Roles of the jejunum and ileum in the first-pass effect as absorptive barriers for orally administered tacrolimus.

Background: The immunosuppressant tacrolimus shows poor and variable bioavailability following oral administration in clinical use. Recently, the hepatic and intestinal metabolisms, or first-pass effect, of tacrolimus have been suggested to be responsible for its bioavailability. In the present study, we investigated the respective contribution of the jejunum and ileum to the first-pass effect of tacrolimus in rats.

Inhibitory effect of loxiglumide (CR 1505), a cholecystokinin receptor antagonist, on N-nitrosobis(2-oxopropyl) amine-induced biliary carcinogenesis in Syrian hamsters.

We evaluated the cholecystokinin (CCK) receptor antagonist loxiglumide (CR1505) for a possible inhibitory effect on biliary carcinogenesis in a hamster model. Experimental group I underwent cholecystoduodenostomy and ligation of the distal end of the common bile duct, after which the animals were injected with N-nitrosobis(2-oxopropyl)amine (BOP) alone. Group II, after the same surgical procedure as in group I, were given injections of BOP and then given loxiglumide in their diet.

Dioxin detection based on immunoassay using a polyclonal antibody against octa-chlorinated dibenzo-p-dioxin (OCDD).

An enzyme-linked immunosorbent assay (ELISA) using a polyclonal antibody against octa-chlorinated dibenzo-p-dioxin (OCDD) is presented. This method is based on a competitive reaction between OCDD and OCDD-HRP (horseradish peroxidase) conjugate against the antibody, whereby OCDD-HRP is detected colorimetrically at 450 nm. The detection limit of OCDD was 0.

Epithelial pigment slide in contact lens wearers: a possible marker for contact lens-associated stress on corneal epithelium.

Purpose: To compare the incidence of epithelial pigment slide among wearers of various types of contact lenses.

Methods: Prospectively, we studied 432 eyes of 432 patients. The patients were separated into 6 groups: hard contact lens (HCL) wearers (n = 166), conventional soft contact lens (CSCL) wearers (n = 30), extended disposable lens (EDCL) wearers (n = 46), frequent replacement SCL (FRCL) wearers (n = 60), daily disposable SCL (DDCL) wearers (n = 65), and normal controls (n = 65).

Role of loop D of the alpha7 nicotinic acetylcholine receptor in its interaction with the insecticide imidacloprid and related neonicotinoids.

1. The nitroguanidine insecticide imidacloprid along with a second generation of related compounds including nitenpyram, all nicotinic acetylcholine (ACh) receptor ligands, are used increasingly in many countries. Site-directed mutagenesis and heterologous expression in Xenopus laevis oocytes have been deployed to investigate mutants (G189D and G189E) of the chicken alpha7 homomer-forming nicotinic receptor subunit which are predicted to enhance the negative charge at the negative subsite (loop D) of the ACh binding site.

Induction of choline acetyltransferase activity in cholinergic neurons by stolonidiol: structure-activity relationship.

The effect of stolonidiol (1), a bioactive marine diterpenoid from the Japanese soft coral Clavularia sp., on choline acetyltransferase (ChAT) activity was examined using cultured cholinergic neurons. Stolonidiol (1) showed potent ChAT inducible activity in primary cultured basal forebrain cells and clonal septal SN49 cells, suggesting that it may act as a potent neurotrophic factor-like agent on the cholinergic nervous system.

Kanji lexicality effect in partial repetition priming: the relationship between Kanji word and Kanji character processing.

Two experiments are described using a partial repetition priming paradigm. The prime type was whether a kanji character is used as a word by itself (word type) or not (nonword type). This property is called kanji lexicality.

[Migration-of Kanji characters and their radicals in rapid serial visual presentation].

We investigated the spatio-temporal characteristics of visual attention. In rapid serial visual presentation (RSVP) tasks using Kanji characters, we found temporal migration of characters (Experiment 1) and radicals (Experiment 2). In Experiment 1, the migration was more frequent for the word condition than for the pseudoword condition.

Effects of intestinal and hepatic metabolism on the bioavailability of tacrolimus in rats.

Purpose: Tacrolimus, an immunosuppressive agent, has poor and variable bioavailability following oral administration in clinical use. We investigated the contribution of intestinal metabolism to the first pass effect of tacrolimus in rats.

Methods: Tacrolimus was administered intravenously, intraportally or intraintestinally to rats.

[Temporal illusory conjunction in RSVP tasks: effects of target complexity].

We examined the complexity effects of stimuli and tasks on temporal illusory conjunction in the Rapid Serial Visual Presentation (RSVP) tasks. Subjects were asked to report the partially defined target. We found that error patterns greatly depended on the visual complexity of stimuli.

[A case of anti-basement membrane (BM) mediated disease presenting renal and pulmonary symptoms by divergent timing].

A case of 49-year-old man with anti-GBM antibody and who manifested pulmonary and renal symptoms at divergent times. Thirty-six years previously, renal disease with unneglectable degree of proteinuria was noticed. One month before admission, he was found by chance to have elevated serum creatine (Scr); 3.

Cyclic peptides from higher plants. 24.1 yunnanin C, a novel cyclic heptapeptide from Stellaria yunnanensis.

A novel cytotoxic cyclic heptapeptide, yunnanin C (1), was isolated from the roots of Stellaria yunnanensis. The structure of 1, cyclo(-Gly-Ile-Gly-Phe-Tyr-Ser-Pro-), was elucidated from spectroscopic evidence and by chemical degradation.

Sequence-specific DNA binding by covalently constrained peptide dimers of the basic leucine zipper protein GCN4.

DNA binding of covalently bonded peptide dimers was studied by using enantiomeric and C2-symmetric templates as a dimerization module. Amino acid sequence of the peptide is derived from that of DNA contact region of the basic leucine zipper protein GCN4. These peptide dimers were designed to possess different constraints with respect to the orientation of two peptides.

Polymorphism of immunoglobulin heavy chain switch region gene in children with severe IgA nephropathy.

We examined restriction fragment length polymorphisms (RFLPs) of the switch region genes of the IgM (S mu) and IgA1 (S alpha 1) heavy chain in 78 Japanese children with IgA nephropathy and 88 normal Japanese controls. Genomic DNA obtained from patients and controls was digested with the restriction endonuclease SacI, transferred to nylon membrane using Southern blot procedure, and hybridized with a DNA probe homologous to S mu. This probe detects RFLPs at the S mu and S alpha 1 loci by enhanced chemiluminescence.

[The ameliorative effect of probucol on adriamycin (ADR) induced nephrotic rats].

This paper reports the ameliorative effect of Probucol (Pb) on ADR-induced nephrotic rats. Male Wistar rats underwent unilateral nephrectomy followed by one-week subsequent intravenous injection of 4.0 mg/kg of ADR.

IgG-associated primary glomerulonephritis in children.

Ten children with IgG-associated primary diffuse mesangial proliferative glomerulonephritis are presented. All cases showed diffuse global IgG deposits in the mesangium. IgG was the sole immunoglobulin deposited in the mesangium in 8 patients and was the predominant immunoglobulin in 2.

Charge isomers of urinary bikunin (trypsin inhibitor).

It was observed that the purified urinary bikunin (trypsin inhibitor) consisted of four major isomers with different electric charges which could be separated by HPLC using a Mono Q column. These isomers revealed the same antitrypsin activity and did not show any differences in the apparent molecular weight by SDS-PAGE, amino-acid composition, N-terminal amino-acid sequence (1-40) and C-terminal amino acid (Leu). The contents of sialic acid and uronic acid were also identical among these isomers.

Intra-GBM site of the functional filtration barrier for endogenous proteins in rats.

The passage of various endogenous proteins [such as albumin, transferrin, immunoglobulin G (IgG), and immunoglobulin M (IgM)] across GBM was studied in vivo in normal Munich-Wistar rats. Glomeruli were fixed by three different methods: in situ drip-fixation, perfusion- and immersion-fixation; then they were processed for immunogold electron microscopy. The most reproducible results were obtained with in situ drip-fixation.

Pharmacokinetics of meropenem in patients with various degrees of renal function, including patients with end-stage renal disease.

The pharmacokinetics of meropenem were studied after intravenous infusion in 13 patients grouped according to the impairment of their renal function. Creatinine clearance (CLCR) was greater than 50, 50 to 30, and less than 30 ml/min in groups I, II, and III, respectively. Two other groups, groups IV and V, each comprising four patients with end-stage renal disease (CLCR, < 5 ml/min), were also studied, the former on days off of hemodialysis and the latter on days of hemodialysis.

32P-postlabeling analysis of DNA adducts in rats during estrogen-induced hepatocarcinogenesis and effect of tamoxifen on DNA adduct level.

DNA adduct formation in the liver, pancreas, kidneys and uterus in ethynylestradiol (EE)-induced carcinogenesis and the effect of tamoxifen (TAM) on DNA adduct formation were evaluated in female Wistar JCL rats using the 32P-postlabeling method. Hyperplastic nodules were noted in the liver of all rats 4 months after the first oral administration of 0.075 mg of EE, and hepatocellular carcinoma was detected in 8.

Sequence-specific DNA recognition by basic peptides.

A chiral template with C2 symmetry has been used for modeling a dimeric interface of DNA binding protein. An oligopeptide derived from the basic region of MyoD, a recently described "helix-loop-helix" class of DNA binding protein, has been tethered to the template. Among the four models which differ in chirality and polarity with respect to the arrangement of two subunits, only one dimer model with right-handed and C-terminus to C-terminus arrangement of the peptide subunits binds DNA containing native MyoD binding sequence.