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Aspergillus candidus is a newly recognized source of sphaeropsidin A: Isolation, semi-synthetic derivatization and anticancer evaluation
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-11-04 , DOI: 10.1016/j.bmcl.2017.11.001
Yan Li , Robert Scott , Annie R. Hooper , Geoffrey A. Bartholomeusz , Alexander Kornienko , Gerald F. Bills

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 (15) 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 14.



中文翻译:

曲霉曲霉是新近发现的球形菌素A的来源:分离,半合成衍生化和抗癌评估

该报告详细介绍了产生中sphaeropsidin A(SPHA)的二萜类化合物的替代菌株搜索A. candidus的从USDA北方地区研究实验室培养物保藏菌株。我们使用一组有限的测试培养基鉴定了两种产生SphA的菌株。导致采购足量SPHA的NRRL 313和隔离努力的初始放大的发酵,以制备5半合成类似物(1 - 5)和评估对成胶质细胞瘤细胞D423和Gli56生长在2D和3D培养他们的抗癌作用。尽管合成类似物的有效性随细胞系和细胞培养类型的不同而变化,化合物5轴承在C16芳环,显示更强的毒性朝向三维培养既D423和Gli56细胞系在2D培养和D423球状体比任SPHA或化合物1 - 4

更新日期:2017-11-04
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