Search PubMed⌕ Search

Biomedical subjects

Y Takiguchi

Publications and source records attributed to Y Takiguchi.

At least 145 records · Page 8Linked to original sources

Milbemycins, a new family of macrolide antibiotics. Fermentation, isolation, physico-chemical properties and bioconversion of milbemycins J and K.

Strain Rf-107, a mutant of Streptomyces hygroscopicus subsp. aureolacrimosus, obtained with ultraviolet irradiation, produced two new macrolide antibiotics, milbemycins J and K without production of any of the other milbemycins described in the previous paper. Fermentation studies on the strain were conducted in shake flasks and 30-liter jar fermentors. Isolation of the antibiotics was performed by adsorption on resinous adsorbent followed by elution with aqueous MeOH. Purification of milbemycins J and K was completed with Lobar Si 60 column chromatography to give colorless crystals. Physico-chemical data, such as UV, IR and NMR spectra are described. Milbemycins J and K were readily converted by the intact cells of the parent strain to milbemycins alpha 1 and alpha 3, respectively. Physico-chemical characterization and the bioconversion studies revealed that milbemycins J and K were new antibiotics having the 16-membered macrocyclic lactone with a 6,6-membered spiroketal ring system.

Anti-Bacterial Agents↗

Milbemycins, a new family of macrolide antibiotics. Studies on the biosynthesis of milbemycins alpha 2, alpha 4 and D using 13C labeled precursors.

The biosynthetic origins of the carbon skeleton of milbemycins alpha 2, alpha 4 and D were studied. 13C Labeled antibiotics, milbemycins alpha 2, alpha 4 and D, were isolated from the culture broth of Streptomyces hygroscopicus subsp. aureolacrimosus strain Au-3 after feeding [1-13C]acetate, [1-13C]-propionate, [3-13C]propionate, [1-13C]isobutyrate, DL-[2-13C]valine and L-[methyl-13C]methionine, and 13C NMR spectra of the antibiotics thus obtained were measured. It was revealed that the carbon skeleton, except for carbon 25, of milbemycins alpha 2, alpha 4 and D are derived from seven acetate units and five propionate units. It was also shown that the methyl, ethyl and isopropyl groups at carbon 25 in milbemycins alpha 2, alpha 4 and D are derived from acetate, propionate and isobutyrate or DL-valine, respectively, and the methyl carbon of the methoxy group at carbon 5 in milbemycins alpha 2 and alpha 4 was enriched by L-[methyl-13C]methionine.

Acetates↗

Aortic cholesterol esterase and other lysosomal enzyme activities in DOCA-salt, renal and spontaneous hypertension in the rat.

In spontaneously hypertensive rats, prolonged hypertension caused a decrease in aortic cholesterol esterase activity with N-acetyl-beta-D-glucosaminidase activity increased and acid phosphatase activity unchanged [3]. The present study was undertaken to compare these changes with those caused by other experimentally induced types of hypertension. Treatment with DOCA-salt for one month significantly elevated both aortic cholesterol esterase and acid phosphatase activities. In contrast, to spontaneous hypertension, venous changes were also observed. An intake of 1% NaCl ad libitum produced results similar to those with the DOCA-salt treatment, despite the fact that blood pressure did not increase. This suggested that humoral factors were the main cause of the elevated enzyme activities in DOCA-salt hypertension. In rats made hypertensive by unilateral renal arterial constriction with contralateral nephrectomy (one clip--one kidney hypertension) or without contralateral nephrectomy (one clip--two kidney hypertension), aortic cholesterol esterase activities were unchanged, while aortic N-acetyl-beta-D-glucosaminidase, and aortic and venous acid phosphatase activities were increased. These results show distinct differences in the response of lysosomal enzymes during the three hypertensive states.

Acetylglucosaminidase↗

Effect of cellular reaction in gastric cancer tissue and in regional lymph nodes on the mitotic activity of cancer cells.

An in vivo stathmokinetic technique was used to analyze the mitotic activity of cancer cells from 47 gastric cancer patients. The effect of cellular reaction in cancer tissues and regional lymph nodes on the mitotic activity of cancer cells was examined. Based on the main kind of infiltrating cells in cancer tissues, the cellular reaction was classified into agranulocyte (lymphoid leukocyte) type and granulocyte type. Agranulocyte type was found in 40 cases. The mitotic activity of cancer cells was examined in relation to the degree of agranulocyte infiltration: the average mitotic index in cancer cells 16 hr aft a single dose (0.02 mg/kg body weight) of vincristine sulfate was 91.5% in 22 cases of trace and slight infiltration, 81.3% in 12 cases of moderate infiltration and 53.2% in 6 cases of marked infiltration. The 3 values of mitotic index were significantly different from one another. The relationship between the average mitotic index of cancer cells in primary cancer lesions and the 4 groups of regional lymph node reaction was examined. However, statistically significant results were not obtained. These results suggest that the infiltration of agranulocytes in cancer tissues affects the mitotic activity of cancer cells, and that moderate and marked degrees of infiltration suppress the mitotic activity. It was also suggested that the reaction of regional lymph nodes does not affect the mitotic activity of cancer cells in primary cancer lesions.

Adenocarcinoma↗

Hemodynamic effects on aortic enzyme activities in spontaneously hypertensive rats.

Spontaneously hypertensive rats (SHRSP and SHR) and normotensive WKR were treated with hypotensive drugs, and arterial and venous enzyme activities were compared between treated and nontreated hypertensive groups. With the 4 month experiment, cholesterol esterase activity in the aorta from hypertensive SHRSP and SHR was significantly lower than that in the respective treated groups, whereas venous activity did not differ. By contrast, aortic NAGA activity was significantly higher in the hypertensive groups without any changes in venous activity. Acid phosphatase activity was unaltered. No effects of treatment were observed in the normotensive WKR. Accompanying a decrease in aortic cholesterol esterase, there was a marked increase in aortic cholesteryl esters accompanying hypertension. Aortic phosphodiesterase activity was significantly elevated in the hypertensive SHRSP and SHR compared with the respective treated groups. These results suggest that hypertension of long duration specifically decreased aortic cholesterol esterase activity with a consequent accumulation of cholesteryl esters in the aorta, and that this hemodynamic effect seemed to be partly mediated by cyclic AMP with an effect on the lysosomal membrane. These results could provide the biochemical bases for the relationship between hypertension and atherosclerosis.

3',5'-Cyclic-AMP Phosphodiesterases↗

New Selective Growth Inhibitors of Sphaerotilus natans, Anslimins A and B.

Selective growth inhibitors of Sphaerotilus natans were detected in the culture broths of several strains of Streptomyces. Anslimins A and B were isolated from the culture broth of Streptomyces oganonensis by adsorption on resinous adsorbent followed by elution with 50% aqueous acetone. The A and B components were then separated by cellulose powder chromatography. Physicochemical parameters of anslimins A and B revealed that these compounds are new peptide-containing structures. Anslimins A and B inhibited growth of S. natans at 0.78 and 0.39 mug/ml, respectively, but showed no activity against any of the other test microorganisms at 100 to 200 mg/ml. The anslimins had no harmful effect on guppies at a concentration of 100 mg/liter.

Journal Article↗

Milbemycins, a new family of macrolide antibiotics: fermentation, isolation and physico-chemical properties.

A search for novel insecticides has yielded the milbemycins, a new family of macrolide antibiotics with insecticidal and acaricidal activity. They are produced in submerged cultures of Streptomyces hygroscopicus subsp. aureolacrimosus. Fermentation studies on the strain were conducted in shaken flasks and 30-liter jar fermentors. From the culture broth 13 milbemycins were purified to homogeneity by column and thin-layer chromatography on silica gel and alumina. Physico-chemical data, such as mass spectra, UV and IR absorption spectra, optical rotations and melting points of the milbemycins are described.

Anti-Bacterial Agents↗

A new sesquiterpene antibiotic, heptelidic acid producing organisms, fermentation, isolation and characterization.

A new sesquiterpene antibiotic, heptelidic acid, was found in the culture filtrate of three different strains of fungi isolated from soil samples. These strains were identified as Gliocladium virens, Chaetomium globosum and Trichoderma viride. Heptelidic acid was produced by conventional submerged culture and purified by successive column chromatography on silica gel and Sephadex LH-20 and finally by preparative TLC on silica gel. The molecular formula of heptelidic acid was determined as C15H20O5 on the basis of elementary analysis and high resolution mass spectrometry of its monomethyl ester. The antimicrobial spectrum of the antibiotic revealed its specific activity against anaerobic bacteria, especially against Bacteroides fragilis.

Animals↗

Attached Growth of Sphaerotilus natans in Continuous-Flow Apparatus and Its Growth Inhibition by 9-beta-d-Arabinofuranosyladenine.

Sphaerotilus natans grew at the maximum specific growth rate (mu(max)) of 0.43/h when cultivated on PGY medium at 25 degrees C. The organism mainly grew attached to inside of the culture vessels when the culture medium was fed to the completely mixed continuous-flow apparatus at a dilution rate above mu(max) and the attached growth was directly related to the dilution rate. When a low concentration of the medium was supplied to the apparatus, almost all of the cells grown were filamentous and attached to the inside of the vessels. When a high concentration of the medium was fed, the organism grew as single cells or short chains and flowed out into the effluent. The attached growth of S. natans in the continuous-flow apparatus was inhibited by the minimal inhibitory concentration of 0.5 to 1.0 mug of 9-beta-d-arabinofuranosyladenine per ml. 9-beta-d-Arabinofuranosyladenine showed bacteriocidal activity against S. natans at a concentration of 50 to 100 mug/ml.

Journal Article↗

Herbicidins C and E, two new necleoside antibiotics.

Streptomyces saganonensis No. 4075 used for production of herbicidins A and B has also produced other two antibiotics, herbicidins C and E in submerged culture. Isolation of the antibiotics was performed by adsorption on resinous adsorbent followed by elution with aqueous MeOH and completed by silica-gel chromatography. Physico-chemical characteriation revealed that herbicidins C and E are new nucleoside antibiotics having an adenine moiety in their structures. Herbicidins C and E indicated inhibitory activity against germination of chinese cabbage at 12.5 micrograms/ml and 25 micrograms/ml, respectively, and Anacystis nidulans, a blue green algae, at 100 approximately 200 micrograms/ml.

Anti-Bacterial Agents↗

Herbicidins F and G, two new nucleoside antibiotics.

A mutant of Streptomyces saganonensis No. 4075, obtained with N-methyl-N'-nitro-N-nitrosoguanidine treatment, produced herbicidins F and G without herbicidins A and B. Isolation of the antibiotics was performed by adsorption on resinous adsorbent followed by elution with aqueous MeOH. Herbicidin F was obtained as colorless needles after extraction of the eluate using methylene dichloride. Purification of herbicidin G was completed with silica-gel chromatography to give a crystalline powder. physico-chemical characterization revealed that herbicidins F and G were new nucleoside antibiotics having an adenine moiety in their structures. There was no inhibition activity at 100 micrograms/ml of herbicidins F and G against all of bacteria and yeast tested. Herbicidin F, as well as herbicidin G, are inhibitory activity against some of fungi such as Tricophyton rubrum (MIC; 6.25 micrograms/ml), T. asteroides (6.25 micrograms/ml), T. mentagrophytes (6.25 approximately 12.5 micrograms/ml), Botrytis cinerea (12.5 micrograms/ml), Blastomyces brasiliensis (12.5 approximately 25 micrograms/ml).

Animals↗

Selective Growth Inhibition of Sphaerotilus natans and Beggiatoa sp. by Nucleosides.

9-beta-d-Arabinofuranosyladenine (ara-A) has been found to specifically inhibit the growth of Sphaerotilus natans and Beggiatoa sp. at a low concentration (0.78 mug/ml). The nucleoside had no antimicrobial activity against various microorganisms other than Candida albicans at 1,000 mug/ml. 3'-Deoxyadenosine, 2'-deoxyadenosine, formycin, and some derivatives of ara-A also showed inhibitory activity against Sphaerotilus natans. The growth of Beggiatoa sp. was also inhibited by 9-beta-arabinofuranosylhypoxanthine, 3'-deoxyadenosine, 2'-deoxyadenosine, formycin, toyocamycin, tubercidin, and some derivatives of ara-A. ara-A was quite stable in water and had no harmful effect on fish at 200 mug/ml. The possible uses of ara-A and some nucleosides in controlling the proliferation of S. natans and Beggiatoa sp. in the environment are discussed.

Journal Article↗