HPLC and TLC profiling was carried out for leaf and fruit extracts of five Schisandraceae species: Schisandra chinensis, S. rubriflora, S. spehenanthera, S. henryi and Kadsura japonica. HPLC measurements confirmed presence of lignans and phenolic compounds in fruits and leaves of all tested species. The most abundant in lignans was S. chinensis fruit extract in which 15 compounds were detected (e. g.: schisandrol A, schisanhenol, γ-schisandrin, gomisin N). The effect-directed detection, i. e., TLC-direct bioautography against Bacillus subtilis, showed exceptionally high activity for S. chinensis and S. rubriflora fruit extracts. On the other hand, TLC-DB enzyme tests (α-glucosidase, lipase, tyrosinase and acetylcholinesterase (AChE) inhibition assays) showed that all fruit and leaf extracts have ability to inhibit the above-mentioned enzymes (except for the K. japonica fruit). The leaf extracts showed much stronger antioxidant activity than the fruit ones, which were assessed and compared using both TLC-direct bioautography and spectrophotometric measurements based on ABTS, DPPH and FRAP tests.