Document Type
Oral Presentation
Location
Oxford Conference Center
Event Website
https://oxfordicsb.org/
Start Date
23-4-2026 8:30 AM
End Date
23-4-2026 10:00 AM
Description
Over the past decade, natural product research has undergone a methodological revolution [1]. Modern approaches now integrate advanced metabolite profiling techniques for compound annotation and prioritization, together with high-resolution chromatographic methods that enable seamless transition from analytical to preparative scales [2]. These tools have facilitated the detection and identification of minor bioactive constituents. Nevertheless, plant extracts typically contain abundant common scaffolds with limited relevance for drug discovery. In this context, enzymatic biotransformation emerges as a promising strategy to enhance chemical diversity and unlock new structural space. Two complementary biotechnological approaches have been developed: enzymatic transformation using fungal secretomes (crude extracellular enzyme mixtures) and whole-cell biotransformation with saprophytic fungi such as Botrytis cinerea and Trametes versicolor. Selected substrates included stilbenes, chalcones, phenylpropanoids, and terpenes from the Swiss flora. Analytical-scale reactions were monitored by UHPLC-PDA-ELSD-HRMS to detect novel metabolites, and promising transformations were scaled up to gram quantities for purification via high-resolution preparative chromatography with dry load injection. Enantiomers were further resolved by chiral chromatography, and structures elucidated using HRMS, 2D NMR, and ECD spectroscopy. The resulting library comprised over 280 compounds, several exhibiting unprecedented scaffolds and potent antibacterial or antiviral activity [3-5]. Mechanistic investigations enabled the proposal of plausible biosynthetic pathways and the identification of candidate enzymes involved. These integrated, green-chemistry-based approaches substantially expand the accessible NP chemical space, opening new avenues for drug discovery
References 1. Wolfender JL, Litaudon M, Touboul D, Queiroz EF. Innovative omics-based approaches for prioritisation and targeted isolation of natural products - new strategies for drug discovery. Nat Prod Rep. 2019;36(6):855-68. doi: 10.1039/c9np00004f. 2. Queiroz EF, Guillarme D, Wolfender JL. Advanced high-resolution chromatographic strategies for efficient isolation of natural products from complex biological matrices: from metabolite profiling to pure chemical entities. Phytochem Rev. 2024;23:1415-42. doi: 10.1007/s11101-024-09928-w. 3. Huber R, Koval A, Marcourt L, Heritier M, Schnee S, Michellod E, et al. Chemoenzymatic synthesis of original stilbene dimers possessing wnt inhibition activity in triple-negative breast cancer cells using the enzymatic secretome of Botrytis cinerea Pers. Front Chem. 2022;10. doi: 10.3389/fchem.2022.881298. 4. Huber R, Marcourt L, Quiros-Gurerrero LM, Luscher A, Schnee S, Michellod E, et al. Chiral separation of stilbene dimers generated by biotransformation for absolute configuration determination and antibacterial evaluation Front Chem. 2022;10:912396, DOI: 10.3389/fchem.2022. doi: 10.3389/fchem.2022.912396. 5. Huber R, Marcourt L, Koval A, Schnee S, Righi D, Michellod E, et al. Chemoenzymatic synthesis of complex phenylpropanoid derivatives by the Botrytis cinerea secretome and evaluation of their wnt inhibition activity. Front Plant Sci. 2021;12:805610. doi: 10.3389/fpls.2021.805610.
Recommended Citation
Queiroz, Emerson, "Expanding Natural Product Diversity Through Biotransformation" (2026). Oxford ICSB. 41.
https://egrove.olemiss.edu/icsb/2026_ICSB/Schedule/41
Publication Date
April 2026
Accessibility Status
Screen reader accessible, Searchable text
Included in
Expanding Natural Product Diversity Through Biotransformation
Oxford Conference Center
Over the past decade, natural product research has undergone a methodological revolution [1]. Modern approaches now integrate advanced metabolite profiling techniques for compound annotation and prioritization, together with high-resolution chromatographic methods that enable seamless transition from analytical to preparative scales [2]. These tools have facilitated the detection and identification of minor bioactive constituents. Nevertheless, plant extracts typically contain abundant common scaffolds with limited relevance for drug discovery. In this context, enzymatic biotransformation emerges as a promising strategy to enhance chemical diversity and unlock new structural space. Two complementary biotechnological approaches have been developed: enzymatic transformation using fungal secretomes (crude extracellular enzyme mixtures) and whole-cell biotransformation with saprophytic fungi such as Botrytis cinerea and Trametes versicolor. Selected substrates included stilbenes, chalcones, phenylpropanoids, and terpenes from the Swiss flora. Analytical-scale reactions were monitored by UHPLC-PDA-ELSD-HRMS to detect novel metabolites, and promising transformations were scaled up to gram quantities for purification via high-resolution preparative chromatography with dry load injection. Enantiomers were further resolved by chiral chromatography, and structures elucidated using HRMS, 2D NMR, and ECD spectroscopy. The resulting library comprised over 280 compounds, several exhibiting unprecedented scaffolds and potent antibacterial or antiviral activity [3-5]. Mechanistic investigations enabled the proposal of plausible biosynthetic pathways and the identification of candidate enzymes involved. These integrated, green-chemistry-based approaches substantially expand the accessible NP chemical space, opening new avenues for drug discovery
References 1. Wolfender JL, Litaudon M, Touboul D, Queiroz EF. Innovative omics-based approaches for prioritisation and targeted isolation of natural products - new strategies for drug discovery. Nat Prod Rep. 2019;36(6):855-68. doi: 10.1039/c9np00004f. 2. Queiroz EF, Guillarme D, Wolfender JL. Advanced high-resolution chromatographic strategies for efficient isolation of natural products from complex biological matrices: from metabolite profiling to pure chemical entities. Phytochem Rev. 2024;23:1415-42. doi: 10.1007/s11101-024-09928-w. 3. Huber R, Koval A, Marcourt L, Heritier M, Schnee S, Michellod E, et al. Chemoenzymatic synthesis of original stilbene dimers possessing wnt inhibition activity in triple-negative breast cancer cells using the enzymatic secretome of Botrytis cinerea Pers. Front Chem. 2022;10. doi: 10.3389/fchem.2022.881298. 4. Huber R, Marcourt L, Quiros-Gurerrero LM, Luscher A, Schnee S, Michellod E, et al. Chiral separation of stilbene dimers generated by biotransformation for absolute configuration determination and antibacterial evaluation Front Chem. 2022;10:912396, DOI: 10.3389/fchem.2022. doi: 10.3389/fchem.2022.912396. 5. Huber R, Marcourt L, Koval A, Schnee S, Righi D, Michellod E, et al. Chemoenzymatic synthesis of complex phenylpropanoid derivatives by the Botrytis cinerea secretome and evaluation of their wnt inhibition activity. Front Plant Sci. 2021;12:805610. doi: 10.3389/fpls.2021.805610.
https://egrove.olemiss.edu/icsb/2026_ICSB/Schedule/41
Comments
Dr. Queiroz was born in Campina Grande, Paraíba, Brazil, in 1971. He obtained his degree in Pharmaceutical Sciences in 1994 and later completed a Ph.D. under the supervision of Professor André Cavé at the University of Paris XI. In 1999, he joined the University of Lausanne as a postdoctoral researcher in the laboratory of Professor Kurt Hostettmann, where he specialized in advanced analytical techniques, including LC/MS and LC/NMR, for the on line identification of bioactive compounds from higher plants. In recognition of his contributions to medicinal plant research, Dr. Queiroz received the Ecosol award from the Swiss Society of Medical Phytotherapy in 2005. From 2006 to 2011, he served as Scientific Director at Aché Laboratórios Farmacêuticos S.A., South America’s largest pharmaceutical company, where he led research programs dedicated to drug development from Brazil’s biodiversity. Since May 2011, Dr. Emerson Ferreira Queiroz has been a Senior Scientist (MER) in the School of Pharmaceutical Sciences at the University of Geneva. His research focuses on exploiting fungal enzymatic biotransformations to expand the chemical diversity of natural products, thereby generating novel bioactive molecules and improving access to drug-like lead structures. In parallel, Dr. Queiroz develops innovative strategies for natural product isolation from higher plants and fungi, combining preparative-scale methodologies with miniaturized, high-resolution analytical workflows for rapid dereplication and online structural characterization of bioactive metabolites. In 2023, Dr. Queiroz was awarded the PSE–Pierre Fabre Prize, which distinguished his pioneering contributions to phytochemistry, especially in the valorization of natural products and the development of biotransformation-based strategies for the discovery of new lead compounds Throughout his career, Dr. Queiroz has authored three books, twelve chapters, 175 peer-reviewed journal articles, and twelve patents, and has delivered more than 250 scientific presentations worldwide. He serves as Editor of Planta Medica, Co-Editor of Frontiers in Natural Products and Frontiers in Ethnopharmacology, and is a member of the editorial boards of Phytochemistry and Molecules. Since 2016, he has been an elected member of the Board of Directors of the Society for Medicinal Plant and Natural Product Research (GA).