The chemical synthesis of bestatin.
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Biomedical subjects
Publications and source records attributed to T Aoyagi.
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The activity of pyridindolol in inhibiting beta-galactosidases obtained from various sources has been studied. Whereas acid bovine liver beta-galactosidase (optimal pH 4.0) was not affected by this compound, neutral bovine liver beta-galactosidase (pH-optimum = 7.0) was inhibited by pyridindolol in reaction mixtures of pH 4.0 approximately 5.0. There was no inhibition at pH 7.0. The type of inhibition is non-competitive by formation of a pyridindolol-enzyme complex. Since beta-galactosidases from other sources are not affected by pyridindolol, the inhibitory action of this compound seems to be rather specific for neutral bovine liver beta-galactosidase.
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The effect of six protease inhibitors, isolated from various species of actinomycetes, on focus formation by murine sarcoma virus was examined. Pepstatin was the only inhibitor. The treatment of cells with pepstatin at various times possibly retards the early stage of infection with murine sarcoma virus.
A patient with aortitis syndrome had a pleural effusion which subsided but reappeared with an exacerbation of aortitis symptoms while under antituberculosis treatment. The character of the fluid was that of an exudate, and the glucose concentration was normal. Clinical and laboratory features of the case suggest that the effusion was part of the aortitis syndrome per se.
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Pyridindolol is a product of a streptomyces and exhibits inhibitory activity against bovine liver beta-galactosidase. The structure of pyridindilol, 1-[1(R), 2-dihydroxyethyl]-3-hydroxymethyl-9H-pyrido[3,4-b] indole, has been established by spectroscopic analyses and an X-ray structure determination.
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Therapeutic effects of lividomycin (LVDM) were studied in 33 patients with respiratory infections including pneumonia, lung abscess, chronic bronchitis, etc. LVDM was intramuscularly administered at the dose of 1 or 2 g per day for consecutive 4 to 25 days. The results obtained are summarized below: 1. At the end of the first week of the treatment, rate of improvement in such parameters as cough, sputum, rales, fever and blood sedimentation rate were 69%, 56.7%, 60%, 79.2% and 70% respectively. Also, in 16% of the patients, abnormal shadow noted in X-ray film of the chest was disappeared and in 20% of the patients, size of the same was reduced during the first week of treatment. 2. Therapeutic effects of LVDM were evaluated synthetically and were graded as excellent, good, fair and ineffective. LVDM was effective in about 70 per cent of the patients, that is, excellent results were obtained in 4 patients, good in 12 patients, fair in 6 patients, and in 10 patients this antibiotic was ineffective. 3. In one patient with slight loss of high frequency perception was observed on the audiogram, but no other ototoxic effects such as subjective hearing loss, tinnitus, etc. In addition, no untoward effects on renal and hepatic function were observed. 4. The MIC values of LVDM for clinically isolated 20 strains of Pseudomonas aeruginosa were examined, using kanamycin for comparison. The MIC values of LVDM for many strains were superior to those of kanamycin. In view of the test results mentioned above, LVDM would appear to be useful medication for the treatment of some of respiratory infections.
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