Blasticidin A Derivatives with Highly Specific Inhibitory Activity toward Aflatoxin Production in Aspergillus parasiticus

Sakuda, S.; Ikeda, H.; Nakamura, T.; Kawachi, R.; Kondo, T.; Ono, M.; Sakurada, M.; Inagaki, H.; Ito, R.; Nagasawa, H.

The Journal of Antibiotics 53(12): 1378-1384

2000


DOI: 10.7164/antibiotics.53.1378
Accession: 068516887

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Abstract
Blasticidin A (1), an antibiotic, has strong inhibitory activity toward aflatoxin production by Aspergillus parasiticus. 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. 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.