Acetylated mangostin attenuates intrinsic apoptotic and anti-transforming activities of mangostin

Mangostin is a dietary supplement known for anti-cancer effects. To modulate its anti-cancer effects, acetyl-mangostin was synthesized via reaction with acetic anhydride, followed by purification using an HPLC column. The MTT assay showed that mangostin treatment decreased the cell growth at 20 µM or greater concentrations; however, this effect was delayed in acetyl-manogostin. Annexin V staining showed that 20 μM of mangostin induced apoptosis, compared with acetyl-mangostin at similar concentrations. FACS analysis suggests that the delayed cell death following acetyl-mangostin treatment was related to significant G1 arrest during cell cycle progression. The cell migration assay showed that acetyl-mangostin reduced the anti-transforming activity of mangostin. Western blot analysis confirmed that activation of cell death markers such as PARP and caspase 3 was delayed in the acetyl-mangostin-treated group. The Bcl-2 expression was increased by acetyl-mangostin at lower concentrations compared with mangostin. Therefore, acetylation of mangostin may be an appropriate mechanism for long-term supplemental treatment to reduce the side effects of anti-cancer drugs.