Human buprenorphine N-dealkylation is catalyzed by cytochrome P450 3A4

Buprenorphine (BN) is a thebaine derivative with analgesic properties. To identify and characterize the cytochrome P450 (CYP) enzyme(s) involved in BN N-dealkylation, in vitro studies using human liver microsomes and recombinant human CYP enzymes were performed. Norbuprenorphine formation from BN was measured by a simple HPLC-UV assay method, without extraction. The BN N-dealkylation activities in 10 human liver microsomal preparations were strongly correlated with microsomal CYP3A-specific metabolic reactions, i.e. triazolam 1'-hydroxylation (r = 0.954), midazolam 1'-hydroxylation (r = 0.928), and testosterone 6beta-hydroxylation (r = 0.897). Among the eight recombinant CYP enzymes studied (CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4), only CYP3A4 could catalyze BN N-dealkylation. The apparent KM value for recombinant CYP3A4 was similar to that for human liver microsomes (23.7 vs. 39.3 +/- 9.2 microM). The demonstration of BN N-dealkylation by recombinant CYP3A4 and the agreement in the affinities (apparent KM values) of human liver microsomes and recombinant CYP3A4 provide the most supportive evidence for BN N-dealkylation being catalyzed by CYP3A4.     

Efficacy of microwave coagulation therapy (MCT) in patients with liver tumors

We evaluated the efficacy of microwave coagulation therapy (MCT) in 84 patients with hepatocellular carcinomas (HCC) and 40 with metastatic liver tumors (MLT). The response rates calculated with diagnostic imaging were 92% in HCC and 80% in MLT. The regional recurrence rates were relatively higher in patients with MLT (33%) than in HCC (14%). The average surgical margin in operative MCT group was 11 mm. The cumulative survival rates at three and five years were 63% and 38% in HCC and 43% and 33% in MLT, respectively. The complications were similarly encountered in HCC and MLT (12% versus 13%). When these observations are taken together, MCT is a radical and safe locoregional therapy which can keep an adequate surgical margin and assure long survival.     

Short-term algal toxicity test based on phosphate uptake

In order to develop a short-term algal toxicity test, the growth of and the phosphate uptake by the green alga Selenastrum capricornutum during batch culture were observed. In the control medium, S. capricornutum took up phosphate earlier than it grew. It was also observed that the phosphate uptake was inhibited by the presence of a toxicant. From these results, phosphate uptake was considered as one of the useful effect parameters for a short-term algal toxicity test. As the removal rate of phosphate from the medium is a function of the amount of algal cell initially inoculated, the test period is variable. The relationship between the amount of inoculation and phosphate uptake was examined and the test conditions suitable for a 3-h toxicity test were established as one example. According to this test procedure, the inhibitory effect of some toxicants on the phosphate uptake was determined. For comparison, a conventional algal assay based on algal growth was also performed. The EC50s for both tests were close. This indicated that the algal toxicity test method proposed in this paper would be useful for the uses where rapidity is required.     

Removal of extracellular materials by HCL-tween treatment

Glutaraldehyde-fixed tissues were treated with HCl and tween 20 to remove such extracellular materials as collagen fibers and basal laminae. In the HCl-treatment the collagen fibers were digested, while in the tween-treatment the basal laminae were removed. By this method the basal interdigitations of cells of the proximal tubule and the pericytes on th capillary wall were clearly demonstrable by scanning electron microscopy (SEM).     

Preparation and phase transition of Gd4(Al1 − xGax)2O9 solid solutions

The solid-solution compounds of Gd₄(Al_{1 – x} Ga _x )₂O₉ (x = 0.0–1.0) were prepared at 1600°C for 5 h in air. The unit cell volume of the compounds increased from 0.853 to 0.878 nm³ with x. Phase transitions having a temperature hysteresis were observed from 1100° to 1400°C by calorimetry and dilatometry. The transition temperature increased with x. The volume of the high-temperature phase was 0.5% smaller than that of the low-temperature phase at the transition temperature. The volume changes were independent of x. The hysteresis width observed by the dilatometry was about 300°C for the Gd₄Al₂O₉ ceramics (grain size: about 1 m) and decreased to 50°C for the Gd₄(Al_0.2Ga_0.8)₂O₉ ceramics (grain size: over 10 m). Gd₄Ga₂O₉ was unstable at low temperature and decomposed to Gd₃GaO₆ and Gd₃Ga₅O₁₂ during the thermal analyses.     

Proportion of aflatoxin B1 contaminated kernels and its concentration in imported peanut samples

Moldy and split peanut kernels were separated from peanuts exported from Brazil, Sudan, India and Taiwan by visual inspection. The remaining peanuts from Brazil, Sudan and India were roasted lightly and the skins were removed. Stained peanuts were separated from the others. Aflatoxin was detected in moldy and stained peanuts. There was a positive correlation between % of aflatoxin-contaminated peanut kernels and aflatoxin B1 concentration in whole samples. Aflatoxin concentration of moldy peanuts was higher than that of stained peanut kernels.     

Incorporation of Dust Particles into a Growing Film During Silicon Dioxide Deposition from a TEOS/O2 Plasma

The effects of gas flow rate on particle formation and film deposition during the preparation of silica thin film using a TEOS/O₂ plasma were investigated. Particle formation and growth are suppressed with increasing gas flow rates. The film deposition rate increases with increasing gas flow rate, reaches a maximum value, and eventually decreases again. However, the uniformity of the film tends to degrade at high gas flow rates. At a high gas flow rate, some particles trapped in the sheath near the grounded electrode pass through the sheath to reach the substrate and are then embedded in the growing film. A self-consistent sheath model combined with particle force balance based on charge fluctuation was developed to explain these experimental findings qualitatively. The model reveals that charge fluctuation is a key factor for the particle to overcome the potential barrier of the negatively charged particles to pass through the sheath, eventually reaching the substrate. The model further shows that the probability of a particle being deposited on the substrate is higher for increased gas flow rates, which correctly predicts the experimentally observed trend.     

Hydrocracking of diphenylmethane and tetralin over bifunctional NiW sulfide catalysts supported on three kinds of zeolites

Hydrocracking reactions of diphenylmethane and tetralin were carried out over three kinds of zeolites with or without NiW sulfide to discuss the roles of catalytic bifunctionality in two types of hydrocracking reactions. It was found that strong acid sites were not needed for the hydrocracking of diphenylmethane, while the conversion of tetralin required relatively strong acid sites. Ultra-stable Y zeolite with strong acidity exhibited high hydrocracking activity for both reactions. In contrast, mordenite catalysts did not show high activity for either hydrocracking, though isomerization of tetralin and excess hydrocracking to gaseous products proceeded. The superior performances of ultra-stable Y zeolite in the tetralin hydrocracking were suggested to be related to the hydrogen transfer ability. In most cases, the loading of NiW sulfide enhanced catalytic activity. In the diphenylmethane hydrocracking, the role of NiW sulfide was found to supply active hydrogen to the hydrocracking active sites on zeolite and to prevent polymerization of benzyl cations. In the tetralin hydrocracking, the dehydrogenated products from tetralin were re-hydrogenated over NiW sulfide.     

Observations of bound Tween80 surfactant molecules on single-walled carbon nanotubes in an aqueous solution

The slow diffusion of Tween80 surfactant molecules in a single-walled carbon nanotube (SWCNT) aqueous dispersion was directly observed using the pulsed field gradient nuclear magnetic resonance method. The slow diffusion of Tween80 molecules was attributed to the strongly adsorbed molecules on the SWCNTs in the aqueous dispersion. The amount of bound Tween80 molecules was estimated to be approximately 12% of the total amount of Tween80 molecules, contributing to the stability of the SWCNT aqueous dispersion. Using dynamic light scattering and total organic carbon measurements, this SWCNT/Tween80 aqueous dispersion was found to be very stable for at least 3 weeks. The observed zeta potentials of this SWCNT dispersion are between −10 and 0 mV, indicating that the stability of the SWCNTs in the Tween80 solution was maintained by steric interactions between the small amount of adsorbed Tween80 molecules on the SWCNTs, while the effect of electrostatic interactions between adsorbed Tween80 was minimal. This proposed method to investigate the amount of bound Tween80 molecules on SWCNTs has potential benefits in the field of the production of functional materials and nano-toxicity assessments.