Pentobarbital inhibits glucose uptake, but not water transport by glucose transporter type 3
Pentobarbital inhibits glucose uptake, but not water transport by glucose transporter type 3
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戊巴比妥抑制葡萄糖摄取，但不抑制 3 型葡萄糖转运蛋白的水转运
DOI：
10.1097/wnr.0b013e328355d6fc
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发表时间：
2012
期刊：
影响因子：
1.7
通讯作者：
Shigemasa Tomioka
中科院分区：
文献类型：
--
作者：
Shigemasa Tomioka;Tatsumi Nagahama;Reiko Tokuyama,Seiko Tatehara;Kazuhito Satomura;Shigemasa Tomioka
为了了解巴比妥类神经保护功效的机制，在表达 3 型葡萄糖转运蛋白 (GLUT3) 的爪蟾卵母细胞中测定了戊巴比妥对葡萄糖摄取和水转运的影响。戊巴比妥对葡萄糖摄取产生 50% 的浓度依赖性抑制，但对 GLUT3 的水转运没有影响。 Eadie-Hofstee 分析表明，戊巴比妥显着降低了 2-脱氧-D-葡萄糖的 GLUT3 的 V max ，但没有降低 K m 。尽管蛋白激酶 C (PKC) 激活剂显着降低了 GLUT3 的葡萄糖摄取，但在 PKC 激活剂和戊巴比妥之间没有观察到相加或协同相互作用。我们的结果表明，戊巴比妥可能通过涉及 PKC 的机制抑制 GLUT3 的葡萄糖摄取，从而在神经保护中发挥重要作用。
To understand the mechanisms underlying the neuroprotective efficacy of barbiturates, the effect of pentobarbital on glucose uptake and water transport was determined in Xenopus oocytes expressing glucose transporter type 3 (GLUT3). Pentobarbital induced a 50% concentration-dependent inhibition in glucose uptake, but exerted no effect on water transport by GLUT3. Eadie–Hofstee analysis showed that pentobarbital decreased V max significantly, but not K m of GLUT3 for 2-deoxy-D-glucose. Although the protein kinase C (PKC) activator significantly decreased glucose uptake by GLUT3, no additive or synergistic interactions were observed between the PKC activator and pentobarbital. Our results suggest that pentobarbital may play an important role in neuroprotection by inhibition of glucose uptake by GLUT3 by a mechanism involving PKC.