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Biomedical subjects

J Shimada

Publications and source records attributed to J Shimada.

At least 109 records · Page 6Linked to original sources
PubMed1995

[A successful usage of latissimus dorsi muscle flap in the surgery of synchronous gastric and pulmonary double cancer in an elderly patient--a case report].

A 77-year-old man, with both an advanced gastric cancer Borrman IV type (CME) S2N1P0 M0 stage II and lung cancer of left upper lobe pT3N1M0 stage IIIA, simultaneously received total gastrectomy with R2 lymph node dissection, and Roux-Y reconstruction, and left upper lobectomy with R2 lymph node dissection combined with partial pericardiectomy. A latissimus dorsi muscle flap with thoracodorsal artery and vein was used for covering the intrathoracic esophagojejunostomy, repairing of the pericardial defect and separating the thoracic cavity from the abdominal cavity. Postoperative esophagograms showed a leakage, which was localized by the muscle flap coverage without extensive spread. The leakage healed spontaneously after a left sub-diaphragmatic drainage. Our experience described here indicates that a latissimus dorsi muscle flap coverage is a useful operative method for double cancers of the lung and stomach requiring intrathoracic procedures.

Aged↗
PubMed1995

Closure of leaks by fibrin gluing. Effects of various application techniques and temperatures.

This study was performed to determine the differences in covering power obtained with fibrin gluing using three different methods, layered, mixing, and spraying. The experimental system consisted of a 2 x 2 cm plastic plate with a hole 1 mm in diameter, a plastic syringe, and a digital manometer. The internal pressure of the syringe barrel was measured with the digital manometer. Five minutes after fibrin glue membranes (1 mm in thickness) had been prepared on the plastic plate with the layered, mixing, or spray method, the plunger of the syringe was pushed slowly, and the maximum internal pressure in the syringe barrel was measured, just before the breakage of the membrane. Experiments were performed five times at each four temperatures, 12 degrees C, 17 degrees C, 22 degrees C and 37 degrees C. Covering power of fibrin glue membranes (units: mmHg; atmospheric pressure 760 mmHg) were as follows: 1) Layered method (12 degrees C: 810.0 +/- 68.6, 17 degrees C: 769.0 +/- 10.2, 22 degrees C: 812.0 +/- 112.4, 37 degrees C: 773.6 +/- 24.4). 2) Mixing method (12 degrees C: 956.6 +/- 219.3, 17 degrees C: 972.4 +/- 243.5, 22 degrees C: 1045.2 +/- 233.0, 37 degrees C: 1059.0 +/- 220.2). 3) Spray method (12 degrees C: 1010.0 +/- 231.1, 17 degrees C: 1144.4 +/- 170.6, 22 degrees C: 1148.0 +/- 234.7, 37 degrees C: 1250.0 +/- 111.8).(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Topical↗
PubMed1995

Everninomicin, a new oligosaccharide antibiotic: its antimicrobial activity, post-antibiotic effect and synergistic bactericidal activity.

Antimicrobial activity of everninomicin (SCH) 27899) in comparison with two glycopeptides (vancomycin, teicoplanin) and six beta-lactam agents was evaluated against recent clinical isolates of Gram-positive bacteria. Everninomicin showed the highest activity against the species tested and MICs90% of everninomicin against Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecalis, Enterococcus faecium and Clostridium difficile were 0.1, 0.1, 0.2, 0.39, 0.1 microgram/ml, respectively. MICs90% of everninomicin against methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE) were 0.78 microgram/ml. Laboratory induced resistance to everninomicin in strains of S. aureus and E. faecalis occurred in a stepwise manner and at a very slow rate. Post-antibiotic effect against strains of S. aureus and E. faecalis were 1.8 and 2.6 h, respectively, and a little longer than that of vancomycin. Adherence to glass surface of an MRSA strain was strongly repressed by the addition of sub MIC of everninomicin in combination with fosfomycin.

Aminoglycosides↗
PubMed1995

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↗
PubMed1994

Anti-human immunodeficiency virus type 1 activity of phosphorothioate analogs of oligodeoxynucleotides: penetration and localization of oligodeoxynucleotides in HIV-1-infected MOLT-4 cells.

Phosphorothioate antisense oligodeoxynucleotide against HIV-1 rev (S-ODN-rev) inhibits virus-induced cytopathic effects (CPE) in acute infection and inhibits the expression of HIV-1 core protein, p24, in chronically infected cells in vitro. HIV-1 reverse transcriptase activity was not affected by S-ODN-rev at the high concentrations of 5-25 microM, which were 250-1250 times higher than the concentration required to achieve 100% HIV-1-induced CPE inhibition. [32P]-labeled S-ODN-rev was rapidly uptaken by MOLT-4 cells, whereas [32P]-SO-ODN-rev and [32P]-O-ODN-rev were not. In the observation of FITC-S-ODN-rev-treated MOLT-4 cells by a confocal laser scanning microscope, diffuse fluorescence was apparently observed in the cytoplasm. Interestingly, fluorescence signals were accumulated in the nuclear region of chronically infected MOLT-4/HIV-1 cells 60 min after incubation. FITC-labeled homooligomer, FITC-S-dC20 and FIT-C-S-dT20, also accumulated in the nucleus of MOLT-4/HIV-1 cells, but weak fluorescence was observed on the cell membrane and in the cytoplasm of the FITC-S-random treated MOLT-4/HIV-1 and MOLT-4 cells.

Cell Line, Transformed↗
PubMed1994

Possible physiological role of endogenous adenosine in defecation in rats.

Evacuated feces after intraperitoneal administration of selective adenosine receptor antagonists were evaluated in rats. The selective adenosine A1 receptor antagonists, 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) (100-300 micrograms/kg i.p.) and (R)-7,8-dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1 -i]purin- 5(4H)-one (KF20274) (30-300 micrograms/kg i.p.), significantly increased defecation, whereas the selective adenosine A2 receptor antagonist 4-amino-8-chloro-1-phenyl[1,2,4]triazolo[4,3-a]quinoxaline (CP-66,713) failed to cause a significant increase at up to 10 mg/kg i.p. The defecation caused by DPCPX (100 micrograms/kg) was markedly alleviated by (2S)-N6-(2-endo-norbornyl)adenosine ((S)-ENBA) (30-300 micrograms/kg s.c.), a selective adenosine A1 receptor agonist, but not influenced by 2-[p-(2-carboxyethyl)phenethylamino]-5'-N-ethylcarboxamidoadenosin e (CGS 21680) (30-1000 micrograms/kg s.c.), a selective adenosine A2 receptor agonist. These results suggest that endogenous adenosine plays a physiological role in sustained inhibition of defecation via adenosine A1 receptors.

Adenosine↗
PubMed1994

KF17837 ((E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine), a potent and selective adenosine A2 receptor antagonist.

8-(3,4-Dimethoxystryryl)-1,3-dipropyl-7-methylxanthine exhibited high affinity and selectivity for adenosine A2A receptors in binding assay using rat striatal A2A receptors labeled with [3H]2-[p-(2-carboxyethyl)-phenethylamino]-5'-N-ethylcarboxamido adenosin e (CGS21680). The affinity was stereo selective: the E isomer, KF17837, showed a Ki value of 1.0 +/- 0.057 nM for the A2A receptors, whereas the Z isomer showed much lower affinity. KF17837 had 62-fold selectivity for the A2A receptors versus rat forebrain A1 receptors labeled with [3H]N6-cyclohexyladenosine (CHA). KF17837 was rapidly photoisomerized to form a stable equilibrium mixture (18% E - 82% Z), KF17837S, which showed Ki values of 7.9 +/- 0.055 nM and 390 +/- 68 nM for the A2A and A1 receptors, respectively. The inhibition type was competitive for [3H]CGS21680 binding. In rat pheochromocytoma PC12 cells KF17837S antagonized cAMP accumulation induced by 1 microM CGS21680 via the A2A receptors, with an IC50 value of 53 +/- 10 nM. cAMP accumulation induced by 10 microM 5'-N-ethylcarboxamidoadenosine via the A2B receptors in Jurkat cells (human T-cell line) was inhibited by KF17837S with an IC50 value of 1500 +/- 290 nM. These results indicate that KF17837S (and hence KF17837) is a highly potent and selective adenosine A2A receptor antagonist.

Adenosine↗
PubMed1994

KF17837: a novel selective adenosine A2A receptor antagonist with anticataleptic activity.

KF17837 is a novel selective adenosine A2A receptor antagonist. Oral administration of KF17837 (2.5, 10.0 and 30.0 mg/kg) significantly ameliorated the cataleptic responses induced by intracerebroventricular administration of an adenosine A2A receptor agonist, CGS 21680 (10 micrograms), in a dose-dependent manner. KF17837 also reduced the catalepsy induced by haloperidol (1 mg/kg i.p.) and by reserpine (5 mg/kg i.p.). These anticataleptic effects were exhibited dose dependently at doses from 0.625 and 2.5 mg/kg p.o., respectively. Moreover, KF17837 (0.625 mg/kg p.o.) potentiated the anticataleptic effects of a subthreshold dose of L-3,4-dihydroxyphenylalanine (L-DOPA; 25 mg/kg i.p.) plus benserazide (6.25 mg/kg i.p.). These results suggested that KF17837 is a centrally active adenosine A2A receptor antagonist and that the dopaminergic function of the nigrostriatal pathway is potentiated by adenosine A2A receptor antagonists. Furthermore, KF17837 may be a useful drug in the treatment of parkinsonism.

Adenosine↗
PubMed1994

Inhibition of the renal excretion of tazobactam by piperacillin.

A 1:4 by weight of combination of tazobactam, a new beta-lactamase inhibitor, and piperacillin, is now under development in Japan. After bolus iv administration of the combination to beagle dogs, piperacillin both significantly raised the area under plasma concentration time curve (AUC0 approximately infinity) and significantly decreased the total body clearance (Cltot) of tazobactam. The percentage binding of tazobactam and piperacillin to dog and human serum protein was the same for the combination as for the individual compounds. Piperacillin significantly decreased the renal clearance (Clr) and the clearance ratio (Cr) of tazobactam in dogs. Further, probenecid significantly decreased Clr of both tazobactam and piperacillin, and the Cr of tazobactam and piperacillin approximately reached unity. These results indicate that piperacillin inhibits the renal excretion of tazobactam. Both tazobactam and piperacillin are secreted by a tubular anion transport system which is identical to the probenecid secretion system.

Animals↗
PubMed1994

Effect of topical preparation of mycophenolic acid on experimental allergic contact dermatitis of guinea-pigs induced by dinitrofluorobenzene.

The effects of a topical preparation of mycophenolic acid on the experimental allergic contact dermatitis induced by dinitrofluorobenzene was investigated. Visual assessment of skin reactions showed significant efficacy of a topical preparation of mycophenolic acid. This efficacy appeared from the early stage and endured up to 3 days. Morphological changes in the epidermis and dermis layers of animals treated with a mycophenolic acid cream were moderate compared with that in animals treated with vehicle only. In particular, hyperkeratosis was strongly suppressed. Since suppression of inflammatory cell infiltration was also observed, this efficacy might reach to the epidermis and dermis layer.

Administration, Topical↗
PubMed1994

Overview of a new carbapenem, panipenem/betamipron.

Carbapenems are beta-lactam antibiotics with a broad antibacterial spectrum and a potent bactericidal activity against both aerobic and anaerobic Gram-positive and Gram-negative organisms. They have been widely investigated in the past, and imipenem/cilastatin (IPM/CS), panipenem/betamipron (PAPM/BP), meropenem (MEPM) and biapenem (BIPM) are presently in clinical use or under trial. Of the carbapenems, imipenem is not readily hydrolysed by microbial beta-lactamase but is hydrolysed to open the beta-lactam ring by DHP-I from kidney and other tissues. In order to achieve greater stability to the enzyme and to prolong the action of the carbapenem in vivo, the co-administration of CS with IPM or the attainment of the chemical construction of the 1-beta methylcarbapenem derivatives in the case of MEPM and BIPM have been performed. However, some difference was found in the DHP-I activity with these carbapenems, but there was no significant difference in the pharmacokinetic parameters: AUC, CLtot, t1/2 and MRT except urinary clearance after administration of these compounds to humans. Considering that MRT as the amount of the antibiotics retained in the body is a clinically important parameter, the structural susceptibility of the carbapenems to the decomposition by DHP-I was suggested to have no clinically meaningful correlation with the pharmacokinetics of these compounds.

Alanine↗
PubMed1994

[Problems of epidural droperidol administration].

We describe three cases of extrapyramidal reactions apparently caused by epidural administration of droperidol. These patients suffered from chronic pain and was treated with epidural lidocaine and droperidol. Two patients received continuous administration of droperidol, and experienced acute dystonia and another after a single dose, developed akathisia. Adverse reactions occurred at 15, 20 and 24 hours after the administration of droperidol. The first patient received droperidol 6 mg, the second 8.5 mg and the third 5 mg. We consider that extrapyramidal reactions are due to overdoses because the patients who had been given less than 2.5 mg of droperidol a day, showed no adverse reaction. Although we use higher doses with NLA or for management of fever than with epidural administration of droperidol, we seldom encounter cases of side effects with droperidol. Epidurally administrated droperidol spreads rostral within the neuraxis and causes delayed extrapyramidal reactions as epidural morphine develops delayed respiratory depression. We must be careful in caring patients suffering from chronic pain with continuous epidural administration of droperidol.

Adult↗
PubMed1994

Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes.

The potential of 8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-[3H] methylxanthine ([3H]Kf17837S) as a highly selective antagonist radioligand for the adenosine A2A receptor was examined and compared with the properties of the adenosine A2A receptor agonist radioligand 2-[p-(2-[3H]carboxyethyl)phenethylamino]-5'-N-ethyl- carboxamidoadenosine ([3H]CGS21680). [3H]KF17837S specific binding to rat striatal membranes was saturable and reversible. Saturation studies showed that the binding of [3H]KF17837S occurred at a single site, with high affinity (Kd, 7.1 +/- 0.91 nM) and limited capacity (Bmax, 1.3 +/- 0.23 pmol/mg of protein). Adenosine receptor antagonist ligands competed with the binding of 1 nM [3H]KF17837S with the following order of activity: CGS15943 > KF17837S > N-[2-(dimethylamino)ethyl]-N-methyl- 4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)benzenesul fonamide > or = xanthine amine congener > 8-cyclopentyl-1,3-dipropylxanthine > 8-(noradamantan-3-yl)-1,3-dipropylxanthine > caffeine. Adenosine receptor agonists inhibited [3H] KF17837S binding in the following order: 5'-N-ethylcarboxamidoadenosine > or = CGS21680 > 2-phenylaminoadenosine > or = (R)- N6-phenylisopropyladenosine > N6-cyclopentyladenosine > (S)- N6-phenylisopropyladenosine. The Ki values of the antagonists for [3H]KF17837S binding and the rank order of potency were similar to those for [3H]CGS21680 binding. The affinities of the agonists were lower with [3H]KF17837S binding than with [3H] CGS21680 binding. However, a strong positive correlation (r = 0.98) was observed between the pharmacological profiles for these two radioligand assays. The inhibition curve for CGS21680 was best fitted to a two-component binding model and addition of GTP shifted the inhibition curve to the right, suggesting that [3H]KF17837S labeled two agonist coupling states. Other pharmacological agents had negligible affinities for the [3H]KF17837S binding site. Autoradiographic study of [3H]KF17837S binding using rat brain sections revealed that the binding site was highly enriched in the striatal region. These data indicate that [3H] KF17837S labels the adenosine A2A receptor in rat brain.

Adenosine↗