Three new thymol derivatives, 7-formyl-9-isobutyryloxy-8-hydroxythymol (1), 7,9-di-isobutyryloxy-8,10-dehydrothymol (2) and 2α-methoxyl-3β-methyl-6-methylol-2,3-dihydrobenzofuran (3), along with five known ones (4-8), were isolated from the aerial parts of the invasive plant . Their structures were elucidated by extensive spectroscopic analysis and they were all isolated from the aerial part of for the first time. These compounds, except 8, selectively showed antimicrobial activity against three Gram-(+) and two Gram-(-) bacterial strains. In particular, compounds 1 and 5 showed notable antimicrobial activity against all five bacterial strains with IC values ranging from 3.9 to 15.6 μg mL , as compared to reference compound kanamycin sulfate with a MIC value 1.9-3.9 μg mL . Compounds 1 and 5 were further revealed to show cytotoxic activity against three tested human tumor (MCF-7, NCI-H460 and HeLa) cell lines, with IC values ranging from 7.45 to 28.63 μM. Compounds 7 and 8 selectively showed slight but detectable cytotoxicity toward MCF-7 and NCI-H460 cell lines, with IC values 44.65-83.19 μM. No cytotoxic effects were detected in the bioassay of the other four thymol derivatives. The present results provide new data to support that the aerial parts of are a rich source of bioactive chemicals valuable in medicinal applications.