Machilus thunbergii, and Neolitsea sericea) by species distribution models (SDMs). The distribution data (presence/absence) of the target species in Korea and Japan were used as response variables for SDMs, and climatic data were used as explanatory variables. Three general circulation models under A2 emission scenarios were used as future climate scenarios for the years 2070–2099. Potential habitats masked by land-use data (PHLUs) were projected to assess the impact of anthropogenic activities. Highly accurate SDMs were obtained for all the target species. The current PHs were decreased to 21–35 % by the anthropogenic activities. Future PHLUs for all the target species were projected to increase by 2.0–18.5 times of current PHLUs. These results suggest that all the target species are applicable as indicator species for monitoring in the Korean Peninsula, even if anthropogenic effects are incorporated. Variation of the increasing rate was caused by the differences in the response to temperature changes. M. thunbergii responded sensitively to the increase of minimum temperature of coldest month and had a largest increase in PHLUs under future climate. Therefore, M. thunbergii is considered to be most appropriate species for monitoring the changes of horizontal distributions above all focal evergreen broad-leaved tree species.     

Utilization of free amino acids, yolk proteins and lipids in developing eggs and yolk-sac larvae of walleye pollock Theragra chalcogramma

ABSTRACT:   To elucidate the utilization of the major yolk nutrient stocks in eggs and larvae of walleye pollock Theragra chalcogramma , the contents of free amino acids (FAA), the major yolk protein (180 kDa lipovitellin originated from vitellogenin B in ovulated eggs: oLv B), and lipids were measured. Most eggs hatched 18 days after fertilization at 5°C, and all larvae absorbed almost all their yolk mass by 28 days. The total FAA content showed no change during the first 6 days, and then decreased to 28% of the initial level by 18 days. The oLv B contents, measured by an enzyme-linked immunosorbent assay using a specific antiserum against oLv B, gradually decreased from 6 to 18 days, followed by a rapid decline. The content of phospholipids (PL) and triacylglycerols (TG) showed no marked change until hatching, and then decreased until disappearance of yolk sac. From these results, it is proposed that there are two main periods for nutrient utilization in embryos and larvae of walleye pollock. In the first period, FAA was mainly utilized until 18 days after fertilization. Active utilization of oLv B and lipids (PL and TG) instead of FAA occurred during the second period from 18 to 28 days.