The extraction of Kaempferia galanga rhizome using steam distillation and supercritical fluid extraction (SFE) was carried out. After fractionation, the major compound of the K. galanga extract, ethyl p-methoxycinnamate (EPMC) was transformed using Aspergillus niger into ethyl p-hydroxycinnamate (EPHC). The biological anticancer activity of EPMC and its biotransformed product (EPHC) was established by cytotoxicity activity on the human breast cancer (MCF-7) cell line using MTT assay. Ethyl p-hydroxycinnamate (EPHC) was most cytotoxic against MCF-7 at 1000 µg/mL where percentage of cell viability was 9.87 %, while IC 50 was 340 µg/mL. EPHC showed slightly higher cytotoxicity activity compared to EPMC. The results of this study show that the biotransformation process was able to produce a metabolite (EPHC) with higher cytotoxicity activity compared to its parent compound (EPMC).