Search PubMed⌕ Search

Biomedical subjects

A Fujii

Publications and source records attributed to A Fujii.

At least 199 records · Page 11Linked to original sources
PubMed1988

Synthesis and biological activity of spergualin analogues. I.

Stable spergualin analogues were synthesized by substitutions of the alpha-hydroxyglycine residue of spergualin with various alpha- or omega-amino acids. The antitumor activity of these analogues against L1210 and their immunosuppressive effects on delayed-type hypersensitivity and antibody formation was then examined. Analogues substituted with glycine and L-serine showed significant biological activity but were less potent than 15-deoxyspergualin. Among the analogues synthesized so far, 10-[N-4-(4-guanidinophenyl)butyryl-L-seryl]-1,5,10-triazadecane has possessed the strongest antitumor and immunosuppressive activities.

Animals↗
PubMed1988

In vivo effects of deoxyspergualin (NKT-01) on lymphocyte activation in response to alloantigens.

We studied the effects of deoxyspergualin (NKT-01) on the events of lymphocyte activation in vivo by inoculating mice in the footpad with allogeneic spleen cells, and compared the effects with those of cyclosporin A (CyA). The administration of NKT-01 increased the numbers of cells recovered from the popliteal lymph node (PLN) 7 days after inoculation, but inhibited the proliferation of these cells in the presence of exogenous interleukin 2 (IL-2). NKT-01 enhanced IL-2 production, but suppressed the production of macrophage activating factor (MAF) in the mixed lymphocyte reaction between the PLN cells and allogeneic spleen cells treated with mitomycin C. CyA decreased the numbers of PLN cells little, and suppressed the response to exogenous IL-2 and the production of both IL-2 and MAF. Results with tumor cells used as allogeneic cells suggested that there was a close relationship between the suppression of MAF production by NKT-01 and its inhibition of allograft rejection. The findings showed that NKT-01 inhibited both the MAF production by and the response to IL-2 of PLN cells, and that these effects were involved in the suppression of allograft rejection by NKT-01.

Animals↗
PubMed1988

[Pharmacokinetics and urinary excretion of aspoxicillin after consecutive administration at a dose of 4 grams].

Aspoxicillin (ASPC), a new injectable penicillin, was administered to 5 healthy male adult volunteers once a day at a daily dose of 4 g for 5 consecutive days to study its absorption and excretion. The results of this study are summarized as follows: 1. In consecutive administration of ASPC for 5 successive days, no remarkable changes were observed in serum concentrations and urinary excretion after each administration of ASPC. Therefore, no tendency of accumulation of the drug was recognized. 2. The serum ASPC concentration showed its peak values ranged from 212.3 to 224.8 micrograms/ml at completion of the intravenous drip infusion of ASPC. 3. Urinary recovery rates of ASPC ranged from 70 to 80%. 4. There were neither abnormal findings in subjective and objective symptoms nor abnormal values in physical and clinical laboratory test due to the administration of ASPC.

Adult↗
PubMed1988

[Radical endoscopic treatment of early gastric cancer-indication for and evaluation of endoscopic resection].

In the endoscopic treatment of early gastric cancer, it is absolutely necessary to adapt a radical approach. The indication for this technique in 545 surgically resected cases of single gastric cancer was studied and technical evaluation was made of endoscopic resection (ER) in 98 of early gastric cancer lesions. Except for 2 special lesions of early gastric cancer, invasion depth m and sm minute invasion [sm(+)] cancer did not show lymph node metastasis [n(+)], but this was recognized in sm(++) cancer showing more than moderate invasion and which was deeper than pm cancers. The applicable lesions were selected excluding the n(+)-risk group with invasion deeper than sm(++) based on histological type, macroscopic type, size and the presence or absence of ulcers(Ul). These were differentiated type II a less than 2 cm in size, differentiated type Ul(-) II c of less than 1 cm and undifferentiated type Ul(-) II c of less than 5 mm in areas excluding the fundic gland mucosa. Our method of ER is endoscopic double snare polypectomy. II a or II c lesion is artificially squeezed into a pedunculated form. The cutting snare is placed over the peduncle, the grasping forceps are replaced with another snare to grasp the tumor firmly. Then cutting snare is applied to include sufficient normal mucosa surrounding the lesion and coagulating current is passed through to slowly resect the ared. The 1st-ER healing ratio, remnant ratio and recurrence ratio of standard ER in 55 II a and 30 II c lesions were 83.5, 12.9 and 3.5% respectively. The recurrent cases were retrospectively found originals in the remnant. Among remnant and recurrences, the 2nd-ER healing ratio was 43% (6/14) and surgically treated cases were 8 (6 inapplicable cases), the final ER healing ratio being 90.6% and satisfactory. Most of the remnant lesions were II a of more than 2 cm, and II c of more than 1 cm for differentiated type and II c for undifferentiated type. As ER could not be applied to these lesions, its indication was confirmed to be technically satisfactory.

Gastroscopy↗
PubMed1988

[Characteristics of gastric cancer detected by mass survey. Comparison with those of outpatients].

The characteristics of gastric cancers detected by mass survey were studied by comparison with those of outpatients attending our hospital. Form 1966 to 1985, a total of 290,987 examinees were screened by gastric mass survey at our Mass Survey Center. Among them, 474 cases (0.16%) of gastric cancer were detected, and of these, 254 cases (52%) were early gastric cancer. Upon comparison of macroscopic types of surgically treated cancers, there were 152 cases (39.6%) out of 784 cases in the mass survey group and 658 cases (21.3%) out of 3,091 cases in the outpatient group having the depressed type and 11% in the former and 5.5% in the latter having the elevated type of early gastric cancer. As for the prognosis of cancers in both groups, the 5- and 10-year survival rates of 274 cases in the mass survey group and 1,859 cases in the outpatient group undergoing resection between 1964 and 1974 were compared. It was found that 80.0% for 5 years and 78.5% for 10 years in relative survival rates were obtained in the mass survey group, and 56.2% for 5 years and 55.1% for 10 years in the outpatient group. This difference in survival rate was due to the fact that the mass survey group had a high ratio of early gastric cancer than the outpatient group, and that even the advanced serosal cancer former group had less lymph node metastasis than the latter group.

Ambulatory Care↗
PubMed1987

Comparison of N-acetyl-beta-D-glucosaminidase and alanine aminopeptidase activities for evaluation of microangiopathy in diabetes mellitus.

The activities of urinary N-acetyl-beta-D-glucosaminidase (NAG) and alanine aminopeptidase (AAP) were measured in 207 diabetic patients and 57 healthy controls, and the relationship of these enzymes to different stages of diabetic microangiopathy was studied. Diabetics with clinical proteinuria had higher urinary NAG and AAP (17.7 +/- 1.9 and 42.8 +/- 4.9 U/g creatinine, mean +/- SE, respectively) than healthy controls (1.8 +/- 0.1 and 10.0 +/- 0.4) or diabetics without proteinuria. Among diabetics without proteinuria, NAG excretion in those with retinopathy was slightly higher than in those without (6.4 +/- 0.5 v 5.4 +/- 0.4), and AAP in those with retinopathy was significantly higher than in those without (23.0 +/- 1.5 v 17.4 +/- 0.8, P less than 0.01). Urinary albumin measured by radioimmunoassay and lysozyme in diabetics with retinopathy but without proteinuria was higher than those without retinopathy (P less than 0.001 and P less than 0.01). The increase in albumin was the greatest in diabetics with long duration of the disease (greater than or equal to 8 years); however, NAG and AAP increased more significantly in those with high hemoglobin A1c than in patients with long duration.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetylglucosaminidase↗
PubMed1987

[Antitumor effects of royal jelly (RJ)].

Antitumor effects of Royal Jelly (RJ) were investigated employing the transplantable tumors of mouse advance leukemia L1210 and P388 strains and Ehrlich, Sarcoma-180 ascites and solid tumor strains. RJ was administered orally in a prophylactic-therapeutic (30 days before and 30 days after the transplantations of tumor cells) or a therapeutic (30 days after the transplantations of tumor cells) manner. Tumor cells were transplanted i.p. (ascites tumor) or s.c. (solid tumor). The daily dose of RJ was 0 (control), 10, 100, or 1000 mg/kg. In the case of the therapeutic experiments employing advance leukemia L1210 and P388 strains, which gave quite a short survival period of 8 approximately 9 days, RJ did not show any antitumor effect. In the case of the therapeutic RJ application employing the Sarcoma-180 ascites tumor, which gave a moderate survival period of 16 days, the increased life span was 9.3 approximately 19.3%; and with the Ehrlich ascites tumor (survival period of 22.1 days), the increased life span was 20.4% (RJ 10 mg/kg . day) and 17.6% (RJ 1,000 mg/kg . day), but no antitumor effect was observed at the dose of 100 mg/kg . day. In the case of the therapeutic experiment employing Ehrlich solid tumor, tumor growth inhibition was 25.3 approximately 54.8%, where as the use of the prophylactic-therapeutic regimen gave a tumor growth inhibition of 38.3 approximately 45.7%. In the case of the therapeutic RJ application employing Sarcoma-180 solid tumor, tumor growth inhibition was 45.1 approximately 59.7%, where as the prophylactic-therapeutic regimen gave a tumor growth inhibition of 49.1 approximately 56.1%.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1987

Synthesis and antitumor activity of spergualin analogues. II. Chemical modification of the spermidine moiety.

Chemical modifications of the spermidine moiety of an antitumor antibiotic, spergualin (Ia), and the structure-activity relationship are described. Replacement of spermidine with other polyamines decreased the antitumor activity against mouse leukemia L1210. Analogues containing an oxidized spermidine moiety that probably formed during oxidation with amine oxidase were inactive. Spermidine is indispensable for the antitumor activity. A facile method for the synthesis of glyoxyloyl polyamine, a key intermediate of spergualin-related compounds, is also reported.

Animals↗
PubMed1987

Synthesis and antitumor activity of spergualin analogues. III. Novel method for synthesis of optically active 15-deoxyspergualin and 15-deoxy-11-O-methylspergualin.

Optically active 15-deoxyspergualin (II) and 15-deoxy-11-O-methylspergualin (IIa) were synthesized, and their antitumor activities were examined. The (-)-enantiomers of both II and IIa were active against mouse leukemia L1210, while the (+)-enantiomers were almost inactive. The optical resolution of the key intermediate, (+/-)-N-(7-guanidinoheptanoyl)-alpha-alkoxyglycine (VI) was achieved by use of an exopeptidase, serine (acid) carboxypeptidase [EC 3.4.16.1] and (+/-)-N-(7-guanidinoheptanoyl)-alpha-alkoxyglycyl-L-amino acid (VIII) as the substrate. Considering the enzymatic susceptibility of the substrate (VIII), we deduced that the absolute configuration of the carbon at 11 (C-11) of the bioactive (-)-enantiomer, and so that of natural spergualin (I), is S. This is, to our knowledge, the first report of the use of carboxypeptidase for the resolution of N-acyl amino acid.

Animals↗