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J Mizoguchi

Publications and source records attributed to J Mizoguchi.

At least 19 recordsLinked to original sources
PubMed2000

Preparation and characterization of two crystalline forms of 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-1-ethyl-2-hydroxymethyl-4-pyrroli dinyl]benzamide (TKS159).

For 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-1-ethyl-2-hydroxymethyl-4-pyrrolid inyl]benzamide (TKS159), two polymorphs, forms alpha and beta, were prepared and characterized by means of X-ray powder diffractometry, thermal analysis, infrared spectroscopy and 13C-NMR spectroscopy, both in the solution and solid phases. The X-ray powder diffraction analysis gave different patterns for forms alpha and beta. In the thermogravimetry and differential thermal analysis profiles, form beta exhibited characteristic endo- and exothermic peaks at 112.7 degrees C and 116.2 degrees C, respectively, due to the partial melting-induced phase transition to form alpha without accompanying weight loss, and these were followed by an additional endothermic peak at 138.2 degrees C due to fusion. For form alpha, only an endothermic peak at 137.8 degrees C due to fusion was observed. The IR spectroscopic analyses of forms alpha and beta gave different absorption bands assigned to N-H and O-H stretching, N-H bending, and C=O stretching vibrations. From the data obtained by thermal analysis, form alpha was shown to be thermodynamically more stable than form beta.

Benzamides↗
PubMed1999

Synthesis and pharmacological activity of 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-1-ethyl-2-hydroxymethyl-4- pyrrolidinyl]benzamide (TKS159) and its optical isomers.

Of 4-amino-5-chloro-2-methoxy-N-(1-ethyl-2-hydroxymethyl-4- pyrrolidinyl)benzamide, four optical isomers, (2S,4S)-1 (TKS159), (2S,4R)-25, (2R,4S)-26 and (2R,4R)-27, were prepared from optically active 4-amino-1-ethyl-2-hydroxymethylpyrrolidine di-p-toluenesulfonate [(2S,4S)-14, (2S,4R)-17, (2R,4S)-20 and (2R,4R)-23, respectively]. The requisites, (2S,4S)-14, (2S,4R)-17, (2R,4S)-20 and (2R,4R)-23, were prepared from a commercially available trans-4-hydroxy-L-proline. The absolute configurations of (2S,4S)-1 (TKS159), (2S,4R)-25, (2R,4S)-26 and (2R,4R)-27 were spectroscopically determined. Of the benzamide derivatives, four optical isomers, (2S,4S)-1, (2S,4R)-25, (2R,4S)-26 and (2R,4R)-27, showed a relatively potent affinity for 5-hydroxytryptamine 4 (5-HT4) receptors in a radioligand binding assay ([3H]GR113808). The activities of 25-27 were less effective than that of 1 for the gastric emptying of a phenol red semisolid meal in rats. All this suggests that the most potent of the isomers was 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-1-ethyl-2- hydroxymethyl-4-pyrrolidinyl]benzamide (1).

Animals↗
PubMed1999

[Influence of scalp shaving on prevention of postoperative intracranial infection].

Shaving of the whole scalp is ordinarily performed prior to neurosurgical operation. Although it is performed in order to prevent postoperative intracranial infection, there has been no apparent basis for this practice published in previous reports. We examined whether shaving the whole scalp reduced the rate of postoperative infection or not. We divided 274 cases, who received their first intracranial operation in the last 2 years, into two groups; a whole shaving group and a partial shaving group. We compared the rate of postoperative intracranial infection between the two groups according to age, diagnosis, operation, operation time and placement of drainage. Overall, 12 cases out of 274 (4.38%) had postoperative intracranial infection. The long operation time and the long term placement of drainage mechanism increased the postoperative intracranial infection rate. There was no postoperative intracranial infection in 74 patients who received burr-hole/twist-drill operation. As for craniotomy/craniectomy operations, 7 cases out of 83 (8.4%) in the partial scalp-shaving group whole scalp shaving group and 5 cases out of 117 (4.2%) had postoperative intracranial infections. Thus, there was no significant difference in the rate of postoperative intracranial infection between the two groups, if anything, the whole scalp shaving group tended to show a higher rate. According to these results, partial scalp shaving did not increase the rate of postoperative intracranial infection. Considering that patients who have lost their hair find it embarrassing to return to society, it is well to know that the whole scalp shaving is not absolutely necessary for all first craniotomy.

Craniotomy↗
PubMed1996

Detection of HIV-1 and HIV-2 antibodies among Chlamydia trachomatis infected pregnant women in Japan.

An anonymous unlinked HIV antibody test was conducted on 1632 Chlamydia trachomatis (C. trachomatis) antibody positive women from 10 institutes of 7 prefectures in Japan. All the sera were negative for both HIV-1 and HIV-2 antibodies. The result may support the suggestion that HIV prevalence is low among general population in Japan. Such a test as this study will be useful not only for developing a reliable HIV surveillance system but also for the study of sexual behavior of general population, since C. trachomatis infection is sensitive to reflect sexual contact.

Adult↗
PubMed1993

In vivo stimulation of endosteal bone formation by basic fibroblast growth factor in rats.

Intravenous administration of human basic fibroblast growth factor (bFGF) for 2 weeks stimulated osteoblast proliferation and new bone formation in various skeletal bones in young and aged rats at dosage levels of 0.1 mg/kg/day and greater. Morphometry of the soft X-ray radiograms of cross sections of the tibia indicated about a 20% increase in the calcified bone area of the diaphysis at 0.1 mg/kg/day. The Ca and hydroxyproline contents showed statistically significant increases at this dosage. The new bone formation was found only on the endosteal side, and no periosteal bone formation was found. Similar systemic osteogenic potential was seen after intravenous administration of other growth factors of the FGF family, human acidic FGF and human heparin-binding secretory transforming protein-1. The above results suggest a potential therapeutic role for these growth factors in bone-loss diseases such as osteoporosis.

Aging↗
PubMed1992

A non-radioisotopic reverse transcriptase assay using biotin-11-deoxyuridinetriphosphate on primer-immobilized microtiter plates.

We developed a non-radioisotopic (non-RI) reverse transcriptase assay (RTA). The reverse transcriptase (RT) incorporates biotin-11-deoxyuridine-triphosphate (bio-dUTP) using a poly(rA) template hybridized with oligo(dT) primer that is immobilized on the surface of a 96-well microtiter plate. This assay is thus semi-automated by adapting it to an ELISA testing format. The incorporation of bio-dUTP was enhanced by adding cold dTTP to the reaction mixture, optimally in a molar ratio 4:1 (dTTP:bio-dUTP). This non-RI RTA is more sensitive than the conventional RI assay for the detection of purified Rous-associated virus 2 (RAV-2) and of human immunodeficiency virus type 1 (HIV-1) lysate. Because of its simple procedure, higher sensitivity and non-use of RI materials, the assay can be utilized not only for virological studies but also for routine safety screening of biological products for retroviral contamination.

Avian Leukosis Virus↗
PubMed1991

Tissue specific expression of the plasma glutathione peroxidase gene in rat kidney.

Rat plasma glutathione peroxidase (GSH-Px) was purified 1,400-fold from rat serum by a combination of phenyl Sepharose, DEAE Sephacel, blue Sepharose and Sephacryl S-200 column chromatographies. The purified GSH-Px migrated as a single band corresponding to a molecular weight of 22,500 on sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The enzyme was used for the immunization of chickens to obtain a specific antibody and for determination of its amino acid sequence. Two overlapping cDNA clones for rat plasma GSH-Px were isolated from a placental cDNA library. The composite nucleotide sequence is 1,529 base-pairs long and encodes 226 amino acids. The deduced amino acid sequence completely coincided with the sequences of five individual peptide fragments derived from the purified plasma GSH-Px on digestion with lysyl endopeptidase. In order to identify the tissue(s) generating this plasma GSH-Px, immunoblot analysis was performed on homogenates prepared from 13 tissues. A single immunoreactive band of 22.5 kDa, corresponding to plasma GSH-Px, was detected for the kidney homogenate. A much fainter band was observed for the lung preparation, but liver, spleen, bone marrow, and other tissues examined were negative. Northern blot analysis further revealed that the expression level of the plasma GSH-Px gene was high in kidney and low in lung. No transcript was detected in liver or spleen. These results indicate that plasma GSH-Px is predominantly synthesized and secreted by renal cells.

Amino Acid Sequence↗
PubMed1991

Serum-free cultivation of anchorage-dependent cells on microcarrier: effective production of human macrophage colony-stimulating factor.

For the purpose of establishing a large scale production process of biologically active substances by cultivation of anchorage-dependent mammalian cells, basic studies were carried out on the following items; establishment of a new cell line and derivation of high productivity; construction of optimal serum-free medium; optimization of cultivation method using microcarrier in serum-free medium; and establishment of purification process. The cell line, TRC-29SF, used in this study was newly established from human renal carcinoma with a function of producing macrophage colony-stimulating factor constitutively. Improvement of M-CSF productivity upon TRC-29SF cell line was performed by M-CSF gene amplification with dhfr-MTX system and by truncation of membrane-binding amino acid sequence by recombinant DNA technique. Two kinds of serum-free media, IPEG-85 and IREG-89, were formulated for the growth of TRC-29SF cell and its transformant, respectively. A new cell-adhesion method which permits homogeneous attachment to microcarrier in short term was developed by equalizing the sedimentation velocity between cells and microcarrier by addition of 7% Ficoll into the medium. High cell density perfusion culture of TRC-29SF cells was achieved by microcarrier method using IPEG-85 medium, and final cell density reached over 10(7) cells/ml. Based on the results obtained, long-term perfusion cultures were performed using Mn10-5 and Mn10-5/R600 cell lines, which were created by M-CSF gene transfection and amplification. We found that the productivity of M-CSF per cell began to decrease from the end of logarithmic growth phase. Long-term cultivation with high productivity was accomplished by perfusing medium containing 2 mM sodium butyrate. Purification process for M1-CSF from the culture supernatant of transformed cell line was also established.

Amino Acid Sequence↗
PubMed1990

Primary structure of human plasma glutathione peroxidase deduced from cDNA sequences.

Human plasma glutathione peroxidase (GSHPx) has been shown to be a selenium-containing enzyme immunologically distinct from cellular GSHPx. Oligonucleotide probes, based on the partial amino acid sequence of plasma GSHPx, were synthesized and used to screen a human placenta cDNA library. Nucleotide sequence analysis of the obtained clones revealed that GSHPx consisted of a 678-base pair open reading frame coding for a 226-amino acid polypeptide with a Mr of 25,389. About 50% of the deduced amino acid sequence was confirmed by partial amino acid sequencing of the peptides in a lysine endopeptidase-digest of the purified enzyme. The amino acid sequence exhibited only 44% homology with that of human cellular GSHPx. Northern blot analysis revealed a single transcript of 2.2 kilobases in the poly(A)+ RNA fractions of human placenta and HepG2 (a human hepatic cell line), but not that of human liver and endothelial cells.

Amino Acid Sequence↗
PubMed1990

Molecular cloning of cDNA coding for rat plasma glutathione peroxidase.

The plasma glutathione peroxidase (PGSH-PO), which is different from erythrocyte glutathione peroxidase (EGSH-PO) in immunochemical property and substrate specificity, was purified from male Wistar rat serum. The amino acid sequence of 5 independent peptides were determined and a cDNA clone for this enzyme was isolated from placental cDNA library. The nucleotide sequence of the cDNA revealed that, similar to EGSH-PO cDNA, the seleno-cysteine was genetically encoded by "TGA" codon. On comparing the nucleotide sequences of EGSH-PO and PGSH-PO, no significant homology was found in the vicinities of "TGA" codons of both enzymes.

Amino Acid Sequence↗
PubMed1989

Development and distribution of the major pollen allergen (Cry j I) in male flower buds of Japanese cedar (Cryptomeria japonica).

We investigated the production of the major pollen allergen [Cry j I] of Japanese cedar (Cj) in the course of male flower bud development. We found that most of the pollen was at the tetrad stage in early September, and they developed to the mature stage in mid-October (1987) or early November (1988). Large amounts of Cry j I seemed to be extractable to ABS solution from the mature stage pollen but not from the pollen at other stages, that is, the tetrad and immature stages. Mature pollen could be ruptured with ammonium bicarbonate buffer, but tetrad and immature pollen could not. By immunofluorescent technique, antigen Cry j I was detected in the pollen only at the mature stage of Cj pollen development. Therefore, we think that Cry j I is produced at the time of pollen maturation.

Allergens↗
PubMed1987

Decrease in amylase (EC 3.4.21.4) synthesis in lactating rats.

The amylase (EC 3.4.21.4) and trypsin (EC 3.2.1.1) activities in the pancreas in rats during pregnancy, lactation and after the weaning period, and the secretory responses to a secretagogue (caerulein) in the exocrine pancreas of lactating rats were measured. Trypsin activity increased as lactation progressed and reached twice that of unmated rats in the second half of the lactation period. The amylase activity fell before parturition and failed to recover even after the start of lactation and was significantly decreased throughout the lactation period. The total amount of pancreatic juice produced in the lactating rats was significantly greater than that of unmated rats; the amylase output was significantly less than that of unmated rats. When the pups were removed, amylase activity in the pancreas returned to the value in unmated rats. Furthermore, the amylase activity in lactating rats receiving a daily injection of insulin significantly exceeded that of normal lactating rats. These results indicate that the decrease in amylase activity in lactating rats is due to the reduction of amylase synthesis and there is a possibility that insulin is required for normal or elevated rates of amylase synthesis in lactating rats.

Amylases↗
PubMed1986

Effect of oestrogen on Pasteurella pneumotropica in rat vagina.

The effects of ovarian hormones on the vaginal population of Pasteurella pneumotropica in rats were investigated. Specified-pathogen-free adult female Wistar-Imamichi rats with a 4 day oestrous cycle were inoculated with P. pneumotropica in the vagina. Cyclic changes in the vaginal population of P. pneumotropica were not observed in ovariectomized rats and the bacterial population was at a similar level to that at normal dioestrus. Administration of oestrogen to ovariectomized rats caused an increase in the numbers of P. pneumotropica and total bacteria in the vagina nearly equal to that at oestrus in intact rats. The numbers of these organisms in the vagina of ovariectomized rats treated with progesterone did not change and were similar to those of control ovariectomized rats treated with sesame oil. Vaginal smears of ovariectomized rats treated with oestrogen were characterized by abundant cornified non-nucleated epithelial cells with many adherent Gram-negative coccobacilli and were similar to smears from intact rats at oestrus. These findings suggest that the proliferation of P. pneumotropica at oestrus in rat vagina may be primarily due to the environment provided by the degeneration of vaginal epithelial cells promoted by oestrogen secretion from the ovaries.

Animals↗
PubMed1986

[An outbreak of Trichophyton mentagrophytes infection in a rat breeding stock and its successful control].

An outbreak of dermatophytosis by Trichophyton mentagrophytes infection was observed in a breeding stock of the Wistar-Imamichi rat. Typical cutaneous lesions such as alopecia and hyperkeratosis due to the fungus were observed in 10% and 44% of adult females, and males respectively. No infection was seen in infant, even in those fostered by infected females. By 3 repeated cultivations of the hair, T. mentagrophytes was isolated from 107 (90.7%) of 118 rats clinically diagnosed as dermatophytosis. In order to maintain the original stock, the usual wholesale slaughter program was avoided and the following control measures were taken. After sacrificing all rats with the cutaneous lesions, the breeding colony was transferred temporarily to a separate animal room. The resulting vacant room was then disinfected 3 times with 10% formalin, followed by spraying with 3% sodium propionate solution 3 month later. The progenies from the non-infected mothers were dipped into 3% sodium propionate solution and transferred back into the disinfected animal room for re-colonization. Frequent sterilization of all equipment with iodophor, balsam and formalin was carried out. The room sterilized monthly with iodophor and 70% alcohol. Daily observation of all rats and monthly screening by culture test was done thereafter. As a result, no infection has been detected 4 month after recolonization, except for the 3 rats which were sacrificed immediately after detection. On the basis of the culture test and clinical observation, no infection was observed in the treated rat colony for the next five following years. Therefore, the effectiveness of these procedures of the eradication of T. mentagrophytes infection from a rat colony was shown to be quite reliable.

Animals↗