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Biomedical subjects

N Tamura

Publications and source records attributed to N Tamura.

At least 181 records · Page 10Linked to original sources

Optically active antifungal azoles. IV. Synthesis and antifungal activity of (2R,3R)-3-azolyl-2-(substituted phenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanols.

(2R,3R)-3-Azolyl-2-(substituted phenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanols (III) were prepared from (2R,3S)-3-methyl-2-(substituted phenyl)-2-(1H-1,2,4-triazol-1-yl)methyloxiranes (21a-f) by a ring-opening reaction with 1H-1,2,3-triazole and 1H-tetrazole and evaluated for antifungal activity against Candida albicans in vitro and in vivo. The optically active oxiranes (21a--f) which serve as the key synthetic intermediates, were synthesized from 1-[(2R)-2-(3,4,5,6-tetrahydro-2H-pyran-2-yl)oxypropanoyl]morpholin e (24) and substituted phenylmagnesium bromide (23) via six steps in a stereocontrolled manner. The 3-(1H-1,2,3,-triazol-1-yl)-(IIIa) and 3-(2H-2-tetrazolyl)-2-butanol (IIId) derivatives showed strong protective effects against candidosis in mice.

Animals↗

[Pharmacological profile of F-0401, a novel dihydropyridine derivative. III. The anti-aggregatory action of F-0401 on rabbit platelets].

F-0401 is a newly synthesized dihydropyridine derivative with both antagonistic activity on platelet-activating factor (PAF) and inhibitory action on thromboxane A2(TXA2) synthetase activity. In the present study, we examined the effects of F-0401 on platelet aggregations in vitro and ex vivo in rabbits. F-0401 prevented PAF-, arachidonic acid (AA)- and collagen-induced platelet aggregations in vitro, but did not prevent the aggregation by ADP. The inhibitory effect of F-0401 on the aggregation by PAF (IC50 value: 3.4 x 10(-6) M) or by the threshold amount of AA (IC50 value: 4.3 x 10(-6) M) had the same potency as that of CV-3988 (a PAF antagonist) and ozagrel a (TXA2 synthetase inhibitor). Ex vivo studies also revealed that the anti-aggregatory effect occurred 1 h after the treatment of F-0401 (> 10 mg/kg, p.o.) and this effect had a tendency to last for 6 h. Nicardipine prevented the platelet aggregation only by PAF (IC50 value: 6.6 x 10(-5) M) in vitro. However, the preventive effect was not seen ex vivo. On the other hand, neither nifedipine nor flunarizine showed any effect on the stimulant-induced platelet aggregation in rabbits. These results suggest that F-0401 has anti-aggregatory action, which is attributable to both PAF antagonistic action and TXA2 synthetase inhibition in vitro and ex vivo.

Animals↗

[Pharmacological profiles of F-1322, a novel anti-asthmatic agent. (1). Mechanisms of action].

The pharmacological effects of N-[2-(4-(benzhydryloxy)piperidino)ethyl]-3-hydroxy-5-(3-pyridyl methoxy)-2- naphthamide (F-1322), a novel anti-asthmatic agent, was investigated in vitro. The results obtained were as follows: 1) In the isolated trachea of guinea pigs, F-1322 showed a markedly potent antagonistic action against the contraction induced by histamine, while it had little or no effect on 5-hydroxytryptamine-, acetylcholine-, leukotriene D4- or U-46619-induced contractions. 2) In rabbit platelets, F-1322 did not affect the platelet aggregation induced by platelet activating factor. 3) F-1322 significantly inhibited the thromboxane (TX) A2 synthetase (IC50 value: 1.7 x 10(-8) M) and 5-lipoxygenase (IC50 value: 9 x 10(-7) M) activities. 4) F-1322 had no effect on phospholipase A2, cyclooxygenase, Ca2+/calmodulin-dependent phosphodiesterase and phosphodiesterase activities. These in vitro studies suggest that the anti-asthmatic action of F-1322 is associated with histamine antagonism and an inhibitory action on TXA2 synthetase and 5-lipoxygenase activities.

Animals↗

Hepatitis C virus infection and membranoproliferative glomerulonephritis in Japan.

The prevalence of hepatitis C virus (HCV) infection was determined in 146 adult patients with various types of glomerulonephritis and renal diseases monitored between 1990 and 1993. Serum HCV antibody (HCV Ab) was evaluated, and positive cases were tested for HCV RNA by polymerase chain reaction. HCV infection was present in 1 (1.7%) of 58 cases of immunoglobulin A nephropathy, 0 (0%) of 14 cases of lupus nephritis, 0 (0%) of 12 cases of minimal change nephrosis, and 0 (0%) of 28 cases of other renal diseases, which is similar to the 2% prevalence observed in healthy blood donors in Japan. In contrast, HCV Ab was observed in 2 (8.3%) of 24 cases of membranous nephropathy and 6 (60%) of 10 cases of membranoproliferative glomerulonephritis (MPGN) Type I. The prevalence of HCV infection in MPGN patients was significantly higher than the frequency of HCV infection observed in the other patients with renal diseases (P < 0.001). HCV RNA was present in all cases in which HCV Ab was present. The six patients with HCV-MPGN were similar to the four patients with idiopathic MPGN with respect to age, presence of nephrotic syndrome, and renal dysfunction, but had a higher incidence of liver dysfunction, cryoglobulinemia, rheumatoid factor, and hypocomplementemia (low C3). HCV infection is present in a large percentage of patients with MPGN in Japan and clinically may differ slightly from other cases of MPGN.

Adolescent↗

Human obese gene expression. Adipocyte-specific expression and regional differences in the adipose tissue.

The obese (ob) gene, the mutation of which results in severe hereditary obesity and diabetes in mice, has recently been isolated through positional cloning. In this study, we isolated a full-length human ob complementary DNA (cDNA) clone and examined the tissue distribution of ob gene expression in humans. The nucleotide sequences of the human ob cDNA coding region were 83% identical to those of the mouse and rat ob cDNA coding regions. Analysis of the deduced amino acid sequences revealed that the human ob protein is a 166-amino acid polypeptide with a putative signal sequence and is 84 and 83% homologous to the mouse and rat ob proteins, respectively. Northern blot analysis using the cloned human ob cDNA fragment as a probe identified a single messenger RNA (mRNA) species 4.5 kb in size found abundantly in the adipose tissues obtained from the subcutaneous, omental, retroperitoneal, perilymphatic, and mesenteric fat pads. However, no significant amount of ob mRNA was present in the brain, heart, lung, liver, stomach, pancreas, spleen, small intestine, kidney, prostate, testis, colon, or skeletal muscle. The ob mRNA level in the adipose tissue varied from region to region even in the same individual. Furthermore, in the human adipose tissue, ob gene expression occurred in mature adipocytes rather than in stromal-vascular cells. This study is the first report of the elucidation of ob gene expression in human tissues, thereby leading to better understanding of the physiological and clinical implications of the ob gene.

Adipocytes↗

Nuclear proteins involved in cell division in the ciliate, Tetrahymena.

For the purpose of clarifying the presence of nuclear proteins which may induce cell division, we conducted experiments using ciliate Tetrahymena which can be synchronized at the G2 phase in the cell cycle easily by periodic heat shock treatment (HST): We obtained proteins from the nuclei isolated from the cells grown at the early mid log-phase, at the G2 phase (60 min) and at the G1 phase (150 min), after HST. The proteins were studied by comparing the spots separated by isoelectric point, 10-20% gradient SDS two-dimensional electrophoresis. As a result, in comparison with the intranuclear protein at the log-phase, the proteins at the G2 phase showed a marked increase, but with no great change in the electrophoretic pattern. Meanwhile, the proteins at the G1 phase differed greatly from those at the G2 phase not only in the quantitative changes, but in the electrophoretic patterns. It is considered that the level of the accumulation of the nuclear proteins which should be closely involved in cell division must increase markedly at the G2 phase and decrease at the G1 phase. We confirmed the presence of four proteins: pI 5.8 MW 68 kDa, pI 6.1 MW 75 kDa, pI 8.6 MW 48 kDa and pI 6.6 MW 57 kDa, and then prepared monoclonal antibodies using these nuclear proteins as antigens. Among them, the antibody (IgM) against the pI 8.6 MW 48 kDa polypeptide (p48) was recognized the nuclei by indirect immunofluorescence in ancellular system at the S, G2 and the mid-M phases. However, nuclei at the late M and G1 phases were not stained.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

TGF-beta upregulates interleukin 6 production by rat glomerular epithelial cells in vitro.

BACKGROUND: Glomerular epithelial cells (GECs) play an important role in maintaining normal glomerular permselectivity in vivo. Recent in-vitro studies have suggested that GECs are able to secrete substances which may modulate glomerular injury. Interleukin 6 (IL-6) has been shown to be a potent mediator of glomerular injury. It is also known that IL-6 could be produced by various cells. METHODS: IL-6 production by rat GECs in culture was examined in this study. IL-6 bioactivity in conditioned medium collected from cultured GECs (GEC-CM) was measured using IL-6 dependent murine hybridoma cell line, namely B9 cells. IL-6 gene expression by GECs was analysed by reverse transcriptase polymerase chain reaction (RT-PCR). Effects of recombinant IL-6 on the proliferation of GECs and type IV collagen secretion by GECs were evaluated to examine the possible role of GECs derived IL-6. RESULTS: GEC-CM stimulated B9 cells growth in a dose dependent fashion. The mitogenic activity was inhibitable by anti-murine IL-6 antibody. De-novo synthesis of IL-6 was suggested by the demonstration of IL-6 mRNA by GECs using the RT-PCR. Secretion of IL-6 by GECs was increased by transforming growth factor beta but not by IL-1 beta. Recombinant murine IL-6 stimulated GECs growth and their type IV collagen secretion. CONCLUSIONS: These results indicate that rat GECs could produce IL-6 which may modulate glomerular inflammation and that IL-6 may function as an autocrine factor for GECs.

Animals↗

[A study of skin surface temperature in patients with unilateral cerebral infarction--with special reference to central autonomic regulation of skin vasomotor response].

Skin surface temperature was examined using thermography in 26 patients with unilateral ischemic cerebrovascular disease (5 with pontine lesions, 5 with lateral medullary lesions and 16 with hemispheric lesions). Three of the 5 patients with pontine lesions and 4 of the 5 with medullary lesions showed hemihyperthermia on the ipsilateral body surface. However, the face showed no impairment with pontine lesions, whereas it appeared as a hyperthermic area with medullary lesions. Ten of 11 patients with lesions of the internal capsule or putamen had hypothermia on the contralateral body surface except for the face. All the patients with thalamic lesions showed no skin temperature asymmetry. These observations suggest the following: (1) sympathetic skin vasomotor fibers descend through the ipsilateral side of the brainstem; (2) at the level of the medulla, skin vasomotor fibers innervating the body trunk and limbs and those innervating the face descend contiguously, while at the level of the pons the two fiber groups descend separately; (3) hypothermia in patients with cerebral infarction could be explained by interruption of the inhibitory neural pathway that controls vasomotor function on the contralateral side of the body; (4) these inhibitory pathways descend in the vicinity of the pyramidal tract.

Adult↗

[Cardiovascular alpha-, beta 1- and beta 2-adrenoceptor functions in neurogenic orthostatic hypotension].

It has been believed that patients with neurogenic orthostatic hypotension (NOH) usually develop denervation supersensitivity of cardiovascular alpha-, beta 1- and beta 2-adrenoceptors, because the majority studies have shown augmented cardiovascular responses to intravenously given noradrenaline (NA) or isoprenaline (IP) in these patients. This view, however, leaves room for discussion. First, drugs were administered by means of drip infusion method in most of the previous studies. Since this method necessarily provokes baroreflex, which is buffering fluctuations in blood pressure and heart rate, the results may reflect diminished baroreflex rather than denervation supersensitivity. Second, adrenoceptor functions are modulated by multiple factors, such as ageing, thyroid hormone and chronic inflammation. It is, thus, inappropriate to explain the whole picture of functional change in adrenoceptors by the denervation mechanism only. In order to look over the cardiovascular adrenoceptor functions in NOH, we performed bolus infusion tests of NA and IP on the patients. The subjects comprised 7 cases of NOH with pre-ganglionic sympathetic deficit (NOH-I), 6 cases with post-ganglionic deficit (NOH-II) and 15 healthy controls. NOH-I group included 6 patients with multiple system atrophy and one with Parkinson disease, while NOH-II group consisted of 3 patients with idiopathic orthostatic hypotension (pure autonomic failure) and 3 with diabetic autonomic neuropathy. Both NA and IP infusion tests were carried out under the continuous measurement of blood pressure and heart rate. In NA test, different bolus doses (0.01, 0.02, 0.05 and 0.1 microgram/kg) of NA were intravenously administered, and a degree of subsequent rise in mean blood pressure was used as an index for alpha-adrenoceptor function. IP test was performed in the same manner, and an increase in heart rate and a fall in mean blood pressure in response to the drug (0.001, 0.002 and 0.005 microgram/kg) were measured as indices for beta 1- and beta 2-functions, respectively. A rise in blood pressure following the administration of any dose of NA did not statistically differ among three groups. An increase in heart rate in IP test was generally lower in both NOH groups, and a significant difference was obtained between NOH-I and control when a given dose was 0.005 microgram/kg) (p < 0.02). A fall in blood pressure in IP test was significantly greater in NOH-I compared to control when doses were 0.002 and 0.005 microgram/kg (p < 0.02 and 0.01, respectively). It was also greater in NOH-II than in control when a dose was 0.002 microgram/kg (p < 0.01). In disagreement with most of the previous studies, the present results suggest that alpha-adrenoceptor function is hardly altered, beta 1-function is suppressed, and beta 2-function is augmented in NOH.

Adult↗

Aptameric inhibition of in vitro DNA polymerization by phosphorothioate oligonucleotides.

DNA polymerization in the presence of phosphorothioate oligonucleotides (S-oligomers) was investigated. Oligonucleotides consisting of three or four consecutive guanosine residues (G4 and G3, respectively) inhibited chain elongation by AMV reverse transcriptase or Sequenase (polymerase function of T7 DNA polymerase). S-oligomers bearing G4 caused greater inhibition of chain elongation by both enzymes than those with G3. AMV reverse transcriptase was more susceptible to S-oligomers bearing consecutive guanosines than was Sequenase. Electrophoresis on a polyacryl amide gel revealed that G4 and G3-oligomers formed high-order polymeric complexes, and that S-oligomers with G4 formed much more complex than those with G3.

Base Sequence↗

[Clinical study of bronchial asthma in adult, intractable asthmatics after introduction of guideline therapy].

Introduction of Guideline for asthma treatment proposed by the committee of Japanese allergology have a tremendous impact on patients with bronchial asthma. Intractable asthmatics who have had to take some oral steroid to overcome disease severity, may have also some merit by this treatment, so that some of them might be no longer considered as intractable asthmatics. To clarify this, multicenter study was conducted. In this study, a case who have had more than 5 mg of prednisolone and/or 800 mu g of beclomethasone dipropionate throughout the year, was diagnosed as intractable asthmatics. In 845 case, 14.7%, 123 cases were diagnosed as intractable. These cases were significantly to be non-atopic and adult onset. Also, they have a significant tendency to be deteriorated by infection and careless drug administrations. Using the multiquantification method to examine the most powerful factor on intractable asthmatics, type of asthmatics was the most important and the past history of severe attack was the second. When intractable asthmatics diagnosed mainly by their BDP usage (BDP-intractable) were compared with intractable diagnosed by oral PSL (PSL-intractables), BDP-intractables were significantly atopic compared to PSL-intractables.

Asthma↗

Molecular cloning of the complementary DNA and gene that encode mouse brain natriuretic peptide and generation of transgenic mice that overexpress the brain natriuretic peptide gene.

Brain natriuretic peptide (BNP) is a cardiac hormone that occurs predominantly in the ventricle. To study the roles of BNP in chronic cardiovascular regulation, we isolated mouse BNP cDNA and genomic clones, and generated transgenic mice with elevated plasma BNP concentration. The mouse BNP gene was organized into three exons and two introns. Two BNP mRNA species were identified, which were generated by the alternative mRNA splicing. The ventricle was a major site of BNP production in mice. Mouse preproBNP was a 121- (or 120-) residue peptide, and its COOH-terminal 45-residue peptide was the major storage form in the heart. Transgenic mice carrying the human serum amyloid P component/mouse BNP fusion gene were generated so that the hormone expression is targeted to the liver. In the liver of these mice, considerable levels of BNP mRNA and peptide were detected, reaching up to 10-fold greater than in the ventricle. These animals showed 10- to 100-fold increase in plasma BNP concentration accompanied by elevated plasma cyclic GMP concentration, and had significantly lower blood pressure than their nontransgenic littermates. The present study demonstrates that these mice provide a useful model system with which to assess the roles of BNP in cardiovascular regulation and suggests the potential usefulness of BNP as a long-term therapeutic agent.

Alternative Splicing↗

Molecular cloning of hamster brain and atrial natriuretic peptide cDNAs. Cardiomyopathic hamsters are useful models for brain and atrial natriuretic peptides.

Brain and atrial natriuretic peptides (BNP and ANP) are cardiac hormones with diuretic, natriuretic, and vasodilatory activities. Cardiomyopathic hamsters are widely used animal models of heart failure. Due to the structural divergence of BNP among species, examination on pathophysiological roles of BNP using cardiomyopathic hamsters is so far impossible. We therefore isolated hamster BNP and ANP cDNAs, and investigated synthesis and secretion of these peptides in normal and cardiomyopathic hamsters. The COOH-terminal 32-residue peptide of cloned hamster preproBNP with 122 amino acids, preceded by a single arginine residue, supposedly represents hamster BNP showing < 50% homology to rat BNP. Alpha-hamster ANP, 28-residue peptide, is identical to alpha-rat ANP. In hamsters, BNP and ANP occur mainly in the ventricle and the atrium, respectively. The 32-wk-old hypertrophic cardiomyopathic BIO14.6 strain exhibited ventricular hypertrophy. The 32-wk-old dilated cardiomyopathic BIO53.58 strain remained at the stage without apparent heart failure. In BIO14.6 and BIO53.58 strains at this age, ventricular BNP and ANP gene expressions are augmented, and the plasma BNP concentration is elevated to 136 and 108 fmol/ml, respectively, three times greater than the elevated plasma ANP concentration, which well mimics changes of the plasma BNP and ANP concentrations in human heart failure. Cardiomyopathic hamsters, therefore, are useful models to investigate the implication of BNP in human cardiovascular diseases.

Amino Acid Sequence↗

Optically active antifungal azoles. III. Synthesis and antifungal activity of sulfide and sulfonamide derivatives of (2R,3R)-2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2-b utanol.

In an effort to find potent antifungal agents, optically active sulfur-containing triazole derivatives, sulfides (3) and sulfonamides (4), were prepared and evaluated for antifungal activity against Candida albicans in vitro and in vivo. The sulfides (3) were prepared by the reaction of (2R,3R)-2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl )-2-butanol (1) with various heteroarylmethyl chlorides in the presence of sodium methoxide. The sulfonamides (4) were synthesized starting from the disulfide (15) in three steps including oxidation of the corresponding sulfenamides (17). Some of the sulfur-containing triazole derivatives (3, 4) showed strong protective effects against candidosis in mice.

Antifungal Agents↗

Modification of plasmid and bacteriophage DNA by aromatic amines: effects on survival, template activity, and mutagenicity.

The carcinogenic and mutagenic effects of the aromatic amines are believed to depend on their covalent modification of DNA, primarily through the formation of adducts at C8 of guanine. The actual biologic and biochemical responses to these adducts can be envisioned as the consequence of the abilities of the cell to repair the lesions, with or without fidelity, and the introduction of errors through bypass of the adducts by polymerases. A key question is whether changes in DNA sequence arise through the participation of common repair processes that cause mutations independent of adduct structure. Alternatively, do mutations arise through miscoding during polymerase bypass at the site of the adducts and are, therefore, more likely to produce sequence changes that are more characteristic of adduct structure? This question has been approached using single, site-specific, or randomly introduced aromatic amine DNA adducts in bacterial cells, and in vitro studies with DNA polymerases that employ site-specifically modified templates. The results of both approaches demonstrate that these adducts are distinguished readily by virtue of their structures, thus supporting the conclusion that mutagenic effects of the aromatic amines arise from their structures rather than from their triggering a common inaccurate repair response.

Amines↗

[The gamma delta T-cell receptors in sarcoidosis].

T-cells recognize specific antigen (s) through the T-cell antigen receptors (TCR). gamma delta T-cells compose a minor population of the peripheral blood lymphocytes (PBL). These lymphocytes play a central role in recognizing the mycobacterial antigens and granuloma formation in tuberculosis and leprosy. Significant increase of gamma delta T-cells in PBL is observed in a subgroup of sarcoidosis. The majority of gamma delta T-cells showed V gamma 9/V delta 2 recombination, which is common in normal blood. To evaluate the clonality of the increased gamma delta T-cells in PBL, several V gamma 9 and V delta 2 cDNA clones were established. Analysis of V-J junctional sequences of V gamma 9 clones revealed oligoclonal expansion in some cases. Most of V delta 2 clones showed unique sequences. Although no clonal expansion of gamma delta T-cells were observed, TCR-gamma chain might recognize limited numbers of putative antigens in sarcoidosis.

Amino Acid Sequence↗