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Biomedical subjects

A Fujii

Publications and source records attributed to A Fujii.

At least 289 records · Page 16Linked to original sources

Biological studies on the degradation products of 3-[(S)-1'-phenylethylamino]propylaminobleomycin: a novel analog (pepleomycin).

Pepleomycin (PEP), 3-[(S)-1'-phenylethylamino]propylaminobleomycin has potent activity and is less pulmonary toxic than bleomycin (BLM). Biological activity and toxicity of the following degradation products of PEP have been studied in detail: the product of carbamoyl migration (ISO), the product of decarbamylation (DC), the product of ring closure of the side chain on the pyrimidine moiety (RC), the depyruvamide product (DP) and the product of an enzymatic inactivation (DA). These degradation products showed much lower activity than PEP in vitro: antimicrobial and anti-HeLa activities, inhibition of DNA synthesis in AH66 cells and the DNA strand cleavage. Acute toxicity and pulmonary toxicity were tested in mice. Results indicated much lower acute toxicity corresponding to the decreased in vitro activity when compared to PEP. DP and RC did not cause lung fibrosis in mice, while ISO and DC showed 1/2.6 and 1/5.7 degree of pulmonary toxicity, respectively, in comparison with PEP.

Animals↗

Comparison of stationary phases in reversed-phase TLC for correlation between structure and biological response of probiotics.

A series of C16,C18 and C20 fatty acids and their ethyl esters and alcohols were investigated as possible stationary phases in reversed-phase TLC for the correlation between structure and biological response (antistaphylococcal activity). Ten probiotics (omego-amino acids and their L-histidine dipeptides) were used as the biologically active compounds. The mobile phase was 70% acetone in water. The best correlations were obtained with hexadecanoic acid (palmitic acid) or cis9,cis-12,cis-15-octadecatrienoic acid, 1-hexadecanol or cis-9-octadeconol, and ethyl hexadecanoate for the fatty acids, their alcohols, and their ethyl esters, respectively. Among all compounds, the following relation was obtained: fatty acids = alcohols greater than ethyl esters greater than white paraffin oil.

Anti-Bacterial Agents↗

[Comparative results of cephacetrile with cefazolin in complicated urinary tract infections by means of double-blind trials (author's transl)].

In order to elucidate the usefulness of cephacetrile (CEC), comparative trials with cefazolin (CEZ) were carried out in the patients with complicated infections of the urinary tract, and the following results were obtained: 1. There were no statistically significant differences or tendencies observed between the groups given CEC and CEZ in either of the global effects, bacteriological effects, rate of superinfection, relapse, relapse with bacterial alternation, drug usefulness, rate of improvements in symptoms and findings in all the cases. 2. According to a result of stratified analyses, there were statistically significant differences observed, showing more inferior results of CEC than CEZ in either stratum of "below 50" in the age, "acute" in the disease phase, "infections of the upper urinary tract" in the disease pattern, and "E. coli including mixed infections with gram-positive organisms" in the pathogenic strains. However, it should be taken into consideration that certain background factors influence greatly in the effects and there were some problems on deviated backgrounds in these strata. On the other hand, CEC displayed better bacteriological effects than those of CEZ in higher stratum of "chronic" in the disease phase and "Klebsiella, Proteus, Citrobacter, Enterobacter including mixed infections" in the pathogenic strains, and statistically significant differences were not observed. 3. In consequence of bacteriological studies, CEC showed stronger resistance than CEZ against beta-lactamase produced in all the strains of gram-negative bacilli. Particularly there were significant differences or tendencies observed in those of Proteus, Cirtobacter, and Enterobacter, and at the same time there were great differences in the activity of beta-lactamase between CEC and CEZ as the substrate. 4. In correlation of the MIC and effects, CEC showed weaker actions than CEZ against susceptible organisms, but slightly stronger actions against moderately or highly resistant strains. A study of the relationship between the MIC of pathogenic strains, beta-lactamase, and bacteriological effects, showed possibilities that even the high activity of beta-lactamase results in remarkable effects in susceptible strains and the drugs with stronger resistance against beta-lactamase given better results in moderately or highly resistant organisms. 5. The incidence rate of adverse reactions was 2 out of 51 cases in the CEC group (3.9%) and 3 out of 50 cases in the CEZ group (6.0%), showing no significant difference, and those symptoms were similar. In conclusion, when the usefulness of CEC in complicated infections of the urinary tract is compared with that of CEZ, the former is said to be equal to the latter without significant difference as a whole...

Adult↗

Probiotics. Antistaphylococcal and antifibrinolytic activities of omega-amino-and omega-guanidinoalkanisulfonic acids.

A series of omega-aminoalkanesulfonic acids (1-5) and omega-guanidinoalkanesulfonic acids (6-9) has been tested for antistaphylococcal and antifibrinolytic activities. Most of the omega-aminoalkanesulfonic acids and 6 produced better protection against Staphylococcus aureus infections in mice than gamma-aminobutyryl-L-histidine. Compound 4 was the best antistaphylococcal agent among the omega-aminoalkanesulfonic acids and compound 6 among the omega-guanidinoalkanesulfonic acids. Most of the omega-aminoalkanesulfonic acids have antifibrinolytic activity, while none of the omega-guanidinoalkanesulfonic acids has significant antifibrinolytic activity. Compound 4 possessed the highest antifibrinolytic activity which was equal to or greater than that of epsilon-aminohexanoic acid.

Alkanesulfonates↗