Abstract: Two new caryophyllene-type sesquiterpenoids, pestathenols A ( 1 ) and B ( 2 ) and one new α-furanone, pestatheranone A ( 6 ), along with five known compounds ( 3 – 5 , 7 and 8 ) have been isolated from the crude extract of the plant endophytic fungus Pestalotiopsis theae. Their structures were unambiguously established by extensive spectroscopic analyses. The absolute configuration of the 5,6-diol moiety in 1 was assigned using Snatzke’s method. Compounds 1 and 2 showed weak cytotoxicity against HeLa cell line.