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Biomedical subjects

M Kojima

Publications and source records attributed to M Kojima.

At least 595 records · Page 33Linked to original sources

Enhancing effect of combining two pyrrolidone vehicles on transdermal drug delivery.

The enhancing effect of combining 1-methyl-2-pyrrolidone (MP) and 1-lauryl-2-pyrrolidone (LP) as the vehicles for transdermal penetration of phenolsulphonphthalein (phenol red) has been investigated by using an in-vitro technique with excised rat skin. LP had a higher enhancing effect on the penetration of phenol red than MP, but there was a long lag time before steady-state penetration was attained. A potent effect with a shorter lag time was obtained when MP and LP were used together. This potentiation was maintained when the concentration of MP was decreased by 95%. The combined vehicle also enhanced the skin accumulation of phenol red. MP promoted the rapid penetration of LP into the skin and potentiated the enhancing effect of LP on the penetration of phenol red and thereby shortened the lag time. The combined vehicle also enhanced the penetration of the hydrophilic anticancer agent, 5-fluorouracil.

Administration, Cutaneous↗

[Type-specific antibody to type Ia, Ib, II and III group B Streptococcus in maternal and neonatal sera measured by ELISA].

In order to determine the type-specific antibody to group B streptococcus (GBA) type Ia, Ib, II and III, the ELISA system was established in Research laboratories, Toyo Jozo Co., Ltd. We assayed type-specific antibody by this ELISA system in both maternal and neonatal (or cord) sera. The cut off levels were determined by the antibody levels of maternal and neonatal sera of 26 infected cases and 90 GBS carriers, that type Ia, Ib, II were 0.20 and type III was 0.15. Prevalence of type-specific antibody levels were studied in 356 maternal sera (14 affected cases, 100 GBS carriers and 242 non carriers). Antibody levels were positive in 47.2% of maternal sera to type Ia, 34.0% to type Ib, 46.9% to type II and 45.5% to type III. Antibody levels to type Ia, Ib, II and III were positive, respectively, in 100%, 88.2%, 25.0% and 42.9% of the sera of carrier mothers whose infants were not affected. Antibody levels in 50 pair sera of maternal and cord blood were well correlated.

Antibodies, Bacterial↗

[Quantitation of IgG antibodies to type Ia group B streptococcal type-specific polysaccharides measured by enzyme-linked immunosorbent assay].

The type-specific polysaccharide antigen of the group B streptococcus (GBS) type Ia as extracted and purified according to the procedures of Kane and Karakawa. Using this purified polysaccharide antigen, we made a sensitive and specific assay system of enzyme-linked immunosorbent assay (ELISA) and measured the titres of of the type-specific antibodies in maternal sera and cord blood sera. The titres of antibodies in 78 pregnant women (26 Ia carriers, 18 other types of GBS carriers and 34 non carriers) were compared. A mother of an infant affected by early onset infection of GBS Ia had a titre of antibody 1:10 at delivery, while 2 years later she became a non carrier and had a titre of antibody over 1:160. The titres of antibodies in 27 pair sera of mothers and cords were well correlated.

Antibodies, Bacterial↗

Comparison between Topcon SL-45 and SL-45B with different correction methods for factors influencing Scheimpflug examination.

Topcon Tokyo manufactured the first series of SL-45 in 1980 and a second in 1982/83, which were completed in Bonn with all technical improvements developed so far. In 1987, the SL-45B was manufactured which included all previously added improvements. To compare both camera types, we carried out a test with 10 volunteers and the following technical variables for the SL-45: (1) miosis; (2) mydriasis; (3) flashbulb 1; (4) flashbulb 2; (5) film batch 1; (6) film batch 2, and (7) different types of film. Afterwards, 5 of these volunteers were photographed with the SL-45B. Photographer and reader were identical in all cases. Based on microdensitometry it could be demonstrated that, with the exception of a different film type, all variables can be compensated for by using the corneal peak as an external standard.

Anterior Eye Segment↗

Imaging characteristics of three cameras using the Scheimpflug principle.

We studied the handling and the potentials of three different cameras operating according to the Scheimpflug principle and which currently are commercially available. The examinations were performed with the cameras Topcon SL-45, Topcon SL-6E with cataract attachment and Zeiss SLC system. Pigmented Brown-Norway rats with ultraviolet-B-induced cataract were used as the examination model. The image characteristics of the three cameras can be summarized as follows: The Topcon SL-45 camera produces very sharp images with small distortion; the Tocpon SL-6E camera with cataract attachment has the advantage to record simultaneously a slit image and a retroillumination image on the same film frame, but the slit image is quite distorted at the vertical axis; as regards the Zeiss SLC system, the quality of the video image is not as good as a film negative; however, this camera offers a superimposed image to the observer for easy orientation, as for example with small animal eyes. In addition, the direct quality control of the image on the screen increases the reproducibility significantly. However, the slit image is quite distorted at the horizontal axis.

Animals↗

Enhancing effect of pyrrolidone derivatives on the transdermal penetration of sulfaguanidine, aminopyrine and Sudan III.

The enhancing effect of pyrrolidone derivatives on the percutaneous penetration of sulfaguanidine, aminopyrine and sudan III was investigated using in vitro technique and excised rat skin. 1-Methyl (MP), 1-hexyl (HP) and 1-lauryl-2-pyrrolidone (LP) were used as penetration enhancers. Aminopyrine showed high penetration through skin although sulfaguanidine and sudan III showed little penetration. Pyrrolidone derivatives enhanced their penetrations. Especially HP and LP enhanced the penetration of sulfaguanidine to a high extent. Sudan III was not detected in the receptor phase regardless of the presence of enhancer. Pyrrolidone derivatives significantly increased the skin accumulation of sulfaguanidine, aminopyrine and sudan III. Penetration of pyrrolidone derivatives was also determined. MP and HP showed high penetrations. LP was not detectable in the receptor phase. MP, HP and LP showed high skin accumulations. These results suggested the usefulness of pyrrolidone derivatives as percutaneous penetration enhancers.

Administration, Cutaneous↗

Production of highly specific anti-testosterone antiserum by an immunotolerance method.

Anti-testosterone antisera were produced by pretreatment of rabbits with 15 alpha-carboxymethyl-5 alpha-dihydrotestosterone linked to a copolymer of D-glutamic acid and D-lysine (D-GL) before immunization with the bovine serum albumin conjugate of 15 alpha- and 15 beta-carboxymethyltestosterone. The specificity for 5 alpha-dihydrotestosterone of the antitestosterone antisera was considerably improved.

Animals↗

Synthesis and in vitro affinity for dopamine D-2 receptor of N-fluorine-substituted analogs of eticlopride.

With the aim of developing fluorinated benzamides that may be useful as radioligands for positron emission tomography, fluorine analogs of eticlopride, in which the N-ethyl group was replaced by 2-fluoroethyl, 3-fluoropropyl and p-fluorobenzyl groups, were synthesized. These derivatives were tested for their ability to displace [3H]spiperone from its specific dopamine D-2 receptor. Their potencies were decreased when compared with eticlopride, but the two fluoroalkylated analogs were in the same order of magnitude as that of haloperidol.

Animals↗

Acute toxicity and skin irritation of pyrrolidone derivatives as transdermal penetration enhancer.

We investigated preliminary acute toxicity and primary skin irritation of nine pyrrolidone derivatives which had been previously developed as transdermal penetration enhancers. The acute toxicity was observed at a dose of 500 mg/kg after intraperitoneal administration in mice. Their primary skin irritations were examined with rabbit dorsal skin. 1-Lauryl-2-pyrrolidone induced the most severe irritation among the derivatives. Pyrrolidone derivatives having methyl group and methyloxycarbonyl group caused little irritation. The primary irritation indices of pyrrolidone derivatives were not relative to their accumulations in the skin but to their enhancing effects. In conclusion, 1-hexyl-4-methyloxycarbonyl- and 1-lauryl-4-methyloxycarbonyl-2-pyrrolidone are suggested to be adequate enhancers, judging from the balance of their enhancing activity and irritation.

Administration, Cutaneous↗

Enhancing effect of pyrrolidone derivatives on transdermal penetration of phenolsulfonphthalein and indomethacin from aqueous vehicle.

We investigated the enhancing effect of three alkyl-2-pyrrolidones on transdermal penetration of phenolsulfonphthalein (phenol red) and indomethacin from an aqueous vehicle by using an in vitro technique with excised rat skin. The enhancers included 1-methyl- (I), 1-hexyl- (II) and 1-lauryl-2-pyrrolidone (III). These derivatives effectively enhanced the penetration and skin accumulation of phenol red and indomethacin. Lipophilic enhancers such as II and III showed particularly high enhancing effects. The penetration profiles of phenol red and indomethacin showed a lag phase followed by a linear increase. Compounds II and III showed long lag times. The enhancer penetration was also determined. Compounds I and II showed a slight penetration. Compound III showed little penetration but high skin accumulation.

Animals↗

Characteristics of anti-testosterone antisera produced by bovine serum albumin conjugates of 15 alpha- and 15 beta-carboxymethyltestosterone: use of [125I]iodinated tracers.

Each testosterone [125I]iodinated histamine derivative where [125I]iodinated histamines were linked to respective 15 alpha- and 15 beta-carboxymethyltestosterone (15 alpha- and 15 beta-CMT), testosterone-3-(O-carboxymethyl)oxime (T-3-CMO) and testosterone-17 beta-hemisuccinate (T-17-HS) were tested for their usefulness as radiotracers in testosterone immunoassay. In the use of anti-15 alpha- and 15 beta-CMT antisera produced in rabbits against 15 alpha- and 15 beta-CMT-bovine serum albumin (BSA) conjugates, the antisera with 15 alpha- and 15 beta-CMT-[125I]iodinated tracers showed low sensitivity and somewhat low specificity in comparison with those of the antisera with tritiated testosterone (T-3H). On the other hand, the antisera with T-3-CMO-[125I]iodinated tracer showed high sensitivity but low specificity for 5 alpha-dihydrotestosterone (5 alpha-DHT) in comparison with T-3H. The T-17-HS-[125I]iodinated tracer was not bound to the antisera. In the use of anti-15 alpha- and 15 beta-CMT antisera produced in rabbits by pretreatment with 15 alpha-carboxymethyl-5 alpha-DHT linked to a copolymer of D-glutamic acid and D-lysine followed by immunization with 15 alpha- and 15 beta-CMT-BSA, the antisera with homologous [125I]iodinated tracer showed high sensitivity and specificity.

Animals↗

Specificity of nucleotide sequence in DNA cleavage induced by D-glucosamine and D-glucosamine-6-phosphate in the presence of Cu2+.

32P-End-labeled restriction fragments derived from pBR322 and pUC9 DNAs were reacted with D-glucosamine or D-glucosamine-6-phosphate in the presence of Cu2+, and, after being heated at 90 degrees C in aqueous piperidine, the DNA products were analyzed on polyacrylamide gels for the sequence-specificity of alkali-labile cleavaged sites. The intensity of oligonucleotide bands of cleavaged sites was directly proportional to the concentration of aminosugars, indicating that the DNA cleavage was caused by the action of aminosugars themselves. The preferred DNA cleavage sites induced by these aminosugars were identical, both at pyrimidine-purine (5'----3') sequences, especially at thymineguanine ones, and to some extent at pyrimidine-pyrimidine (5'----3') sequences. The 6-phosphate moiety of D-glucosamine did not affect the specificity of DNA cleavage.

Base Sequence↗

[Novel method to observe the interface between adhesive resin and dentin by staining Fe3+ with tannic acid].

The reaction of Fe3+ and tannic acid was used in a new visual method to confirm the Fe3+ incorporated with dentin during the pretreatment with a 10% citric acid-3% ferric chloride solution or EDTA ferric ammonium salt solution. The combination of Fe3+ and tannic acid was also effective to investigate the state of incorporated resin (resin tags and resin reinforced dentin) with the dentin. The adhered dentin treated by staining with tannic acid was examined. The incorporation of Fe3+ with dentin enhanced the monomer infiltration and resulted in a high bond strength. Addition of 4-META into the MMA-TBB resin increased the resin content in dentin by promoting the rate of monomer diffusion.

Acrylic Resins↗

Ontogenesis of transmembrane signaling systems for control of cardiac Ca2+ channels.

Cardiac ICa is primarily controlled by the Ca2+ influx across the cell membrane during the action potential. Neurotransmitters and hormones are known to play an important role in controlling the availability of cardiac Ca2+ slow channels and [Ca]i through the transmembrane signaling systems, such as the receptor-adenylate cyclase system and the PI hydrolysis system. This article has reviewed some of the important properties of the transmembrane signaling systems for the control of Ca2+ channels and how they changed during development, especially in the rat heart. Since the phosphorylation hypothesis was first proposed over 15 years ago, considerable advances have been made in understanding the mechanisms for regulation of Ca2+ slow channels at the molecular level. During development, the properties of the cardiac Ca2+ channels, as well as the transmembrane signaling systems, change electrophysiologically, pharmacologically, and biochemically. Because conflicting data have been reported on the developmental changes in these properties, it is still not clear how the complex physiological function of the Ca2+ channels is gradually integrated during development. To answer this question, more data, new concepts, and new approaches are required.

Aging↗

Regional enzymatic analysis of UV-B and streptozotocin induced diabetic cataract lens.

As the UV-B cataract and early stages of diabetic cataract in rats only touches the epithelium and anterior superficial cortex, a whole lens analysis is not meaningful, but a regional analysis with the freeze-sectioning device has to be performed. Scheimpflug photography with microdensitometric image analysis enables the scientist to discern in vivo single layers along the optical axis of the lens. UV-B cataracts (0.2 J/cm2, every 2nd day) and diabetic cataracts (Streptozotocin (STZ), 70 mg/kg BW) were induced in Brown-Norway rats. The stages of lens opacification were documented by Scheimpflug photography. 8 weeks after start of UV-B treatment and at several dates before onset of visible diabetic cataractous changes, the animals were sacrificed. The lenses were divided reproducibly into 4 or 7 parts such as an equatorial ring and several layers of the central cylinder from anterior to posterior part. The enzyme activity spectrum shows highly region related pattern that would not have been found in a whole lens analysis. Aldose reductase was activated before appearance of visible cataractous changes due to diabetes compared to normal lenses. In contrast Fructose-1,6-biphosphate-aldolase activity was lower before onset of visible changes than in normal lenses, but only within the 1st section where later visible cataractous changes of UV-B cataract could be detected.

Aldehyde Reductase↗

Accumulation and metabolism of 2,4,6-trichlorophenyl-4'-aminophenyl ether by carp.

1. Accumulation of 2,4,6-trichlorophenyl-4'-aminophenyl ether (CNP-amino) in carp was investigated for 14 days. CNP-amino in carp could be divided into free CNP-amino [CNP-amino(I)] and bound CNP-amino [CNP-amino(II)]. 2. The bioconcentration factors (BCF) of CNP-amino(I + II) in carp were 90 +/- 38 (mean +/- SD, n = 3) for muscle, 402 for liver, 501 for kidney and 5368 for gallbladder after 14 days exposure. 3. 2,4,6-Trichlorophenyl-4'-acetamide phenyl ether (CNP-acetamide) was detected as metabolites of CNP-amino in muscle and viscera of carp.

Animals↗

Bioconcentration and excretion of diazinon, IBP, malathion and fenitrothion by carp.

1. Bioconcentration and excretion of diazinon, IBP, malathion and fenitrothion were studied for carp (Cyprinus carpio L.). 2. The concentrations of these pesticides in muscle and viscera of the carp reached plateaus in 12-48 hr exposure. 3. The average values of bioconcentration factors (BCF) for diazinon were 20.9 in muscle, 60.0 in liver, 111.1 in kidney and 32.2 in gallbladder over the 168 hr exposure period. Similarly, those values were 4.3-26.7 for IBP, 2.7-17.3 for malathion, and 36.0-157.1 for fenitrothion. 4. The excretion rate constants of malathion (hr-1) were 0.13 for muscle, 0.12 for liver, 0.08 for kidney and 0.06 for gallbladder. Those of diazinon, IBP and fenitrothion (g.ng-1.hr-1) were 0.002-0.024 for muscle, 0.001-0.020 for liver, 0.0004-0.004 for kidney and 0.002-0.023 for gallbladder, respectively.

Animals↗

Blood-ocular barrier permeability in experimental myopia.

Vitreous fluorophotometry (VFP) was performed for myopic eyes induced by unilateral eyelid suturing of six young cynomolgus monkeys in order to study the permeability of the blood-ocular barrier. The eyelid fusion was temporarily cut and opened at about five-month intervals, and the dioptric power and axial length of test and control eyes were measured. VFP was carried out before and after intravenous injections of fluorescein-Na. The inward permeability of the blood-retinal barrier (P(in)) was estimated by our computer simulation method, and the index of permeability of the blood-aqueous barrier (AQ) was also obtained. Significant prolongation of the length of the vitreous cavity was first seen 10 months after suturing, with the degree of myopia progressing subsequently. P(in) and AQ values increased as myopia progressed: significant increases were observed at 10 and 16 months after suturing, respectively. These results indicate a close relationship between the occurrence and progress of myopia and increased permeability of the blood-ocular barrier.

Animals↗