THRAZARINE, A NEW ANTITUMOR ANTIBIOTIC: I. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL PROPERTIES

Thrazarine, O-((3R)-2-diazo-3-hydroxybutyryl)-L-serine, is a new antitumor antibiotic produced by Streptomyces coerulescens MH802-fF5. Thrazarine was isolated from culture filtrate by Sephadex LH-20 column chromatography and reversed phase HPLC. Thrazarine induced cytolysis of tumor cell lines co-cu...

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Bibliographic Details
Published in:Journal of antibiotics 1988/11/25, Vol.41(11), pp.1561-1567
Main Authors: KAMEYAMA, TOSHIYUKI, TAKAHASHI, ATSUSHI, MATSUMOTO, HIROSHI, KURASAWA, SHOGO, HAMADA, MASA, OKAMI, YOSHIRO, ISHIZUKA, MASAAKI, TAKEUCHI, TOMIO
Format: Article
Language:English
Subjects:
Animals
Antibiotics, Antineoplastic - isolation & purification
Antibiotics, Antineoplastic - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
antitumor antibiotics
Antiviral drugs
Azaserine - pharmacology
Biological and medical sciences
Biotechnology
DNA
Fermentation
Fundamental and applied biological sciences. Psychology
Health. Pharmaceutical industry
Humans
Hydroxybutyrates
Industrial applications and implications. Economical aspects
macrophages
Macrophages - immunology
Medical sciences
Mice
Miscellaneous. Antibiotics with multiple activities
Pharmacology. Drug treatments
Production of active biomolecules
Serine - analogs & derivatives
Serine - isolation & purification
Streptomyces - classification
Streptomyces - metabolism
Streptomyces coerulescens
taxonomy
thrazarine
tumor cell lines
Tumor Cells, Cultured - drug effects
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Summary:Thrazarine, O-((3R)-2-diazo-3-hydroxybutyryl)-L-serine, is a new antitumor antibiotic produced by Streptomyces coerulescens MH802-fF5. Thrazarine was isolated from culture filtrate by Sephadex LH-20 column chromatography and reversed phase HPLC. Thrazarine induced cytolysis of tumor cell lines co-cultured with nonactivated macrophages. This effect was tumor specific because the nontumorigenic cells were not lysed by macrophages in the presence of thrazarine. Thrazarine inhibited DNA synthesis and growth of tumor cells directly. It showed neither antimicrobial activity nor the inhibition of transamidation reactions in contrast to azaserine. Toxicities of thrazarine were much weaker than those of azaserine.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.41.1561