Trichopolyn VI: a new peptaibol insecticidal compound discovered using a recombinant <i>Saccharomyces cerevisiae</i> screening system

Abstract

In the course of searching for insecticides from soil microorganisms, we found that a fermentation broth of the fungus, Trichoderma brevicompactum FKI-6324, produced Trichopolyn VI, a new peptaibol, which possessed significant insecticidal potential. Spectroscopic analysis showed the compound to be a new trichopolyn I derivative. This paper describes the isolation, structure elucidation and biological activity of trichopolyn VI.

Characterization of two adenine nucleotide translocase paralogues in the stink bug, <i>Plautia stali</i>

“…We recently established a screening method to discover substances that inhibit the function of the insect adenine nucleotide translocase (ANT), a protein that is evolutionarily conserved in vertebrate species and also known as the ADP/ATP carrier (AAC) in yeasts. 1,2) In this screening program, Saccharomyces cerevisiae lacking its AAC genes was complemented by the expression of insect or vertebrate ANT genes, and the inhibitory activities of substances for each ANT were easily monitored by investigating the survival of the transformants. Accordingly, this system enables us to explore a compound that is harmful to some insect species but not to vertebrates or other insects.…”

Decatamariic acid, a new mitochondrial respiration inhibitor discovered by pesticidal screening using drug-sensitive Saccharomyces cerevisiae

“…S. cerevisiae WB-12 pRS314YA2P, an endogenous AAC-disrupted and single-copy yeast shuttle vector pRS314YA2P-expressing strain (empty vector strain), was grown on a glucose-containing medium as the references. 5,6 Sterile filter discs impregnated with each compound solution (10 μl) were placed on the agar plate, and the plates were incubated at 30°C for 48 h. After incubation, the inhibition zones were measured.…”

“…Thus we could obtain cultured broths that may affect mitochondrial function. 5,6 As a result, our screens showed that Aspergillus tamarii strain FKI-6817 produced a new compound (FKI-6817A; 1) that inhibited the growth of drug-sensitive BY25929 strain of S. cerevisiae. Compound 1 inhibited the growth of drug-sensitive budding yeast only in a glycerol-containing medium, and it elicited~50% inhibition of the ATP production in isolated mitochondria.…”

“…They have proved to be safe for mammals by their selective activity against arthropods. Recently, we have established a new screening system aimed at finding a mitochondrial inhibitor, using a recombinant Saccharomyces cerevisiae, and have found two new mitochondrial inhibitors, ascosteroside C 5 and trichopolyn VІ, 6 produced by fungi. In the field of natural products chemistry and chemical biology, S. cerevisiae has been widely used for screening and functional study of bioactive compounds, 7 and it is suitable for bioassay-guided screening of various drug candidates.…”