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首页> 外文期刊>Chemistry: A European journal >Characterisation of Taxlllaids A-G; Natural Products from Xenorhabdus indica
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Characterisation of Taxlllaids A-G; Natural Products from Xenorhabdus indica

机译：紫杉A-G的表征;印度Xenorhabdus的天然产物

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摘要

Six new lipodepsipeptides and an additional linear derivative named taxlllaids A-G (1-7) have been identified in the entomopathogenic bacterium Xenorhabdus indica. The structures of the main compounds have been solved by detailed NMR spectroscopic analysis and the structures of minor derivatives were elucidated by a combination of labelling experiments and detailed MS experiments. The absolute configuration of the taxlllaids was deduced by using the advanced Marfey method and analysis of the biosynthesis gene cluster showing the presence of epimerisation domains, which was subsequently proved to be correct by solid-phase peptide synthesis of all taxlllaids. The exchange of a single amino acid in the adenylation domain was shown to be responsible for substrate promiscuity of the third A domain, resulting in the incorporation of leucine, phenylalanine or tyrosine. Bioactivity testing revealed the taxlllaids to be weakly active against Plasmodium falciparum and against a number of eukaryotic cell lines.
机译：在昆虫致病杆菌印度en线虫中已经鉴定出六个新的脂二肽和一个名为taxelllaids A-G（1-7）的线性衍生物。主要化合物的结构已通过详细的NMR光谱分析得以解析，次要衍生物的结构通过标记实验和详细的MS实验的结合得以阐明。通过使用先进的Marfey方法和对生物合成基因簇的分析显示了差向异构域的存在，推断了紫杉醇的绝对构型，随后通过所有紫杉醇的固相肽合成证明是正确的。已显示腺苷酸化结构域中单个氨基酸的交换是第三个A结构域的底物混杂的原因，从而导致亮氨酸，苯丙氨酸或酪氨酸的掺入。生物活性测试表明，紫杉对恶性疟原虫和许多真核细胞系具有弱活性。

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