SEARCH FOR ANTI-OBESE AND ANTIDIABETOGENIC PRINCIPLES FROM THE AYURUVEDIC NATURAL MEDICINES

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The genus Salacia have been used as a specific remedy at the initial stages of diabetes in the Ayuruvedic system of Indian traditional medicine. The aqueous methanolic extract from the roots and stems of S.reticulata, S.oblonga, and S.chinensis were found to show hypoglycaemic activity in rats and α-glucosidase inhibitory activity. By bioassay-guided separation, salacinol and kotalanol, which having the unique thiosugar sulfonium sulfate inner salt structures, were isolated as the active constituents. Particularly, sucrase and maltase inhibitory activities (in vitro) and inhibitory effects on serum glucose levels in sucrose-and maltose-loaded rats (in vivo) of salacinol were more potent than those of commercial medicine as α-glucosidase inhibitor, acarbose. In addition, the water extract of S.reticulata and its polyphenolic constituents indcuding mangiferin found to show anti-obese activity. Furthermore, seven new triterpenes and two new sesquiterpenes were isolated from the stems of S.chinensis and its triterpene constirutens found to show inhibit aldose reductase inhibitory activity and radical scavenging activities.The methanolic extract from artichoke exhibited anti-hyprelipidemic activity and several sesquiterpenes were isolated as the active components.To clarify structural requirements for aldose reductase, AGEs formation, and radical scavenging activities, various flavonoid compounds were examined above-mentioned screening tests and suggested several structure-activity relationships.