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.     

Enhancement of photosynthesis and growth of tomato seedlings by forced ventilation within the canopy

A forced ventilation system that directs airflow upward or downward within a canopy was developed for plant culture in order to enhance photosynthesis and growth of the plant canopy. Tomato seedling canopies including the seedlings, growing medium, and a plastic tray were used for the experiments. In the upward and downward ventilation systems, air flows upward and downward, respectively, within the plant canopy; this is achieved by blowing and drawing air from holes (Ø 6 mm) made in plastic pipes positioned on the surface of the growing medium. A horizontal airflow system was used as a conventional system to compare the performance of the experimental ventilation systems. Using the upward and downward ventilation systems, the effects of air directions and air velocities on the CO₂ exchange rate of the tomato seedling canopy and the growth of the seedlings were compared with those observed using the conventional horizontal airflow system. The forced ventilation within the plant canopy enhanced the CO₂ exchange rate of the canopy and the dry masses of the seedlings by 1.4–1.5 and 1.2–1.3 times, respectively, as compared to the conventional horizontal airflow. When the leaf area index (LAI) increased from 1.2 to 2.4, there was only a 5% decrease in the CO₂ exchange rate per unit leaf area in the downward ventilation system, whereas there was a 20% decrease in the CO₂ exchange rate per leaf area in the horizontal airflow system. The coefficient of variation for the dry mass of the seedlings was higher in the downward system than in the other systems. These results demonstrate that forced ventilation within the canopy is an effective technique to enhance the gas exchange of the plant canopy and the consequent plant growth.     

'Looking up' behavior in the holding area of the milking parlor: its relationship with step-kick, flight responses and productivity of commercial dairy cows

Commercial dairy cows milked in a parlor system are packed close together in the holding area before milking. The present study examined the relationships of ‘looking up’ behavior with some other behaviors and the productivity of 1116–1153 cows from five farms. The individual identities of the cows looking up in the holding area were recorded at 5 min intervals during six intermittent afternoon milking sessions. Entrance into the milking parlor and the numbers of steps and kicks by cows while the milking person was attaching the milking cups, were recorded in six milking sessions. Flight responses in the pasture after milking were recorded over four days intermittently. The frequency of ‘looking up’ behavior weakly, but significantly correlated with flight starting distance (r = 0.10, P < 0.05), while the correlation with the number of step‐kicks during milking was not significant. As for productivity, lactation number (r = ?0.18, P < 0.001), milk yield (r = ?0.15, P < 0.001) and fat content (r = ?0.15, P < 0.001) were negatively correlated with the frequency of ‘looking up’ behavior. Age of cows was correlated with the frequency of ‘looking up’ behavior as well as lactation number (r = ?0.21, P < 0.001). Entrance order was positively correlated with the frequency of ‘looking up’ behavior (r = 0.15, P < 0.001). The ‘looking up’ behavior was observed more frequently in cows in their third or less lactation compared with cows which were in their fourth or greater lactation (P < 0.05). The lactation number of cows was correlated with their milk yield (r = 0.36, P < 0.001) and flight starting distance (r = ?0.21, P < 0.001). In conclusion, ‘looking up’ behavior shown by cows in the holding area before milking might be an indicator of low motivation for milking, mainly because of fear of humans, and an aversion to milking caused by insufficient experience in being milked.     

Factors affecting agonistic interactions of pigs after regrouping in pens with a box

To determine the factors affecting agonistic interactions after regrouping, 24 pigs were allocated to six pens that each had a box. Half of the pigs were experienced in using the box. One castrated male and one female pig were transferred from each pen to another pen at random. The number of pigs attacked was particularly large for the pigs that had no experience in using the box and were transferred on the first day ( P <  0.05). The duration of access to the box was markedly longer for the pigs that had experience in using the box and were not transferred on the first day ( P <  0.05). The number and duration of attacks were significantly larger and longer toward unfamiliar individuals than toward familiar ones (both P < 0.01). The number of attacks toward the same sex was significantly larger than toward the opposite sex ( P <  0.01). A negative correlation was found between the number of agonistic interactions on the first day and the range of body weights in the pen mates ( r =  −0.78, P  = 0.07). In conclusion, regrouping with unfamiliar individuals should be avoided, but when unavoidable, the following methods are recommended to reduce agonistic interactions: (1) ensure the intruders are experienced in using a box, (2) move experienced intruders in with residents that have no experience in using a box, (3) mix different sexes, and (4) have wide variations in body weights in a pen.     

The effect of estrogen on phosphorylation of prolactin in the mouse pituitary gland

Several studies have indicated that prolactin (PRL) assumes oligomeric, proteolytically cleaved, phosphorylated and glycosylated forms. Phosphorylated PRL (PPRL) is considered to be the most important posttranslationally modified form in the rat. In the present study, we examined whether or not PRL is present in the mouse pituitary gland in the phosphorylated form. Mouse pituitary PRL was digested with acid phosphatase, resolved by two-dimensional gel electrophoresis, stained with Coomassie brilliant blue, and then immunoblotted against the anti-PRL, anti-phosphoserine and anti-phosphothreonine antibodies. We also examined whether PRL is phosphorylated by protein kinases and semi-quantified the ratios of PPRL to PRL in the pituitary gland. The results indicated that three types of PRL are present in the pituitary glands of both male and female mice. One was non-phosphorylated (isoform 1), and the other two were immunoreactive to anti-phosphoserine (isoform 2) and/or anti-phosphothreonine (isoform 3) antibodies. The ratio between isoforms 2 and 1 of the 30-day-old female mice was higher than that of the 20-day-old female mice. However, the ratios among the three isoforms in the male pituitary glands did not differ with age. The ratio of PPRL to isoform 1 was obviously reduced after ovariectomy (OVX), and it recovered with estrogen replacement. These results suggest that estrogen influences PRL phosphorylation in female mice.     

Quantitative structure-activity analysis of larvicidal 1-(substituted benzoyl)-2-benzoyl-1-tert-butylhydrazines against Chilo suppressalis

The larvicidal activity of a number of 1-(substituted benzoyl)-2-benzoyl–1 -ten-butylhydrazines against the rice stem borer (Chilo suppressalis Walk.) was measured. Variations in the activity were examined quantitatively using physico-chemical substituent and molecular parameters and regression analysis. The results indicated that the molecular hydrophobicity and the electron-withdrawing inductive/ field effect of ontho substituents are favourable to larvicidal activity. The bulkiness of substituents at the meta and para positions was unfavourable to activity, substitution at the para position being more unfavourable than that at the meta position in terms of van der Waals' volume. The 2,3–, 2,5- and 2,6-disubstitution patterns were also unfavourable to activity. Reductions in larvicidal activity caused by the 2,6-,- 2,3,5- and 2,3,4,5-substitutions were greater than those induced by the 2,3- and 2,5-disubstitutions. When the sum of contributions from favourable effects is greater than that from unfavourable effects, the larvicidal activity is expected to be superior to that of the unsubstituted compound.     

Time-course comparison of pulmonary inflammation induced by intratracheal instillation of four different nickel oxide nanoparticles in male Fischer rats

Occupational exposure to nickel oxide (NiO) is an important cause of respiratory tract cancer. Toxicity is known to be associated with the dissociated component, i.e. nickel (II) ions. To address the relationship between physicochemical properties, including solubility in artificial lysosomal fluid, of NiO and time-course changes in the pulmonary response, we conducted an intratracheal instillation study in male Fischer rats using four different well-characterized NiO products, US3352 (NiO A), NovaWireNi01 (NiO B), I small particle (NiO C), and 637130 (NiO D). The NiOs were suspended in purified water and instilled once intratracheally into male F344 rats (12 weeks old) at 0 (vehicle control), 0.67, 2, and 6 mg/kg body weight. The animals were euthanized on days 3, 28, or 91 after instillation, and blood analysis, bronchoalveolar lavage fluid (BALF) testing, and histopathological examination were performed. The most soluble product, NiO B, caused the most severe systemic toxicity, leading to a high mortality rate, but the response was transient and surviving animals recovered. The second-most-soluble material, NiO D, and the third, NiO A, caused evident pulmonary inflammation, and the responses persisted for at least 91 days with collagen proliferation. In contrast, NiO C induced barely detectable inflammation in the BALF examination, and no marked changes were noted on histopathology. These results indicate that the early phase toxic potential of NiO products, but not the persistence of pulmonary inflammation, is associated with their solubility.     

Quantitative structure-activity studies of substituted benzyl chrysanthemates: 7. Relationship between induction of repetitive discharges and effects on the action potential

The effects of substituted benzyl (1R)-trans-chrysanthemates and related compounds on the action potential of the crayfish giant axon were investigated using an intracellular microelectrode. The effects are broadly classified into three types: deceleration of the falling-phase of the action potential (type A), elevation of the depolarizing after-potential (type B), and the combination type (type C). The potency of the type A compounds to decelerate the rate of the falling-phase was determined in terms of the concentration required for reducing the rate to a specified degree. This potency was shown to correlate with the potency to induce repetitive discharges in the cockroach central nerve cord in terms of minimum effective concentration, which was determined previously. The potency of the types B and C compounds to elevate the after-potential was, however, not related directly with the cockroach nerve repetitive activity. The elevation of the after-potential is one of the critical factors but other effects such as a depolarization of the resting potential may be involved in determining the repetitive activity.     

Mangrove Habitat Formation and Response to Holocene Sea-level Changes on Kosrae Island,Micronesia

Mangrove habitats on Kosrae are divided into three types, i.e., an estuary or delta type, a backmarsh or lagoon type and a coral reef or tidal-flat type. Most of the mangrove forests of Kosrae have been developed during the last 2000 years by accumulating mangrove peat with the gradual sea-level rise of 1 to 2 mm/yr except the landward part of the estuary or delta type. On the other hand, during the period of rapid sea-level rise of about 10 mm/yr between 4100 and 3700 yr B.P., the mangrove forests ceased peat accumulation and retreated landward. Until 3500 yr B.P., mangrove forests were distributed only in narrow bands in the inlets. Therefore, the critical rate of mangrove peat accretion with sea-level rise is estimated at more than 2 mm/yr and less than 10 mm/yr. If the anticipated sea-level rise exceeds this critical rate, all of the mangrove forests of Kosrae will retreat landward and reduce rapidly.