Promising cytotoxic effects of several Gardenia species (Rubiaceae) have been established 
by many studies. The current study evaluated MTT-based cytotoxic activities of the crude 
extract from Gardenia thunbergia L. f. aerial parts and four fractions thereof, including n-hexane, dichloromethane (DCM), ethyl acetate, and aqueous, against human leukemia (HL-60) 
and hepatoma (HepG2) cell lines, as well as the normal (WI38) cell line. Both non-polar 
fractions, n-hexane and dichloromethane, showed tumor-selective toxicities against both tested 
cancerous cell lines. These results sparked our interest in chemically characterising these 
bioactive fractions to reveal their cytotoxic components. The composition of n-hexane-soluble 
fraction was investigated via GC-MS analysis, while column chromatographic separation was 
used to isolate the components of DCM-soluble fraction. These isolated phytochemicals were 
identified via spectroscopic analyses. Besides, the chemotaxonomic value of the detected 
phytochemicals and their reported cytotoxic profiles were discussed