Gambogic Acid

2752-65-0

C38H44O8

H2O : < 0.1 mg/mL (insoluble); DMSO : >= 100 mg/mL (159.05 mM)

Autophagy; Apoptosis

Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC₅₀s of 1.47 uM, 1.21 uM, 2.02 uM, 0.66 uM, 1.06 uM and 0.79 uM. IC50 & Target: IC50: 1.47 uM (Bcl-X_L), 1.21 uM (Bcl-2), 2.02 uM (Bcl-W), 0.66 uM (Bcl-B), 1.06 uM (Bfl-1) and 0.79 uM (Mcl-1)^[1] In Vitro: Gambogic Acid (Beta-Guttiferrin) is a medicinal compound derived from the gamboges resin of the tree, Garcinia hanburyi. Gambogic Acid has documented cytotoxic activity against tumor cell lines in culture, with concentrations required for killing 50% of cells (LD₅₀ of ca.1 uM). The activity of Gambogic Acid against the 6 human anti-apoptotic Bcl-2-family proteins is contrasted, using FPAs. Gambogic Acid displaces to various extents FITC-BH3 peptide binding to all 6 proteins, with apparent IC₅₀ 1.47 uM for Bcl-X_L, 1.21 uM for Bcl-2, 2.02 uM for Bcl-W, 0.66 uM for Bcl-B, 1.06 uM for Bfl-1, and 0.79 uM for Mcl-1^[1]. The growth inhibitory effects of Gambogic Acid or Cisplatin (CDDP) on A549, NCI-H460, and NCI-H1299 cells are assessed by the MTT assay after 48?h exposure. A concentration-dependent inhibition of cell growth is observed with Gambogic Acid and CDDP, with IC₅₀s of 3.56+/-0.36 and 21.88+/-3.21?uM for A549 cells, 4.05+/-0.51 and 25.76+/-4.03?uM for NCI-H460 cells, and 1.12+/-0.31?uM and 25.21+/-4.38?uM for NCI-H1299 cells^[2]. In Vivo: To further investigate whether Gambogic Acid (Beta-Guttiferrin) synergises CDDP against tumour growth in vivo, A549 tumors are implanted in SCID mice. When mice are treated with CDDP combined with Gambogic Acid, the tumor inhibition rate is 69.3%, whereas those of mice treated with CDDP and GA alone are 57.2% and 29.0%, respectively^[2].