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Volume 26 (1973)
- Issue 6 Pages 501-
- Issue 5 Pages 427-
- Issue 4 Pages 321-
- Issue 3 Pages 197-
- Issue 2 Pages 89-
- Issue 1 Pages 1-
Predecessor
Volume 26, Issue 2
Displaying 1-13 of 13 articles from this issue
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SUSUMU MITSUHASHI, SATONORI KURASHIGE, NORIO YAMAGUCHI, ZENSHO INAFUKU ...1973 Volume 26 Issue 2 Pages 89-96
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS1) DKB showed especially high antibacterial activity against Pseudomonas aeruginosa of clinical origin.
2) DKB showed antimicrobial activity against gram-positive and gram-negative bacteria, but it was somewhat inferior to that of GM except Pseudomonas.
3) The activity of DKB is reduced by a pH of acidic media, but on Staphylococcus aureus Rosenbach FDA 209-P JC-1, it is reduced by a pH of alkaline media.
4) The activity of DKB is not influenced by a bovine serum, horse serum, rabbit serum and bovine serum albumin.
5) Rate of binding to serum protein of DKB and GM, at the concentrations of 100-1,000 mcg as free base per 1 ml of calf serum was 6.3-13.9% and 26.7-41.2% respectively, apparently smaller in DKB.
6) The bactericidal action of DKB was showed at the minimal inhibitory concentration (MIC) on Pseudomonas aeruginosa H1, Proteus vulgaris OX19, and Bacillus subtilis ATCC 6633, and at twice the MIC on Escherichia coli K-12 IAM-1264 and Kiebsiella pneumoniae 602.
7) DKB was found superior to GM in the ED50 against experimental mice infection with the strains of Pseudomonas aeruginosa, and it was almost equal against experimental mice infections with other gramnegative enteric bacteria.View full abstractDownload PDF (1057K) -
TAKEHIKO IWASAWA1973 Volume 26 Issue 2 Pages 97-103
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSMinocycline is a new tetracycline family antibiotic which has a broad antibacterial spectrum, and is more potent than other tetracyclines. Minocycline was tested with the following results:
1.In vitro antibacterial activity: The minimum inhibitory concentration of minocycline was estimated by an agar-plate dilution method. Minocycline inhibited the growth of 60 strains of coagulase-positive Staphylococcus aureus at <0.19-50mcg/ml. Minocycline sensitivity is higher than other tetracyclines.
2. Serum level: A peak serum level of 2.3mcg/ml was reached 2 hours after oral administration of 100mg minocycline dry-syrup in healthy children, followed by a gradual decrease in the level. An effective level of 0.9mcg/ml was still demonstrable after 24 hours.
3. Concentration in tissues: Two hours after the oral administration of 100mg minocycline drysyrup, 1.5mcg/g was found in a human platine tonsilla specimen, and 0.9mcg/g in a human maxillary sinusitis specimen, while 2.2 mcg/ml in serum.
4. Clinical effect: By the oral administration of 4mg/kg minocyclne dry-syrup, 27 of 30 cases (90%) of infections in otorhinolaryngological field showed good results. No side effect was observed.View full abstractDownload PDF (3600K) -
HAJIME SATO, OSAMU WATANABE, KENJI NIINOH, SUSUMU NAKAZAWA, TAKESHI YA ...1973 Volume 26 Issue 2 Pages 104-108
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSDownload PDF (628K) -
TAKAAKI AOYAGI, SETSUKO KUNIMOTO, TOMIO TAKEUCHI, HAMAO UMEZAWA1973 Volume 26 Issue 2 Pages 109-114
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS -
Physicochemical and Biological PropertiesTAKASHI OSONO, KUNIICHIRO YANO, KEISUKE MURAKAMI, FUMIO MIYAMOTO, KYOK ...1973 Volume 26 Issue 2 Pages 115-121
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSPhysicochemical and biological properties of josamycin propionate (JM-P) were studied, and the following results were obtained.
1. Josamycin propionate is a new derivative of josamycin (JM) having no bitter taste, physicochemical properties of which were described.
2. Like josamycin, josamycin propionate showed strong antibacterial activity against gram-positive bacteria, but very weak activity against enteric gram-negative bacteria. Its MIC's were 0.78-1.56 mcg/ml against Staphylococcus aureus, 7.8mcg/ml against Streptococcus hemolyticus and 0.09 mcg/ml against Diplococcus pneumoniae, which were equal to or a little weaker than those of josamycin. It showed cross resistance to macrolides but not to other antibiotics.
3. Antibacterial activity of josamycin propionate increased at the alkaline side of medium pH, but was not so affected by inoculum sizes.
4. Josamycin propionate showed bactericidal activity against Staphylococcus aureus SC-17 at 6.25 mcg/ml which was 8 times MIC.
5. Josamycin propionate showed strong propective effect against gram-positive infections in mice. ED50'S of oral josamycin propionate were as follows:
JM-P JM
Staphylococcus aureus Smith 143 217mg/kg
Streptococcus hemolyticus S-23 95 116
Diplococcus pneunsoniae Type I 540 620
Escherichia coli NIHJ >1000 >1000
6. In protection of subcutaneous staphylococcal infections in mice, josamycin propionate was as active as josamycin.View full abstractDownload PDF (775K) -
II. DISTRIBUTION AND METABOLISMAKIO TACHIBANA, MASAKATSU SHIBATA, FUMIKO KUMAGAI, KIRUKO MORIYAMA, KU ...1973 Volume 26 Issue 2 Pages 122-129
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSDistribution of josamycin propionate (JM-P) and josamycin (JM) after oral administration was studied in rats, dogs and man. Their metabolites excreted into urine were also studied by thin-layer chromatography.
1. In rats, josamycin propionate showed lower blood, kidney and spleen levels than josamycin, but almost same levels in heart, lungs and liver. Especially in lungs, josamycin propionate gave a high peak level comparable to josamycin. The level was more than twice higher than that of josamycin after 10 hours.
2. In dogs and man, peak blood levels of josamycin propionate were 1/4 to 1/2 those of josamycin, although sustaining of blood levels was observed.
3. As main metabolites in rat urine, josamycin gave deisovaleryl josamycin (DeIv-JM), and josamycin propionate gave deisovaleryl josamycin and deisovaleryl josamycin propionate (DeIv-JM-P).
In dogs, josamycin gave four main metabolites, i. e. metabolite O (hydroxylated josamycin), deisovaleryl josamycin and two unidentified metabolites in Rf order. Josamycin propionate gave these metabolites accompanied by a couple of other spots.
Josamycin taken by man gave metabolite O as the main metabolite, and a considerable amount of unchanged josamycin as well was excreted into urine. Oral josamycin propionate in man gave spots corresponding to those of josamycin and metabolite 0 as main metabolites. However, no unchanged josamycin propionate was detected.
4. The metabolite O was isolated as crystals from urine of human adults whoo took josamycin, and identified as hydroxylated josamycins. The metabolite O was further separated into O1, a hydroxylated product at josambose (demycarosyl josamycin) moiety, and O2, a hydroxylated product at isovaleryl moiety.View full abstractDownload PDF (1043K) -
PHARMACOLOGICAL STUDIESTOKUICHI TAKAGI1973 Volume 26 Issue 2 Pages 130-135
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSPharmacological effects of josamycin propionate, a new macrolide antibiotic derivative, were studied, and the following results were obtained.
(1) No influence was observed on behavior patterns of mice and dogs, barbital induced sleeping time, convulsion caused by pentyleneterazol, strychnine and MES in mice, rectal temperature of rats and EEG of cats when 1,000mg/kg of josamycin propionate were administered orally.
(2) The spontaneous motility of isolated guinea-pig intestine by MAGNUS' method was not affected at a high concentration (10-3g/ml) of the compound. No influence was detected on constriction produced by acetylcholine, histamine, barium, serotonin and nicotine, but a slight inhibition was recognized at a high concentration (10-3g/ml). Josamycin propionate at 10-5 g/ml and higher caused dosedependent decrease in contractility of isolated rat uterus by MAGNUS' method. No influence on heart rate, blood pressure or contraction of nictitating membrane evoked by autonomic nerve stimulation was observed at intra-duodenal 300mg/kg.
(3) No influence was shown on respiration, blood pressure, heart rate or ECG with oral 1,000 mg/kg of josamycin propionate in unanesthetized dogs and with intra-duodenal 1,000mg/kg in the anesthetized. Josamycin propionate caused slight drop in blood pressure, and increase of respiration rate and heart rate in anesthetized dogs injected with 300mg/kg intraperitoneally, but no abnormal ECG pattern was recorded. On isolated guinea-pig atria, a slight depression of amplitude of contraction and a slight decrease of heart rate were observed at a high concentration (10-3 g/ml). Transient vasodilation of isolated rabbit ear vessel was recognized at a concentration of 5 × 10-5 g/ml.
(4) On neuromuscular junction in rats, no effect was observed at 1,000 mg/kg given orally.
(5) On urinary excretion in rats, josamycin propionate showed no significant difference from control at oral 1,000mg/kg.View full abstractDownload PDF (3504K) -
ToxicityHIKOZAEMON HAZATO, TADASHI YAMAMOTO, ICHIRO TADOKORO, AKIYOSHI KAWAMUR ...1973 Volume 26 Issue 2 Pages 136-147
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSAcute and subacute toxicities of josamycin propionate were studied, and the following results were obtained.
1. MLDs of josamycin propionate in male and female ICR-JCL mice and Sprague-Dawley-JCL rats were more than 4,000mg/kg (expressed as equivalent weight of josamycin) by oral, more than 4,000 mg/kg by subcutaneous and more than 2,000mg/kg by intraperitoneal administrations.
2. Male and female Wistar-Imamichi rats were given orally 2,000, 1,000,300 and 100mg/kg/day doses of josamycin propionate for 32 successive days. All animals survived except a female rat of 2,000 mg/kg group killed by an accident on the 24th day.
No significant change was observed in growth curves, hematological findings and biochemical examinations of blood sera as compared with the control group.
Histological examinations of tissues revealed no significant changes related to toxic effect of the drug.View full abstractDownload PDF (22891K) -
V. TERATOROGICAL STUDIESTOSHIHIKO OSHIMA, MASANORI IWADARE1973 Volume 26 Issue 2 Pages 148-153
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSTeratological effects of josamycin propionate on ICR-SLC mice and SD-SLC rats were studied, and the following results were obtained.
Josamycin propionate was administered orally at the daily dose of 200, 1,000 and 2,000mg/kg body weight for 7 days to pregnant mice of 7th-13th day of gestation and pregnant rats of 8th-14th day of gestation.
1) In mice, the increase in body weight was suppr essed in animals given 1,000 and 2,000mg/kg of the compound as compared with the control group.
2) A dose of 2,000mg/kg caused a marked increase in wet weight of the spleen in 3 out of 25 mother mice, and in these amimals the resorption rate of fetuses was 75%.
3) In growth of fetuses of mice and rats, no significant difference was observed between the control and the medicated group.
4) No teratological effect was observed on the fetuses of mice and rats.View full abstractDownload PDF (742K) -
TAIRA TAKANO, HIDEYUKI ISHIKAWA, MASAKAZU YOSHIOKA, YOSHIGORO OGURO1973 Volume 26 Issue 2 Pages 154-156
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSBlood level of penicillin V (PV), erythromycin (EM), tetracycline (TC) and chloramphenicol (CP) after intraduodenal injection with and without bromelain was studied im rabbits.
Remarkable effect of bromelain to accelerate and enforce the blood levels of PV and EM was observed, while the effect was slight or weak with TC and CP.View full abstractDownload PDF (330K) -
KEIYU NINOMIYA, KUNITOMO WATANABE, KAZUE UENO, SHOICHIRO SUZUKI, IZUMI ...1973 Volume 26 Issue 2 Pages 157-162
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSThe minimal inhibitory concentrations of about 200 clinical isolates of anaerobic bacteria to lincomycin (LCM) and clindamycin (CLDM) were determined by agar-dilution technique employing agar as basic medium and steel-wool method.
Many strains of Peptococcus, Peptostreptococcus and Veillonella were sensitive to the concentration of 6.25mcg/ml LCM and of 3.13mcg/ml CLDM, though one strain of Peptococcus prevotii was resistant to 100mcg/ml LCM and CLDM, and 5 strains of Peptococcus variabilis had no susceptibility to CLDM (100mcg/ml).
Many strains of Bacteroides were inhibited by 6.25 mcg/ml LCM as well as by 3.13mcg/ml CLDM.
Whereas Fusobacterium varium and F. glutinosum had low susceptibility to LCM and CLDM in comparison with Peptococcus, Peptostreptococcus, Veillonella and Bacteroides. Most of them were resistant to these drug at concentration of 25mcg/ml.
Antibacterial activity of CLDM against anaerobes tested in this study excelled erythromycin and rifampicin (RFP). LCM had less activity than RFP.View full abstractDownload PDF (696K) -
1973 Volume 26 Issue 2 Pages 163-173
Published: April 25, 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESSDownload PDF (734K) -
1973 Volume 26 Issue 2 Pages 103-
Published: 1973
Released on J-STAGE: May 17, 2013
JOURNAL FREE ACCESS
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