1444763-31-8Relevant articles and documents
Synthesis and antitumor activities of α-,γ-mangostin derivatives
Cheng, Kai,Zhang, Gui-Lin,Qiu, Sheng-Xiang,Liu, Yan-Qing,Wang, Yan-Fei,Liu, Song,Shan, Yan,Yu, Bo,Lu, Yu
, p. 586 - 593 (2014/05/20)
The α-Mangostin and γ-Mangostin were mainly isolated from Garcinia Mangostana L. as representative Xanthone's natural products of plant origin, revealed high activity of antitumor, antioxidation and other diverse pharmacological activities. A series of α, γ-Mangostin derivatives LT-1～17 has been synthesized, and confirmed by 1H NMR, 13C NMR, MS(supplement file). Compounds LT-2～17, as novel Xanthone, have been reported for the first time. Their antitumor activities have been investigated by MTT method in cell lines: A549, K562, CNE, KB-3-1, MCF-7 and HepG2. A number of compounds showed potent anti-tumor activity, in some cases even higher (more effective) than Mangostins. Compound 3 with an IC 50 value of 1.73 μM in the A549 cell line, which was two-fold, acted more active than ADM (adriamycin) and α-, γ-Mangostin, and had the most potent anti-tumor activity (IC50=2.15 μM) for the MCF-7 cell line in all synthetic derivatives. α-, γ-Mangostin and ADM showed potent anti-tumor activity (IC50=2.82 μM) for HepG2 cell line, and less potent anti-tumor activity in other cell lines compared with the compound LT-12. It was obtained by esterification of the C-3, C-7 phenolic-OH of the α-Mangostin with acetyl group resulted the potent anti-tumor acvitity, which indicated that the phenolic-OH of the Mangostins had a great impaction on the anti-tumor activity of Mangostins.
