Guttiferone F from the fruit of Garcinia multiflora and its anti-hepatocellular carcinoma activity

Abstract Garcinia multiflora is an evergreen arbor, which belongs to the family of Guttiferae. It grows mainly at the lower altitudes of the mountains in the Hengchun Peninsula, which is in southern Taiwan. In this study, bioactivity-guided screening was conducted to evaluate the anti-hepatocellular carcinoma bioactivity of the fruit's methanol extract of G. multiflora . The methanol extract residue was partitioned with various solvents. It was then separated and purified using flash chromatography. The active component was confirmed to be guttiferone F. In our present study, cytotoxicity assay revealed that the IC 50 of guttiferone F was 14.15 ± 2.36 μM in PLC/PRF/5 cells, 10.17 ± 0.51 μM in HepG2 cells and 9.71 ± 1.28 μM in Hep3B cells. In the in vitro anticancer study, we found guttiferone F induced apoptosis by up-regulating cleaved pro-caspase-3 and PARP expressions in PLC/PRF/5 cells. The antitumor potency is similar to sorafenib, a therapeutic drug for liver cancer. Further in vivo study showed that guttiferone F inhibits minor tumor growth on s.c. xenograft tumor of human liver cancer cell line in female SCID mice. Although antitumor efficiency of guttiferone F is not superior to sorafenib, the dose (i.p., 25 mg/kg × 5 days) is proved safe to animal. According to our studies, guttiferone F can be a promising lead for liver cancer therapy and become a new liberator for liver cancer patients after modification of the drug.