A prenylated xanthone with anticancer activity
Gartanin is a prenylated xanthone that has been found in G. mangostana and has anticancer activity.1,2 It inhibits the growth of T24, UM-UC-3, HT-1376, and TCCSUP bladder cancer cells (IC50s = 4.1-18.1 ?M).1 Gartanin (10 and 50 ?M) increases the number of LC3 puncta, a marker of autophagy, in T24 cells expressing pEGFP-LC3, as well as induces apoptosis in T24 and RT4 cells. It binds to NEDD8-activating enzyme (NAE) and inhibits NEDDylation of cullin 1 and ubiquitin-conjugating enzyme 12 (UBC12) in PC3 and 22Rv1 prostate cancer cells.2
1.Liu, Z., Antalek, M., Nguyen, L., et al.The effect of gartanin, a naturally occurring xanthone in mangosteen juice, on the mTOR pathway, autophagy, apoptosis, and the growth of human urinary bladder cancer cell linesNutr. Cancer65 Suppl. 1 (0 1)68-77(2013) 2.Pham, V., Rendon, R., Le, V.X., et al.Gartanin is a novel NEDDylation inhibitor for induction of Skp2 degradation, FBXW2 expression, and autophagyMol. Carcinog.59(2)193-201(2020)
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