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

在印度传统医学的阿育吠陀系统中，沙拉西亚属已被用作糖尿病初始阶段的特定补救措施。网状、长叶、五味子根、茎甲醇水提物对大鼠具有降糖活性和α-葡萄糖苷酶抑制活性。通过生物测定引导分离，分离出具有独特的硫代糖硫酸钠内盐结构的水杨醇和蛇柳醇。特别是，与α-葡萄糖苷酶抑制剂阿卡波糖相比，salacinol对蔗糖酶和麦芽糖酶的体外抑制活性和对蔗糖和麦芽糖负荷大鼠（体内）血清葡萄糖水平的抑制作用更强。此外，发现网状木参水提物及其多酚类成分芒果苷具有抗肥胖活性。此外，从三叶草茎中分离到7个新的三萜和2个新的倍半萜，发现其三萜组成物具有抑制醛糖还原酶和清除自由基的活性。洋蓟甲醇提取物具有抗高脂血症的活性，并分离出多种倍半萜化合物。为了阐明醛糖还原酶、AGEs形成和自由基清除活性的结构要求，我们对上述筛选试验中各种类黄酮化合物进行了研究，并提出了几种构效关系。

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.