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Open Access Chemical Diversity of Natural Resources and the Bioactivity of their Constituents

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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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Keywords: BIOACTIVE NATURAL PRODUCTS; DRUG DISCOVERY; METABOLOMICS; MICROFLOW NMR; STRESS INDUCTION; UHPLC-TOF-MS

Document Type: Research Article

Affiliations: 1: Phytochimie 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-lu[email protected] 2: Phytochimie et Produits Naturels Bioactifs Ecole de Pharmacie Genève-Lausanne Section des Sciences Pharmaceutiques Université de Genève Quai Ansermet 30, CH-1211 Genève 4, Switzerland

Publication date: May 1, 2012

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  • International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions

    CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.

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