From the Center for Pharmacogenetics and Department of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, Pittsburgh, Pennsylvania 15261.
J Biol Chem. 2014 Mar 21;289(12):8086-97. doi: 10.1074/jbc.M113.535914. Epub 2014 Feb 4.
The steroid sulfatase (STS)-mediated desulfation is a critical metabolic mechanism that regulates the chemical and functional homeostasis of endogenous and exogenous molecules. In this report, we first showed that the liver expression of Sts was induced in both the high fat diet (HFD) and ob/ob models of obesity and type 2 diabetes and during the fed to fasting transition. In defining the functional relevance of STS induction in metabolic disease, we showed that overexpression of STS in the liver of transgenic mice alleviated HFD and ob/ob models of obesity and type 2 diabetes, including reduced body weight, improved insulin sensitivity, and decreased hepatic steatosis and inflammation. Interestingly, STS exerted its metabolic benefit through sex-specific mechanisms. In female mice, STS may have increased hepatic estrogen activity by converting biologically inactive estrogen sulfates to active estrogens and consequently improved the metabolic functions, whereas ovariectomy abolished this protective effect. In contrast, the metabolic benefit of STS in males may have been accounted for by the male-specific decrease of inflammation in white adipose tissue and skeletal muscle as well as a pattern of skeletal muscle gene expression that favors energy expenditure. The metabolic benefit in male STS transgenic mice was retained after castration. Treatment with the STS substrate estrone sulfate also improved metabolic functions in both the HFD and ob/ob models. Our results have uncovered a novel function of STS in energy metabolism and type 2 diabetes. Liver-specific STS induction or estrogen/estrogen sulfate delivery may represent a novel approach to manage metabolic syndrome.
甾体硫酸酯酶 (STS) 介导的去硫酸化是一种关键的代谢机制,调节内源性和外源性分子的化学和功能平衡。在本报告中,我们首先表明 STS 在高脂肪饮食 (HFD) 和肥胖症和 2 型糖尿病的 ob/ob 模型以及进食到禁食过渡期间诱导肝脏表达。在定义 STS 诱导在代谢疾病中的功能相关性时,我们表明 STS 在转基因小鼠肝脏中的过表达减轻了 HFD 和肥胖症和 2 型糖尿病的 ob/ob 模型,包括体重减轻、改善胰岛素敏感性以及减少肝脂肪变性和炎症。有趣的是,STS 通过性别特异性机制发挥其代谢益处。在雌性小鼠中,STS 可能通过将生物活性雌激素硫酸酯转化为活性雌激素来增加肝脏中的雌激素活性,从而改善代谢功能,而卵巢切除术则消除了这种保护作用。相比之下,STS 在雄性中的代谢益处可能归因于白色脂肪组织和骨骼肌中炎症的雄性特异性减少,以及有利于能量消耗的骨骼肌基因表达模式。雄性 STS 转基因小鼠的代谢益处在去势后仍保留。用 STS 底物雌酮硫酸酯治疗也改善了 HFD 和 ob/ob 模型的代谢功能。我们的结果揭示了 STS 在能量代谢和 2 型糖尿病中的新功能。肝脏特异性 STS 诱导或雌激素/雌激素硫酸酯的递送可能代表一种治疗代谢综合征的新方法。