[A case of pacemaker lead fracture due to displacement of pulse generator (author's transl)].
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Biomedical subjects
Publications and source records attributed to N Fujii.
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A new devised arginine derivative, NG-mesitylene-2-sulfonylarginine, Arg(Mts), was employed for the synthesis of hypothalamic substance P and neurotensin. The former was obtained in 74% yield by treatment of the protected undecapeptide amide, Z - Arg(Mts) - Pro - Lys(Z) - Pro - Gln - Gln - Phe - Phe - Gly - Leu - Met(O)-NH2, with methanesulfonic acid in the presence of anisole followed by reduction of the sulfoxide with 2-mercaptoethanol. The latter was obtained in 54% yield by the similar treatment of the protected tridecapeptide ester, Z - Pyr - Leu - Tyr - Glu(OBzl) - Asn - Lys(Z) - Pro - Arg(Mts) - Arg(Mts) - Pro - Tyr - Ile - Leu - OBzl, with methanesulfonic acid. As scavenger, a mixture of anisole-thioanisole-o-cresol (1:1:1, by vol.) was employed to suppress the side reaction, O-mesitylene-2-sulfonation of the Tyr residue.
1. An enzyme which hydrolyzes the acetamido groups of N-acetylgalactosamine residues in N-acetylated polygalactosamine was found in the supernatant fraction of Aspergillus parasiticus AHU 7165, a polygalactosamine-producing strain. 2. N-Acetylated polygalactosamine was used as a substrate in the purification and characterization of this enzyme. A 140-fold purification was obtained by means of ammonium sulfate fractionation followed by chromatography on carboxymethylcellulose and DEAE-cellulose. 3. The enzyme releases about 60-70% of the acetyl groups of N-acetylated polygalactosamine, giving a product with free amino groups. Whereas the enzyme also deacetylates oligosaccharides with 14 or more N-acetylgalactosamine units at a rate similar to that of deacetylation of the polymer, it deacetylates shorter oligosaccharides (trimer to hexamer of N-acetylgalactosamine) much more slowly and is virtually inactive toward disaccharide. Deacetylation can not be detected with bacterial cell wall peptidoglycan, N-acetylated heparin, partially O-hydroxyethylated chitin or monomeric N-acetylgalactosamine derivatives as substrates. 4. This enzyme shows double pH optima of 5.3 and 9.3. The Km value for N-acetylated poly-galactosamine is 0.15 g/l (or 0.54 mM with respect to monosaccharide residues). 5. The occurrence of this enzyme may account for the formation of polygalactosamine with free amino groups.
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An intravenous preparation of doxycycline (DOTC, Vibramycin 'Pfizer'), a long-lasting tetracycline, was administered mainly by drip infusion for a series of study in the pediatrics field, and the results were as follows: 1) DOTC (100 mg) was dissolved in a 100 ml of glucose solution and 2--3 mg/kg was administered intravenously. When the total infusion time was adjusted between one to two hours, the peak serum level of DOTC was seen at the end of infusion in each case. The serum level in a two-hour infusion time, however, the serum level was delectable for a long period of time: the serum level after 10 hours was 0.82--1.23 micrograms/ml. Above results suggest that DOTC intravenous should be given in a two-hour infusion twice a day for applicable infections in the pediatrics field. 2) Urine excretion of DOTC was about a half (50%) of the administered dosage. 3) DOTC was given mostly at about 3--5 mg/kg per day (twice a day) infusion to 25 children with five infections, viz. acute angina lacunaris, acute bronchitis, bronchopneumonia, Mycoplasma pneumonia and acute urinary tract infections. A clinical improvement seemed attributable to DOTC was clearly observed in 23 out of 25 patients (92%). 4). DOTC infusion was also effective for Mycoplasma meningoencephalitis, severe Mycoplasma pneumonia associated with pleuritis, bronchitis and bronchopneumonia with a lot of Staphylococcus aureus identified in the sputum medium, acute urinary tract infections caused by E. coli. 5) Before and ten days after DOTC infusion, laboratory tests for liver and renal functions and blood were performed. No noticeable abnormalities were found except one case with transient GOT and GPT elevations. Above summary was presented at the 26th annual meeting of Japan Society of Chemotherapy in June 1978.
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Inhibition of thymidine incorporation into DNA in cells treated with DNA-suppressing factor (DSF) has been studied. After 16 hr treatment with DSF, transport of labeled thymidine across the cell membrane was not inhibited, since equilibrium of labeled thymidine with the acid-soluble pool occurred at the same rate and the radioactivity was at the same level as in untreated cells. The values of Vmax and Km in the kinetics of transport of exogenous thymidine were not changed by DSF. Phosphorylation of labeled thymidine to deoxythymidine triphosphate (dTTP) was not inhibited by DSF. After a chase of labeled thymidine, radioactivity of the acid-soluble fraction in DSF-treated cells decreased more rapidly but that of the acid-insoluble fraction remained at a lower level than in untreated cells. It was assumed that DSF might block the entry of dTTP into DNA.
Human lymphoid cells (NC-37) persistently infected with either measles virus (Schwarz and TYCSA strains) or subacute sclerosing panencephalitis (SSPE) virus (Halle and Mantooth strains) were destroyed in the presence of complement by anti-measles sera as well as by sera from SSPE patients. The cytotoxic activity was demonstrated in both IgG and IgM fractions of measles convalescent sera, but only in IgG fraction of SSPE sera. Measles convalescent sera completely lost the cytotoxic activity to all the cell lines, when absorbed with any one of the cell lines, indicating that the viral surface antigens of these cell lines infected with measles or SSPE virus are identical. On the other hand, the cytotoxic activity of SSPE sera could not be readily absorbed with these cells. Thus, the affinity of SSPE sera for the viral surface antigens might be lower than that of measles convalescent sera.
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Fundamental and clinical studies of PC-904, a newly developed penicillin with a broad spectrum, were performed and the following results were obtained. (1) The serum levels of PC-904 after 1.5 hours drip infusion reached the peak at 1 hour or at the end of the infusion and the detectable levels of PC-904 were maintained up to 2 or 3 hours after the end of the infusion. (2) The urinary excretion rates up to 6 hours after the onset of the infusion were 19.2 approximately 25.5%. (3) Forty-one patients were treated with PC-904 and the majority of the diseases were acute respiratory infections. The treatment by the drip infusion of 50 approximately 100 mg/kg/day resulted in good responses to whooping cough, and lacunar tonsillitis, lymphadenitis and staphylococcal scald skin syndrome resistant to the treatment by ampicillin and cephalexin. The satisfactory results were also obtained by the treatment of almost the same dosage in the patients with acute bronchitis, bronchopneumonia and measles pneumonia. (4) Staphylococcus aureus and Klebsiella pneumoniae were isolated from the sputum culture of the patients with bronchopneumonia and they responded well to the treatment with PC-904. (5) The drip infusion of 60 approximately 70 mg/kg/day for 5 approximately 6 days was shown to be useful in the treatment of urinary tract infection of which the causative organism was E. coli. (6) No side effects were observed except rubella-like eruption in one case. (7) Clinical evaluation was examined in all cases except one patient of which the medication was withdrawn due to eruption, and the overall clinical efficacy was excellent or good in all of 40 cases.
Purified host DNA-suppressing factor (DSF) produced into culture fluid of HeLa C-9 cells infected with measles virus inhibited cellular DNA synthesis in HeLa cells. When purified DSF was added into cultures of synchronous HeLa cells at the early G1-phase, cellular DNA synthesis was irreversibly inhibited. However, DSF did not affect the stability of native double-stranded DNA nor the chain-elongation of single-stranded DNA in cells of the S-phase.
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