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Biomedical subjects

Y Takase

Publications and source records attributed to Y Takase.

At least 55 records · Page 3Linked to original sources
PubMed1997

Hepatic coma recovered after interventional obliteration for ileocecal-inferior vena cava shunt--report of one case.

We performed interventional angiography (IVA) in a patient with liver cirrhosis (LC) and hepatoma (HCC) who experienced repeated attacks of unconsciousness due to hyperammonemia caused by ileocecal-inferior vena cava (IC-IVC) shunt and succeeded in the treatment. We report the results below. The patient, 53-year-old male, underwent endoscopic injection sclerotherapy for esophageal varix due to LC followed by splenectomy for pancytopenia in 1986. He made good progress. However intraarterial anticancer therapy was conducted for HCC in 1994. From that time hepatic coma began to appear and its frequency gradually increased. Hepatic coma occurred once every 3 weeks from June 1996. He was thus admitted to our hospital. Hematobiochemical testes showed that ammonia level was 297 mcg/dl. Albumin 2.8d/dl, and Total-Bilirubin 10.78 mg/dl. Arterioportography from superior mesenteric artery showed most of portal blood flowed away from the liver though the ileocolic vein to IVC. We decided to conduct IVA for treatment. Specially, a 6Fr balloon catheter was inserted from the right inguinal region into a shunt to the portal vein though IVC by the Seldinger technique. The balloon was inflated in the shunt to close the shunt. Six ml of 5% ethanolamime oleate with iopamidol was injected because retrograde angiography showed that iopamidol was flowed out via testicular vein to IVC. The balloon catheter was retained for 24 hours. Angiography, conducted from the catheter again 24 hours later, showed that the shunt was occluded, blood ammonia level was 71 mcg/dl after occlusion. Hepatic coma was not observed after treatment. We encountered a very rare case who repeated hepatic comas due to IC-IVC shunt and recovered dramatically after IVA.

Angiography↗
PubMed1996

Primary sclerosing cholangitis associated with increased peripheral eosinophils and serum IgE.

Symptoms of cholestasis, including epigastralgia, fever, and jaundice, with marked increases in peripheral eosinophils and serum IgE in a 20-year-old man are reported here. Endoscopic retrograde cholangio-pancreatography (ERCP) detected constrictions of the bile ducts, compatible with primary sclerosing cholangitis (PSC). The symptoms and blood parameters of liver dysfunction were associated with the degree of eosinophilia and high serum IgE levels. During corticosteroid therapy, all of these parameters improved, and morphologic improvements of the bile ducts were also observed. The pathogenesis of PSC may be explained, in part, by the concept of hypereosinophilic syndrome or allergic reaction.

Adult↗
PubMed1996

Thrombin in the synovial fluid of patients with rheumatoid arthritis mediates proliferation of synovial fibroblast-like cells by induction of platelet derived growth factor.

OBJECTIVE: To investigate the clotting and fibrinolytic activities in synovial fluid (SF) from patients with rheumatoid arthritis (RA) and to examine the role of thrombin in synovial hyperplasia. METHODS: We measured the amounts of thrombin-antithrombin-III complex (TAT), antithrombin-III (AT-III), thrombin, plasminogen, alpha 2-plasmin inhibitor (alpha 2-PI), and plasmin-alpha 2-antiplasmin complex (PAP) in SF of 20 patients with RA and 16 patients with osteoarthritis (OA). The proliferative response of synovial fibroblast-like cells to thrombin was measured using [3H] thymidine incorporation. Expression of platelet derived growth factors (PDGF) in conditioned medium was analyzed using a Western blot method, and expression of the mRNA of PDGF and their receptors was analyzed by reverse transcription polymerase chain reaction. RESULTS: The amounts of clotting factors (TAT, AT-III) and fibrinolytic factors (plasminogen, alpha 2-PI, and PAP) were significantly higher in the patients with RA than in patients with OA (p < 0.01). Moreover, SF thrombin concentrations of patients with RA correlated significantly with erythrocyte sedimentation rates (rs = 0.751, p < 0.01) and serum C-reactive protein concentrations (rs = 0.531, p < 0.05). Thrombin exhibits mitogenic activity toward synovial fibroblast-like cells in vitro, and this mitogenic activity is associated with an increase in the expression of mRNA of both PDGF-alpha receptor and PDGF-beta-receptor. CONCLUSION: The high levels of thrombin activity in the SF of patients with RA and strong mitogenic activity of thrombin toward the synovial fibroblast-like cells suggest that thrombin plays an important role in the pathogenesis of RA.

Adult↗
PubMed1995

[In vitro studies on the combined effects of arbekacin and fosfomycin on methicillin-resistant Staphylococcus aureus].

We investigated the bactericidal activity and post-antibiotic effect (PAE) of arbekacin (ABK) and fosfomycin (FOM) on clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) strain 1936, and the morphological changes of the bacterium. Both antibiotics were used in combination at concentrations lower than their respective MICs. The following results were obtained. 1. When the bacterium was simultaneously exposed to ABK and FOM, growth inhibition and a PAE longer than that effected by ABK alone were observed. 2. When exposed to ABK after treatment with and removal of FOM, bactericidal activity was stronger than that obtained when exposed to ABK alone. However, no increase in bactericidal activity was obtained when exposed to FOM after pretreatment with ABK. 3. Transmission electron microscopy revealed that, when the bacterium was exposed to ABK after treatment with and removal of FOM, large bacterial cells with cross walls at irregular sites and lysed cells showing destruction of the cell wall at the site of bacterial segmentation caused by ABK and FOM. These results demonstrated that ABK in combination with FOM shows stronger bactericidal activity against MRSA in vitro than ABK alone.

Aminoglycosides↗
PubMed1995

A selective type V phosphodiesterase inhibitor, E4021, dilates porcine large coronary artery.

We investigated the inhibitory effects of a newly synthesized compound, sodium 1-[6-chloro-4-(3,4-methylenedioxybenzyl)-aminoquinazolin-2-y l]piperidine-4- carboxylate sesquihydrate (E4021), on five phosphodiesterase (PDE) isozymes isolated from porcine aortic smooth muscle. E4021 specifically inhibited type V phosphodiesterase (cyclic guanosine monophosphate [cGMP]-specific PDE) in a competitive manner. A comparison of the inhibitory profiles of zaprinast and E4021 indicated that E4021 is 100 times more potent and selective as a type V PDE inhibitor. E4021 caused a significant and sustained increase in the cGMP level in endothelium-denuded porcine coronary artery, but it had no effect on the cAMP level. This compound had a relaxant effect in porcine coronary artery precontracted by prostaglandin F2 alpha in the absence of endothelial cells and relaxed it more markedly in the presence of endothelial cells. E4021 had a synergistic effect with nitroglycerin in both the increase in cGMP level and the relaxant effect in isolated porcine coronary artery. E4021 caused a dose-dependent dilation of the large epicardial coronary artery, with a reduction in mean pulmonary arterial pressure, in conscious pigs instrumented chronically with a pair of piezoelectric crystals. These results suggest that the highly selective and potent inhibitor of type V phosphodiesterase E4021 causes relaxation of the large coronary artery via an increase in the cGMP level.

Animals↗
PubMed1995

Idiopathic thrombocytopenic purpura complicated by intracranial hemorrhage in a 78-year-old male.

A 78-year-old male was admitted to our hospital with cutaneous hemorrhage, aphasia and somnolence. On physical examination, he appeared drowsy and complained of epistaxis and multiple purpura. His platelet count was 8,000/microliters with a high level of PA-IgG, but the coagulation time was normal. A CT scan of the head revealed a left temporal and right frontal hemorrhage. Bone marrow aspiration revealed abundant megakaryocytes. He was diagnosed as having idiopathic thrombocytopenic purpura with intracranial hemorrhage. He was treated with prednisolone and azathioprine in addition to platelet infusions and high doses of gamma-globulin. After two months of treatment, the platelet count had risen to 40,000/microliters and his symptoms had subsided.

Aged↗
PubMed1994

Determination of a novel and potent cyclic GMP phosphodiesterase inhibitor, 4-([3,4-(methylenedioxy)-benzyl]amino)-6,7,8-trimethoxyquinazoline, in dog plasma by high-performance liquid chromatography.

A simple and accurate method for determining levels of 4-([3,4-(methylenedioxy)benzyl]amino)-6,7,8-trimethoxyquinazoline, a novel cyclic GMP phosphodiesterase inhibitor, in dog plasma was developed. This method involves extraction with diethyl ether and reversed-phase high-performance liquid chromatography with ultraviolet detection. Regression analysis showed that the method was linear over the range 1.0-1000 ng/ml. The method was employed for the analysis of plasma samples in a preliminary pharmacokinetic study in beagle dogs.

3',5'-Cyclic-GMP Phosphodiesterases↗
PubMed1994

Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.

We synthesized various 4-[[3,4-(methylenedioxy)benzyl]amino]quinazolines substituted at the 5- to 8-positions and evaluated their inhibitory activities toward cyclic GMP phosphodiesterase (cGMP-PDE) from porcine aorta. Monosubstitution at the 6-position was essential for the inhibitory activity, and the preferred substituents were compact and hydrophobic: methoxy (3b, IC50 = 0.23 microM), methyl (3c, 0.10 microM), chloro (3d, 0.019 microM), thiomethyl (3f, 0.031 microM), and cyano (3p, 0.090 microM) groups. Compounds 3b-d,f,p lacked inhibitory activity toward other PDE isozymes (all IC50 values > 100 microM), and their relaxing activities in porcine coronary arteries were well correlated with the inhibitory activities toward cGMP-PDE (r = 0.88, p < 0.05). One of these compounds, 3b, elevated the intracellular cGMP level in isolated porcine coronary arteries without causing any change in the cAMP level. We consider that this series of compounds dilates coronary arteries via potent and specific inhibition of cGMP-PDE.

3',5'-Cyclic-GMP Phosphodiesterases↗
PubMed1994

[Antibacteriological activities of arbekacin and vancomycin against strains of MRSA].

The activities of arbekacin (ABK) and vancomycin (VCM) against MRSA were compared, and the results are as follows. 1. In antibacterial activities (MIC value) against 142 strains of MRSA, MIC50 of ABK was two times less than that of VCM. MIC90's were both 1.56 micrograms/ml. 2. ABK was also superior to VCM in bactericidal activities within a short time against 100 strains of MRSA. After 4 hours, 42 strains were killed to below 10(-2) by 2 MIC of ABK, but 6 strains were killed to 10(-2) by 4 MIC of VCM. 3. Against the MRSA 1936 strain, neither ABK nor VCM was active, when an inoculum size of about 10(8) CFU/ml was used. At an inoculum size of 10(5) CFU/ml, ABK showed strong bactericidal activity in a dose dependent manner, while bacteria killing activity of VCM was time dependent. 4. In experimental infections with the MRSA 1936 strain, ABK showed high bactericidal activity rapidly, and area of body that showed bacterial inhibition appeared to be large compared to that obtained with VCM. 5. As to protection from MRSA infections, ABK was significantly superior to VCM in activities against 3 out of 4 strains of MRSA tested. ABK showed more pronounced efficacy when administered in a single dose than in divided doses. These results indicated that ABK would exhibit therapeutic efficacy in a short time.

Aminoglycosides↗
PubMed1994

[Evaluation of bactericidal activity of arbekacin in mixed culture with MRSA and Pseudomonas aeruginosa using an in vitro pharmacokinetic simulation system].

The bactericidal activities of arbekacin (ABK), vancomycin (VCM), gentamicin (GM) and netilmicin (NTL) in mixed culture with Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa were examined using an in vitro computer programmed pharmacokinetic simulation system and also the protective effect of these agents on systemic infection in neutropenic mice was examined. In a mixed culture of S. aureus No. 235 (MRSA) and P. aeruginosa E7, ABK showed a strong bactericidal activity and an inhibition of regrowth against both bacteria, and GM and NTL showed similar effects. On the other hand, VCM showed a bactericidal activity against S. aureus No. 235, but not against P. aeruginosa. In the protective study, ABK was evidently more effective than GM, NTL or VCM against a systemic mixed infection of mice with S. aureus No. 235 and P. aeruginosa E7. In brief, the ED50 values of ABK, VCM, GM and NTL were 19.5, > 100, 40.5 and 45.2 mg/kg, respectively.

Aminoglycosides↗
PubMed1994

[Basic studies on combination effects of arbekacin and beta-lactam antibiotics on methicillin-resistant Staphylococcus aureus].

Combination effects were studied with arbekacin (ABK) and beta-lactam antibiotics including imipenem/cilastatin (IPM/CS), flomoxef (FMOX), and cefotiam (CTM) for bactericidal activities, post-antibiotic effects (PAE's) and bactericidal activities of beta-lactam antibiotics after removal of ABK using methicillin-resistant Staphylococcus aureus (MRSA) strain 1936. The following results were obtained. 1. When ABK was administered in combination with IPM/CS, FMOX or CTM against MRSA strain 1936, low FIC index was not obtained. 2. Higher bactericidal activity was observed when ABK was given before beta-lactam than when beta-lactam was given before ABK. 3. Combination of ABK and each of beta-lactam antibiotic led a longer PAE than ABK alone. 4. When each beta-lactam antibiotic was administered after a treatment and removal of ABK, greater bactericidal activity and growth inhibition were observed than when administered each beta-lactam alone. These findings basically demonstrated that ABK was effectively bactericidal against MRSA when administered in combination with beta-lactam antibiotic such as IPM/CS, FMOX or CTM, even when the FIC index did not indicate a favorable effect.

Aminoglycosides↗
PubMed1993

Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.

A newly synthesized compound, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline (6), had a potent (IC50 = 0.36 microM) inhibitory action on cyclic GMP phosphodiesterase (cGMP-PDE) isolated from porcine aorta; its inhibitory activities toward other PDE isozymes were at least 10-fold weaker. In addition, 6 relaxed porcine coronary arteries precontracted with PGF2 alpha (EC50 = 1.96 +/- 0.58 microM). At the concentration of 30 microM, 6 caused elevation of the intracellular cGMP level in porcine coronary arteries without any change in cAMP level. Various other 4-substituted 6,7,8-trimethoxyquinazolines were also synthesized and evaluated for cGMP-PDE inhibitory activity. From their structure-activity relationships, we concluded that the 4-((3,4-(methylenedioxy)benzyl)-amino) group is essential for potent inhibition of cGMP-PDE.

3',5'-Cyclic-GMP Phosphodiesterases↗
PubMed1993

Structure-activity relationship of N-[2-(dimethylamino)-6-[3-(5-methyl-4-phenyl-1H-imidazol-1-yl)propoxy] phenyl]-N'-pentylurea and analogues. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity.

We have discovered N-butyl-N'-[2-(dimethylamino)-6-[3-(4-phenyl-1H- imidazol-1-yl)propoxy]phenyl]urea (4), a novel, potent, and systemically bioavailable inhibitor of ACAT (acylCoA:cholesterol O-acyltransferase). The structure-activity relationships (SARs) of this lead compound 4 were investigated by systematic modification of four regions in the molecule. The compounds prepared in this study were tested for in vitro inhibitory activity toward both aortic and intestinal ACATs, and selected compounds were further tested for in vivo hypocholesterolemic activity. The studies not only resulted in the discovery of N-[2-(dimethylamino)-6-[3-(5-methyl-4-phenyl-1H-imidazol-1-yl) propoxy]phenyl]-N'-pentylurea (24), with potent activity and moderate plasma level after oral administration, but also revealed the SAR in each modified region. Four compounds (4, 13, 14, 24) were further selected for testing of in vivo antiatherosclerotic activity; 4, 13, and 24 reduced atherosclerotic plaque development to 38-45% of the control value in terms of area, while 14 did not have a significant antiatherosclerotic effect.

Animals↗
PubMed1993

Superficial and protruding type of esophageal adenocarcinoma mucocellulare and muconodulare confined mostly to the lamina propria mucosa and partly in the submucosal layer.

We report a case with an adenocarcinoma mucocellulare and muconodulare of the esophagus which is limited to the lamina propria mucosa and the submucosal layer. The patient, a 74-year-old man had the chief complaints of hematemesis and melena. A superficial and protruding (0-I) type of lesion was found at the lower thoracic portion of the esophagus by X-ray and endoscopic examination. The surgically resected esophageal specimen showed 0-I and predominantly subepithelial (Sep) type. The tumor is presumed to have arisen from the cardiac glands in the lamina propria mucosa of the lowermost region of the esophagus.

Adenocarcinoma↗
PubMed1992

Esophageal ulcer due to ingestion of melted copper.

We report a patient with esophageal stricture as a result of the accidental swallowing of melted copper by a 49-year-old male. As a result, esophagogastric ulcers developed and left a cicatrical stricture. The patient could only manage to swallow liquid food. Radiology of the upper gastrointestinal tract showed marked stricture of the esophagus from the middle thoracic portion to the esophagogastric junction and shortening of the lesser curvature of the stomach. The patient underwent a single-session total gastrectomy, and excision of the thoracic esophagus and construction of anterior thoracic esophagocolic and duodenocolic anastomoses were performed by right thoracotomy and laparotomy, respectively. Macroscopic findings of the surgical specimens showed extensive circular ulcers at the esophagus, and microscopic findings showed deep ulcers extending to the muscle layer with marked fibrosis. The postoperative course was uneventful.

Accidents, Occupational↗
PubMed1992

[Early-onset benign autosomal dominant limb-girdle myopathy with contractures (Bethlem myopathy) in a Japanese family].

We report a family showing an early-onset benign autosomal dominant limb-girdle myopathy with contractures. The clinical features in our family included; 1) slowly progressive limb-girdle muscle weakness since childhood. 2) contractures of fingers, elbows and ankles, 3) mild motor impairment with preserved activities of daily living. The disease was inherited through an autosomal dominant trait. Muscle pathology revealed variation in fiber size, slightly increased central nuclei, mild endomysial fibrosis, type 1 fiber predominance and type 2 fiber atrophy. The above clinical features were similar to those seen in patients reported by Bethlem (1976) and Mohire (1988), and therefore we made a diagnosis of Bethlem myopathy on this familial patients which was extremely rare in Japan.

Ankle↗