Gambogic-Acid

Gambogic acid (GA) is a xanthonoid that has been found in G. hanburyi resin and has anticancer activity. It binds covalently to the regulatory subunit B (SPTSSB) of the serine palmitoyltransferase complex (Ki = 1.5 µM; kinact = 0.05 min-1) and inhibits de novo sphingolipid biosynthesis. GA activates caspases in T47D breast cancer cells (EC50 = 0.78 µM) and inhibits binding of anti-apoptotic proteins to a BH3 peptide (IC50s = 1.47, 1.21, 2.02, 0.66, 1.06, and 0.79 μM for Bcl-xL, Bcl-2, Bcl-W, Bcl-B, Bfl-1, and Mcl-1, respectively), as well as decreases the expression of Bcl-2 and increases the...