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A new ursane-type triterpene, 3β,23,24-trihydroxyurs-12-en-28-oic acid (1), together with eight known compounds (2–9) were isolated from the aerial parts of Ophiorrhiza baviensis. Among them, compounds 2–5 were found for the first time from the genus Ophiorrhiza, while compounds 6–9 were reported from O. baviensis for the first time. Their structures were elucidated by analysis of HR-ESI-MS and NMR (1H-NMR, 13C-NMR, HSQC, and HMBC) spectra, as well as comparison with those reported in the literature. Moreover, all isolated compounds were evaluated for their cytotoxic activities against MCF-7, Hela, KB, A549, and SK-LU-1 cancer cell lines and their effects on LPS-induced NO production in RAW264.7 cells. This is the first report of chemical constituents and biological activities of O. baviensis. [ABSTRACT FROM AUTHOR]