Aspergillus candidus is a newly recognized source of sphaeropsidin A: Isolation, semi-synthetic derivatization and anticancer evaluation

文献类型： 外文期刊

第一作者： Li, Yan

作者： Li, Yan;Bills, Gerald F.;Li, Yan;Scott, Robert;Hooper, Annie R.;Kornienko, Alexander;Bartholomeusz, Geoffrey A.

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关键词： Diterpenes;Sphaeropsidin A;Synthetic analogues;Anticancer evaluation

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS （ 影响因子：2.823； 五年影响因子：2.677 ）

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收录情况： SCI

摘要： Graphical abstract Display Omitted Abstract This report details a search for alternative strains that produce the diterpenoid sphaeropsidin A (SphA) among A. candidus strains from the USDA Northern Regional Research Laboratories Culture Collection. We identified two strains that produced SphA using a limited set of test media. An initial scaled-up fermentation of NRRL 313 and isolation effort led to the procurement of sufficient quantities of SphA to prepare five semi-synthetic analogues ( 1 – 5 ) and evaluate their anticancer effects against glioblastoma cells D423 and Gli56 grown in 2D and 3D cultures. Although, the effectiveness of the synthetic analogues varied depending on the cell line and the type of cell culture, compound 5 , bearing an aromatic ring at C16, displayed a stronger toxicity towards both D423 and Gli56 cell lines in 2D cultures and D423 spheroids in 3D culture than either SphA or compounds 1 – 4 .

分类号： R9

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