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埃默里胺,一种源自新型真菌代谢产物的抗糖尿病β-氨基甜菜碱。

Emeriamine, an antidiabetic beta-aminobetaine derived from a novel fungal metabolite.

作者信息

Kanamaru T, Shinagawa S, Asai M, Okazaki H, Sugiyama Y, Fujita T, Iwatsuka H, Yoneda M

出版信息

Life Sci. 1985 Jul 22;37(3):217-23. doi: 10.1016/0024-3205(85)90647-2.

Abstract

Emeriamine [(R)-3-amino-4-trimethylaminobutyric acid], derived from a novel fungal metabolite "emericedin" [(R)-3-acetylamino-4-trimethylaminobutyric acid], was proved to be a strong and specific inhibitor of carnitine-dependent oxidation of long chain fatty acid (IC50; 3.2 X 10(-6)M) and its main inhibition site was shown to be carnitine palmitoyltransferase I located on the outer-surface of the mitochondrial inner membrane. Emeriamine also showed hypoglycemic and antiketogenic activities in a dose-dependent manner (1 - 10 mg/kg) when administered orally to fasted normal and diabetic animals.

摘要

Emeriamine [(R)-3-氨基-4-三甲基氨基丁酸],源自一种新型真菌代谢产物“emericedin” [(R)-3-乙酰氨基-4-三甲基氨基丁酸],被证明是长链脂肪酸肉碱依赖性氧化的强效特异性抑制剂(IC50;3.2×10^(-6)M),其主要抑制位点为位于线粒体内膜外表面的肉碱棕榈酰转移酶I。当对禁食的正常和糖尿病动物口服给药时,Emeriamine还以剂量依赖性方式(1 - 10 mg/kg)表现出降血糖和抗生酮活性。

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