Abstract：
Gastrodiae Rhizoma was proven to have anti-inflammatory activity based on its main component of 4-hydroxybenzyl alcohol (4-HBA) and gastrodin (GAS). However, the anti-inflammatory activity of other phenols has been less reported. In this study, the n-BuOH extract was selected as the active anti-inflammatory part of Gastrodiae Rhizoma based on the LPS-induced inflammatory BV-2 cells. The spectral-effect relationship analysis of the n-BuOH extract showed the main effective components were GAS, 4-HBA, parishin A (PA), parishin B (PB), and parishin C (PC). Among them, PB could reduce LPS-induced expression of nitric oxide (NO), intracellular ROS, TNF-α, IL-6, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2). Molecular docking predicted that PB had a good binding capacity to AMPKα and SIRT1 proteins of -12.1 kJ/mol and -7.6 kJ/mol, respectively. The Western Blot results further demonstrated that PB could inhibit NF-κB pathway by activating AMPK/SIRT1 pathway, thus exerting anti-LPS-induced neuroinflammatory effects. This study provides a referable idea for solving the problem of unclear action of TCM with complex compositions and is of great significance for the development of innovative medicines of traditional Chinese medicine.
摘要：
天麻被证明具有基于其主要成分4-羟基苯甲醇（4-HBA）和天麻素（GAS）的抗炎活性。然而,其他酚类的抗炎活性报道较少。在这项研究中,基于LPS诱导的炎性BV-2细胞，选择n-BuOH提取物作为天麻的活性抗炎部分。n-BuOH提取物的光谱-效应关系分析表明，主要有效成分为GAS，4-HBA,ParishinA(PA),教区B（PB），和教区C（PC）。其中,PB可以降低LPS诱导的一氧化氮（NO）的表达，细胞内ROS，TNF-α,IL-6，诱导型一氧化氮合酶（iNOS），和环氧合酶-2(COX-2)。分子对接预测PB对AMPKα和SIRT1蛋白的结合能力分别为-12.1kJ/mol和-7.6kJ/mol,分别。WesternBlot结果进一步证明,PB可通过激活AMPK/SIRT1通路抑制NF-κB通路,从而发挥抗LPS诱导的神经炎症作用。本研究为解决中药成分复杂作用不清的问题提供了可借鉴的思路,对中药创新药物的开发具有重要意义。
