A simple method for high-throughput extract prefractionation for biological screening

被引：34

作者：

Appleton, David R. ^{[1
]}

Buss, Antony D. ^{[1
]}

Butler, Mark S. ^{[1
]}

机构：

[1] MerLion Pharmaceut Pte Ltd, Singapore 117528, Singapore

来源：

CHIMIA | 2007年 / 61卷 / 06期

关键词：

automation; high-throughput screening; natural product; prefractionation; NATURAL-PRODUCT CHEMISTRY; DRUG DISCOVERY; DEREPLICATION; IDENTIFICATION; SEPARATION; LIBRARIES; RELEVANT; QUALITY;

D O I：

10.2533/chimia.2007.327

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The screening of crude natural product extracts can be problematic, especially in enzyme/protein-based assays, due to promiscuous inhibitors and interference compounds, while high salt and lipid content can significantly dilute compounds of interest. Described herein is a simple method for high-throughput fractionation of crude extracts that can help address some of these issues. Results obtained indicate a significant improvement in assay hit rates without a reduction of hit quality and show how prefractionation aids the discovery of compounds that would be undetected by screening crude extracts alone.

引用

页码：327 / 331

页数：5

共 52 条

[1] Modern methods to produce natural-product libraries [J].

Abel, U ;

Koch, C ;

Speitling, M ;

Hansske, FG .

CURRENT OPINION IN CHEMICAL BIOLOGY, 2002, 6 (04) :453-458

[2]

Alvi KA, 2000, BIOLOGICALLY ACTIVE NATURAL PRODUCTS: PHARMACEUTICALS, P185

[3] RAPID IDENTIFICATION OF ELAIOPHYLIN AND GELDANAMYCIN IN STREPTOMYCES FERMENTATION BROTHS USING CPC COUPLED WITH A PHOTODIODE-ARRAY DETECTOR AND LC-MS METHODOLOGIES [J].

ALVI, KA ;

PETERSON, J ;

HOFMANN, B .

JOURNAL OF INDUSTRIAL MICROBIOLOGY, 1995, 15 (02) :80-84

[4] Separation of crude plant extracts with high speed CCC for primary screening in drug discovery [J].

Armbruster, JA ;

Borris, RP ;

Jimenez, Q ;

Zamora, N ;

Tamayo-Castillo, G ;

Harris, GH .

JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES, 2001, 24 (11-12) :1827-1840

[5] Pure compound libraries; a new perspective for natural product based drug discovery [J].

Bindseil, KU ;

Jakupovic, J ;

Wolf, D ;

Lavayre, J ;

Leboul, J ;

van der Pyl, D .

DRUG DISCOVERY TODAY, 2001, 6 (16) :840-847

[6] Cluster analysis as selection and dereplication tool for the identification of new natural compounds from large sample sets [J].

Boroczky, Katalin ;

Laatsch, Hartmut ;

Wagner-Dobler, Irene ;

Stritzke, Katja ;

Schulz, Stefan .

CHEMISTRY & BIODIVERSITY, 2006, 3 (06) :622-634

[7] The role of natural product chemistry in drug discovery [J].

Butler, MS .

JOURNAL OF NATURAL PRODUCTS, 2004, 67 (12) :2141-2153

[8]

Butler MS, 2005, NAT PROD REP, V22, P162, DOI 10.1039/b402985m

[9] A CHEMICAL-SCREENING STRATEGY FOR THE DEREPLICATION AND PRIORITIZATION OF HIV-INHIBITORY AQUEOUS NATURAL-PRODUCTS EXTRACTS [J].

CARDELLINA, JH ;

MUNRO, MHG ;

FULLER, RW ;

MANFREDI, KP ;

MCKEE, TC ;

TISCHLER, M ;

BOKESCH, HR ;

GUSTAFSON, KR ;

BEUTLER, JA ;

BOYD, MR .

JOURNAL OF NATURAL PRODUCTS, 1993, 56 (07) :1123-1129

[10] Drug discovery from natural sources [J].

Chin, Young-Won ;

Balunas, Marcy J. ;

Chai, Hee Byung ;

Kinghorn, A. Douglas .

AAPS JOURNAL, 2006, 8 (02) :E239-E253

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