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Journal of Biomolecular Screening
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Screening of Natural Products Extracts for the Presence of Phosphodiesterase Inhibitors Using Liquid Chromatography Coupled Online to Parallel Biochemical Detection and Chemical Characterization

T. Schenk

Kiadis B.V., Niels Bohrweg 11-13, 2333 CA Leiden, the Netherlands

G. J. Breel

Kiadis B.V., Niels Bohrweg 11-13, 2333 CA Leiden, the Netherlands

P. Koevoets

Kiadis B.V., Niels Bohrweg 11-13, 2333 CA Leiden, the Netherlands

S. van Den Berg

Kiadis B.V., Niels Bohrweg 11-13, 2333 CA Leiden, the Netherlands

A. C. Hogenboom

Kiadis B.V., Niels Bohrweg 11-13, 2333 CA Leiden, the Netherlands

H. Irth

Kiadis B.V., Niels Bohrweg 11-13, 2333 CA Leiden, the Netherlands, Vrije Universiteit Amsterdam, Faculty of Sciences, Division of Chemistry, Department of Analytical Chemistry and Applied Spectroscopy, De Boelelaan 1083, 1081 HV Amsterdam, the Netherlands

U. R. Tjaden

Leiden/Amsterdam Center for Drug Research, Division of Analytical Biosciences, Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands

J. van Der Greef

Leiden/Amsterdam Center for Drug Research, Division of Analytical Biosciences, Leiden University, P.O. Box 9502, 2300 RA Leiden, the Netherlands

The ability to rapidly identify active compounds in a complex mixture (e.g., natural products extract) is still one of the major problems in natural products screening programs. An elegant way to overcome this problem is to separate the complex mixture by gradient liquid chromatography followed by online biochemical detection parallel with chemical characterization, referred to as high-resolution screening (HRS). To find and identify phosphodiesterase (PDE) inhibitors in natural products extracts using the HRS technology, the authors developed a continuous-flow PDE enzymatic assay. The suitability of the continuous-flow PDE enzymatic assay for natural products screening was demonstrated. After optimization of the continuous-flow PDE assay, the limit of detection for 3-isobutyl-1-methyl-xanthine (IBMX) was 1 [.proportional]M, with a dynamic range from 1 to 100 [.proportional]M IBMX. The applicability of the HRS technology for the detection of PDE inhibitors in natural products extracts was demonstrated by the analysis of a plant extract spiked with 2 naturally occurring PDE inhibitors. The plant extract was analyzed with 2 assay lines in parallel, enabling background fluorescence correction of the sample. The simultaneous quantification of the active compounds using evaporative light-scattering detection allowed the estimation of the IC50 value of the active compounds directly in the crude extract.

Key Words: phosphodiesterase assay • biochemical detection • natural product screening • high-resolution screening • dereplication

Journal of Biomolecular Screening, Vol. 8, No. 4, 421-429 (2003)
DOI: 10.1177/1087057103255973
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