Abstract

In this study, we report three novel naturally occurring compounds, blapsins A (1) and B (2), and blapsamide (3) from the ethanol extract of the stink beetle, Blaps japanensis. The structures of these compounds were determined using spectroscopic methods. Compound 3 is a phenolic compound bearing a formamido group in the structure. Functional studies revealed that compounds 1 and 2 potently inhibited 14-3-3 protein–protein interactions (PPIs) with IC50 values of 9.2 and 10.0μM as determined by an ELISA assay, and 2.0 and 2.5μM in an FP assay, respectively. These compounds represent the first example of natural small-molecule 14-3-3 inhibitors.

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