间苯二酚类化合物：来自MST-91080菌株的杂合聚酮类大环内酯化合物。
Resorculins: hybrid polyketide macrolides from sp. MST-91080.
作者信息
Lacey Heather J, Chen Rachel, Vuong Daniel, Lacey Ernest, Rutledge Peter J, Chooi Yit-Heng, Piggott Andrew M, Booth Thomas J
机构信息
Microbial Screening Technologies, Smithfield, NSW 2164, Australia.
School of Chemistry, The University of Sydney, NSW 2006, Australia.
出版信息
Org Biomol Chem. 2023 Mar 22;21(12):2531-2538. doi: 10.1039/d2ob02332f.
Fourteen-membered macrolides are a class of compounds with significant clinical value as antibacterial agents. As part of our ongoing investigation into the metabolites of sp. MST-91080, we report the discovery of resorculins A and B, unprecedented 3,5-dihydroxybenzoic acid (α-resorcylic acid)-containing 14-membered macrolides. We sequenced the genome of MST-91080 and identified the putative resorculin biosynthetic gene cluster ( BGC). The BGC is hybrid of type I and type III polyketide synthases. Bioinformatic analysis revealed that the resorculins are relatives of known hybrid polyketides: kendomycin and venemycin. Resorculin A exhibited antibacterial activity against (MIC 19.8 μg mL), while resorculin B showed cytotoxic activity against the NS-1 mouse myeloma cell line (IC 3.6 μg mL).
十四元大环内酯类化合物是一类具有重要临床价值的抗菌剂。作为我们对sp. MST-91080代谢产物持续研究的一部分，我们报告了间苯二酚A和B的发现，这是前所未有的含有3,5-二羟基苯甲酸（α-间苯二酚酸）的十四元大环内酯类化合物。我们对MST-91080的基因组进行了测序，并鉴定出假定的间苯二酚生物合成基因簇（BGC）。该BGC是I型和III型聚酮合酶的杂合体。生物信息学分析表明，间苯二酚与已知的杂合聚酮化合物：肯多霉素和维内霉素是同类物。间苯二酚A对（MIC 19.8 μg mL）表现出抗菌活性，而间苯二酚B对NS-1小鼠骨髓瘤细胞系表现出细胞毒性活性（IC 3.6 μg mL）。
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