Proposed method for the effective generation of pharmaceutical lead compounds

Abstract

We propose a method to enhance the development of natural product drug discovery. Japan is located in a cool-temperate to subtropical zone where 12,300 fungal species have been recorded. At least 188,500 species are expected to be discovered in future. Of these fungal taxa, Hypocreales is one of the most attractive groups for the discovery of secondary metabolites. During the past ten years, we have established a diverse fungal collection mainly from Japan, containing 668 genera, 1,122 species, and 15,069 strains. We used these fungi to produce over 30,000 samples in a cultured extract library ready for assay. Previous successes in natural product drug discovery indicate that most lead candidates have a weak antifungal activity. Thus, it would be useful to prescreen a huge number of extracts against highly susceptible yeasts or fungi, to identify new active metabolites. A collection of these active compounds could then readily be evaluated by pharmaceutical companies.