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Biomedical subjects

Y Inamoto

Publications and source records attributed to Y Inamoto.

At least 37 records · Page 2Linked to original sources
PubMed1992

Ovarian and hepatic metastases of gastric carcinoma associated with high serum levels of human chorionic gonadotropin (hCG), alpha-fetoprotein (AFP), and carcinoembryonic antigen (CEA): a case report.

A 45-year-old woman who underwent gastrectomy for gastric carcinoma which had metastasized to the liver and ovaries, showed high serum levels of hCG, AFP and CEA. To locate the source, an immunohistochemical technique was utilized. HCG-producing cells were detected in poorly differentiated adenocarcinoma of a primary tumor and an ovarian metastatic site, and AFP-producing cells in poorly differentiated adenocarcinoma forming a medullary pattern of primary site and metastatic foci. CEA-producing cells were found diffused in primary tumor and metastatic foci. From the viewpoint of oncodevelopmental gene expression (Cancer Res 36:3423, 1976), it is interesting that the serum levels of these three tumor markers (hCG, AFP, CEA) were elevated simultaneously.

Biomarkers, Tumor↗
PubMed1992

[A new oral cephem, cefdinir: its structure-activity relationships and biological profile].

This article reviews structure-activity relationships and biological properties of a new oral cephem, cefidinir (CFDN). It also describes a hypothesis concerning the absorption mechanism from the intestine. Antibacterial activities and the oral absorption efficiencies were studied with regard to 3-vinyl cephalosporins with various 7-acyl side chains. From the study, 2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetyl group was selected and various 3-substituents were screened. As a result, it was found that the vinyl compound, CFDN, showed excellent antibacterial activity and good oral absorption in rats. In vitro and in vivo antibacterial activities, the affinity for PBPs and the stability to beta-lactamases revealed that CFDN had well balanced antimicrobial activities against Gram-positive and Gram-negative bacteria and good biological properties. The pharmacokinetics of CFDN in healthy volunteers showed that serum concentration and half life were good enough to make CFDN an effective therapeutic agent. The mechanism of intestinal absorption of CFDN and related oral cephems are discussed and a hypothesis for molecular recognition by the carrier protein in the intestine is proposed.

Animals↗
PubMed1991

Effect of hyperbaric oxygenation on macrophage function in mice.

Hyperbaric oxygenation (HBO) has an immunosuppressive effect. The possible mechanisms of this immunosuppressive effect were assessed by determining the production of interleukin-1 (IL-1), interleukin-6 (IL-6), and prostaglandin E2 (PGE2), as well as phagocytosis by splenic macrophages from HBO-treated mice. Although HBO treatment did not have any significant effect on IL-6 production and phagocytotic activity, a marked decrease in IL-1 production and a significant decrease in PGE2 production were observed. These results suggest that the reduction of IL-1 production may play an important role in the immunosuppressive effect of HBO.

Animals↗
PubMed1991

Studies on beta-lactam antibiotics. XIX. Structure-activity relationships of cephalosporins having a thiadiazolylthiomethyl group at the C-3 side chain.

The synthesis and antibacterial activity of 7 beta-[(Z)-2-(2-amino-4-thiazolyl)-2-(hydroxy or alkoxy)iminoacetamido]cephalosporins with various thiadiazolylthiomethyl moieties at the 3-position are discussed. Of the compounds (1a-1e, 7a-7d), 7 beta-[(Z)-2-(2-amino-4-thiazolyl)-2-hydroxyiminoacetamido]-3-[(1,2 ,4- thiadiazol-5-yl)thiomethyl]cephalosporin (1d: FK312) exhibited the highest activity against Gram-positive and Gram-negative bacteria, especially, against methicillin-resistant Staphylococcus aureus. Furthermore, the pharmacokinetic profiles of the compound 1d showed longer serum levels than that of ceftriaxone in rats.

Anti-Bacterial Agents↗
PubMed1990

Effect of interleukin 1 (IL-1) on the levels of cytochrome P-450 involving IL-1 receptor on the isolated hepatocytes of rat.

In the present study, the expression of IL-1 receptor (IL-1 R) on the primary cultured hepatocytes was determined and the effect of IL-1 on the intracellular amount of cytochrome P-450 was investigated. The kinetics of IL-1R on the hepatocytes was studied by [125I]-IL-1 alpha and revealed that 5,000 molecules of IL-1 bound to a hepatocyte with a Kd of 4.0 x 10(-9) M. Incubation of the hepatocytes with IL-1 for 18 hrs decreased the contents of cytochrome P-450 in a dose-dependent manner. These findings suggest that IL-1 potentially depresses the drug metabolism involving IL-1R which is expressed on hepatocytes.

Animals↗
PubMed1990

[Studies on FK482 (Cefdinir). IV. Synthesis and structure-activity relationships of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]- 3-substituted cephalosporin derivatives].

The synthesis of 7 beta-[(Z)-2-(aminothiazol-4-yl)-2-hydroxyiminoacetamido] cephalosporins (Ia-i) modified at the C-3 position of a cephem nucleus and the effect of the C-3 substituents on the antibacterial activity and oral absorbability are discussed. The cephems (Ie, h and i) having a C-3 substituent such as 1-propenyl, ethylthio and vinylthio group as well as FK482 (cefdinir) exhibited excellent antibacterial activities against both gram-positive and gram-negative bacteria. However, those compounds showed poor absorption rate after oral administration in rats. It is concluded that the vinyl moiety at the 3-position is necessary to display fairly oral absorptivity in a series of 7 beta-[(Z)-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]c eph ems.

Animals↗
PubMed1990

[Studies on FK482. II. Synthesis and structure-activity relationships of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-substituted acetamido]-3-vinyl-3-cephem-4-carboxylic acid derivatives].

Various 7 beta-[2-(2-aminothiazol-4-yl)-2-substituted acetamido]-3-vinyl-3-cephem-4-carboxylic acid derivatives (Ia--e, IIa--g) were synthesized in order to find a new orally active cephalosporin improving the antibacterial activity of cefixime (CFIX) against Staphylococcus aureus. These derivatives include three types of alpha-substituted 2-(2-aminothiazol-4-yl)acetyl side chain; i) mono or non substituted acetyl moiety, ii) carboxyalkoxyimino acetyl moiety, iii) phosphonomethoxyimino and hydroxyimino acetyl moiety. Their structure-activity relationships and urinary recoveries in rats were studied. As a result, the compound with a hydroxyimino acetyl side chain (IIg, FK482) showed good oral absorption and excellent antibacterial activity against both gram-positive and gram-negative bacteria and was selected as a candidate for clinical trial.

Animals↗
PubMed1990

[Studies on FK482 (Cefdinir). III. Synthesis and structure-activity relationships of 7 beta-[(Z)-2-aryl-2-hydroxyiminoacetamido]-3-vinyl-3- cephem-4-carboxylic acid derivatives].

The synthesis, antibacterial activity and oral absorption of the 7 beta-[(Z)-2-aryl-2-hydroxyiminoacetamido]-3-vinylcephalosporins (Ia--e) are described. All of these compounds exhibited excellent activity against Staphylococcus aureus. Against Gram-negative bacteria FK482 exhibited more excellent activity than the other compounds (Ia--e). These compounds except Ie showed good oral absorption. The relationship between the oral absorption rates and the lipophilicity of these cephalosporins is discussed.

Animals↗
PubMed1990

Synthesis and structure determination of FR109615, a new antifungal antibiotic.

The structure of FR109615, a new antifungal antibiotic, was determined to be (1R,2S)-2-aminocyclopentane-1-carboxylic acid ((-)-cis-2-ACPC: 8a) by X-ray analysis. (-)-cis-2-ACPC (8a) was also synthesized via optical resolution of 3a and 3b derived from (+/-)-cis-2-ACPC hydrochloride (1). 8a showed potent antifungal activity, while its antipode (+)-cis-2-ACPC (8b) had no activity.

Antifungal Agents↗
PubMed1989

[A case of intermittent ventricular pre-excitation syndrome with a Mahaim fiber].

A 61 year-old woman with intermittent ventricular pre-excitation syndrome using a Mahaim fiber was reported. The electrocardiogram showed QRS-complex with small delta wave (100 msec in QRS width) or without small delta wave (80 msec in QRS width). On electrophysiological study, during sinus rhythm, A-H interval was 100 msec. H-V intervals were 25 msec in QRS-complex with small delta wave and 45 msec in QRS-complex without small delta wave. From these findings, it was considered that the small delta wave was produced by a Mahaim fiber.

Electrocardiography↗
PubMed1989

Multiple myeloma in husband and wife.

A married couple with multiple myeloma (MM) is reported. Although we could not find any definite pathogenetic factors of MM in the spouses examined, the salient features of the 10 couples with MM reviewed, including ours, were summarized to obtain a better understanding of the pathogenesis of MM. The appearance of MM in spouses suggests that environmental factors are involved in the pathogenesis of MM.

Aged↗