Automated High-Throughput System to Fractionate Plant Natural Products for Drug Discovery

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• 作者：Ying Tu ; Cynthia Jeffries ; Hong Ruan ; Cynthia Nelson ; David Smithson ; Anang A. Shelat ; Kristin M. Brown ; Xing-Cong Li ; John P. Hester ; Troy Smillie ; Ikhlas A. Khan ; Larry Walker ; Kip Guy ; Bing Yan
• 刊名：Journal of Natural Products
• 出版年：2010
• 出版时间：April 23, 2010
• 年：2010
• 卷：73
• 期：4
• 页码：751-754
• 全文大小：124K
• 年卷期：v.73,no.4(April 23, 2010)
• ISSN：1520-6025

文摘

The development of an automated, high-throughput fractionation procedure to prepare and analyze natural product libraries for drug discovery screening is described. Natural products obtained from plant materials worldwide were extracted and first prefractionated on polyamide solid-phase extraction cartridges to remove polyphenols, followed by high-throughput automated fractionation, drying, weighing, and reformatting for screening and storage. The analysis of fractions with UPLC coupled with MS, PDA, and ELSD detectors provides information that facilitates characterization of compounds in active fractions. Screening of a portion of fractions yielded multiple assay-specific hits in several high-throughput cellular screening assays. This procedure modernizes the traditional natural product fractionation paradigm by seamlessly integrating automation, informatics, and multimodal analytical interrogation capabilities.