Four novel compounds consisting of two new pimaranes, lecheronol A (1) and lecheronol B (2), an acylated cycloartane, 3-O-beta-lauroyl-cycloart-(23E)-en-25-ol (10), and a highly oxygenated novel chalconoid, alpha,beta,3,4,5,2',4',6'-octahydroxydihydrochalcone (12), were isolated along with seven known triterpene derivatives and three flavonol glucosides from Mycobacterium tuberculosis growth-inhibiting fractions of the CH(2)Cl(2)/MeOH (1:1) extract of the aerial parts of Sapium haematospermum. Compounds 1, 3 (3 alpha-hydroxyolean-12-ene), 8 [3 alpha-hydroxylup-20(29)-en], and 9 (cycloartanol) were found most active, with MIC values of 4, 12.2, 13.4, and 8 microg/mL, respectively. Cytotoxicity tests in Vero cells for compounds 1, 3, 8, and 9 gave IC(50) values of 104.8, 127.2, 127.2, and 102.4 microg/mL, respectively.