Quantitative structure—activity relationships of light-dependent herbicidal 4-pyridone-3-carboxanilides I. Effect of benzene ring substituents at the anilide moiety

A number of substituted 4-pyridone-3-carboxanilide derivatives show various degrees of light-dependent herbicidal activity. The effects of substituents at the anilide moiety on the activity against Echinochloa oryzicola were analysed quantitatively with physicochemical substituent parameters. The activity was shown to vary parabolically with total hydrophobicity (Σπ) of the anilide ring substituents as well as with the steric parameter (E_s) of the ortho-substituents. The E_s parameter for only the bulkier ortho-substituent, with the more negative value, but not for the two, was significant. The effect of substituents at the 1-position was expressible by indicator variables assigned to each 1-substituted series, the physicochemical rationalization being left for future analyses.     

Permeability of the fish intestinal membrane to bulky chemicals

The ability to predict the environmental behavior of chemicals precisely is important for realizing more rational regulation. In this study, the bioaccumulation of nine chemicals of different molecular weights absorbed via the intestinal tract was evaluated in fish using the everted gut sac method. The amounts of chemicals that passed through the intestinal membrane after a 24-hr exposure were significantly decreased for chemicals with MW≥548 and D_{max min}≥15.8 Å (or D_{max aver}≥17.2 Å). These thresholds are consistent with those previously proposed in terms of MW (>800) and molecular size (D_{max min}>15.6 Å or D_{max aver}>17.1 Å) for the limit of permeable chemicals through the gill membrane. The results show that the same MW and D_max criteria can be used to predict low bioaccumulation through both the gill membrane and the intestinal tract. These findings are helpful in reducing the need to conduct animal tests in environmental safety studies.     

The use of micro-beam X-ray diffraction for the characterization of starch crystal structure in rice mutant kernels of waxy, amylose extender, and sugary1

Micro-beam X-ray diffraction analyses were carried out on slices from wild-type rice and mutants. The method permitted the crystalline structure to be analyzed with less destruction of cells and fewer artificial effects that occur during the purification of starch from tissue and provided information concerning the localization and crystalline structure of starches distributed in the endosperm. The starch on kernel slices from the wild-type and waxy mutant, carrying a defect for the Granule-bound starch synthase I (GBSSI) gene, displayed an A-type of diffraction pattern; no difference in the crystalline patterns between starches located in the inner and outer region in a kernel were observed. A double mutant of the waxy and amylose extender (ae) mutant carrying a defect for the Starch branching enzyme IIb gene accumulated amylose-free B-type starches. The kernel slice from the double mutant of waxy and sugary1, mutated on the Isoamylase I locus, displayed an A-type diffraction pattern in the outer region and was amorphous in the inner region. A chain-length distribution analysis of polyglucans in kernels from wild-type and mutants showed that ae amylopectin had more long chains and less short chains than the wild-type and waxy amylopectin. On the other hand, the water-soluble polysaccharide in the inner region of the sugary1 endosperm had more short chains than the amylopectin in the outer region counterparts. These results indicate that branch chain length in amylopectin is crucial in determining the formation of A- and B-type starches.     

Quantitative structure–activity studies of insect growth regulators: XVI. Substituent effects of dibenzoylhydrazines on the insecticidal activity to Colorado potato beetle Leptinotarsa decemlineata

Insecticidal activity against the Colorado potato beetle, Leptinotarsa decemlineata, was measured for a series of substituted N-tert-butyl-dibenzoylhydrazines, in which one of the benzoyl moieties closer to the tert-butyl group was fixed as being 2-chloro-substitued and the other variously substituted singly or doubly. The effects of substituents on the activity were quantitatively analysed using the classical quantitative structure–activity relationship (QSAR) procedure. The activity against the Colorado potato beetle increases with the molecular hydrophobicity. In addition, various types of steric effect are at work, depending upon the positions. Hydrogen-bonding acceptor substituents at the para position enhance the activity. There seem to be threshold (or optimum) values, albeit position-dependent, in the molecular hydrophobicity, above which the activity starts to decrease. This biphasic contribution of the molecular hydrophobicity to activity against coleopterous larvae is the most conspicuous difference in substituent effects from those found for similar compounds against lepidopterous pest insects, and may be the basis of the variations in the activity spectrum for certain compounds in this series. The introduction of bulkier substituents into the meta- and para-positions of the benzene ring, apart from the tert-butyl group, is unfavorable to activity. LD₅₀ values against Colorado potato beetle larvae of methoxyfenozide (RH-2485) and tebufenozide (RH-5992) were in the order of 10⁻⁷ mol per insect, whereas those of RH-5849, and halofenozide (RH-0345) were very low, 10⁻⁹–10⁻¹⁰ mol per insect being selective to the coleopterous larvae. © 1999 Society of Chemical Industry     

Greater disruption due to failure of inhibitory control on an ambiguous distractor

Considerable evidence indicates that a stimulus that is subthreshold, and thus consciously invisible, influences brain activity and behavioral performance. However, it is not clear how subthreshold stimuli are processed in the brain. We found that a task-irrelevant subthreshold coherent motion led to a stronger disturbance in task performance than did suprathreshold motion. With the subthreshold motion, activity in the visual cortex measured by functional magnetic resonance imaging was higher, but activity in the lateral prefrontal cortex was lower, than with suprathreshold motion. These results suggest that subthreshold irrelevant signals are not subject to effective inhibitory control.     

Structure of Fucoidan from Brown Seaweed Turbinaria ornata as Studied by Electrospray Ionization Mass Spectrometry (ESIMS) and Small Angle X-ray Scattering (SAXS) Techniques

The purpose of this study is to elucidate both the chemical and conformational structure of an unfractionated fucoidan extracted from brown seaweed Turbinaria ornata collected at Nha-trang bay, Vietnam. Electrospray ionization mass spectrometry (ESI-MS) was used for determining the chemical structure and small angle X-ray scattering (SAXS) provided conformational of the structure at the molecular level. The results showed that the fucoidan has a sulfate content of 25.6% and is mainly composed of fucose and galactose residues (Fuc:Gal ≈ 3:1). ESIMS analysis suggested that the fucoidan has a backbone of 3-linked α-l-Fucp residues with branches, →4)-Galp(1→ at C-4 of the fucan chain. Sulfate groups are attached mostly at C-2 and sometimes at C-4 of both fucose and galactose residues. A molecular model of the fucoidan was built based on obtained chemical structure and scattering curves estimated from molecular model and observed SAXS measurement were fitted. The results indicated that fucoidan under study has a rod-like bulky chain conformation.     

Muscle biochemical constituents of cultured amberjack <Emphasis Type="Italic">Seriola dumerili</Emphasis> and their influence on raw meat texture

The study was conducted to evaluate the meat texture, muscle proximate composition, lipid class composition, and collagen content of cultured amberjack and to compare these parameters with those of the yellowtail. Our results showed that the meat texture of cultured amberjack was tougher and had a lower degree of seasonality than that of cultured yellowtail. Muscle lipid and collagen content also varied in the two fish species over the study period. Meat breaking strength was not correlated with any of the muscle constituents, indicating that variations in the meat texture of cultured amberjack was not directly influenced by the changes in the muscle biochemical constituents.     

N applications that increase plant N during panicle development are highly effective in increasing spikelet number in rice

Efficient use of nitrogen fertilizer is critical in improving yield stability in rice. The objective of this study was to determine the effect of nitrogen (N) top-dressing on the number of total spikelet (fertile plus sterile) production and evaluate the effect among rice cultivars. We analyzed 136 sets of experimental data on growth and spikelet production for three lowland cultivars, grown under various regimes of N over 10 seasons at Kyoto, Ibaraki and Kanagawa, Japan. In each season, one to three of the lowland cultivars, Nipponbare (japonica), Koshihikari (japonica) and Takanari (indica), were studied. In 1986, 1995 and 1999-2001, the N regimes included basal application only, light basal and heavy top-dressing from the panicle initiation stage onward, heavy basal and heavy top-dressing from the spikelet formation stage onward, and no applications. In 2002 and 2005-2008, we set up experimental plots with varied time of N top-dressing, with or without N basal application. Takanari had the largest spikelet number averaged over all plots and was considered better efficient in spikelet production per applied N than the other cultivars. Although the trend is not clear, the effect of time of top-dressing on spikelet number was generally the greatest when N was top-dressed from 35 to 30 days before heading. The variation of observed spikelet number was analyzed with a linear regression of plant N 14 days before heading and by a model that estimates spikelet production accounting for plant N 14 days before heading and crop growth rate (CGR) during the 14-day period preceding heading. For the variation of spikelet number within each cultivar, the linear function model expressed the observed spikelet number than the two function model with R² 0.43** versus 0.13*-0.28** for the former and later models, respectively. When the results of all cultivars were combined, the two function model was much better for estimation of spikelet number than the linear function model (R² = 0.36** vs. 0.20*). This indicates that yearly and varietal variation of spikelet number was caused mainly by plant N status at the late spikelet differentiation stage. The varietal variation in spikelet production efficiency is explained by CGR during this 14-day period. We concluded that N applications that increase plant N 14 days before heading is highly effective in maximizing spikelet production among cultivars.