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National Cancer Institute (NCI) Program for Natural Products Discovery: Rapid Isolation and Identification of Biologically Active Natural Products from the NCI Prefractionated Library.
ACS Chemical Biology ( IF 4 ) Pub Date : 2020-04-07 , DOI: 10.1021/acschembio.0c00139
Tanja Grkovic 1 , Rhone K Akee 1 , Christopher C Thornburg 1 , Spencer K Trinh 1 , John R Britt 1 , Matthew J Harris 1 , Jason R Evans 2 , Unwoo Kang 3 , Susan Ensel 4 , Curtis J Henrich 3, 5 , Kirk R Gustafson 3 , Joel P Schneider 6 , Barry R O'Keefe 2, 3
Affiliation  

An automated, high-capacity, and high-throughput procedure for the rapid isolation and identification of biologically active natural products from a prefractionated library is presented. The semipreparative HPLC method uses 1 mg of the primary hit fraction and produces 22 subfractions in an assay-ready format. Following screening, all active fractions are analyzed by NMR, LCMS, and FTIR, and the active principle structural classes are elucidated. In the proof-of-concept study, we show the processes involved in generating the subfractions, the throughput of the structural elucidation work, as well as the ability to rapidly isolate and identify new and biologically active natural products. Overall, the rapid second-stage purification conserves extract mass, requires much less chemist time, and introduces knowledge of structure early in the isolation workflow.

中文翻译:

美国国家癌症研究所(NCI)天然产物发现计划:从NCI预分馏文库中快速分离和鉴定具有生物活性的天然产物。

提出了一种自动化,高容量和高通量的程序,用于从预分离的文库中快速分离和鉴定具有生物活性的天然产物。半制备型HPLC方法使用1 mg初次命中级分,并以易于检测的形式产生22个亚级分。筛选后,通过NMR,LCMS和FTIR分析所有活性级分,并阐明活性成分的结构类别。在概念验证研究中,我们显示了产生亚组分的过程,结构阐明工作的通量以及快速分离和鉴定具有生物活性的新天然产物的能力。总体而言,快速的第二阶段纯化可节省提取物的质量,所需的化学试剂时间更少,
更新日期:2020-04-23
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