Lycopus lucidus root, harvested from two sites at three different times, was analysed for nutritional profiles; phenolics by HPLC-MS and NMR; enzymatic activity of phenylalanine ammonia-lyase (PAL), tyrosine aminotransferase (TAT), cinnamic acid 4-hydroxylase (C4H), and polyphenol oxidase (PPO); and DNA damage protective effect. The results showed that the moisture first increased and then decreased, and the crude fat and crude fibre increased continuously during the harvesting period. Sucrose and fructose were the predominant sugars with different changing patterns. Linolelaidic, linoleic, palmitic, and stearic acids were the predominant fatty acids. No significant difference was observed of vitamin B 2 accompany with an increase of vitamin C with the harvest time delayed among the three harvest times investigated. Caffeic, rosmarinic, and protocatechuic acid; rosmarinic acid methylester; protocatechualdehyde; Danshensu; 3, 4-dihydroxyphenyl caffeate; and N-trans-feruloyl tyramine were identified in L. lucidus root and their variations were discrepant in the period of harvest. There was no significant correlation between phenolics and enzymatic activity except for insoluble cell-wall-bound phenolics (ICP) and C4H, as well as protocatechualdehyde and TAT. The FP exhibited higher DNA damage protective activity than ICP.