39731-31-2Relevant academic research and scientific papers
Design and synthesis of gambogic acid analogs as potent cytotoxic and anti-inflammatory agents
Yen, Chiao-Ting,Nakagawa-Goto, Kyoko,Hwang, Tsong-Long,Morris-Natschke, Susan L.,Bastow, Kenneth F.,Wu, Yang-Chang,Lee, Kuo-Hsiung
, p. 4018 - 4022 (2012)
Prenyl- and pyrano-xanthones derived from 1,3,6-trihydroxy-9H-xanthen-9- one, a basic backbone of gambogic acid (GA), were synthesized and evaluated for in vitro cytotoxic effects against four human cancer cell lines (KB, KBvin, A549, and DU-145) and anti-inflammatory activity toward superoxide anion generation and elastase release by human neutrophils in response to fMLP/CB. Among them, prenylxanthones 7-13 were generally less active than pyranoxanthones 14-21 in both anticancer and anti-inflammatory assays. Furthermore, two angular 3,3-dimethypyranoxanthones (16 and 20) showed the greatest and selective activity against the KBvin multidrug resistant (MDR) cell line with IC 50 values of 0.9 and 0.8 μg/mL, respectively. An angular 3-methyl-3-prenylpyranoxanthone (17) selectively inhibited elastase release with 200 times more potency than phenylmethylsulfonyl fluoride (PMSF), the positive control.
Identification of Xanthones as Selective Killers of Cancer Cells Overexpressing the ABC Transporter MRP1
Genoux-Bastide, Estelle,Lorendeau, Doriane,Nicolle, Edwige,Yahiaoui, Samir,Magnard, Sandrine,DiPietro, Attilio,Baubichon-Cortay, Helene,Boumendjel, Ahcene
, p. 1478 - 1484 (2012/06/18)
Multidrug-resistance protein1 (MRP1) belongs to the ATP-binding cassette (ABC) transporter family. MRP1 mediates MDR (multidrug resistance) by causing drug efflux either by conjugation to glutathione (GSH) or by co-transport with free GSH (without covalen
