Synthesis and insecticidal/acaricidal activity of novel 3‐(2,4,6‐trisubstituted phenyl)uracil derivatives

A series of novel 3‐(2,4,6‐trisubstituted phenyl)uracil derivatives has been synthesised and assayed for insecticidal/acaricidal activity. The assay indicated certain requirements for optimal insecticidal activity, which can be summarised as follows: (a) the substituents on the phenyl ring should possess hydrophobicity and electron‐withdrawing properties, and the sum of their volumes determines the level of activity; (b) the substituent at the 6‐position on the uracil ring should also possess electron‐withdrawing properties and hydrophobicity, together with the correct volume; (c) the 1‐position on the uracil ring should be unsubstituted for activity against Nephotettix cincticeps and Epilachna vigintioctopunctata, but substituents with length C3 to C4 may be optimal for activity against Tetranychus urticae; (d) certain substituents at the 5‐position of the uracil ring give activity against E vigintioctopunctata and T urticae, but not against N cincticeps; (e) a thiocarbonyl group at the 2‐position of the uracil ring is less effective than a carbonyl group. Of the compounds assayed, 3‐(2,6‐dichloro‐4‐trifluoromethylphenyl)‐6‐trifluoromethyluracil showed high activity against all the species assayed. © 2000 Society of Chemical Industry     

Oral administration of lactoferrin inhibits inflammation and nociception in rat adjuvant-induced arthritis

Lactoferrin (LF) is a ubiquitous protein which exists in milk, plasma, synovial fluids, cerebrospinal fluid and other biological fluids. LF is also well known as a natural immunomodulator. Recently, we found that bovine milk-derived LF (BLF) produced micro-opioid receptor-mediated analgesia. In this study, we examined whether oral administration of BLF causes anti-nociceptive and anti-inflammatory effects, and also whether it modulates LPS-induced TNF-alpha and IL-10 production in rat model of rheumatoid arthritis (RA), rat adjuvant arthritis. BLF was administrated once daily, starting 3 hr before (preventive experiment) or 19 days after (therapeutic experiment) adjuvant injection. In both experiments, BLF suppressed the development of arthritis and the hyperalgesia in the adjuvant-injected paw. The single-administered BLF produced a dose-dependent analgesia, which was reversed by naloxone, in the adjuvant arthritis rats. Both repeated and single administration of BLF suppressed TNF-alpha production and increased IL-10 production in the LPS-stimulated adjuvant arthritis rats. These results suggest that orally administered BLF has both preventive and therapeutic effects on the development of adjuvant-induced inflammation and pain. Moreover, the immunomodulatory properties of BLF, such as down-regulation of TNF-alpha and up-regulation of IL-10, could be beneficial in the treatment of RA. Thus, we concluded that LF can be safely used as a natural drug for RA patients suffering from joint pain.     

Changes in peripheral lymphocyte subsets in the type 1 diabetic dogs treated with insulin injections

Plasma metabolites and peripheral lymphocyte subsets were measured in ten diabetic and ten control dogs to investigate their significances as indicators to evaluate immune states in the diabetic dogs. Diabetic dogs were treated with insulin injections, however their plasma glucose and fructosamine concentrations were significantly higher than those of the controls. There were no significant differences in counts of total white blood cells (WBC) and lymphocyte CD8(+) cells (cytotoxic T cells) between the control and the diabetic dogs. In the diabetic dogs, the counts of CD3(+) (T cells), CD4(+) (Helper T cells) and CD21(+) (B cells) cells and the peripheral lymphocytes CD4/CD8 ratio were significantly lower than those in the control dogs. We confirmed abnormality of lymphocyte subsets in insulin treated diabetic dogs and it may relate to depression of immunocompetence and high susceptibility to common infectious diseases.     

Biochemical properties of the cell wall in the Arabidopsis mutant bor1‐1 in relation to boron nutrition

We examined concentrations of boron (B) and dimerization of rhamnogalacturonan II (RG‐II), a B‐binding polysaccharide, in the cell wall of a low‐B sensitive mutant of Arabidopsis thaliana, bor1‐1, to investigate possible effects of the bor1‐1 mutation on the biochemical form of pectins in the cell wall. In the bor1‐1 mutant, B concentrations in the cell wall from shoots were lower than those in the wild type at low B supply, whereas they were similar at sufficient B supply. The amount of B present as borate ester of the RG‐II dimer (dRG‐II‐B) in the bor1‐1 mutant was lower than that in the wild type at low B supply. In the wild type, about 90 % of RG‐II was present as dRG‐II‐B, both, at low and sufficient B supply. In the bor1‐1 mutant, about 60 % of RG‐II was in its monomeric form (mRG‐II) at low B supply, whereas more than 85 % of it was present as dRG‐II‐B at sufficient B supply. However, similar as the wild type, mRG‐II derived from the bor1‐1 mutant was able to form dRG‐II‐B in vitro in the presence of borate and lead. Sugar composition of cell wall fractions was similar in both genotypes. These results suggest that the polysaccharide composition in the cell wall was not strongly affected by the bor1‐1 mutation. The observed difference in dimerization of RG‐II at low B supply is most likely due to a reduced B concentration in the shoots of the bor1‐1 mutant.     

Purification and characterization of lipoxygenase from Pleurotus ostreatus

Lipoxygenase was purified homogeneously from cups of Pleurotus ostreatus by Sephacryl S-400 HR gel filtration, Dyematrex Green A affinity, and DEAE-Toyopearl 650M ion-exchange chromatographies. The molecular weight of the enzyme was estimated to be 67,000 by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and 66,000 by gel filtration; the isoelectric point was pH 5.1. The optimum pH and temperature of the enzymatic activity were 8.0 and 25 degrees C, respectively. The enzyme contained non-heme iron, and a thiol group seemed to be involved in its activity. The K(m), V(max), and k(cat) values of the enzyme for linoleic acid were 0.13 mM, 23.4 micromol.min(-1).mg(-1), and 25.7 s(-1), respectively. The enzyme showed high specificity toward linoleic acid. When linoleic acid was incubated with the enzyme, 13-hydroperoxy-9Z,11E-octadecadienoic acid was found to be the main oxidative product.     

高温高压蒸汽条件下木材的拉伸应力松弛

为进一步探讨木材在高温高压蒸汽干燥过程中的应力释放机理,该研究以日本柳杉木材为研究对象,利用新开发的耐热、耐压应力传感器和专用夹具,对高温高压蒸汽条件下木材的拉伸应力松弛特性进行了较为详细、全面的系统研究.结果表明:温度条件对木材应力松弛的影响远比应变水平的影响显著,随着温度的增加、木材应力松弛急剧增大,残余应力迅速下降;木材应力的松弛除了受温度的影响外,受环境相对湿度的影响显著.无论木材的径向还是弦向,其拉伸应力松弛过程中的残余应力和木材干燥过程中的最大收缩应力随温度变化的关系十分吻合.该结果充分证明了木材在高温高压过热蒸汽干燥过程中的收缩应力 显著降低,是由于收缩变形而引起的收缩应力在长时间处于拉伸状态下应力释放所致.      

Absorption of 6-O-caffeoylsophorose and its metabolites in Sprague-Dawley rats detected by electrochemical detector-high-performance liquid chromatography and electrospray ionization-time-of-flight-mass spectrometry methods

Absorption and metabolism of a natural compound, 6-O-caffeoylsophorose (CS) from acylated anthocyanins in a red vinegar fermented with purple sweet potato, were clarified. The absorption of CS and conjugated CS in blood from orally administrated Sprague-Dawley rats at a dose of 400 mg/kg was investigated by electrochemical detection-high performance liquid chromatography. As a result, CS was successfully detected in rat plasma (AUC(0-6h), 108.6 ± 8.1 nmol h/mL) and was found to be an intact absorbable polyphenol. In addition, half of the absorbed CS was detected as its conjugates (AUC(0-6h), 50.7 ± 5.7 nmol h/mL) as well as caffeic and ferulic acids from CS. By a time-of-flight-mass spectrometric analysis of CS-administered plasma sample, glucuronide and methylated conjugates of CS were identified, in addition to glucuronide, methylated, or sulfate conjugates of caffeic and ferulic acids. Consequently, CS was absorbed in intact form into rat blood and partly degraded to caffeic and ferulic acids or metabolized by glucuronidation, methylation, or sulfatation.     

Optimum digestible protein and energy levels and ratio for greater amberjack Seriola dumerili (Risso) fingerling

A study was conducted to determine optimum dietary digestible protein (DP) and digestible energy (DE) levels and DP DE⁻¹ ratio for growth of greater amberjack Seriola dumerili fingerlings. A 3 × 3 factorial design with duplication was used in this study. Nine experimental diets were formulated to contain three levels of crude protein (CP; 420, 470 and 530 g kg⁻¹) and three levels of crude lipid (CL; 130, 180 and 230 g kg⁻¹). Nine groups of fingerling (initial weight 51.8 g) were fed each experimental diet for 40 days. Final body weight, feed efficiency, specific growth rate and energy efficiency were significantly affected by dietary protein and lipid level. These parameters tended to improve with increasing dietary protein level. Conversely, an increase of lipid level negatively affected these parameters. High growth rate and feed efficiency were obtained from fish fed the diet containing 393 g kg⁻¹ DP and 14.2 MJ kg⁻¹ DE (27.7 g MJ⁻¹ DP DE⁻¹). The high DP DE⁻¹ (27.7 g MJ⁻¹) indicates that greater amberjack fingerling are highly dependent on dietary protein as an energy source.     

Association between bacterial community structures and mortality of fish larvae in intensive rearing systems

Bacterial community structures were analyzed in water used for rearing fish larvae by fluorescence in situ hybridization. In Experiment 1, red sea bream Pagrus major larvae were reared in two commercial seed production tanks. The survival rate in Tank 1 was higher than in Tank 2, even though phytoplankton, Nannochloropsis sp., was added to both tanks. In Tank 2, γ-proteobacteria became dominant (∼70% of total bacteria) on day 13, there after heavy larval mortalities occurred. In Tank 1, however, α-proteobacteria and the Cytophaga-Flavobacterium cluster were predominant from day − 1 until day 13; no significant mortality was recorded. In Experiment 2, marble goby Oxyeleotris marmoratus larvae were cultured with or without Nannochloropsis sp. At the end of the experiment, larval survival rates in aquaria with Nannochloropsis sp. were significantly (P <0.05) higher than those without. In rearing water without Nannochloropsis sp., γ-proteobacteria increased during rearing. In rearing water with Nannochloropsis sp., α-prote obacteria and the Cytophaga-Flavobacterium cluster were predominant at the beginning of the experiments and the relative abundance of γ-proteobacteria was maintained at a lower level throughout the experiments. The predominance of α-proteobacteria and the Cytophaga-Flavobacterium cluster appears to be a good indicator of successful larval production.     

A mesoscale iron enrichment in the western subarctic Pacific induces a large centric diatom bloom

We have performed an in situ test of the iron limitation hypothesis in the subarctic North Pacific Ocean. A single enrichment of dissolved iron caused a large increase in phytoplankton standing stock and decreases in macronutrients and dissolved carbon dioxide. The dominant phytoplankton species shifted after the iron addition from pennate diatoms to a centric diatom, Chaetoceros debilis, that showed a very high growth rate, 2.6 doublings per day. We conclude that the bioavailability of iron regulates the magnitude of the phytoplankton biomass and the key phytoplankton species that determine the biogeochemical sensitivity to iron supply of high-nitrate, low-chlorophyll waters.