Search PubMed⌕ Search

Biomedical subjects

K Umezu

Publications and source records attributed to K Umezu.

At least 55 records · Page 3Linked to original sources

Gastroenteritis in suckling mice caused by human rotavirus can be prevented with egg yolk immunoglobulin (IgY) and treated with a protein-bound polysaccharide preparation (PSK).

Oral inoculation of human rotavirus MO strain (serotype 3) into 5-day-old BALB/c mice cause gastroenteritis characterized by diarrhea. Clinical symptoms, histopathological changes in the small intestine, and the detection of rotavirus antigen in enterocytes were all characteristic of rotavirus-induced gastroenteritis. Using this small animal model, passive protection of suckling mice against human rotavirus infection was achieved with the use of immunoglobulin (IgY) from the yolks of eggs of rotavirus-immunized hens. When IgY against a rotavirus strain homotypic to the challenge virus (MO strain) was administered in the mice, complete protection against rotavirus infection was achieved. On the other hand, with oral administration of IgY against a heterotypic strain (serotype 1, Wa strain), a lower protective effect was nevertheless obtained. The four different strains of human rotavirus (Wa, KUN, MO, and ST3) were inactivated in vitro by treatment with PSK, a protein-bound polysaccharide preparation, in a dose-dependent manner. Oral administration of 2.5 mg of PSK caused a therapeutic effect on experimentally MO-infected suckling mice. The antiviral effect of PSK was indicated by the reduction of the duration of diarrhea.

Animals↗

Anti-human immunodeficiency virus type 1 activities and pharmacokinetics of novel 6-substituted acyclouridine derivatives.

The novel 6-substituted acyclouridine derivatives 1-[(2-hydroxyethoxy)methyl]-6-phenylthiothymine (HEPT), 1-[(2-hydroxyethoxy)methyl]-6-(3-methylphenylthio)thymine (HEPT-M), 6-cyclohexylthio-1-[(2-hydroxyethoxy) methyl]thymine (HEPT-H), and 1-[(2-hydroxyethoxy)methyl]-6-phenylthio-2- thiothymine (HEPT-S) have proved to be potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) replication in a variety of cell systems, including peripheral blood lymphocytes. They are not inhibitory to the replication of HIV-2. HEPT-S emerged as the most active congener, with a 50% inhibitory concentration of 1.6 microM for HIV-1 (human T-cell lymphotropic virus type IIIB) in MT-4 cells. We also examined the pharmacokinetics of the compounds following oral administration to rats. The pharmacokinetic profile varied considerably from one compound to another. The highest concentration in plasma (7.4 micrograms/ml, or 22.8 microM) was achieved by HEPT-S within 30 min after administration of an oral dose of 20 mg/kg of body weight. HEPT-S can be considered a promising candidate for the treatment of HIV-1 infections.

Animals↗

Solitary brain metastasis from renal cell carcinoma 14 years after nephrectomy: a case report.

We report a case of solitary brain metastasis from renal cell carcinoma (RCC) 14 years after nephrectomy. A 46-year-old female had sudden onset of headaches, aphasia, gait disturbance and right hemiparesis. A brain CT revealed a cystic tumor in the left parietal area, which was surgically removed completely. Microscopic appearances of the brain tumor were similar to those of the primary RCC. Positive immunoreaction for epithelial membrane antigen (EMA) and keratin confirmed the diagnosis of metastatic RCC. This is the second case of solitary brain metastasis from RCC occurring more than 10 years after nephrectomy.

Brain Neoplasms↗

[A case of Fournier's gangrene: was it triggered by prostatic massage?].

We have experienced a case of Fournier's gangrene which progressed rapidly after prostatic massage. The patient was a 70-year-old man who had poorly controlled diabetes mellitus, hemorrhoid, urethral stricture and benign prostatic hyperplasia. He visited an urologist complaining of pollakisuria and miction pain. Under the diagnosis of prostatitis, prostatic massage was performed. From that night, he developed a high grade fever. Simultaneously, redness, swelling and pain of the scrotum progressed rapidly, and 11 days later, he was admitted to our hospital. An X-ray examination revealed subcutaneous gas formation in the scrotum. Immediately, incision and drainage with extensive debridement of necrotic tissue were performed combined with chemotherapy using broad spectrum antibiotics and insulin therapy. About 3 months later, the gangrene and the wound were healed with granulation and scarring. Cultures of the pus and the necrotic tissue from the scrotum were positive for Bacteroides fragilis and several aerobes including Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae, Enterococcus and Staphylococcus epidermidis. The case proved to be non-clostridial gas gangrene.

Aged↗

[Clinical study of S 6472 in urinary tract infection].

Clinical studies on S 6472, a longer lasting preparation of cefaclor (CCL), were performed and the following results were obtained. S 6472 was administered orally to 102 patients with urinary tract infections including 16 with acute uncomplicated pyelonephritis, 32 with acute uncomplicated cystitis, 31 with complicated pyelonephritis and 23 with complicated cystitis. 95 patients were treated with 375 mg of S 6472 2 times daily and 7 patients were treated with 750 mg of S 6472 2 times daily. The overall clinical efficacy was evaluated on the basis of the criteria proposed by the Japanese UTI Committee. 1. Clinical efficacies in 11 cases of acute uncomplicated pyelonephritis were excellent in 10 and moderate in 1, with an overall efficacy rate of 100%. Bacteriologically, all 12 strains identified in the acute uncomplicated pyelonephritis cases were eradicated, with an eradication rate of 100%. 2. Clinical efficacies in 21 cases of acute uncomplicated cystitis were excellent in 17, moderate in 3 and poor in 1, with an overall efficacy rate of 95%. As to bacteriological responses, 22 strains identified in the acute uncomplicated cystitis cases (except 1 of Escherichia coli) were eradicated, with an eradication rate of 95%. 3. Clinical responses in 43 cases of complicated urinary tract infections were excellent in 20, moderate in 15 and poor in 8, with an overall efficacy rate of 81%. Bacteriologically, 39 strains, including only one strain of P. aeruginosa, in the complicated urinary tract infection cases (except 4 of E. coli, 1 of Klebsiella pneumoniae, 1 of Enterococcus faecalis and 2 of Enterobacter cloacae) were eradicated, with an eradication rate of 83%. As side effects, slight stomatitis and gastric discomfort were noted in 1 patient each but we were able to continue the medication. Abnormal laboratory test values found were: 1 case of a slight and transient increase of lymphocytes in peripheral blood and 1 case of a slight and transient increase of serum creatinine level.

Administration, Oral↗

[A double-blind comparative study of S 6472 (a long-acting cefaclor) versus a conventional cefaclor preparation in complicated urinary tract infections].

For an objective evaluation of the clinical efficacy, safety and usefulness of S 6472 (a long acting cefaclor) in non-catheterized patients with complicated urinary tract infections, a double-blind comparative study was performed using conventional cefaclor preparation (hereafter, CCL) as the control drug. S 6472 was administered orally at a single dose of 750 mg twice daily, and CCL at a single dose of 500 mg 3 time daily. The duration of the treatment was 5 days for either drug. Clinical efficacies were evaluated according to the criteria for evaluation of drug efficacy by the Japanese UTI Committee (3rd edition), and the following results were obtained. 1. The initial distribution of the patients' background characteristics was not significantly different between the S 6472 and CCL groups. 2. The overall clinical efficacy rates were 76.2% in the S 6472 group and 75.5% in the CCL group, indicating no significant difference between the 2 groups. When clinical efficacies evaluated according to different types of infections (UTI groups), the differences between the 2 drug groups were not significant in any of disease groups 2, 3, 4, and 6. 3. Clinical efficacy rates as evaluated by attending physicians were not significantly different between the 2 groups, either. 4. Bacteriological responses were evaluated as eradicated in 81.2% in the S 6472 group and 78.3% in the CCL group, suggesting no statistically significant difference. 5. The incidences of side effects were 2.9% (4/139) in the S 6472 group and 0.7% (1/141) in the CCL group, thus no significant differences existed between the 2 groups. On laboratory examination, 4 and 5 abnormal test values, respectively, were detected in 3/94 patients in the S 6472 group and 5/100 patients in the CCL group, but the difference was not significant between the 2 groups, either. All of these side effect symptoms and abnormal laboratory test values were mild in severity and transient. The results of the overall safety rating which was based on the evaluations of the side effects and laboratory test values indicated no significant difference between the 2 groups. 6. According to judgement by the attending doctors, the clinical usefulness rates evaluated based on the results of the efficacy and safety ratings were not significantly different between the S 6472 and CCL groups. These findings suggest that S 6472 produces excellent therapeutic results in complicated UTI patients without indwelling catheters and its clinical efficacy, safety, and usefulness are equal to those of the conventional CCL.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗

Traumatic dislocation of the testis: a case report.

We report a case of a traumatic dislocation of the testis in a 17-year-old male. He noticed lack of right scrotal contents three months after a motorcycle accident. The right testis, located at the inguinal subcutaneous region, was surgically replaced into the scrotum. The biopsy specimen of the dislocated testis showed partial atrophy of the seminiferous tubules that resulted in impaired spermatogenesis. Our case represents the 57th case of traumatic dislocation of the testis reported in Japan.

Accidents, Traffic↗

An automated analysis of chemotaxis in vitro using a computer-assisted scanning densitometer.

The quantitation of chemotaxis in vitro was developed with a computer-assisted scanning densitometer. The method of estimating the number of cells on a filter was based on the photo-reflection from the nuclei of stained cells. Samples obtained from a 48-well micro chemotaxis assembly were successfully analyzed by this method. This assay system could quantitate chemotaxis much faster and more accurately than by cell counting under the microscope. It was sensitive enough to determine the responsiveness of SMCs and fibroblasts to various chemoattractants. This system could be applied to medical and biological screening tests for drugs and clones in laboratories.

Animals↗

[Clinical study of norfloxacin in the treatment of acute epididymitis].

The efficacy and safety of Norfloxacin were studied in the treatment of 20 patients with acute epididymitis. Norfloxacin was orally administered at a dose of 200 mg 3 times a day for 14 days. Clinical efficacy rate on the 7th day was 95% (19/20), excellent in 9 cases, moderate in 10 cases and poor in 1 case, and on the 14th day was 95% (18/19), excellent in 12 cases, moderate in 9 cases and poor in 1 case. On the 14th day, fever, pain and swelling had disappeared in 8 cases (in 2 cases on the 7th day). The efficacy on the 14th day was further investigated compared to that on the 7th day. Before treatment with Norfloxacin, in 13 of the 20 patients, pyuria was observed. Cultivating the bacteria was isolated in 4 of the 13 patients. Norfloxacin remarkably affected the treatment of these patients with pyuria and bacteriuria. In the treatment with Norfloxacin, the count of leukocytes, erythrocyte sedimentation rate and CRP were obviously improved. Side effects and abnormal clinical laboratory findings were not observed. From these results, Norfloxacin 600 mg/day, t.i.d was considered useful and safe in the treatment of acute epididymitis.

Acute Disease↗

[Colon bladder replacement after total cystectomy].

Although ileal conduit diversion is widely accepted in the treatment of the patients undergoing radical cystectomy, many patients would prefer other alternatives which allow continence. and urination through the urethra. We describe a new procedure in which a segment of detuburalized right colon is used as a continent reservoir. Eight patients, 7 after radical cystectomy for bladder cancer and one after total exenteration for rectal cancer, have undergone colon bladder replacement. New created bladder had a capacity of 300 to 600 ml. All patients could pass urine through the urethra but one is on self-catheterization. Five of the 8 patients had no residual urine. Three months after operations 4 were totally continent and 3 were satisfactorily dry during daytime but slightly enuretic. Excretory urography showed no abnormalities in their upper urinary tract. Considering the "quality of life' of a patient, this procedure can be an ideal option for selected patients.

Aged↗

Clinical trial of attenuated vaccinia virus AS strain in the treatment of advanced adenocarcinoma. Report on two cases.

Two cases of advanced adenocarcinoma treated with attenuated vaccinia virus AS strain are reported. One was a primary lung adenocarcinoma with metastatic lesions in brain, right kidney, and rib. The other was a left renal adenocarcinoma with multiple lung and vertebral metastases. In both patients, good antitumor effects against lung and bone lesions were obtained, respectively, and no adverse reactions were noted. Therefore, treatment of patients with AS vaccinia virus appears to suppress the growth of tumor cells without adverse effects on normal human cells. This is the first report to describe the effects of attenuated vaccinia virus AS strain on human cancer.

Adenocarcinoma↗

Suppressive effect of tritoqualine on enzyme leakage induced by D-galactosamine in rat primary-cultured hepatocytes.

Tritoqualine (TRQ) was previously reported to suppress enzyme leakage and lipid peroxidation induced by carbon tetrachloride in isolated hepatocytes. In the present study, we investigated the effect of TRQ on enzyme leakage from rat primary-cultured hepatocytes using D-galactosamine (GalN) which causes hepatic injury without lipid peroxidation. Leakage of GPT and GPT was significantly increased at 18 hr after GalN addition, being saturated at 42-50 hr. This enzyme leakage was suppressed dose-dependently by TRQ at 42 hr, but not by vitamin E. These results suggest that TRQ shows a suppressive effect on enzyme leakage from hepatocytes independently of its inhibitory action on lipid peroxidation.

Alanine Transaminase↗

Effect of tritoqualine on the proliferation of interleukin-3 dependent cell line and sensitive cells.

In this paper, the effect of tritoqualine (TRQ) on the proliferation of interleukin (IL) sensitive cells was investigated. TRQ inhibited the proliferation of FDCp-2 (IL-3 dependent cell line), CTLL-2 (IL-2 dependent cell line) and bone marrow cells (BMC) stimulated by IL, giving an ID50 of about 3 microM equally in the three systems. However, a ten times higher concentration of TRQ was required to inhibit the tumor cell proliferation. TRQ did not affect the unstimulated bone marrow cells. Accordingly, it is suggested that TRQ may show its anti-allergic effect, at least partially, by interfering with the proliferation/differentiation to mast cell and basophils of multi-functional hemato-poietic cells stimulated by IL-3.

Animals↗

Inhibitory mechanism of tritoqualine on histamine release from mast cells.

Tritoqualine (TRQ, (+)-(R*)-7-amino-4,5,6-triethoxy-3-[(R*)-5,6,7, 8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]isoquinolin++ +-5-yl] phthalide) strongly inhibited the increased metabolism of [3H]arachidonic acid-labeled phospholipid and 45Ca2+ influx in mast cells stimulated by compound 48/80 (compd 48/80), Concanavalin A (Con A) plus phosphatidylserine (PS), or 2,4-dinitrophenyl-coupled-ascaris extracts (DNP-asc). However, TRQ did not disturb the binding of 14C-labeled compd 48/80 to the mast cell membrane. The activity of calmodulin purified from mastocytoma P-815 cells was inhibited by TRQ at IC50 1.0 microM. From these results, it is concluded that the inhibitory mechanism of TRQ on stimulus-induced histamine release from mast cells may be mediated at least partially by the inhibition of Ca2+ influx and calmodulin activity.

Animals↗

[Effects of 4-(o-benzylphenoxy)-N-methylbutylamine hydrochloride (MCI-2016, bifemelane hydrochloride) on coagulation, fibrinolysis, hemolysis, hemorheological properties and platelet aggregation].

MCI-2016 showed little influence on coagulation (APTT) and fibrinolysis (plasma clot lysis activated by urokinase) at doses (concentrations) as high as 300 mg/kg, p.o. or 8.6 X 10(-4) M. Hemolytic action of MCI-2016 was only observed at the concentrations above 2 mM. The drug also showed no influence on blood glucose level (30-300 mg/kg, p.o.). Effects of MCI-2016 on hemorheological properties were studied either in vitro or ex vivo. Above the doses (concentrations) of 100 mg/kg, p.o. and 10 microM, MCI-2016 suppressed the mechanical hemolysis and accelerated the membrane filtration rate. These effects of MCI-2016 were superior to those of cinepazide, Ca-hopantenate, meclofenoxate and pentoxyfylline. MCI-2016 also inhibited platelet aggregation induced by collagen with the IC 50 of 35 to 60 microM (rabbit and human platelets). Secondary aggregations of ADP and epinephrine were also inhibited by MCI-2016. As for reference drugs, bencyclane showed inhibitory patterns similar to MCI-2016. Other drugs examined exhibited little effect. In summary, it may be suggested that MCI-2016 exhibits beneficial influences in the clinical fields of cerebrovascular diseases.

Animals↗

[General pharmacological action of 4-(o-benzylphenoxy)-N-methylbutylamine hydrochloride (MCI-2016, bifemelane hydrochloride). Influence on respiratory and cardiovascular systems, renal function, autonomic nervous system, isolated smooth muscle and digestive organs].

MCI-2016 at 3 mg/kg, i.v., caused slight changes in systemic blood pressure (SBP), heart rate (HR), respiratory rate (RR) and ECG but at 10 mg/kg, i.v., it caused a significant increase in RR, decrease in SBP, increase or decrease in HR and a moderate change in ECG. Biphasic changes in SBP, HR and blood flow were sometimes observed after high doses. MCI-2016 also decreased SBP at 30 mg/kg, i.p., in SHR. MCI-2016 (50 mg/kg, p.o./day) showed little influence on SBP, HR and ECG in conscious beagle dogs. In isolated hearts, MCI-2016 decreased HR and contractility at the concentrations above 10(-5) g/ml, and 30 micrograms, i.a. MCI-2016 prolonged the AVCT at 10 mg/kg, i.v. MCI-2016 (i.v. or i.a.) moderately increased cerebral and femoral artery blood flows. MCI-2016 did not change CMRO2, but decreased MVO2. Coronary and renal artery flows were moderately increased by 10 mg/kg, i.v., of MCI-2016. Renal function was suppressed after 10 mg/kg, i.v., or 300 mg/kg, p.o., of MCI-2016. MCI-2016 potentiated the action of NE (increase in SBP, contractions of nictitating membrane and vas deferens), but showed little anti-cholinergic action. In contrast, MCI-2016 moderately increased gastrointestinal motility and salivatory response. As for the influence on isolated smooth muscles, MCI-2016 antagonized the contraction of blood vessels by high K+ at 10(-6) g/ml, or more, and it depressed the contractions by ACh, 5-HT, histamine and BaCl2 and also depressed spontaneous movements of uterus and ileum at 10(-5) M or more, in a nonspecific manner. MCI-2016 had no influence on liver damage and bile secretion, but inhibited stress ulcer and gastric acid secretion on the one hand, and caused gastric damage (125 mg/kg p.o., or more) on the other hand.

Animals↗

[Effect of tritoqualine (TRQ) on bile secretion in rats].

An accelerating effect by TRQ-consecutive administration perorally on bile secretion in rats was investigated in comparison with phenobarbital (PB)-administered rats. The bile secretion velocity was increased significantly by administration of TRQ (25, 50, 100 mg/kg/day) or PB (50 mg/kg/day) compared to the control group. A 24% increase in the ratio of the liver weight to body weight was observed in the PB-administered group, but in the TRQ-administered group, a slight increase (5%) was seen compared with the control group. The concentration of excreted bile acid in the bile of rats to which TRQ and PB were administered were lower than that of the control group. However, when excreted bile acid content was represented in terms of wet liver weight, no difference was seen in the TRQ-administered group, but a 17% decrease was observed in the PB-administered group compared with the control group; and also, almost the same results were obtained with regards to the cholesterol and phospholipid in the bile. Though there was no difference of Na+, K+, or Cl- concentration in bile between the TRQ or PB-administered group and the control group, more Na+, K+ or Cl-/g wet liver was excreted in TRQ-treated group than the PB-administered group. TRQ was excreted through the bile duct promptly after an i.v. injection without an increase in the bile secretion, suggesting that the excretion of TRQ and its metabolites were not accompanied by the increase in bile secretion. These results indicate that the accelerating effect of TRQ on bile secretion was presumably derived from bile acid non-dependent bile secretion such as PB; however, a different pharmacological mechanism between TRQ and PB was presumed from the discrepancy of the decomposition in the secreted bile and of drug-metabolizing enzyme induction. Thus, it was suggested that there was a possibility that the accelerating action of bile secretion by TRQ was attributed to the activating effect of TRQ on the hepatocytes.

Administration, Oral↗