利用粘菌素生物合成中的酶促混杂性生产5-脂氧合酶抑制剂
Harnessing Enzymatic Promiscuity in Myxochelin Biosynthesis for the Production of 5-Lipoxygenase Inhibitors.
作者信息
Korp Juliane, König Stefanie, Schieferdecker Sebastian, Dahse Hans-Martin, König Gabriele M, Werz Oliver, Nett Markus
机构信息
Leibniz Institute for Natural Product Research and Infection Biology, Hans Knöll Institute, Adolf-Reichwein-Strasse 23, 07745, Jena, Germany.
Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Friedrich-Schiller-Universität Jena, Philosophenweg 14, 07743, Jena, Germany.
出版信息
Chembiochem. 2015 Nov;16(17):2445-50. doi: 10.1002/cbic.201500446. Epub 2015 Oct 13.
The siderophore myxochelin A is a potent inhibitor of human 5-lipoxygenase (5-LO). To clarify whether the iron-chelating properties of myxochelin A are responsible for this activity, several analogues of this compound were generated in the native producer Pyxidicoccus fallax by precursor-directed biosynthesis. Testing in a cell-free assay unveiled three derivatives with bioactivity comparable with that of myxochelin A. Furthermore, it became evident that inhibition of 5-LO by myxochelins does not correlate with their iron affinities.
铁载体粘菌素A是一种有效的人5-脂氧合酶（5-LO）抑制剂。为了阐明粘菌素A的铁螯合特性是否是这种活性的原因，通过前体导向生物合成在天然生产者Pyxidicoccus fallax中产生了该化合物的几种类似物。无细胞试验表明，有三种衍生物具有与粘菌素A相当的生物活性。此外，很明显，粘菌素对5-LO的抑制作用与其铁亲和力无关。
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