强效葡萄糖苷酶抑制剂：脱-O-硫酸基波考那醇及其对映异构体。
Potent glucosidase inhibitors: de-O-sulfonated ponkoranol and its stereoisomer.
机构信息
Department of Chemistry, Simon Fraser University, Burnaby, British Columbia, Canada V5A 1S6.
出版信息
Org Lett. 2010 Apr 2;12(7):1632-5. doi: 10.1021/ol1004005.
Ponkoranol, a glucosidase inhibitor isolated from the plant Salacia reticulata, comprises a sulfonium ion with an internal sulfate counterion. An efficient synthetic route to de-O-sulfonated ponkoranol and its 5'-stereoisomer is reported, and it is shown that these compounds are potent glucosidase inhibitors that inhibit a key intestinal human glucosidase, the N-terminal catalytic domain of maltase glucoamylase, with K(i) values of 43 +/- 3 and 15 +/- 1 nM, respectively.
从藤黄科植物波棱瓜子中分离得到的葡萄糖苷酶抑制剂波棱甲素，其结构包含一个带有内部硫酸根基团的𬭩离子。本文报道了去-O-磺化波棱甲素及其 5'-立体异构体的高效合成路线，并证实这些化合物是强效的葡萄糖苷酶抑制剂，对关键的肠道人源葡萄糖苷酶，即麦芽糖淀粉酶的 N-端催化结构域，其抑制常数（Ki）分别为 43±3 和 15±1 nM。
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