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Identification of key anti-neuroinflammatory components in Gastrodiae Rhizoma based on spectrum-effect relationships and its mechanism exploration
Journal of Pharmaceutical and Biomedical Analysis ( IF 3.1 ) Pub Date : 2024-05-29 , DOI: 10.1016/j.jpba.2024.116266 Tianyu Ma 1 , Panpan Chen 2 , Hongjing Dong 3 , Xiao Wang 4
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.
中文翻译：
基于谱效关系的天麻抗神经炎症关键成分鉴定及其机制探讨
天麻因其主要成分4-羟基苯甲醇（4-HBA）和天麻素（GAS）而被证明具有抗炎活性。然而，其他酚类的抗炎活性报道较少。本研究基于LPS诱导炎症BV-2细胞，选择正丁醇提取物作为天麻的活性抗炎部分。正丁醇提取物的谱效关系分析表明，主要有效成分为GAS、4-HBA、parishin A (PA)、parishin B (PB)、parishin C (PC)。其中，PB可降低LPS诱导的一氧化氮（NO）、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）的表达。分子对接预测PB对AMPKα和SIRT1蛋白具有良好的结合能力，分别为-12.1 kJ/mol和-7.6 kJ/mol。 Western Blot结果进一步证明PB可以通过激活AMPK/SIRT1通路来抑制NF-κB通路，从而发挥抗LPS诱导的神经炎症作用。该研究为解决中药成分复杂、作用不明确的问题提供了参考思路，对中药创新药物的开发具有重要意义。
更新日期：2024-05-29
Journal of Pharmaceutical and Biomedical Analysis ( IF 3.1 ) Pub Date : 2024-05-29 , DOI: 10.1016/j.jpba.2024.116266 Tianyu Ma 1 , Panpan Chen 2 , Hongjing Dong 3 , Xiao Wang 4
Affiliation
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中文翻译：
基于谱效关系的天麻抗神经炎症关键成分鉴定及其机制探讨
天麻因其主要成分4-羟基苯甲醇（4-HBA）和天麻素（GAS）而被证明具有抗炎活性。然而，其他酚类的抗炎活性报道较少。本研究基于LPS诱导炎症BV-2细胞，选择正丁醇提取物作为天麻的活性抗炎部分。正丁醇提取物的谱效关系分析表明，主要有效成分为GAS、4-HBA、parishin A (PA)、parishin B (PB)、parishin C (PC)。其中，PB可降低LPS诱导的一氧化氮（NO）、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）的表达。分子对接预测PB对AMPKα和SIRT1蛋白具有良好的结合能力，分别为-12.1 kJ/mol和-7.6 kJ/mol。 Western Blot结果进一步证明PB可以通过激活AMPK/SIRT1通路来抑制NF-κB通路，从而发挥抗LPS诱导的神经炎症作用。该研究为解决中药成分复杂、作用不明确的问题提供了参考思路，对中药创新药物的开发具有重要意义。
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