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。