Synthesis And Biological Activities Of Mangiferin Derivatives

The isolation and modification of natural products have always been important way in finding new drugs. Mangiferin, a xanthone glucoside, is an active phytochemical isolated from Anemarrhenae asphodeloides. Mangiferin has been reported to possess many biological activities. It's anti-diabetes activity is one of the major component of Anemarrhenae asphodeloides to treat diabete.In our previous study, the biological activity of mangiferin aglycon is better than itself in several targets. Several different mangiferins aglycon were synthesized.Based on the combination principles in drug design, substituted-sulfonamide that has anti-diabete activity was introduced to the mangiferin aglycon. Fourty title compounds. were synthesized, 38 compounds were first reported. All intermediates and title compounds were confirmed by means of 1H-NMR, LC-MS and IR.All title compounds were tested for various pharmacological models. Preliminary test show that all compounds has activity on DPP-IV(a target enzyme of diabetes), some substituted-sulfonamide compounds have inhibitory activity against ACAT1/ACAT2 and some benzylized compounds have cytotoxicity against cancer cell. SAR research showed that introducing sulfanilamide pharmacophore to xanthone help to enhance the activity against ACAT1/ACAT2. These results may provide some guidance for the development of novel xanthone lead structures. Currently, further studies along this line are in progress.