School of Pharmacy, Kinki University, 3-4-1 Kowakae, Higashi-osaka, Osaka 577-8502, Japan.
Bioorg Med Chem. 2011 Mar 15;19(6):2015-22. doi: 10.1016/j.bmc.2011.01.052. Epub 2011 Jan 31.
Two hitherto missing members of sulfonium salts family in Salacia genus plants as a new class of α-glucosidase inhibitors, neoponkoranol (7) and neosalaprinol (8), were isolated from the water extracts, and their structures were unambiguously identified. For further SAR studies on this series of sulfonium salts, several epimers of 7 and 8 were synthesized, and their inhibitory activities against rat small intestinal α-glucosidases were evaluated. Among them, 3'-epimer of 7 was found most potent in this class of molecules, and revealed as potent as currently used antidiabetics, voglibose and acarbose.
从 Salacia 属植物的水提取物中分离得到 hitherto 缺失的两个亚砜盐家族成员，作为一类新的α-葡萄糖苷酶抑制剂，neoponkoranol（7）和 neosalaprinol（8），并明确其结构。为了进一步研究该系列亚砜盐的 SAR，合成了 7 和 8 的几个差向异构体，并评估了它们对大鼠小肠α-葡萄糖苷酶的抑制活性。其中，7 的 3'-差向异构体在该类分子中活性最强，与目前使用的抗糖尿病药物 voglibose 和 acarbose 相当。
