Three new 7,20:14,20-diepoxy-ent-kaurane diterpenoids, xerophilusins A-C (1
-3), together with a known one, macrocalin B (4), were isolated from the le
aves of Isodon. xerophilus. Their structures were elucidated on the basis o
f their spectral properties and X-ray crystallographic analysis. Compounds
1, 2, and 4 showed significant cytotoxic activity against K562, HL-60, and
MKN-28 cells.