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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Blasticidin A Derivatives with Highly Specific Inhibitory Activity toward Aflatoxin Production in Aspergillus parasiticus
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Blasticidin A Derivatives with Highly Specific Inhibitory Activity toward Aflatoxin Production in Aspergillus parasiticus

机译:对寄生曲霉中的黄曲霉毒素生产具有高度特异性抑制活性的Blasticidin A衍生物

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摘要

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 of or toxicity.RT-PCR experiments indicated that derivatives 3 and 4 as well as 1 significantly resuced 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 nore specifically than 1 by inhibiting an early step prior to the expression of aflR in the pathway of aflatoxin biosynthesis.
机译:杀虫素A(1)对寄生虫曲霉产生的黄曲霉毒素具有很强的抑制活性。我们制备了1的一些衍生物并检查了它们的生物学活性。其中,没有1的四酸部分的衍生物3和4保持对1的抑制活性。 RT-PCR实验表明,衍生物3和4以及1显着恢复了编码黄曲霉毒素生物合成酶的基因(pksA,ver-1和omtA)和调控基因的表达。这些结果表明,衍生物3和4通过抑制黄曲霉毒素生物合成途径中aflR表达之前的早期步骤,可以抑制黄曲霉毒素的产生而不是1抑制黄曲霉毒素的产生。

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