(+)-Pinoresinol is a putative hypoglycemic agent in defatted sesame (Sesamum indicum) seeds though inhibiting α-glucosidase.
(+)-Pinoresinol is a putative hypoglycemic agent in defatted sesame (Sesamum indicum) seeds though inhibiting α-glucosidase.
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DOI：
10.1016/j.bmcl.2012.06.068
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发表时间：
2012-08
影响因子：
2.7
通讯作者：
Arin Wikul;Thanakorn Damsud;K. Kataoka;P. Phuwapraisirisan
中科院分区：
文献类型：
--
作者：
Arin Wikul;Thanakorn Damsud;K. Kataoka;P. Phuwapraisirisan
据报道，脱脂芝麻籽在小鼠和T2 DM女性中具有降血糖作用。尝试使用α-葡糖苷酶引导的分级分离来鉴定负责这种效应的活性组分，从而分离出各种木脂素。在所分离的化合物中，只有（+）-松醇显示出对大鼠肠麦芽糖酶的抑制活性，IC 50值为34.3μM。动力学研究表明，（+）-松脂醇通过竞争性和非竞争性方式抑制麦芽糖的酶促水解。但EI复合物的解离常数（ki 288 M）较低，表明竞争性抑制作用优于非竞争性抑制作用（k′ i1342 M）。
Defatted sesame seeds have been reported for hypoglycemic effect in mice and T2DM women. An attempted to identify active components responsible for this effect was conducted using α-glucosidase-guided fractionation, resulting in the isolation of various lignans. Of compounds isolated, only (+)-pinoresinol showed inhibitory activity against rat intestinal maltase with an IC50value of 34.3μM. The kinetic study indicated that enzymatic hydrolysis of maltose is inhibited by (+)-pinoresinol through competitive and noncompetitive manners. However, a lower dissociation constant (ki288M) of EI complex suggested that competitive inhibition is predominant over noncompetitive mode (k′i1342M).