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3-巯基吡啶甲酸和绿原酸衍生物(S-3483)对肝脏和胰岛葡萄糖-6-磷酸酶活性的影响。

Effects of 3-mercaptopicolinic acid and a derivative of chlorogenic acid (S-3483) on hepatic and islet glucose-6-phosphatase activity.

作者信息

Khan A, Ling Z C, Pukk K, Herling A W, Landau B R, Efendic S

机构信息

Department of Molecular Medicine, Endocrine and Diabetes Unit, Karolinska Hospital, Stockholm, Sweden.

出版信息

Eur J Pharmacol. 1998 May 22;349(2-3):325-31. doi: 10.1016/s0014-2999(98)00188-5.

Abstract

Glucose-6-phosphatase activity was measured in hepatic microsomes and in pancreatic islets from ob/ob mice. In hepatic microsomes vanadate, phlorizin, 3-mercaptopicolinic acid and a derivative of chlorogenic acid (S-3483) inhibited the translocase activity of the enzyme, vanadate in addition inhibited hydrolase activity. In islets, vanadate inhibited both components of the enzyme, phlorizin inhibited only hydrolase activity while 3-mercaptopicolinic acid and compound S-3483 were without effect. Similarly, when islets were incubated with 3H2O and unlabeled glucose, the incorporation of 3H into medium glucose was inhibited by vanadate and phlorizin, but not by 3-mercaptopicolinic acid and S-3483. These findings suggest that, as with glucokinase, different isoenzymes of glucose-6-phosphatase are present in islets and liver.

摘要

测定了ob/ob小鼠肝脏微粒体和胰岛中葡萄糖-6-磷酸酶的活性。在肝脏微粒体中,钒酸盐、根皮苷、3-巯基吡啶甲酸和绿原酸衍生物(S-3483)抑制了该酶的转位酶活性,钒酸盐还抑制了水解酶活性。在胰岛中,钒酸盐抑制了该酶的两种成分,根皮苷仅抑制水解酶活性,而3-巯基吡啶甲酸和化合物S-3483则无作用。同样,当胰岛与3H2O和未标记的葡萄糖一起孵育时,钒酸盐和根皮苷抑制了3H掺入培养基葡萄糖中,但3-巯基吡啶甲酸和S-3483则无此作用。这些发现表明,与葡萄糖激酶一样,胰岛和肝脏中存在不同的葡萄糖-6-磷酸酶同工酶。

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