Coniothyrione, a Chlorocyclopentandienylbenzopyrone as a Bacterial Protein Synthesis Inhibitor Discovered by Antisense Technology

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• 作者：John G. Ondeyka ; Deborah Zink ; Angela Basilio ; Francisca Vicente ; Gerald Bills ; Maria Teresa Diez ; Mary Motyl ; Gabe Dezeny ; Kevin Byrne ; Sheo B. Singh
• 刊名：Journal of Natural Products
• 出版年：2007
• 出版时间：April 2007
• 年：2007
• 卷：70
• 期：4
• 页码：668 - 670
• 全文大小：42K
• 年卷期：v.70,no.4(April 2007)
• ISSN：1520-6025

文摘

Bacterial protein synthesis inhibitors interact mainly with rRNA and to some extent ribosomal proteins, which arepotential targets for developing new antibacterial agents. Specifically, the ribosomal protein S4 of the 30s ribosomalsubunit known as ribosomal protein small-subunit D (rpsD) may be useful as a target. The antisense-rpsD gene-sensitizedtwo-plate assay led to the discovery of a novel chlorinated cyclopentandienylbenzopyrone antibiotic, coniothyrione,C₁₄H₉ClO₆, isolated from Coniothyrium cerealis MF7209. It exhibited liquid MICs of 16-32 ges/entities/mgr.gif">g/mL againstStaphylococcus aureus, Bacillus subtilis, Haemophilus influenzae, Streptococcus pneumoniae, and Enterococcus faecalisand >64 ges/entities/mgr.gif">g/mL against Escherichia coli. Isolation, structure elucidation, and antibacterial activity of coniothyrione aredescribed.