Neri-Gómez Teresa, Espinosa-Raya Judith, Díaz-Cintra Sofía, Segura-Uribe Julia, Orozco-Suárez Sandra, Gallardo Juan Manuel, Guerra-Araiza Christian
Unidad de Investigación Médica en Farmacología, Hospital de Especialidades, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Ciudad de México, México.
Laboratorio de Farmacología Conductual, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón Col. Sto. Tomás, Ciudad de México, México.
Neural Regen Res. 2017 Apr;12(4):588-595. doi: 10.4103/1673-5374.205098.
Aging is a key risk factor for cognitive decline and age-related neurodegenerative disorders. Also, an age-related decrease in sex steroid hormones may have a negative impact on the formation of neurofibrillary tangles (NFTs); these hormones can regulate Tau phosphorylation and the principal kinase GSK3β involved in this process. Hormone replacement therapy decreases NFTs, but it increases the risk of some types of cancer. However, other synthetic hormones such as tibolone (TIB) have been used for hormone replacement therapy. The aim of this work was to evaluate the long-term effects of TIB (0.01 mg/kg and 1 mg/kg, intragastrically for 12 weeks) on the content of total and hyperphosphorylated Tau (PHF-1) proteins and the regulation of GSK3β/Akt/PI3K pathway and CDK5/p35/p25 complexes in the hippocampus of aged male mice. We observed that the content of PHF-1 decreased with TIB administration. In contrast, no changes were observed in the active form of GSK3β or PI3K. TIB decreased the expression of the total and phosphorylated form of Akt while increased that of p110 and p85. The content of CDK5 was differentially modified with TIB: it was increased at low doses and decreased at high doses. When we analyzed the content of CDK5 activators, an increase was found on p35; however, the content of p25 decreased with administration of low dose of TIB. Our results suggest a possible mechanism of action of TIB in the hippocampus of aged male mice. Through the regulation of Tau and GSK3β/Akt/PI3K pathway, and CDK5/p35/p25 complexes, TIB may modulate neuronal plasticity and regulate learning and memory processes.
衰老为认知能力下降及与年龄相关的神经退行性疾病的关键风险因素。此外,与年龄相关的性类固醇激素减少可能对神经原纤维缠结(NFTs)的形成产生负面影响;这些激素可调节Tau蛋白磷酸化以及参与此过程的主要激酶糖原合成酶激酶3β(GSK3β)。激素替代疗法可减少NFTs,但会增加某些类型癌症的风险。然而,其他合成激素如替勃龙(TIB)已被用于激素替代疗法。本研究旨在评估TIB(0.01mg/kg和1mg/kg,灌胃12周)对老年雄性小鼠海马中总Tau蛋白和过度磷酸化Tau蛋白(PHF-1)含量以及GSK3β/Akt/PI3K信号通路和细胞周期蛋白依赖性激酶5/周期蛋白p35/周期蛋白p25复合物调节的长期影响。我们观察到,给予TIB后PHF-1含量降低。相比之下,未观察到GSK3β或PI3K的活性形式有变化。TIB降低了Akt的总表达量和磷酸化形式的表达量,同时增加了p110和p85的表达量。TIB对细胞周期蛋白依赖性激酶5(CDK5)的含量有不同的影响:低剂量时增加,高剂量时减少。当我们分析CDK5激活剂的含量时,发现p35增加;然而,低剂量TIB给药后p25的含量降低。我们的结果提示了TIB在老年雄性小鼠海马中的一种可能作用机制。通过调节Tau和GSK3β/Akt/PI3K信号通路以及CDK5/p35/p25复合物,TIB可能调节神经元可塑性并调控学习和记忆过程。