Blasticidin A
Blasticidin A, an antibiotic produced by Streptomyces, almost completely inhibit aflatoxin production at 0.5 microM, significantly reduces the expression of genes encoding aflatoxin biosynthetic enzymes (pksA, ver-1 and omtA) and a regulatory gene (aflR) in A. parasiticus.
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J Antibiot (Tokyo). 2010 Jun;63(6):309-14.
Inhibitory activity of blasticidin A, a strong aflatoxin production inhibitor, on protein synthesis of yeast: selective inhibition of aflatoxin production by protein synthesis inhibitors.[Pubmed:
20414321]
Blasticidin A (BcA), an antibiotic produced by Streptomyces, inhibits aflatoxin production without strong growth inhibition toward aflatoxin-producing fungi.
METHODS AND RESULTS:
During the course of our study on the mode of action of BcA by two-dimensional differential gel electrophoresis (2D-DIGE), we found a decrease in the abundances of ribosomal proteins in Saccharomyces cerevisiae after exposure to BcA. This phenomenon was also observed by treatment with blasticidin S (BcS) or cycloheximide. BcA inhibited protein synthesis in a galactose-induced expression system in S. cerevisiae similar to BcS and cycloheximide. BcS, but not cycloheximide, inhibited aflatoxin production in Aspergillus parasiticus without inhibition of fungal growth, similar to BcA. A decrease in the abundances of aflatoxin biosynthetic enzymes was observed in 2D-DIGE experiments with Aspergillus flavus after exposure to BcA or BcS.
CONCLUSIONS:
These results suggested that protein synthesis inhibitors are useful to control aflatoxin production.
J Antibiot (Tokyo). 2000 Dec;53(12):1378-84.
Blasticidin A derivatives with highly specific inhibitory activity toward aflatoxin production in Aspergillus parasiticus.[Pubmed:
11217803]
Blasticidin A (1), an antibiotic, has strong inhibitory activity toward aflatoxin production by Aspergillus parasiticus.
METHODS AND RESULTS:
We prepared some derivatives of 1 and examined their biological activities. Among them, derivatives 3 and 4 without the tetramic acid moiety of 1 maintained inhibitory activity toward aflatoxin production, but did not show antifungal activity or toxicity. RT-PCR experiments indicated that derivatives 3 and 4 as well as 1 significantly reduced the expression of genes encoding aflatoxin biosynthetic enzymes (pksA, ver-1 and omtA) and a regulatory gene (aflR) in A. parasiticus.
CONCLUSIONS:
These results suggested that derivatives 3 and 4 can inhibit aflatoxin production more specifically than 1 by inhibiting an early step prior to the expression of aflR in the pathway of aflatoxin biosynthesis.
J Antibiot (Tokyo). 2000 Nov;53(11):1265-71.
Blasticidin A as an inhibitor of aflatoxin production by Aspergillus parasiticus.[Pubmed:
11213287]
METHODS AND RESULTS:
Blasticidin A, an antibiotic, showed strong inhibitory activity toward aflatoxin production by Aspergillus parasiticus. Its structure was characterized by NMR and chemical degradation experiments as 1, which is a tetramic acid derivative with a highly oxygenated long alkyl chain similar to aflastatin A (2). Absolute configurations of the eight chiral centers at C-4, 6, 31, 32, 33, 34, 35 and 37 of 1 were chemically determined.
CONCLUSIONS:
Blasticidin A almost completely inhibited aflatoxin production at 0.5 microM.
Biosci Biotechnol Biochem. 2004 Feb;68(2):407-12.
Absolute configuration of a polyol fragment of blasticidin A, a specific inhibitor of aflatoxin production.[Pubmed:
14981305]
Blasticidin A (1) and aflastatin A (2), Streptomyces metabolites with similar structures, are specific inhibitors of aflatoxin production by Aspergillus parasiticus.
METHODS AND RESULTS:
The stereochemistry of the polyol fragment of 1 (3a) containing ten chiral centers was elucidated by applying acetonide and MTPA methods to a variety of acetonide derivatives of 3a, which determined the absolute configuration of 3a.
CONCLUSIONS:
By using the similar methods, the absolute configuration of the polyol fragment of 2 (4a) was determined, which was the same as that elucidated by J-based and other chemical methods previously.
