Glycosylation has been widely used to improve the efficacy and bioavailability of certain anticancer drugs. In the present work, artemisinin glucoside was synthesized through glycosylation, and its antimuor effect was investigated both in vivo and in vitro by detecting its effects on suppressing U14 xenograft tumor proliferation, on inducing Hela cell apoptosis, and on affecting p53, Bcl-2 and Bax expressions. In vivo, the tumor growth behaves as a time- and dosedependent inhibitory effect when treated with artemisinin glucoside, and in vitro the apoptosis of Hela cells is induced by adding up to 40 or even 20 μM artemisinin glucoside. Molecular mechanism and structural basis of artemisinin glucoside interactions with galectin were investigated in detail through molecular docking and structure analysis. All of these findings come together to suggest that artemisinin glucoside exhibits a potent antitumor activity through the activation of cytochrome c pathway and the induction of apoptosis.
Keywords: Artemisinin glucoside, Antitumor, Cell apoptosis, Molecular docking, Artemisia annua, Glycosylation, artemisinin derivatives, chromatography, pleiotropic response, dichloromethane