Ungurianu Anca, Margină Denisa, Mihai Dragoș P, Nicolae Alina C, Drăgoi Cristina M, Grădinaru Daniela, Zanfirescu Anca
Department of Biochemistry, Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, Bucharest, Romania.
Department of Biochemistry, Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, Bucharest, Romania.
Adv Med Sci. 2025 Mar;70(1):44-50. doi: 10.1016/j.advms.2024.11.002. Epub 2024 Nov 29.
Caloric restriction (CR), the permanent or periodic reduction of caloric intake, is a dietary strategy that promotes longevity and healthspan, yielding multiple beneficial effects, such as improved insulin sensitivity and mitochondrial function, decreased body weight, and mitigation of cardiometabolic risk factors. The purpose of our study was the in silico and in vitro assessment of the effects exerted by pinostilbene on SIRT1 and SIRT6 compared to those of resveratrol, a known activator of these enzymes.
Molecular docking was carried out to determine the interactions with SIRT1 and SIRT6 and, further, the effect of pinostilbene on their activity was tested in vitro to evaluate if it parallels resveratrol's effects regarding SIRT activation.
Molecular docking indicates that resveratrol and pinostilbene bind similarly to SIRT6, while pinostilbene may be able to activate SIRT1 more efficiently than resveratrol. In vitro activity assays showed that while both resveratrol and pinostilbene activate SIRT1 and SIRT6, the concentration-dependent effects differ. For resveratrol, a greater effect was observed at the medium concentration (25 μM), whereas pinostilbene showed a more pronounced activation at the lowest concentration (5 μM).
Our results offer a glimpse into the structural features and interactions of pinostilbene and resveratrol with SIRT1 and SIRT6, contributing to understanding their potential roles in various cellular processes regulated by SIRT.
热量限制（CR），即永久性或周期性减少热量摄入，是一种促进长寿和健康寿命的饮食策略，可产生多种有益效果，如改善胰岛素敏感性和线粒体功能、减轻体重以及降低心脏代谢风险因素。我们研究的目的是通过计算机模拟和体外实验评估与白藜芦醇（已知的这些酶的激活剂）相比，白皮杉醇对SIRT1和SIRT6的影响。
进行分子对接以确定与SIRT1和SIRT6的相互作用，此外，在体外测试白皮杉醇对其活性的影响，以评估它在SIRT激活方面是否与白藜芦醇的作用相似。
分子对接表明白藜芦醇和白皮杉醇与SIRT6的结合方式相似，而白皮杉醇可能比白藜芦醇更有效地激活SIRT1。体外活性测定表明，虽然白藜芦醇和白皮杉醇都能激活SIRT1和SIRT6，但浓度依赖性效应有所不同。对于白藜芦醇，在中等浓度（25μM）时观察到更大的效应，而白皮杉醇在最低浓度（5μM）时显示出更明显的激活作用。
我们的结果让我们初步了解了白皮杉醇和白藜芦醇与SIRT1和SIRT6的结构特征及相互作用，有助于理解它们在由SIRT调节的各种细胞过程中的潜在作用。
