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Metabolomics for the rapid dereplication of bioactive compounds from natural sources

Author: Nancy Dewi Yuliana, Muhammad Jahangir, Robert Verpoorte, Young Hae Choi


The introduction of high throughput screening in the 1990s aimed to shorten the drugs discovery route. To fully use its high potential, this technology requires a large number of compounds to screen. Thus, increasing the number of chemicals for initial screening is high on the agenda of pharmaceutical companies. High throughput synthesis and combinatorial chemistry were developed to address this demand. However, these technologies cannot fulfill the expectation to increase new lead compounds. One of the reasons is that the obtained compounds lack relevant chemical diversity. On the other hand, it is well known that an enormous molecular diversity and biological functionality are two important features which distinguish plant extracts as a drug source from synthetic chemicals, although a natural products-based drug discovery project also poses some challenges, mostly connected with the presence of an active compound in a complex matrix with all kind of compounds. An elaborative purification to isolate and identify active compounds is thus needed. The possibility of antagonism or synergism between metabolites present in the extracts, and the fact that some common plant products have been found to be active in a number of test systems even make lead finding projects from natural sources become complicated. This review summarizes recent studies reporting metabolomics based techniques to uncover activity related compounds in complex plant matrices.

Phytochemistry Reviews, June 2013, Volume 12, Issue 2, pp 293-304