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Biomedical subjects

H Noguchi

Publications and source records attributed to H Noguchi.

At least 379 records · Page 21Linked to original sources
PubMed1983

Characterization of DNA methyltransferase from bovine thymus cells.

A DNA methyltransferase was partially purified from bovine thymus heavy cells. The enzyme has Mr 130 000, and introduces methyl groups from S-adenosylmethionine into the 5 position of cytosines in DNA. Sequence specificity analysis revealed that about 60% of the total methylation occurred in the 5'd(C-G)3' doublet. Single-stranded and hemi-methylated DNAs were methylated at an elevated rate by the enzyme. The kinetic analysis showed that the reaction obeys a random sequential mechanism. These results suggest that the enzyme serves primarily as a maintenance DNA methyltransferase.

Animals↗
PubMed1983

The postoperative classification for uterine cervical cancer and its clinical evaluation.

A postoperative classification for uterine cervical cancer has been made in consideration of the spatial spreading of cancer, biological malignancy of 120 cases which were treated with radical hysterectomy and pelvic lymphadnectomy. This classification corresponds extremely well to prognosis. The 5-year survival of the cases with prognostic index (P.I.) 9 or less was 96.1%, while those with P.I. above 10 showed 31.8%. In the Shinshu University School of Medicine clinic, this classification has become indispensable for decision of postoperative irradiation, selection of irradiation methods, and chemotherapeutic agents. Using this classification for individualized therapy, the survival rate was elevated in advanced cancer, class III or IV, with lymph node metastasis and P.I. above 10.

Adenocarcinoma↗
PubMed1983

Rapid incorporation of label from ribonucleoside disphosphates into DNA by a cell-free high molecular weight fraction from animal cell nuclei.

A readily sedimentable nuclear fraction from Chinese hamster embryo fibroblast (CHEF/18) cells catalyzes incorporation of 14C-rCDP into DNA. Data indicated that this incorporation is made possible by the conversion of rCDP into a small and functionally compartmentalized, rather than a large and freely diffusible, pool of dCTP. This catalytically active sedimentable fraction from S phase CHEF/18 cells or actively replicating calf thymus cells contains nascent and template DNA, and numerous enzymes required for DNA biosynthesis including ribonucleoside diphosphate reductase, thymidylate synthetase, dihydrofolate reductase, DNA methylase, topoisomerase and DNA polymerase. We have named this catalytically active macromolecule the replitase. The replitase fraction contained spherical particles with a diameter of approximately 24 to 30 nm and had an estimated molecular weight on the order of 5 X 10(6).

Animals↗
PubMed1983

In vitro antibacterial activity of SM-1652, a new broad-spectrum cephalosporin with antipseudomonal activity.

SM-1652 (sodium 7-[D(-)-alpha-(4-hydroxy-6-methylpyridine-3-carboxamido)-alpha-(4-hydroxyphenyl)acetamido]-3-[(1-methyl-1H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylate) is a new semisynthetic cephalosporin derivative with a broad spectrum of antibacterial activity. Its in vitro activity against gram-positive bacteria was comparable to that of cefazolin. SM-1652 exceeded cefazolin in potency and broadness of antibacterial activity against such Enterobacteriaceae as indole-positive Proteus spp., Enterobacter cloacae, and Serratia marcescens. A remarkable feature of the spectrum of SM-1652 is its high activity against Pseudomonadaceae. Against 200 clinical isolates of Pseudomonas aeruginosa, SM-1652 was significantly more active than cefoperazone, cefotaxime, and sulbenicillin and as active as cefsulodin. The activities of SM-1652 against Pseudomonas maltophilia and Pseudomonas cepacia were superior to those of cefoperazone, cefotaxime, cefsulodin, sulbenicillin, and gentamicin. SM-1652 was relatively stable to hydrolysis with plasmid-mediated penicillinases and cephalosporinases produced by gram-negative bacteria.

Anti-Bacterial Agents↗
PubMed1983

Terminal N-sulphoconjugation of an alicyclic amine (piperazine), identified as a new metabolite of tiaramide in mouse and rat.

A new metabolite of tiaramide, 4-[(5-chloro-2-oxo-3(2H)-benzothiazolyl)acetyl]-1-piperazineethanol, found in mouse urine was identified as potassium 4-[(5-chloro-2-oxo-3(2H)-benzothiazolyl)acetyl]-1-piperazinesulphonate (M-I). Sex differences in the excretion of M-I were noted in the mouse following oral administration of tiaramide and female mice excreted about 4.6-fold more M-I in urine than males. M-I could not be detected in the urine of male or female rats treated orally with tiaramide. After oral dosing with 1-[(5-chloro-2-oxo-3(2H)-benzothiazolyl)acetyl]-piperazine (DETR), M-I was detected in the urine, and the urinary excretion by male and female rats was similar to that in mice.

Analgesics↗
PubMed1983

Metabolism of tiaramide in vitro. III. Sulphoconjugation of alicyclic amine and alcoholic hydroxyl group by hepatic 105 000 g supernatants.

Sulphoconjugation of the alicyclic secondary amine, DETR (the N-dealkylated metabolite of tiaramide) and of the alcoholic hydroxyl group of tiaramide were observed in liver 105 000 g supernatants of rats and mice but hardly detected in hepatic microsomes. The activities depended on active sulphate, 3'-phosphoadenosine 5'-phosphosulphate, or its generating system. Sulphoconjugation of DETR and tiaramide by the supernatants of female rats and mice proceeded more rapidly than those of males, and sex differences were observed irrespective of sulphate donors, the active sulphate or its generating system. Sulphoconjugation of the alicyclic amine and of the alcohol exhibited different pH optima and different susceptibilities to salts.

Animals↗
PubMed1983

New broad-spectrum cephalosporins with anti-pseudomonal activity. I. Synthesis and antibacterial activity of 7 beta-[D-2-[(4-hydroxy-1,5-naphthyridine-3-carbonylamino)- and (4-hydroxypyridine-3-carbonylamino)]-2-(4-hydoxyphenyl)acetamido] cephalosporins.

The synthesis and the antibacterial activity of 7 beta-[D-2-[(4-hydroxy-1,5-naphthyridine-3-carbonylamino)- and (4-hydroxypyridine-3-carbonylamino)]-2-(4-hydroxyphenyl)acetamido]-cephalosporins with various substituents at the 3-position in the cephem nucleus are described. These compounds exhibited strong antibacterial activities against a variety of Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa and Enterobacter aerogenes, which are insensitive to cefazolin and cefmetazole. The compounds (3e, 4e) having a 1-methyl-1H-tetrazolylthiomethyl group at the 3-position appeared to show the best activity in each series. The 4-hydroxypyridine-3-carbonylamino derivative 4e gave higher peak serum concentrations and urinary recovery rates than those of the 4-hydroxy-1,5-naphthyridine derivative 3e when administered subcutaneously to mice and intramuscularly to rats.

Animals↗
PubMed1983

New broad-spectrum cephalosporins with anti-pseudomonal activity. II. Synthesis and antibacterial activity of 7 beta-[2-acylamino-2-(4-hydroxyphenyl)acetamido]-3-[ (1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxylic acids.

The influence of the chirality of the 7-acyl side chain and of various N-acyl moieties (A-CO-) on the in vitro activity of 7 beta-[2-acylamino-2-(4-hydroxyphenyl)acetamido ]-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxylic acids (6) was investigated. A cephalosporin having a 7-acyl side chain of S-configuration (6r) was only weakly active against Staphylococcus aureus and Klebsiella pneumoniae and was inactive against the other species tested. Among the various N-acyl moieties in the cephalosporins having a 7-acyl side chain of the R-configuration, the 4-hydroxypyridine-3-carbonyl moiety, unsubstituted or substituted with 5-bromo and/or 6-alkyl groups and the 4-hydroxy-1,5-naphthyridine-3-carbonyl moiety, unsubstituted or substituted with a 6-methyl and a 6-methoxy group gave the most active compounds. N-Ethylation of the 4-hydroxy-1,5-naphthyridine-3-carbonyl derivative and the 4-hydroxypyridine-3-carbonyl derivative (6p, 6q) resulted in a decrease of the in vitro activity.

Bacteria↗
PubMed1983

New broad-spectrum cephalosporins with anti-pseudomonal activity. III. Synthesis and antibacterial activity of 7 beta-[D-2-(4-hydroxy-6-methylpyridine-3-carbonylamino)-2-(4-hydroxyphenyl) acetamido]-3-(methyl or substituted methyl)-ceph-3-em-4-carboxylic acids.

The influence of various 3-substituents on the antibacterial activity of 7 beta-[D-2-(4-hydroxy-6-methylpyridine-3-carbonylamino)-2-(4-hydroxyphenyl) acetamido]ceph-3-em-4-carboxylic acids (III) was investigated. Introduction of an acidic substituent, such as a sulfo or a carboxyl group, to a 3-(1-methyl-1H-tetrazolyl)thiomethyl substituent (IIIf--i) resulted in a marked loss of activity against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus faecalis, Escherichia coli, Klebsiella pneumoniae, and Enterobacter aerogenes, in contrast to an in crease of activity against Proteus mirabilis. Displacement of the acetoxy group of IIIb with pyridines (IIIm--p) enhanced the activity against P. aeruginosa and E. aerogenes: their activity against those strains were superior to that of the cephalosporin IIId having a 3-(1-methyl-1H-tetrazolyl)thiomethyl substituent. As a result of extensive studies in addition to the study of in vitro activity in this series, 7 beta-[D-2-(4-hydroxy-6-methylpyridine-3-carbonylamino)-2-(4-hydroxyphenyl) acetamido]-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxylic acid, code No. SM-1652, cefpiramide (generic name), was selected as a candidate for further biological and clinical investigations.

Bacteria↗
PubMed1983

Pharmacokinetics of prifinium bromide in healthy volunteers.

The pharmacokinetics of prifinium bromide (Riabal), a specific antispasmodic agent, after oral (60 mg) and i.v. (7.5 mg) administration was studied in six healthy male volunteers. After i.v. administration, the drug was rapidly cleared from the serum. Individual serum levels were described by a bi-exponential equation and mean elimination half-life was 2.13 h. The volume of distribution at steady state was about 190% of body weight, and the total serum clearance and renal clearance were 12.5 and 5.80 ml/(min. kg), respectively. The drug reached maximum serum levels (6.76-14.3 ng/ml) within 2-3 h after administration of tablets: the apparent biologic half-life after oral dosing was 2.18 h. The oral bioavailability was low (3.4%), as expected for quaternary ammonium compounds, but the inter-individual variation of bioavailability was small.

Adult↗
PubMed1983

[Significance of serum immunosuppressive substance (IS) levels in the field of gyneco-obstetrics].

To investigate the immune responses of patients with cancer, we assayed a newly found immunosuppressive substance (IS) by the single radial immunodiffusion method. This substance is extracted from ascites of colon cancer. The IS average level in 46 healthy women was 555.4 +/- 112.1 micrograms/ml. The normal upper limit should be 800 micrograms/ml. Seventy cases with uterine cervical cancer had a significantly higher IS level (667.0 +/- 189.8 micrograms/ml) than healthy women (t=3.57, p less than 0.001), especially in Stages III & IV. All 28 patients except one with recurrent cancer showed an IS level higher than 800 micrograms/ml. (1431.7 +/- 480. 9 micrograms/ml). Before recurrence was found clinically, the IS level became higher. In ovarian tumors, assay of the IS level yielded an interesting result: In 16 cases with benign tumors the level was 568.8 +/- 109.7 micrograms/ml. On the other hand, nine patients with ovarian cancer had levels over 800 micrograms/ml. These data suggest that the assay of IS substance may be useful for the staging of uterine cervical cancer, early detection of the recurrence, differentiation between benign and malignant ovarian tumors and so on.

Abortion, Spontaneous↗