Planta Med 2016; 82(S 01): S1-S381
DOI: 10.1055/s-0036-1596178
Abstracts
Georg Thieme Verlag KG Stuttgart · New York

Advanced technologies for exploring the chemical and functional properties of bioactive constituents in food

A Grand-Guillaume Perrenoud
1   Nestlé Institute of Health Sciences, EPFL Innovation park H, 1015 Lausanne, Switzerland
2   School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, 30 quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland
,
P Coulerie
1   Nestlé Institute of Health Sciences, EPFL Innovation park H, 1015 Lausanne, Switzerland
2   School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, 30 quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland
,
S Moco
1   Nestlé Institute of Health Sciences, EPFL Innovation park H, 1015 Lausanne, Switzerland
,
Y Ratinaud
1   Nestlé Institute of Health Sciences, EPFL Innovation park H, 1015 Lausanne, Switzerland
,
L Bultot
1   Nestlé Institute of Health Sciences, EPFL Innovation park H, 1015 Lausanne, Switzerland
,
D Guillarme
2   School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, 30 quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland
,
E Ferreira Queiroz
2   School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, 30 quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland
,
K Sakamoto
1   Nestlé Institute of Health Sciences, EPFL Innovation park H, 1015 Lausanne, Switzerland
,
JL Veuthey
2   School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, 30 quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland
,
JL Wolfender
2   School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, 30 quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland
,
D Barron
1   Nestlé Institute of Health Sciences, EPFL Innovation park H, 1015 Lausanne, Switzerland
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Publikationsdatum:
14. Dezember 2016 (online)

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Deciphering the impact of food on human health involves approaches that may differ in some aspects from the synthetic drug ones. Two aspects will be discussed to illustrate this complex situation. 1) While drug research rather focuses on compounds that mostly satisfy the Lipinski rule-of-five,1 investigations of food have to deal with both the matrix complexity and the extended range of physicochemical properties of its constituents. As any of these latter may contribute individually or in a synergistic manner to the biological activity, food analysis must ensure the most comprehensive coverage of the entire chemical space. Results concerning the comparison of complementary chromatographic approaches hyphenated to high-resolution mass spectrometry for characterizing the natural product chemical space will be presented. These involve examples based on Supercritical Fluid Chromatography, Reversed-Phase chromatography and Hydrophilic Interaction Liquid Chromatography separations. 2) Complex natural extracts also cause specific problems when evidencing a biological activity in HTS campaigns. For example compounds interfering with the assay readout,2 binding non-specifically to proteins,3 or altering biological membranes4 might be present. High-performance fractionation techniques like two dimensional liquid chromatography may solve these issues. A concrete example based on the detection of a modest natural AMPK activator in plant extracts will be discussed. These advances in 1D and 2D analytical techniques coupled to biological screening open new avenues in understanding the effects of complex natural mixtures.

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Acknowledgements: Professor Caroline West is acknowledged for stimulating scientific discussions, Martine Naranjo for plant extracts preparation, Loraine Merminod for AMPK screening.

Keywords: Food, natural product, supercritical fluid chromatography, reversed-phase chromatography, hydrophilic interaction liquid chromatography, two dimensional liquid chromatography, AMPK.

References:

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[2] Baell J, Walters MA. Chemistry: Chemical con artists foil drug discovery. Nature 2014; 513: 481 – 483.

[3] Feng BY, Shelat A, Doman TN, Guy RK, Shoichet K. High-throughput assays for promiscuous inhibitors. Nat Chem Biol 2005; 1: 146 – 148.

[4] Ingolfsson HI, Thakur P, Herold KF, Hobart EA, Ramsey NB, Periole X, de Jong DH, Zwama M, Yilmaz D, Hall K, Maretzky T, Hemmings HC, Blobel C, Marrink SJ, Kocer A, Sack JT, Andersen OS. Phytochemicals perturb membranes and promiscuously alter protein function. ACS Chem Biol 2014; 9: 1788 – 1798.