Prediction of the binding mode of imidacloprid and related compounds to house-fly head acetylcholine receptors using three-dimensional QSAR analysis

The binding activity of imidacloprid and related compounds to nicotinic acetylcholine receptors (nAChR) of house flies was measured by use of radioactive α-bungarotoxin as a ligand. Variations in the activity were examined three-dimensionally using comparative molecular field analysis (CoMFA). The CoMFA results suggest that one conformer among the four stable ones is active and provide support for one of the proposed binding models for this class of compound, in which the nitrogen atom of the pyridine ring and the nitrogen atom at the 1-position of the imidazolidine ring interact with the hydrogen-donating and electron-rich sites of nAChR, respectively. The CoMFA field map showed that the nitroimino moiety and a portion of the imidazolidine ring were mainly surrounded by a sterically and electrostatically sensitive region of nAChR. © 1998 Society of Chemical Industry     

Anethole inhibits growth of recently emerged multidrug resistant toxigenic Vibrio cholerae O1 El Tor variant strains in vitro

To search natural compounds having inhibitory effect on bacterial growth is important, particularly in view of growing multidrug resistant (MDR) strains of bacterial pathogens. Like other bacterial pathogens, MDR Vibrio cholerae, the causative agent of diarrheal disease cholera, is becoming a great concern. As an approach of searching new antimicrobial agents, here, we show that anethole, a well-studied natural component of sweet fennel and star anise seeds, could potentially inhibit the growth of MDR O1 El Tor biotype, the ongoing 7th cholera pandemic variant strains of toxigenic V. cholerae. The minimum inhibitory concentration (MIC) of anethole against diverse O1 El Tor biotype strains is evaluated as 200 µg/ml. Moreover, the effect of anethole is bactericidal and exerts rapid-killing action on V. cholerae cells. This study is the first report which demonstrates that anethole, purified from natural compound, is a potent inhibitor of growth of toxigenic V. cholerae. Our data suggest that anethole could be a potential antimicrobial drug candidate, particularly against MDR V. cholerae mediated infections.     

Evaluating the rumen‐protected lysine stability in forage‐based total mixed rations in vitro and determining the lysine Brix value

Three rumen‐protected lysine (RPL) products (AjiPro^®‐L, LysiPEARL^TM, and Feedtech Bypass Lysine^TM: A, B, and C, respectively) were tested for stability in two forage‐based total mixed rations (TMR1, 41.3% dry matter (DM), and TMR2, 49.5% DM) (experiment 1) and for Brix value (experiment 2). In experiment 1, each RPL product (2 g each) and TMR diet (200 g) were mixed and stored in plastic bags at 20°C for 0, 1, 3, 6, 12, 24, and 48 hr. In experiment 2, each RPL product (2 g) was dispensed into ion‐exchanged water (20 ml) and kept at 20°C for 0, 0.5, 1, 3, 6, 12, 24, and 48 hr. At each time point, free lysine (Lys) content and Brix values of extracts were measured, and Lys release (LR, %) was calculated. All RPL products LR% varied with varying diets DM and increased with increasing of time exposed to diets; it was highest in C, followed by B, and then A. Water LR% positively correlated with that from diets and with Brix values of Lys dissociated in water. Our results indicated that Lys dissociation from RPL products is affected by diet DM content. Brix value may be used as a potential marker for RPL protection efficacy.     

Discrete sandwich compounds of monolayer palladium sheets

Despite the abundance of "sandwich" complexes, in which two cyclic aromatic hydrocarbon ligands flank a metal center, this motif has not been extended to sheets of multiple metal atoms. We prepared and isolated two such compounds. In the first, three palladium centers form a planar triangular array, capped by chlorides, between two cycloheptatrienyl ligands. In the second, a pentapalladium sheet adopts an edge-sharing triangle-trapezoid skeleton between two naphthacene rings. The compounds were characterized by x-ray crystallography and nuclear magnetic resonance spectroscopy. The nature of bonding in the clusters was analyzed by quantum calculations.     

N2O and NO emissions from an Andisol field as influenced by pelleted poultry manure

Animal manures from intensive livestock operations can be pelleted to improve handlings and recyclings of embodied nutrients. The aim of this study was to evaluate the influence of pelleted poultry manure on N₂O and NO fluxes from an Andisol field. In autumn 2006 and summer 2007, poultry manure (PM), pelleted poultry manure (PP), and chemical fertilizer (CF) were applied at a rate of 120 kg N ha⁻¹ in each cultivation period to Komatsuna (Brassica rapa var. peruviridis). Nitrous oxide and NO fluxes were measured using an automated monitoring system. A soil incubation experiment was also conducted to determine the influence of intact and ground pelleted manure on N₂O, NO, and CO₂ production with a water-filled pore space (WFPS) of 30 or 50%. In the field measurements, N₂O emission rates from the organic fertilizer treatments were larger than that from the CF treatment, possibly because organic C stimulated denitrification. The highest N₂O flux was observed from the PP treatment after a rainfall following fertilization, and the cumulative emission rate (2.72 ± 0.22 kg N ha⁻¹ y⁻¹) was 3.9 and 7.1 times that from the PM and CF treatments, respectively. In contrast, NO emission rates were highest from the CF treatment. The NO/N₂O flux ratio indicated that nitrification was the dominant process for NO and N₂O production from the CF treatment. Cumulative N₂O emission rates from all treatments were generally higher during the wetter cultivation period (autumn 2006) than during the drier cultivation period (summer 2007). In contrast, NO emission rates were higher in the drier than in the wetter cultivation period. The incubation experiment results showed a synergistic effect of soil moisture and the pelleted manure form on N₂O emission rates. The intact pelleted manure with the 50% WFPS treatment produced the highest N₂O and CO₂ fluxes and resulted in the lowest soil NO₃⁻ content after the incubation. These results indicate that anaerobic conditions inside the pellets, caused by rainfall and heterotrophic microbial activities, led to denitrification, resulting in high N₂O fluxes. Controlling the timing of N application by avoiding wet conditions might be one mitigation option to reduce N₂O emission rates from the PP treatment in this study field.     

Generation and alteration of norlignans in a transition zone during the drying of a Cryptomeria japonica log

Sugi (Cryptomeria japonica D. Don) produces secondary metabolite norlignans in xylem. Several norlignans are involved in the coloration of heartwood and defense of sapwood against microbial invasion. Their biosynthetic process should be well understood so that their properties can be exploited to improve the quality and utility of C. japonica wood. Unfortunately, information on the norlignan biosynthesis is limited because norlignans are mainly synthesized in a particular season in the transition zone (TZ) along with the heartwood formation, and is difficult to study. Although the generation of two norlignans of C. japonica, agatharesinol and (E)-hinokiresinol, has been reported, systems for producing other norlignans are not yet known. To establish a novel norlignan generating system, we examined the changes occurring in norlignans in a TZ during the process of drying a C. japonica log. On the day of felling, the TZ contained agatharesinol and (E)-hinokiresinol, which increased until they reached a maximum on day 40 after felling. Sequirin-C appeared on day 40 and increased to day 70. The generation of sequirin-C in the TZ can be used to investigate the biosynthetic process of heartwood norlignans. This study describes for the first time the changes that occur in the composition of norlignan during the drying of the TZ.     

Sugar expressions on the vaginal epithelium in pregnant mice

Sugar expressions were examined on the epithelium of both the middle portion of the vagina and the vaginal portion of the cervical canal (CC) in pregnant mice to understand the pathogenesis of bacterial infection in the female reproductive organ by using a panel of lectins. As a result, N-acetylglucosamine was positive before pregnant day (P) 7 but negative after P10 and at diestrus on both the vagina and the CC. In addition, some differences in sugar expressions were seen between them. These results suggest that sugar expressions on the mucosal surface would change not only site-specifically but also time-dependently, and these sugar differences indicate the possibility of the alteration of the settled bacterial species on the vaginal mucosa in pregnancy.     

Seasonal changes in proteolytic enzymes of yellowtail Seriola quinqueradiata (Temminck & Schlegel; Carangidae) fed extruded diets containing different protein and energy levels

Seasonal variations in pepsin, trypsin and chymotrypsin activities and protein digestibility were studied in yellowtails (Seriola quinqueradiata) reared for 1 year with extruded diets containing different levels of protein. Trypsin and chymotrypsin storage levels in the digestive tissues of starved fish were affected by seasonal changes in water temperature. Actual digestion activities of trypsin and chymotrypsin were low at lower water temperatures, but pepsin activity in the stomach tissue was not affected by low temperatures. On the other hand, trypsin and chymotrypsin activities in the intestinal contents were higher during lower water temperature months, while pepsin activity in the stomach contents was low at lower water temperatures. Apparent protein digestibility (APD) did not differ among the dietary treatments in the higher water temperature months, while in colder months it was higher in fish fed diet 1 than in fish fed diets 2 and 3. The APD values reflected pepsin activity in the stomach contents in all sampling months. Therefore, lower APD in colder months seems to be attributed to lower protease activity in the gastric digesta, implying that enhanced pepsin secretion from the stomach tissue might improve protein digestibility and growth performance in yellowtails during winter.     

Characterization of the morphological and physiological traits of rice cultivars with adaptation to unflooded condition during early vegetative growth

This study aimed to characterize the physiological and morphological traits that are associated with adaptation to unflooded soil conditions in rice. Four indica rice cultivars (Puluik Arang, Badari Dhan, Shwe Nang Gyi, and Ratul), which were previously identified as highly or less adaptable to unflooded soil conditions, were grown under flooded and unflooded (soil water potential; －0.10 MPa) soil conditions. Water uptake was measured every day for three weeks, and then the leaf water potential, the stomatal conductance, the dry matter weight, shoot and root morphological traits were measured. Puluik Arang and Badari Dhan exhibited greater leaf area expansion and higher maintenance of root development under the unflooded condition than that by other cultivars. The leaf water potential and stomatal conductance of fully expanded highest leaf in Puluik Arang and Badari Dhan were not affected by unflooded soil regime. Leaf area and root morphological traits were significantly correlated with water uptake regardless of soil moisture regimes. These results suggested that Puluik Arang and Badari Dhan exhibited great water uptake capacity through physiological and morphological adaptation of shoot and root traits to unflooded condition, resulting in great biomass productivity under the condition.