The phytochemical investigation of Buddleja asiatica Lour (family Scrophulariaceae), resulted in the separation and identification of six compounds not isolated previously from B. asiatica, which have been identified as olian-12-en-3-one, taraxaster-12-en-3-one, 4-acetoxybenzaldehyde, 4-acetoxyacetophenone, (E) 3,4-dihydroxycinnamic acid and (E) 3,4-dihydroxy-5-methoxycinnamic acid, in addition to many compounds that were isolated previously from the same species included beta-sitosterol, stigmasterol, oleanane glycosides (3-O-[a-L-rhamnopyranosyl-(1. 4)-beta-D-glucopyranosyl-(1. 3)-beta-D-glucopyranosyl-(1. 2)-beta-D-fucopyranosyl]olean-11,13(18)-dien-3 beta, 23,28-triol, 3-O-[a-L-rhamnopyranosyl-(1. 4)-beta-D-glucopyranosyl-(1. 4)-beta-Dglucopyranosyl-(1. 3)-beta-D-fucopyranosyl]-olean-11,13(18)-dien-3 beta, 23,28-triol and 3-O-[a-L-rhamnopyranosyl(1. 4)-beta-D-glucopyranosyl-(1. 3)-beta-D-xylopyranosyl-(1. 2)-beta-D-glucuronide]-olean-11,13 (18)-dien-3 beta, 23,28triol). The volatile constituents of essential oil, hexane and methylene chloride fractions were identified by GC/MS. Structures of separated compounds were elucidated by spectral analysis. The antimicrobial activities of methylene chloride and ethyl acetate extracts were comparable to ampicillin. The activities against E. coli were 83.3%; 91.7%, respectively, and against S. aureus were 86.4% for both extracts. Antioxidant activity was assessed by DPPH and ABTS methods. By the first one, it decreased in the following order: ascorbic acid < methylene chloride extract < ethyl acetate extract < butanol extract, and by the second one, it decreased in the following order: ascorbic acid < ethyl acetate < butanol < methylene chloride < essential oil Ba2 < hexane < essential oil Ba1. The cytotoxicity against HePG2 were found to be "strong" for ethyl acetate fraction, butanol fraction, methylene chloride fraction and essential oil Ba2, "moderate" for hexane fraction and essential oil Ba1. The cytotoxicity against MCF-7 was found to be "strong" for methylene chloride fraction, essential oil Ba2 and butanol fraction, "moderate" for ethyl acetate fraction, hexane fraction, and essential oil Ba1. The cytotoxicity against HCT-116 was found to be "strong" for ethyl acetate fraction, "moderate" for butanol fraction, and methylene chloride fraction, and "weak" for hexane fraction and essential oil Ba2, "noncytotoxic" for essential oil Ba1. The cytotoxicity against PC3 was found to be "strong" for methylene chloride fraction, "moderate" for ethyl acetate fraction, hexane fraction, butanol fraction and essential oil Ba2, "weak" for essential oil Ba1.