ABSTRACT
Even though natural products (NPs) in general and fungal metabolites in particular still play an important role in modern drug discovery, the introduction of high-throughput screening (HTS) technologies afforded considerable changes in paradigms to keep the workflow for NPs competitive with that of synthetic and combinatorial chemistry. As highly automated prefractionation and subsequent random testing have widely replaced the traditional extract screening, the reduction of redundancies in NP-screening libraries became more important than ever before. The application of chemotaxonomy and polymerase chain reaction (PCR)-based data in a preselection strategy for fungal strains to enhance the quality and structural diversity of the resulting sample pools is discussed. While classical chemotaxonomy constitutes a powerful tool to predict metabolic diversity in plants, alternative methods need to be established to reach this goal with fungi. Previous efforts of PCR fingerprinting to identify redundancies in collectives of morphologically similar fungi are summarized. Correlations between HPLC profiling, PCR-based applications, and
classical morphology are exemplified by the outcome of a recent polyphasic study on Daldinia and allies (Xylariaceae). The relationships between chemotaxonomy and molecular phylogeny are illustrated by some examples of Boletales. Future perspectives for dereplication and screening of fungi in HTS are discussed in relation to the characterization of secondary metabolite gene clusters.
