Showing papers on "Antifungal antibiotic published in 1977"
TL;DR: Rapamycin, a new antifungal antibiotic, was found to inhibit the immune response in rats and appears to be related to inhibition of the lymphatic system.
Abstract: Rapamycin, a new antifungal antibiotic, was found to inhibit the immune response in rats. It totally prevented the development of two experimental immunopathies (experimental allergic encephalomyelitis (EAE) and adjuvant arthritis (AA)) and the formation of humoral (IgE-like) antibody. It was about half as potent as cyclophosphamide in inhibiting EAE. In AA and on antibody formation, rapamycin and cyclophosphamide were about equipotent, whereas methotrexate was more potent. The immunosuppressant activity of rapamycin appears to be related to inhibition of the lymphatic system.
441 citations
TL;DR: The strobilurins are two antifungal antibiotics which were isolated from the mycelium of Strobilurus tenacellus strain No. 21602 and strongly inhibited the incorporation of radioactive leucine, uridine, and thymidine into the acid-insoluble fraction of cells.
Abstract: The strobilurins are two antifungal antibiotics which were isolated from the mycelium of Strobilurus tenacellus strain No. 21602. The strobilurins A and B are highly active against yeasts and filamentous fungi. In vitro antitumor activity was tested using cells of the asciticform of EHRLICH carcinoma. The strobilurins strongly inhibited the incorporation of radioactive leucine, uridine, and thymidine into the acid-insoluble fraction of cells (protein, RNA, and DNA). The molecular formulas as determined by high resolution mass spectrometry are C16H18O3 for strobilurin A and C17H19ClO4 for strobilurin B.
249 citations
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TL;DR: The antibiotic showed a potent activity against molds and yeasts, but exhibited no antibacterial activity, and has relatively low toxicity in mice.
Abstract: Aculeacin A, a new antifungal antibiotic was isolated from the mycelial cake of Aspergillus aculeatus M-4214. The antibiotic is a white amorphous powder soluble in lower alcohols and hardly soluble in other organic solvents or water. Aculeacin A gave palmitic acid and five ninhydrin-positive products including threonine, hydroxyproline upon acid hydrolysis. The antibiotic showed a potent activity against molds and yeasts, but exhibited no antibacterial activity. Aculeacin A has relatively low toxicity in mice.
118 citations
TL;DR: Ambruticin represents a new class of antibiotics isolated from a strain of Polyangium cellulosum var, fulvum, a bacterium belonging to the class Myxobacteriales and is active in vitro against fungi.
Abstract: Ambruticin represents a new class of antibiotics isolated from a strain of Polyangium cellulosum var firlvum, a bacterium belonging to the class Myxobacteriales This antibiotic is a cyclopropyl-polyene-pyran acid and is active in vitro against fungi
116 citations
TL;DR: The mode of action of a new antifungal antibiotic, aculeacin A, was studied with the cells of Saccharomyces cerevisiae, and the distinct decrease of viable cells was observed.
Abstract: The mode of action of a new antifungal antibiotic, aculeacin A, was studied with the cells of Saccharomyces cerevisiae. In the presence of aculeacin A, the distinct decrease of viable cells was observed. The most of cells treated with aculeacin A lysed with releasing intracellular substances at the tips of their buds. This lysis was considered to be due to the inhibition of cell wall synthesis, because the incorporation of glucose into the cell wall glucan was significantly reduced. Aculeacin A also had a weak activity to burst the protoplasts of S. cerevisiae at a relatively high concentration.
95 citations
82 citations
TL;DR: An unknown antibiotic, ophiocordin, was isolated from submerged cultures of Cordyceps ophioglossoides and could be demonstrated for a small number of fungi belonging to different taxonomic groups and antagonized by ammonia and nitrate ions and by certain amino acids.
Abstract: An unknown antibiotic, ophiocordin, C21H22N2O8, MW: 430, was isolated from submerged cultures of Cordyceps ophioglossoides, strain TU 276, grown in a glycerol soybean meal medium at 27 degrees C. The antibiotic was extracted from acidified culture fluids with n-butanol and purified by subsequent column chromatography on DEAE-Sephadex and cellulose. Studies including nuclear magnetic resonance and mass spectrometry resulted in proposals of partial structures of the molecule. Inhibition by ophiocordin could be demonstrated for a small number of fungi belonging to different taxonomic groups. Bacteria were not inhibited. The antifungal effect was antagonized by ammonia and nitrate ions and by certain amino acids.
48 citations
TL;DR: The developmental cycle of Oudemansiella mucida, the producer of a new antifungal antibiotic, was found to be controlled by the mechanism of homogenic tetrapolar incompatibility; under the authors' conditions, the cycle took about 12 weeks to completion.
Abstract: Nuclear ratios were studied in terminal and subterminal cells of various mycelia of the basidiomyceteOudemansiella mucida, the producer of the antifungal antibiotic mucidin (MuciderminR Spofa). The dikaryon, the monokaryon, and the mucidin-producing strain that had been cultivated for a long time under submerged conditions were compared. Dedikaryotization was found to have taken place in the producing strain. The originally dikaryotic culture with characteristic clamp connections on the mycelium and with two nuclei in every hyphal cell lost permanently the clamp connections, probably owing to continuous intense agitation. The hyphae contained solely mononuclear cells. Mating with a compatible monokaryon yielded a dikaryon capable of normal fructification.
39 citations
25 citations
TL;DR: In this paper, the structure of the antifungal antibiotics, ezomycins B1, B2, 21, C1, 3, C2, 4, D1, 5, and D2, were elucidated by degradative and spectrometric studies.
Abstract: Structures of the antifungal antibiotics, ezomycins B1 (1), B2 (21), C1 (3), C2 (4), D1 (5) and D2 (6), were elucidated by degradative and spectrometric studies. Compound 3 was found to be the α-anomer of 1 and 4 was that of 2. Compounds 2, 4 and 6 were easily interconvertible under weak acidic conditions.
14 citations
TL;DR: Nystatin and LPS appeared to cause similar changes in the functions of spleen cells relevant to immunological events, however, antagonism but no additive effect in the adjuvanticity was revealed between the two adjuvants.
Abstract: Adjuvanticity of nystatin, one of the polyenic antifungal antibiotics having as its primary target the membrane sterol of eukaryotic cells, was investigated by examining its effect on several functions of mouse spleen cells relevant to immunological phenomena in vitro. Nystatin was found to stimulate significantly DNA synthesis in thymus-independent (B) cells but not in thymus-dependent (T) cells. Like the other B-cell mitogens such as bacterial lipopolysaccharide (LPS), nystatin elicited nonspecifically polyclonal antibody synthesis in mouse spleen cell cultures, and also restored antibody response of T cell-deficient spleen cells of congenitally athymic nude mice to heterologous erythrocytes (RBC; thymus-dependent antigen). Thus, nystatin and LPS appeared to cause similar changes in the functions of spleen cells relevant to immunological events. However, antagonism but no additive effect in the adjuvanticity was revealed between the two adjuvants. As an interesting finding, the polyclonal generation of anti-RBC antibody-forming cells (AFC) in the spleen cell cultures by stimulation with B-cell mitogen, i.e., either nystatin or LPS, was not inhibited at all by inclusion of any anti-RBC antiserum, whereas, as is well known, the generation of AFC by stimulation with the antigen was specifically suppressed by the corresponding antiserum, indicating a difference in the genesis between the mitogen-induced AFC and the antigen-induced AFC.
TL;DR: Ezomycins A1, A2, B1, B2, C1, C2, D1 and D2, antifungal antibiotics, are anhydrooctose uronic acid nucleosides.
Abstract: Ezomycins A1, A2, B1, B2, C1, C2, D1 and D2, antifungal antibiotics, are anhydrooctose uronic acid nucleosides. Their novel structures were confirmed by studying their natural abundance 13C n.m.r. spectra in detail from gated proton-decoupled, long-range selective proton-decoupled and selective proton-decoupled spectra. The J(CH) value of the anomeric carbon signal (C-1″) supports the β-configuration.
TL;DR: The suggested procedures of the British Pharmacopoeia for the microbiological assay of the polyene antifungal antibiotics amphotericin B, candicidin and nystatin have been compared and a simpler procedure has been examined and shown to be suitable for the microbial assay of all three antibiotics.
Abstract: The suggested procedures of the British Pharmacopoeia for the microbiological assay of the polyene antifungal antibiotics amphotericin B, candicidin and nystatin have been compared. A simpler procedure has been examined and shown to be suitable for the microbiological assay of all three antibiotics. The increased sensitivity of the assay is due to the enhanced solubility of the antibiotics in the diluents used for preparing the assay solutions. The assay has been shown to be accurate and precise.
TL;DR: In erythrocytes prelabeled with radioactive chromium, release of the isotope through polyene-damaged cell membranes was found to occur at lower drug concentrations than measurable hemoglobin release, and the percentage of isotope released at the highest drug dose was consistently greater than the percentageof hemoglobin released.
Abstract: Polyene antifungal antibiotics produce various degrees of membrane damage in sheep erythrocytes in vitro. Mediocidin, filipin, amphotericin B, and candicidin were found to result in greater damage than nystatin, pimaricin, and amphotericin B methyl ester. The degree of sensitivity of the cells varied by 100-fold for mediocidin verus amphotericin B methyl ester as measured by curves of hemoglobin release versus drug concentration. In erythrocytes prelabeled with radioactive chromium, release of the isotope through polyene-damaged cell membranes was found to occur at lower drug concentrations than measurable hemoglobin release, and the percentage of isotope released at the highest drug dose was consistently greater than the percentage of hemoglobin released. Thus, the isotope assay is a more sensitive indicator of polyene-induced membrane damage in the test system. These significant differences in release of molecules through polyene-induced membrane lesions indicate the complex nature of the binding and further interactions of this class of drugs with the plasma membrane.
TL;DR: Mycobacillin, a cyclic polypeptide antifungal antibiotic effectively inhibits the growth of promastigote form of the protozoal organism, Leishmania donovani, strain 81 in liquid medium.
Abstract: Mycobacillin, a cyclic polypeptide antifungal antibiotic effectively inhibits the growth of promastigote form of the protozoal organism, Leishmania donovani, strain 81 in liquid medium. Oxygen uptake by intact cells of the protozoa with exogenous glucose is appreciably reduced within first 30 minutes in presence of the antibiotic at a concentration of 15 microng/ml. Appreciable leakage of intracellular 260 nm and 280 nm absorbing materials takes place from the protozoan cells incubated with the antibiotic at similar concentration.
TL;DR: The development cycle of the fungus Oudemansiella mucida, the producer of a new antifungal antibiotic, was found to be controlled by the mechanism of homogenic tetrapolar incompatibility.
Abstract: The developmental cycle of the fungus Oudemansiella mucida, the producer of a new antifungal antibiotic, was found to be controlled by the mechanism of homogenic tetrapolar incompatibility; under our conditions, the cycle took about 12 weeks to completion. Optimum conditions for a laboratory-scale fructification were investigated. Normal fruiting body formation required sufficient illumination, temperatures below 20 degrees C, and relative humidity in excess of 70%. Flask-grown fruiting bodies did not differ from the naturally occurring ones. The basidiospores of the produced fruiting bodies yielded the reference monokaryons necessary for physiological, cytological and genetical studies.
Journal Article•
TL;DR: The studies showed that replacement of soybean meal by sunflower oil cake meal with simultaneous increasing of the amount of carbohydrates in the medium increased the levorin levels by 60--70 per cent as compared to the media used at present.
Abstract: The possibility of replacing soybean meal and corn-steep liquor by food wastes of the oilpress industry and the meal of the sunflower oil cake in particular is discussed as applied to the fermentation media for production of antifungal antibiotics, such as levorin, mycoheptin, amphotericin. The studies showed that replacement of soybean meal by sunflower oil cake meal with simultaneous increasing of the amount of carbohydrates in the medium increased the levorin levels by 60--70 per cent as compared to the media used at present. When soybean meal and corn-steep liquor were simultaneously replaced by sunflower oil cake meal in amounts of 3--4 per cent the levels of mycoheptin in the fermentation broth increased by 30--65 per cent respectively. Replacement of soybean meal and corn-steep liquor by 3 per cent of sunflow oil cake meal in the medium used presently increased the amphotericin levels by 27 percent as compared to the control. Therefore, sunflower oil cake meal is a substitute of full value for soybean meal and corn-steep liquor in the fermentation media for production of antifungal antibiotics.
TL;DR: A significant increase of aberrations, mostly of chromatid type, was observed over a period of from 15 min to 15 days following the application of Nystatin in mice, indicating a non-random distribution of the breaks.
Abstract: Nystatin, a fungicide of current medical use, was tasted in mice for its effect on chromosomes of bone marrow cells. A significant increase of aberrations, mostly of chromatid type, was observed over a period of from 15 min to 15 days following the application of the drug. Our data indicate a non-random distribution of the breaks.
TL;DR: This report describes the use of four different methods to determine the absolute and relative antifungal activity of bacillomycin S with the fungus Helminthosporium turcicum Pass.
Abstract: Different strains of the soil bacterium Bacillus subtilis (Ehrenberg) Cohn produce a variety of antifungal polypeptides (4). Recently a proteinaceous antifungal antibiotic, bacillomycin S, was isolated and purified from culture filtrates of B. subtilis (3). During the study of the pharmacological properties of bacillomycin S it was necessary to determine the absolute and relative antifungal activity of bacillomycin S. Bacillomycin S is active against a variety of fungi, including certain dermatophytes (5), and it is neither class nor group specific (3). This report describes the use of four different methods to determine the absolute and relative antifungal activity of bacillomycin S with the fungus Helminthosporium turcicum Pass. as a test organism.
Patent•
05 May 1977
TL;DR: A process for the conversion of the major antifungal antibiotic acid S (ATCC No 25532) isolated from the fermentation of Polyangium cellulosum var fulvum into the minor antibiotic, acid F, from the same fermentation is described in this paper, where acid S is methylated with diazomethane to provide acid S methyl ester which is then oxidized with silver carbonate on celite to obtain the corresponding keto ester S, which is subsequently reduced with sodium borohydride to give a mixture of acidS methyl es
Abstract: A process for the conversion of the major antifungal antibiotic, acid S (ATCC No 25532) isolated from the fermentation of Polyangium cellulosum var fulvum into the minor antibiotic, acid F, from the same fermentation is described wherein acid S is methylated with diazomethane to provide acid S methyl ester which is then oxidized with silver carbonate on celite to obtain the corresponding keto ester S, which is subsequently reduced with sodium borohydride to give a mixture of acid S methyl ester and acid F methyl ester These esters are readily separated by preparative thin layer chromatography and the acid F methyl ester is hydrolyzed with sodium hydroxide solution to provide acid F
Journal Article•
TL;DR: Oral dosing with the antifungal antibiotics Nystatin and Amphotericin "B" was shown in samples of stomach contents, to control the ethanol production entirely, and to suppress the yeast numbers partially but not permanently.
Abstract: In the absence of specific dietary lipids, large amounts of ethanol (ethyl alcohol) are produced from glucose in the stomachs of ruminant neonates by the resident yeast Torulopsis glabrata. Using new born lambs, oral dosing with the antifungal antibiotics Nystatin and Amphotericin "B" was shown in samples of stomach contents, to control the ethanol production entirely, and to suppress the yeast numbers partially but not permanently. Of 11 lambs receiving heavy and continous doses orally of the pure antibiotic powders, 7 died, of these 5 had developed adhesive peritonitis.
TL;DR: Only one drug (amphotericin B) out of the fairly numerous polyene antibiotics has found application for the treatment of visceral systemic mycoses and the high toxicity of the drug requires clinical and laboratory control of its administration.
Abstract: Only one drug (amphotericin B) out of the fairly numerous polyene antibiotics has found application for the treatment of visceral systemic mycoses. The broad antifungal spectrum of amphotericin B ensures its effectiveness in fungal diseases of diverse etiology, and particularly in infections in which other polyene antibiotics are ineffective (coccidial mycosis, histoplasmosis, and blastomycosis). Being sparingly soluble in water, amphotericin B is virtually ineffective on oral administration, and it is used as the complex with sodium desoxycholate, administered intravenously in 5% glucose solution. The high toxicity of the drug requires clinical and laboratory control of its administration. The drug is only used under clinical conditions.