5-Hydroxy-2-methoxyxanthone (1), 2-hydroxy-3-methoxyxanthone (2), trans-kielcorin (3), 4-hydroxy-3-methoxyphenyl ferulate (4) and 3beta-O-caffeoylbetulinic acid (5) were isolated from Hypericum hookerianum. Compounds 1-5 were tested against the growth of three human tumor cell lines, MCF-7, NCI-H460