Chemical Diversity of Natural Resources and the Bioactivity of their Constituents

Natural products (NPs) have historically been an important source of lead molecules in drug discovery. However, the interest that the pharmaceutical industry has had in NPs has declined in part because of the lack of compatibility of traditional natural-product extract libraries with high-...

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Main Authors: Jean-Luc Wolfender, Emerson Ferreira Queiroz
Format: Article
Language:deu
Published: Swiss Chemical Society 2012-05-01
Series:CHIMIA
Subjects:
Online Access:https://www.chimia.ch/chimia/article/view/5217
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author Jean-Luc Wolfender
Emerson Ferreira Queiroz
author_facet Jean-Luc Wolfender
Emerson Ferreira Queiroz
author_sort Jean-Luc Wolfender
collection DOAJ
description Natural products (NPs) have historically been an important source of lead molecules in drug discovery. However, the interest that the pharmaceutical industry has had in NPs has declined in part because of the lack of compatibility of traditional natural-product extract libraries with high-throughput screenings and the low hit rate. Furthermore, in contrast to the synthetic libraries, compounds from natural sources are likely to have complex structures which slow down the identification process and contribute to problems related to supply and manufacturing. In this paper, we summarise some of the strategies that are being developed in our research unit to address these issues. On one hand, differential screening strategies were established with the aim of identifying dynamically induced NPs from silent biosynthetic pathways in plants and fungi that had been exposed to different stress situations. On the other hand, high-resolution HPLC techniques were optimised for biological and chemical profiling of crude extracts. This led to an integrated platform for rapid and efficient identification of new drug-leads and biomarkers of interest that were based on miniaturised technological approaches and metabolomics.
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spelling doaj.art-84da8d9cee0e4f35a26b57668dd47d602022-12-22T00:05:34ZdeuSwiss Chemical SocietyCHIMIA0009-42932673-24242012-05-0166510.2533/chimia.2012.324Chemical Diversity of Natural Resources and the Bioactivity of their ConstituentsJean-Luc Wolfender0Emerson Ferreira Queiroz1Phytochimie et Produits Naturels Bioactifs Ecole de Pharmacie Genève-Lausanne Section des Sciences Pharmaceutiques Université de Genève Quai Ansermet 30, CH-1211 Genève 4, Switzerland. jean-luc.wolfender@unige.chPhytochimie et Produits Naturels Bioactifs Ecole de Pharmacie Genève-Lausanne Section des Sciences Pharmaceutiques Université de Genève Quai Ansermet 30, CH-1211 Genève 4, Switzerland Natural products (NPs) have historically been an important source of lead molecules in drug discovery. However, the interest that the pharmaceutical industry has had in NPs has declined in part because of the lack of compatibility of traditional natural-product extract libraries with high-throughput screenings and the low hit rate. Furthermore, in contrast to the synthetic libraries, compounds from natural sources are likely to have complex structures which slow down the identification process and contribute to problems related to supply and manufacturing. In this paper, we summarise some of the strategies that are being developed in our research unit to address these issues. On one hand, differential screening strategies were established with the aim of identifying dynamically induced NPs from silent biosynthetic pathways in plants and fungi that had been exposed to different stress situations. On the other hand, high-resolution HPLC techniques were optimised for biological and chemical profiling of crude extracts. This led to an integrated platform for rapid and efficient identification of new drug-leads and biomarkers of interest that were based on miniaturised technological approaches and metabolomics. https://www.chimia.ch/chimia/article/view/5217Bioactive natural productsDrug discoveryMetabolomicsMicroflow nmrStress inductionUhplc-tof-ms
spellingShingle Jean-Luc Wolfender
Emerson Ferreira Queiroz
Chemical Diversity of Natural Resources and the Bioactivity of their Constituents
CHIMIA
Bioactive natural products
Drug discovery
Metabolomics
Microflow nmr
Stress induction
Uhplc-tof-ms
title Chemical Diversity of Natural Resources and the Bioactivity of their Constituents
title_full Chemical Diversity of Natural Resources and the Bioactivity of their Constituents
title_fullStr Chemical Diversity of Natural Resources and the Bioactivity of their Constituents
title_full_unstemmed Chemical Diversity of Natural Resources and the Bioactivity of their Constituents
title_short Chemical Diversity of Natural Resources and the Bioactivity of their Constituents
title_sort chemical diversity of natural resources and the bioactivity of their constituents
topic Bioactive natural products
Drug discovery
Metabolomics
Microflow nmr
Stress induction
Uhplc-tof-ms
url https://www.chimia.ch/chimia/article/view/5217
work_keys_str_mv AT jeanlucwolfender chemicaldiversityofnaturalresourcesandthebioactivityoftheirconstituents
AT emersonferreiraqueiroz chemicaldiversityofnaturalresourcesandthebioactivityoftheirconstituents