Four known ginsenosides: ginsenoside-Rb 1 (1), Rb 3 (2), Rd (3) and Re (4) were isolated from the methanolic extract of the traditional Chinese medicine Panax ginseng C. A. Meyer. Further enzyme reactions and chemical modifications led us to obtain ginsenoside-M 1 (5) and synthesize three novel mono-esters of ginsenoside-M 1 , ginsenoside-DM 1 (6), PM 1 (7) and SM 1 (8) 30 -50% of yield via a facile and green synthetic strategy. The structures were elucidated on the basis of extensive 1D-and 2D-NMR, as well as high resolution ESI-TOF mass spectroscopic analyses. The isolated and synthetic compounds were tested in an anti-tumor bioassay, and compounds 5-8 showed considerable cytotoxicity (SRB) against several human cancer cell lines (breast cancer MCF-7, skin melanoma SK-MEL-2 and human ovarian carcinoma B16), but moderate effects on lung carcinoma COR-L23. The other ginsenosides showed no effects.