Inhibition on human liver cytochrome P450 3A4 by constituents of fennel (Foeniculum vulgare): identification and characterization of a mechanism-based inactivator

Fennel, a seed of Foeniculum vulgare, is used as a culinary spice and traditional medicine. The methanolic extract of fennel showed a characteristic of mechanism-based inactivation on erythromycin N-demethylation mediated by human liver microsomal cytochrome P450 3A4 (CYP3A4). The present study was conducted to identify the fennel constituent having the inhibition. Thirteen compounds have been isolated from a methanol extract of fennel and tested for their inhibition on CYP3A4. Among them, 5-methoxypsoralen (5-MOP) showed the strongest inhibition with an IC50 value of 18.3 microM and a mixed type of inhibition. In addition, with the preincubation time of 20 min only 5-MOP showed preincubation time dependency; the IC50 value decreased from 18.3 microM with a preincubation time of 0 min to 4.6 microM with a preincubation time of 20 min. Further investigation on 5-MOP showed the characteristics of time-dependent inhibition, requirement of NADPH, lack of protecting effect of nucleophiles, and recovery of CYP3A4 activity by the competitive inhibitor. This result suggests that the inhibitory activity of CYP3A4 by 5-MOP was a mechanism-based inactivation. The kinetic parameter for mechanism-based inactivation was characterized by a KI value of 15.0 microM and a kinact value of 0.098 min(-1).     

Analysis of strigolactones,germination stimulants for striga and orobanche,by high-performance liquid chromatography/tandem mass spectrometry

A simple and rapid analytical method for strigolactones, germination stimulants for the root parasitic weeds witchweed (Striga spp.) and broomrape (Orobanche spp.), has been developed using high-performance liquid chromatography connected to tandem mass spectrometry (LC/MS/MS). The natural strigolactones (strigol, sorgolactone, orobanchol, and alectrol) were clearly separated and identified by LC/MS/MS. As low as 0.1 pg/microL of strigol and 0.5 pg/microL of sorgolactone could be quantified, whereas 1 pg/microL was needed for the quantification of orobanchol (S/N > 10). Using this method, it was found that red clover produces orobanchol and alectrol but not strigol. The roots of red clover seedlings were found to produce 13, 70, 58, and 65 pg of orobanchol/plant 1, 2, 3, and 4 weeks after germination, respectively.     

Use of tween 20 as a substrate for assay of lipase activity in soils

Abstract

A method for assaying the soil lipase activity is described. It involves the titrimetric estimation of the amount of lauric acid released by the lipase activity when the soil is incubated with Tween 20 in the presence of toluene at 30°C for 18 h under agitation. The method is simple and precise and incubation without agitation is also possible. The method has been applied to six different kinds of soils. The lipase activity in the cultivated soils ranged from 22.5 to 75.5 mmol min^?1 g^?1 of dried soil. The K _m value for Tween 20 was 1.8 × 10^?4 m. The optimum pH was approximately 7.5. The hydrolysis of liveen 20 in soil was inhibited by glycerol which was the essential moiety of glyceride. The inhibition by glycerol was found to be competitive. These results indicate that Tween 20 is a potential substrate for the assay of the glyceride hydrolytic activity in soils.     

A distributed hydro-environmental watershed model with three-zoned cell profiling

A cell-based distributed watershed model is developed which enables us to simulate the hydrological and hydraulic aspects of the watershed in a refined fashion. With three-zoned cell profiling, the model is composed of three sub-models; tank model for a surface water zone, soil moisture model for a surface soil zone, and unconfined shallow groundwater flow model for a subsurface zone. Inclusion of the soil moisture sub-model modified to reroute the infiltration, routed from the tank sub-model, into the return flow and the groundwater recharge features the model. The groundwater flow sub-model, numerically approximated by use of the finite volume method and the implicit time-marching scheme, considers a network of on-farm drainage canals as internal boundaries, which is an essential need for modeling the watershed including farmlands. Cascade-linking of the three sub-models in a cell and assembling of all the cells over the entire watershed domain provides the global equations system to be solved. Applicability of the model is demonstrated with its practical application to a real watershed in that paddy and upland crop fields take great part of the land-use practice. It is then indicated in a quantified manner that rice farming significantly contribute as a major groundwater recharger in an irrigation period to fostering and conservation of regional water resources. Along with appropriately profiling a cell, the model is so versatile and tough that it can be applied without difficulty to a watershed of diverse terrains and land-uses and the computations can stably be carried out. It is thus concluded that the model presently developed could be a powerful “watershed simulator” to investigate and assess the time-varying hydro-environmental properties of a watershed while separating and integrating the hydrological and hydraulic components of particular importance.     

Effects of photoperiod on gonadotropin-releasing hormone levels in the brain and pituitary of underyearling male barfin flounder

ABSTRACT:   A pleuronectiform fish, the barfin flounder Verasper moseri , expresses three gonadotropin-releasing hormone (GnRH) forms in the brain: salmon GnRH (sGnRH), chicken GnRH-II (cGnRH-II) and seabream GnRH (sbGnRH). To clarify the effects of photoperiod on GnRH systems, changes in brain and pituitary GnRH peptide levels were examined using time-resolved fluoroimmunoassays. In experiment 1, 5-month-old male barfin flounder (mean total length 9.0 cm, body weight 11.0 g) were divided into short (8:16 h light : dark [L:D] cycle; lights on 08.00–16.00 hours) and long photoperiod (16:8 h L:D cycle; lights on 04.00–20.00 hours) groups in mid September and maintained until November under natural water temperature (19.3–15.2°C). Brain sGnRH concentrations were significantly higher in the 16:8 h L:D group than in the 8:16 h L:D group, whereas no significant differences were observed in total length, body weight, plasma testosterone concentration, brain cGnRH-II concentration and pituitary sbGnRH content. In experiment 2, 7-month-old male barfin flounder (mean total length 16.5 cm, body weight 76.8 g) were divided into short and long photoperiod groups in mid December and maintained until February under natural water temperature (12.5–6.6°C). Total length, body weight and condition factor were significantly greater in the 16:8 h L:D group than in the 8:16 h L:D group, whereas no significant differences were observed in plasma testosterone concentration and GnRH levels in the brain and pituitary. These results indicate that levels of sGnRH in barfin flounder are influenced by photoperiodic treatment dependent on water temperature and/or body size.     

Surface deterioration of wood-flour polypropylene composites by weathering trials

The market for wood-fiber plastic composites (WPCs) is expanding rapidly in many countries including Japan, where WPCs are mainly used for exterior products. In such applications, WPCs undergo undesirable color change, chalking, and shrinkage and swelling, and accordingly there is a need to better understand the mechanisms responsible for the weathering of WPC and develop methods of improving their weathering resistance. In this study, weatherability of WPC was assessed by natural and accelerated weathering trials. Discoloration (whitening) of WPC during exposure was caused by degradation of both wood and plastic. Darker color pigments as additives improved the color stability of WPC; however, chalking on the surfaces still occurred. The color stability of WPC was improved by application of exterior coatings. Preweathering of WPC (before coatings were applied) increased the absorption of coatings by the WPC and had a positive effect on the color stability and prevented chalking of the composites. Parts of this study were presented at the IUFRO XXII World Congress Meeting, Brisbane, August 2005 and the IAWPS 2005, Yokohama, November 2005     

Spatial distribution pattern of attack of the oak borer,Platypus quercivorus (Murayama) (Coleoptera: Platypodidae), and scolytid ambrosia beetles (Coleoptera: Scolytidae) on fresh logs

The spatial distribution patterns of the attack on fresh logs ofPasania edulis was studied for the oak borer,Platypus quercivorus (Murayama), and two species of Scolytid ambrosia beetles,Xylosandrus crassiusculus (Motschulsky) andXyleborus attenuatus Blanford, in 1994 and 1995. On the logs where onlyP. quercivorus attacked, the entry holes were distributed uniformly when attack intensity was low. However, the distribution pattern became more aggregated with the increase in attack intensity. On logs where bothP. quercivorus and the two Scolytid species attacked, there was a negative association between the spatial distribution of the entry holes ofP. quercivorus and that of scolytids. Simultaneous attack of two scolytids also increased the degree of aggregation of the entry holes ofP. quercivorus. The entry holes of scolytids were distributed in groups irrespective of the attack intensity of scolytids andP. quercivorus. These results suggest an asymmetrical interspecific relationship betweenP. quercivorus and scolytids. Concentration of the entry holes ofP. quercivorus in a small area may cause a considerable decline in the reproductive success in the galleries constructed there.     

Effect of Moderate Drought-Stress on Flowering Time of Interspecific Hybrid Progenies (Oryza sativa L. × Oryza glaberrima Steud.)

Journal of Crop Science and Biotechnology - We examined the effects of drought stress on flowering time, grain yield, and agronomic traits using 10 upland-adapted rice genotypes, i.e. eight...     

Hemorrhagic necrotizing splenitis in a slaughter pig infected with Arcanobacterium species

A 6-month-old barrow presented with lethargy, inappetence and dysstasia. At necropsy, multiple coalescing hemorrhagic foci were detected in the margins of the spleen. Gram-positive bacilli were isolated from the spleen, kidney, muscle and liver. Comparative 16S rDNA gene sequencing analysis of the isolates (TO16177) revealed that they would be the same species of unpublished Arcanobacterium species strain HJ57-14E (accession no. gi 18873551) (99.7% similarity based on a comparison of 675 bp). Histologic examination of the splenic tissue sections revealed extensive necrosis and inflammation, and gram-positive bacilli were discernible. Multifocal necrosis was also detected in the liver. Immunohistochemically, the isolates were cross-reacted with polyclonal antibodies against Arcanobacterium pyogenes and Actinomyces naeslundii, and the reaction was strong for the latter. Similar reactions were found in the suppurative lesions of the tonsil, and occasionally in the spleen and lymph nodes. The present results indicate that the unpublished Arcanobacterium species induced multiple organ failure accompanied by acute hemorrhagic necrotizing splenitis in this growing-finishing pig.