A phytochemical study of Kadsura heteroclita led to the isolation of eight triterpenoids, including two new compounds, named kadheterilactone A (1) and kadheterilactone B (2), as well as six known compounds, longipedlactone H (3), longipedlactone A (4), longipedlactone F (5), kadsuranic acid A (6), nigranoic acid (7), and schisandronic acid (8). Their structures were elucidated on the basis of spectroscopic methods, including 2D NMR techniques. The cytotoxic activities of 1–8 were tested against several tumor cell lines by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl‐2H‐tetrazolium hydrobromide (MTT) assay in vitro. As a result, 4 and 5 turned out to be significantly cytotoxic against Hep‐G2 and Bel‐7402 tumor cell lines. All compounds were also tested for inhibition on HIV‐1 protease (PR) and reverse transcriptase (RT). Compounds 6 and 7 showed strong inhibition on HIV‐1 PR, while 8 exhibited moderate activity, others were only weakly active. No compounds were active against HIV‐1 RT.