栗精胺在体内可阻断对碳水化合物的高血糖反应：肠道双糖酶抑制的结果。

Castanospermine blocks the hyperglycemic response to carbohydrates in vivo: a result of intestinal disaccharidase inhibition.

作者信息

Rhinehart B L, Robinson K M, Payne A J, Wheatley M E, Fisher J L, Liu P S, Cheng W

机构信息

Merrell Dow Research Institute, Cincinnati, OH 45215.

出版信息

Life Sci. 1987 Nov 16;41(20):2325-31. doi: 10.1016/0024-3205(87)90546-7.

DOI:10.1016/0024-3205(87)90546-7

PMID:3683080

Abstract

Castanospermine is a potent inhibitor of rat intestinal glycohydrolases in vitro and prevents the hyperglycemic response to an oral sucrose challenge in vivo. Among the glycohydrolases tested, castanospermine was most effective against sucrase with an IC50 of 1.1 x 10(-7) M. In vivo, a significant effect was seen at doses less than 1 mg/kg in both normal and streptozotocin-treated rats. Castanospermine has a prolonged duration of activity in vivo with significant activity when administered 4 hours before sucrose.

摘要

栗精胺在体外是大鼠肠道糖水解酶的强效抑制剂，在体内可防止口服蔗糖激发后的高血糖反应。在所测试的糖水解酶中，栗精胺对蔗糖酶的抑制作用最为有效，其半数抑制浓度（IC50）为1.1×10⁻⁷ M。在体内，正常大鼠和经链脲佐菌素处理的大鼠在剂量低于1 mg/kg时均可见显著效果。栗精胺在体内的活性持续时间较长，在蔗糖给药前4小时给药时仍具有显著活性。