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Biomedical subjects

K Ninomiya

Publications and source records attributed to K Ninomiya.

At least 127 records · Page 7Linked to original sources
PubMed1985

[Bacteriological study of cefminox in the field of obstetrics and gynecology].

Cefminox (CMNX, MT-141), a new cephem antibiotic, was determined of its antibacterial activity against 304 clinical isolates with following results. CMNX was inferior to CEZ or CMZ in the activity against 78 isolates of Staphylococcus sp., but it was superior to these antibiotics in the activity against 104 isolates of E. coli. Against 53 isolates of Bacteroides sp., CMNX showed higher activity than CEZ or CMZ. In the activity against 69 isolates of Peptococcus sp. and Peptostreptococcus sp., CMNX was almost equal to CEZ.

Bacteroides↗
PubMed1985

[Fundamental and clinical studies of cefpiramide in the field of obstetrics and gynecology].

Fundamental and clinical studies of cefpiramide (CPM, SM-1652) a new semisynthetic cephalosporin were carried out in the field of obstetrics and gynecology. The results were obtained as follows: In vitro antibacterial activity of CPM against recent 255 clinical isolates was compared with those of cefazolin (CEZ), cefmetazole (CMZ) and cefoperazone (CPZ). CPM showed strong antibacterial activity against Staphylococcus, K. pneumoniae, Peptococcus and Peptostreptococcus. However the minimum inhibitory concentration of CPM was inferior to those of CEZ, CMZ and CPZ against E. coli. The transfer of CPM to the female genital organs was found to be good. Tissue levels over than 5 micrograms/g were maintained after 5 hours. CPM was administered to 10 patients with obstetrical and gynecological infections. Good responses were obtained in all of the cases. Neither adverse reactions nor abnormal laboratory findings were observed except 1 case with slight elevation of BUN.

Adult↗
PubMed1984

[Coronary thrombolysis in acute myocardial infarction].

The effect of early perfusion after intracoronary infusion of urokinase (PTCR) in patients with acute myocardial infarction was assessed. Coronary perfusion was reestablished in 7 of 10 patients receiving intracoronary urokinase. We compared the recanalized group after intracoronary urokinase (n = 7) with the standard therapy group (n = 32). Left ventricular end-diastolic pressure, cardiac index, angiographic ejection fraction, radionuclide ejection fraction, defect score by Thallium-201 scintiscan and regional ejection fraction by the left ventriculogram, measured at about one month after the onset of acute myocardial infarction, were compared according to the site of the main coronary lesion (right coronary artery or left anterior descending coronary artery). No statistically significant differences between the recanalized group after the administration of intracoronary urokinase and the control group were found at each coronary lesion. On the other hand, the comparison between two patients with and without PTCR, who matched the clinical and coronary angiographic findings, showed that PTCR on acute myocardial infarction might be of value. However, evaluation of the long-term effects of coronary thrombolysis on survival and myocardial function will require controlled randomized trials of a large number of patients.

Adult↗
PubMed1984

Selective inhibition of thrombin by (2R,4R)-4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl++ +) sulfonyl]-l-arginyl)]-2-piperidinecarboxylic acid.

The potency of thrombin inhibition by 4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)-sulfony l]- L-arginyl]-2-piperidinecarboxylic acid (MQPA) depended on the stereoconformation of the 2-piperidinecarboxylic acid moiety. Ki values for bovine alpha-thrombin were 0.019 microM with (2R,4R)-MQPA, 0.24 microM with (2R,4S)-MQPA, 1.9 microM with (2S,4R)-MQPA, and 280 microM with (2S,4S)-MQPA. (2R,4R)-MQPA of the four stereoisomers of MQPA was also the most potent inhibitor for other trypsin-like serine proteases with Ki values of 5.0 microM for trypsin, 210 microM for factor Xa, 800 microM for plasmin, and 1500 microM for plasma kallikrein. Examination of the potency of thrombin inhibition by arginine derivatives related to MQPA in structure suggested the presence of a specific binding site for the carboxamide portion (C-terminal side). The relative inhibitory potency of the four stereoisomers of MQPA for trypsin was nearly identical with that for thrombin, suggesting that the specific binding site for the carboxamide portion is present in both enzymes. Modification of thrombin by phosphopyridoxylation or the presence of heparin did not significantly alter the binding of MQPA.

Animals↗
PubMed1984

Effects of late coronary artery reperfusion after myocardial necrosis is complete.

Early reperfusion salvages reversibly injured ischemic myocardium. Late reperfusion, after necrosis is complete, could be beneficial by accelerating healing, or the hemorrhage and contraction-band necrosis associated with reperfusion could impair healing. In closed-chest anesthetized dogs the left anterior descending coronary artery was occluded with a balloon-tipped catheter for either 1 day followed by reperfusion for 6 days (n = 9) or for 7 days without reperfusion (n = 9). All dogs were killed after 7 days. Pathologic changes were studied in transverse whole-mount ventricular histologic sections. When the two groups were compared, no differences were found in: (1) infarct size, 15.7 +/- 9.9% vs 10.2 +/- 8.6 (mean +/- SD); (2) number of transmural infarcts, 5 of 9 vs 6 of 9; (3) ratio of infarcted/normal wall thickness, 0.93 +/- 0.09 vs 0.95 +/- 0.13; (4) thickness of zone of collagen deposition at periphery of infarct, 1.69 +/- 1.16 mm vs 1.67 +/- 0.56; and (5) amount of hemorrhage, calcification, and inflammation. Thus, in this model, reperfusion after necrosis is complete did not improve or impair healing.

Animals↗
PubMed1984

Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants.

A series of substituted (omega- aminoalkoxy )stilbene derivatives has been synthesized and screened for anticonvulsant activity. The effect of structural modification of these molecules on the activities has been systematically examined. Potent anticonvulsant activity was displayed by 2-[4-(4-methyl-1 piperazinyl)butoxy]stilbene (20) and some 2-[4-(3-alkoxy-1-piperidino)butoxy]stilbene derivatives (21, 37, 38, and 40), as determined by maximal electroshock seizure (MES) and pentylenetetrazol-induced convulsion tests in mice. Compound 21 exhibited more potent anti-MES activity than diphenylhydantoin and carbamazepine in further pharmacological tests in rats, and its therapeutic index was superior to those of two antiepileptic drugs.

Animals↗
PubMed1984

Microbial degradation of validamycin A by Flavobacterium saccharophilum. Enzymatic cleavage of C-N linkage in validoxylamine A.

The enzymatic cleavage of C-N linkage in the degradation of validamycin A by Flavobacterium saccharophilum was examined using N-p-nitrophenyl derivatives of validamine and valienamine as synthetic model substrates for validoxylamine A. Incubation of N-p-nitrophenylvalidamine with the membrane fraction from the organism led to formation of N-p-nitrophenyl-3-ketovalidamine, and succeeding cleavage of C-N linkage. As the products of the cleavage step, one was identified as p-nitroaniline and another keto compound could not be purified enough because of its instability. However, on the basis of its hydrogenation products, the structure of the keto compound could be established as 5D-(5/6)-5-C-(hydroxy-methyl)-2,6-dihydroxy-2-cyclohexen-1-one. The same experiment was carried out with N-p-nitrophenylvalienamine. In this case, N-p-nitrophenyl-3-ketovalienamine could be isolated as an intermediate but the desired keto compound from the cleavage step could not be isolated because of its instability. The participation of two enzymes, that is, a dehydrogenase and a C-N lyase on the cleavage of C-N linkage was assured, and moreover, the analysis of its products, together with those of the previous studies allow us to propose a degradation pathway of validamycin A by Flavobacterium saccharophilum.

Flavobacterium↗
PubMed1984

[In vitro activity and clinical evaluation of ceftriaxone in the field of obstetrics and gynecology].

In vitro activity of ceftriaxone (CTRX) was examined by agar plates dilution method against 398 strains isolated from the infections in the field of obstetrics and gynecology. MIC90 of CTRX against Staphylococcus (107 strains), E. coli (54 strains), K. pneumoniae (27 strains), Peptococcus and Peptostreptococcus (106 strains) and Bacteroides (104 strains) was more than 100 micrograms/ml, less than 0.20 micrograms/ml, less than 0.20 micrograms/ml, 6.25 micrograms/ml and 50 micrograms/ml, respectively. The concentrations of CTRX 16.9 hours after 1 hour intravenous drip infusion with 1 g were 46.2 micrograms/ml in the uterine artery, 48.0 micrograms/ml in the cubital vein, 11.0 micrograms/g in the endometrium, myometrium and cervix uteri, and 14.0 micrograms/g in the portio vaginalis. These concentrations of CTRX in the serum and uterine tissues were higher than the level required to inhibit 90% of the strains of E. coli, K. pneumoniae, and Peptococcus and Peptostreptococcus, isolated from the infections in the field of obstetrics and gynecology. Clinical efficacy of CTRX was evaluated in 7 cases consisting of 2 with puerperal fever and one each with puerperal intrauterine infection, intrauterine infection, pyometra, adnexitis and Bartholin's abscess. Clinical and bacteriological efficacies were seen in 6 and 4 cases, respectively. Neither noteworthy adverse reactions nor laboratory abnormalities were observed throughout this study.

Adult↗
PubMed1984

[Experimental studies on oral administration of nitrosourea anti-tumor agent, MCNU].

Experimental studies with orally administered MCNU, a water-soluble nitrosourea, yielded the following results. MCNU produced a significant increase in life span, and 60-day survivors were observed by various schedules in L1210 leukemia. The therapeutic ratios of MCNU were almost similar to those of CCNU. With Lewis lung carcinoma and Ehrlich ascites carcinoma implanted into the stomach wall, its antitumor activity by oral administration was slightly more effective than by intravenous route. In Beagle dogs, hematologic toxicity and gastrointestinal toxicity (vomiting, diarrhea) were noted by oral administration, similar to intravenous administration, but its toxicity was mild. The maximum blood level of MCNU was noted at 30 minutes after oral administration in Beagle dogs. The half life (23.7 min) by oral administration was similar to that by intravenous route. From these results, the oral administration of MCNU deserves the consideration as a form of treatment now given other MCNU routes.

Administration, Oral↗
PubMed1984

[Ceftazidime: antibacterial activity and clinical efficacy in obstetrics and gynecology].

Ceftazidime ( CAZ ) exhibited in vitro activity greater than cefoperazone, cefotiam, cefmetazole and cefazolin and almost equal to cefotaxime (CTX), ceftizoxime (CZX) and latamoxef ( LMOX ) against E. coli and K. pneumoniae isolated from obstetrical or gynecological infections excluding urinary tract infections. This drug demonstrated less activity than other 6 cephems against B. fragilis. Against anaerobic Gram-positive cocci, it showed less activity than other cephems. CAZ was administered to 11 patients with obstetrical and gynecological infections. The clinical results of this drug were as follows; excellent in each 1 case of parametritis , wound infection and BARTHOLIN's abscess, good in 7 cases including 1 of puerperal fever, 2 of intrauterine infection and 4 of adnexitis, and poor in 1 cases of adnexitis. No side effects or haematobiochemical abnormalities were observed throughout this trial.

Adult↗
PubMed1984

[Effect of combination chemotherapy of nitrosourea MCNU with various anti-tumor agents].

The combination chemotherapy of water-soluble nitrosourea MCNU with various anti-tumor agents was studied using L1210 leukemia, Lewis lung carcinoma and B16 melanoma. The combinations of MCNU with 5-fluorouracil, cytosine arabinoside, adriamycin, mitomycin C, carboquone or cyclophosphamide produced significantly enhanced anti-tumor effects in L1210 leukemia. By combination with antimetabolites such as 5-fluorouracil or cytosine arabinoside, marked anti-tumor effects were observed over a wide range of dosage. It was suggested that 2-drug combination of MCNU plus 5-fluorouracil or 3-drug combination of MCNU plus 5-fluorouracil and adriamycin was useful in Lewis lung carcinoma or B16 melanoma. From these results, it was recognized that the multiple drug combination chemotherapy of MCNU was therapeutically useful, when given with 5-fluorouracil or cytosine arabinoside.

Animals↗
PubMed1983

Noninvasive diagnosis of neonatal coarctation and associated anomalies using two-dimensional echocardiography.

Two-dimensional echocardiography (2DE) was used to study 51 neonates in whom coarctation of the aorta had been diagnosed clinically. In 40 patients, studies showed coarctation or arch interruption that was later confirmed at angiography, surgery, or autopsy. Of the remaining 11 studies, one gave a false positive result, one was technically poor, three had echocardiographic evidence of only mild arch narrowing and are being followed clinically, and six were negative. There were two false negative studies. Four studies were apparently true negatives. Many additional lesions were correctly identified by echocardiography although some, such as patent ductus arteriosus and small ventricular septal defect, were frequently missed. Twelve patients underwent surgery without preoperative catheterization. 2DE has proven extremely useful in confirming the diagnosis of neonatal coarctation of the aorta and sometimes obviates the need for invasive catheterization.

Aorta, Thoracic↗
PubMed1983

Porcine liver aminopeptidase. Further characterization of its sulfhydryl groups.

Porcine liver aminopeptidase was inactivated by various sulfhydryl-reactive reagents, whose inactivation rates were in the order: p-chloromercuribenzoate(PCMB) greater than HgCl2 greater than 2,2'-dithiodipyridine greater than 5,5'-dithiobis(2-nitrobenzoic acid)(DTNB). The processes of inactivation by these reagents did not follow pseudo-first-order kinetics, and prolonged incubation did not alter the level of maximum inactivation. The substrates provided no protection against the inactivation by DTNB, and the numbers of sulfhydryl groups titrated with the reagent were not influenced by the presence or absence of puromycin (a competitive inhibitor). The modification of sulfhydryl groups caused a slight increase in the Km value for the enzyme and a significant decrease of the Vmax value. There are two ionizable groups (pKe, 6.2; 7.8 and pKes, 6.0; 7.8) in the catalytic action of the enzyme. From the pKi vs. pH profile of inhibition with PCMB, the pK value of 7.8 does not correspond to the ionization of a sulfhydryl group. The thiol-modified enzyme was activated by cobalt ion, as was the native enzyme (Kawata, S., et al. (1982) J. Biochem. 92, 1093-1101). But in contrast with the native enzyme, the thiol-modified enzyme was activated about 2.5-fold and the maximum activation remained almost constant during prolonged incubation with cobalt ion. These results suggest that the sulfhydryl groups of the enzyme are located apart from the binding site of cobalt ion and do not participate directly in the catalytic process.

Aminopeptidases↗