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Gambogic Acid

CAS No. : 2752-65-0

MCE 站：Gambogic Acid

产品活性：Gambogic Acid (Beta-Guttiferrin) 来自 Garcinia hanburyi 树的藤黄树脂。Gambogic Acid (Beta-Guttiferrin) 抑制 Bcl-X_L，Bcl-2，Bcl-W，Bcl-B，Bfl-1 和 Mcl-1，IC₅₀ 分别为 1.47 μM，1.21 μM，2.02 μM，0.66 μM，1.06 μM 和 0.79 μM。

研究领域：Apoptosis  |  Autophagy

作用靶点：Bcl-2 Family  |  Autophagy

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 ~1 μM). 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 μM for Bcl-X_L, 1.21 μM for Bcl-2, 2.02 μM for Bcl-W, 0.66 μM for Bcl-B, 1.06 μM for Bfl-1, and 0.79 μM for Mcl-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?μM for A549 cells, 4.05±0.51 and 25.76±4.03?μM for NCI-H460 cells, and 1.12±0.31?μM and 25.21±4.38?μM for NCI-H1299 cells.

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.

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