11β-羟基类固醇脱氢酶1型
11β-羟基类固醇脱氢酶1型(HSD11B1),也称为可的松还原酶,是一种NADPH依赖性酶,在包括肝脏、脂肪组织和中枢神经系统在内的关键代谢组织中高度表达。在这些组织中,HSD11B1将可的松还原为激活糖皮质激素受体的活性激素皮质醇。属于短链脱氢酶家族。
功能
这个基因编码的蛋白质是一种微粒体酶,催化应激激素皮质醇转化为非活性代谢物可的松。此外,编码的蛋白质可以催化相反的反应,即可的松转化为皮质醇。过多的皮质醇会导致中枢性肥胖,这种基因的一个特殊变异与儿童肥胖和胰岛素抵抗有关。在这个基因中发现了两个编码相同蛋白质的转录变体。[6]
临床意义
11β-HSD1被通常用于治疗消化性溃疡的药物卡宾诺酮抑制。此外,从甘草(glycyrrhiza glabra)根中提取的18α-甘草酸被发现是一种抑制剂。[7]
水杨酸盐下调肥胖小鼠脂肪组织中11β-HSD1的表达,从而解释了阿司匹林改善2型糖尿病血糖控制的原因。[8]绿茶中的表没食子儿茶素没食子酸酯也能有效地抑制这种酶;[9]绿茶是多种酚类物质的复杂混合物,其含量随着生产和加工的不同而变化,其中一些酚类物质是已知的改变遗传表达的HDAC抑制剂。绿茶中的EGCG通常很难被血液吸收。需要更多的研究才能得出明确的结论。
参见
- 可的松还原酶缺乏症
- 11β-羟基类固醇脱氢酶2型
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