Description
Gambogic acid is a xanthone found in the resin of the Garcinia hanburyi tree and has shown considerable anticancer chemotherapeutic, chemopreventive, and anti-angiogenic activities in both in vitro and in vivo studies. Gambogic acid inhibits cellular growth and induces apoptosis through a variety of mechanisms. This compound induces LRIG1 upregulation and EGFR degradation to inactivate Akt signaling. Additionally, gambogic acid also inhibits NF-κB signaling through interaction with the transferrin receptor, causing reduction of c-MYC expression, inhibition of telomerase activity and mRNA production, and disruption of mitochondrial outer membrane potential.
References
He XY, Liu XJ, Chen X, et al. Gambogic acid induces EGFR degradation and Akt/mTORC1 inhibition through AMPK dependent-LRIG1 upregulation in cultured U87 glioma cells. Biochem Biophys Res Commun. 2013 Jun 7;435(3):397-402. PMID: 23665322.
Gu H, Rao S, Zhao J, et al. Gambogic acid reduced bcl-2 expression via p53 in human breast MCF-7 cancer cells. J Cancer Res Clin Oncol. 2009 Dec;135(12):1777-82. PMID: 19582475.
Nie F, Zhang X, Qi Q, et al. Reactive oxygen species accumulation contributes to gambogic acid-induced apoptosis in human hepatoma SMMC-7721 cells. Toxicology. 2009 Jun 16;260(1-3):60-7. PMID: 19464570.
Pandey MK, Sung B, Ahn KS, et al. Gambogic acid, a novel ligand for transferrin receptor, potentiates TNF-induced apoptosis through modulation of the nuclear factor-kappaB signaling pathway. Blood. 2007 Nov 15;110(10):3517-25. PMID: 17673602.
Wu ZQ, Guo QL, You QD, et al. Gambogic acid inhibits proliferation of human lung carcinoma SPC-A1 cells in vivo and in vitro and represses telomerase activity and telomerase reverse transcriptase mRNA expression in the cells. Biol Pharm Bull. 2004 Nov;27(11):1769-74. PMID: 15516720.
