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Biomedical subjects

H Iguchi

Publications and source records attributed to H Iguchi.

At least 217 records · Page 12Linked to original sources
PubMed1980

PS-6 and PS-7, new beta-lactam antibiotics. In vitro and in vivo evaluation.

Biological properties of two new beta-lactam antibiotics, PS-6 and PS-7, containing the carbapenem nucleus were studied. The in vitro activities of PS-6 and PS-7 were tested against clinical isolates of Gram-positive and Gram-negative bacteria in comparison with those of cefazolin, ampicillin and PS-5. In general, the antibacterial spectra of PS-6 and PS-7 were similar to that of PS-5. PS-7 was slightly less active than PS-5 and ABPC against Staphylococcus aureus. Clinical isolates of Gram-negative bacteria were found to be 2- to 8-fold more resistant to PS-6 than to PS-5, while PS-7 was 2-fold more active than PS-5 against Enterobacter, Klebsiella, Proteus, Serratia and Escherichia coli. The therapeutic effect of PS-6 seemed slightly less than that of PS-5 in an experimental infection with Staph. aureus Smith in mice.

Ampicillin↗
PubMed1980

Biological properties of new acyl derivatives of tylosin.

The antibacterial activity of acyl derivatives of tylosin were examined in vitro and in vivo. The 4"-acyl group in the acylated tylosins enhanced the antibacterial activity and antimycoplasmal activity against some macrolide-resistant strains. The orally administered 3-acetyl-4" -isovaleryltylosin produced a higher blood level in mice and rabbits than tylosin and a good therapeutic effect on the infection of Staphylococcus aureus Smith in mice.

Administration, Oral↗
PubMed1980

[Acute toxicity of aclacinomycin A in mice, rats and dogs (author's transl)].

New antitumor anthracycline antibiotic, aclacinomycin A was given to dd-mice and Wistar rats for acute toxicity study. The LD50 values were 29 approximately 39 mg/kg (i.v., i.p. and s.c.) and 62 approximately 69 mg/kg (p.o.) in mice, and 18 approximately 28 mg/kg (i.v., i.p. and s.c.) and 58 approximately 59 mg/kg (p.o.) in rats, respectively, which were calculated by mortality rate during a 14 day observation period. Depression of spontaneous activity, anorexia, diarrhea and slight alopecia were observed. Autopsy findings in animals killed by drug included atrophy of the thymus and spleen, and hyperemia and hemorrhage in the stomach and intestines. But no remarkable change was found in animals which survived through the observation period. Mongrel dogs were given the drug intravenously at 3, 5, 7.5, 10 and 15 mg/kg, respectively. All dogs (3/3) in the three higher dose groups and 1/3 dog in 5 mg/kg dose group died within day 0 approximately 5. Others survived more than 27 days. Depression of spontaneous activity and anorexia were found from 30 minutes to 2 hours after administration, followed by vomiting and diarrhea. Increase of GOT, GPT and LDH and decrease of WBC count were detected in dogs which died. Hyperemia and hemorrhage of the lungs, stomach and intestine were found among the groups given higher doses, whereas no significant changes were recognized among the two lower dose groups.

Aclarubicin↗
PubMed1980

[Subacute toxicity of aclacinomycin A in rats (author's transl)].

Wistar rats, both male and female, were treated with aclacinomycin A at 4 dosage levels (0.375, 0.75, 1.5 and 3.0 mg/kg/day) by daily intraperitoneal injection for 30 days. Several rats died in the two higher dose groups (1.5 mg/kg/day: male 2/8 and 3.0 mg/kg: male 8/8, female 8/8. Piloerection, anorexia, depression of spontaneous activity, diarrhea and slight incontinence were observed in rats in 3.0 mg/kg/day dose group. Body weight gain decreased after day 3 in rats receiving 1.5 and 3.0 mg/kg/day. A significant decrease in the total WBC count and a slight decrease in RBC count were observed in animals of 1.5 mg/kg/day dose group which were survived for 30 days. Autopsy findings demonstrated atrophy of the thymus and spleen, and hyperemia and hemorrhage in the intestine. The atrophy of the thymus and decreased hematopoiesis in the bone marrow were histologically noted in the two highest dose groups. No cardiotoxicity was observed.

Aclarubicin↗
PubMed1980

[Studies on the absorption, excretion and distribution of aclacinomycin A: absorption, excretion and distribution of 14C- or 3H-aclacinomycin A in mice, rats and rabbits (author's transl)].

A new anthracycline antitumor antibiotic, aclacinomycin A, was labeled with 3H uniformly or with 14C simultaneously at the anthracycline nucleus and L-rhodosamine. These labeled drugs were administered intravenously to normal dd mice, solid type Sarcoma 180 tumor-bearing ICR mice, normal or pregnant Wistar rats and normal rabbits, respectively. 14C-Aclacinomycin A given to rabbits (5 mg/kg) was rapidly cleared from the blood and transferred to tissues. But low level of radioactivity (equivalent to about 0.5 mcg/ml) was remained in the blood even 8 approximately 10 hours after administration. About 45% of the radioactivity were recovered from the urine and 20% from the feces by 72 hours after administration. Tissue levels of 3H-14C-aclacinomycin A given to normal and tumor-bearing mice were highest in the lungs and spleen. Higher distribution was observed also in the liver and kidneys 2 hours after administration. Bioassay revealed that the drug was present in the lungs and spleen in biologically active form and in the liver and kidneys in inactive form, respectively. In the tumor tissue the radioactivity was low but it persisted for 48 hours. Autoradiography with 14C-aclacinomycin A in rats demonstrated that radioactivity due to the drug distributed in the lungs, spleen, kidneys, thymus, intestine, lymph nodes, bone marrow, salivary gland, hypophysis and pineal body but it was rapidly cleared. About 0.2% of radioactivity given to a pregnant rat were transferred to a fetus when 14C-aclacinomycin A was administered intravenously on the 18 approximately 19th day of pregnancy.

Absorption↗
PubMed1980

[Studies on the absorption, excretion and distribution of aclacinomycin A: absorption, excretion and distribution of aclacinomycin A in mice, rabbits and dogs by photometric assay (author's transl)].

An anthracycline antitumor antibiotic, aclacinomycin A, was given to mice, rabbits or dogs intravenously to study the pharmacokinetics by photometric assay based on the absorption of anthracycline ring. The drug was rapidly eliminated from the blood in these animals. Drug levels were much higher in the blood cells than in the plasma. Tissue levels in dogs were 50 approximately 100 times higher than the blood levels, which showed the drug was rapidly transferred from the blood to tissues after administration. Higher levels were observed in the lungs, spleen and lymph nodes, where the drug was present as aclacinomycin A itself and the glycoside-type metabolites that were biologically active. The active form was also detected in the pancreas, heart, thymus, bone marrow and gastrointestinal tract. In the liver and kidneys, biologically inactive aglycone-type metabolites were observed. About 2 approximately 4% of the drug given to rabbits or dogs was recovered in the urine by 72 hours after administration, in which only 10% of the excreted drug was active form in rabbits but about 65% in dogs. The rest was inactive aglycone-type metabolites that were excreted almost in the conjugated form. Biliary excretion also contributed to the total clearance of the drug. Aclacinomycin A was absorbed even by oral administration in rabbits and dogs. Tissue distribution of the drug orally given to dogs was similar to that in intravenous administration, except that higher levels of active form were detected in the gastrointestinal tract and of inactive form in the liver.

Absorption↗
PubMed1980

[Chronic toxicity of aclacinomycin A in rats (author's transl)].

Male and female Wistar rats were treated with aclacinomycin A, a new anthracycline antitumor antibiotic, at 5 dosage levels (0.08, 0.15, 0.3, 0.6 and 1.2 mg/kg/day) by daily intraperitoneal injections for 180 days for a chronic toxicity study. Recovery was also examined for 30 days after completion of the administration. Mortality was as follows: Male 5/24, female 3/24 in 0.6 mg/kg/day dose group and male 19/24, female 8/24 in 1.2 mg/kg/day dose group. Anorexia, depression of spontaneous activity and unformed feces were observed in rats in 0.6 and 1.2 mg/kg/day dose groups after day 90. Body weight gain decreased during the period. No significant change was found in rats receiving the drug at 0.3 and less mg/kg/day all through the observation period. Remarkable decreases in WBC count were noted in rats in the two highest dose groups on day 90. Autopsy findings included atrophy of the thymus and hyperemia and hemorrhage in the gastrointestinal tract and mesenteric lymph node in the animals treated at 0.6 and 1.2 mg/kg/day in the examination on day 90. Histologically, atrophy of the thymus and hyperplasia of the spleen were observed in the higher dose groups on day 90. But no remarkable abnormalities were found in histological examination on day 180. The changes in general symptom and decrease in body weight gain, which were observed during the dosing period in rats in 0.6 mg/kg/day dose group, recovered within 30 days after the drug administration was discontinued but no complete recovery of the WBC count decrease was observed.

Aclarubicin↗
PubMed1979

PS-5, a new beta-lactam antibiotic. II. Antimicrobial activity.

PS-5, a new beta-lactam antibiotic, has relatively potent antimicrobial activity against Gram-positive and Gram-negative bacteria, especially the Enterobacter groups, Serratia marcescens, the Proteus groups and Klebsiella pneumoniae. The activity of PS-5 against many beta-lactamase-producing organisms is greater than that of cefoxitin or cefazolin. PS-5 has good therapeutic activity in mice infected with Staphylococcus aureus Smith or Enterobacter cloacae 45.

Animals↗