Phytochemical investigation on the fruits of Pieris formosa resulted in the isolation of three new highly acylated 3,4-seco-grayanane diterpenoids, pierisformotoxins E-G (1-3). Their structures were elucidated on the basis of extensive spectroscopic analysis, including 1D-, 2D-NMR, electrospray ionization-mass spectra (ESI-MS) and high resolution (HR)-MS. ? 2011 Pharmaceutical Society of Japan.