Ji Mingyue, Wang Congcong, Yang Tieyi, Meng Xiangxi, Wang Xiaoqin, Li Minhui
Inner Mongolia Key Laboratory of Characteristic Geoherbs Resources Protection and Utilization, Baotou Medical College, Baotou, China.
Trauma Orthopedic, The Second Affiliated Hospital of Inner Mongolia Medical University, Hohhot, China.
Front Pharmacol. 2021 Aug 30;12:707687. doi: 10.3389/fphar.2021.707687. eCollection 2021.
Moench has the effect of clearing away heat, detoxification, dispelling wind, and clearing dampness. In this study, the potential anti-inflammatory compounds of were investigated using ultra-high-performance liquid chromatography-mass spectrometry (UPLC-MS/MS) combined with the network pharmacology approach and further confirmed on an LPS-activated RAW 264.7 macrophage model. Monomer compounds were prepared from the active fraction using modern advanced separation and purification methods. UPLC-Q-Exactive HRMS was used to identify the chemical compounds in the active fractions of . D-mannitol, geniposidic acid, salidroside, shanzhiside methyl ester, eleutheroside B, geniposide, 7,8-dihydroxycoumarin, gardoside methyl ester, arenarioside, vanillic acid, p-hydroxy-cinnamic acid, melampyroside, syringaresinol, tricin, and diosmetin were isolated from for the first time. A compound database of was established based on the existing literature to predict the mechanism of in the treatment of rheumatoid arthritis. The results suggest that the PI3K-Akt pathway mediates and deserves more attention in the treatment of RA. Finally, the anti-rheumatoid arthritis effects of the four target compounds were validated with the decreased levels of NO, TNF-, IL-6 and IL-1 in RAW 264.7 macrophage cells treated with LPS. The present study explored the potential targets and signaling pathways of in the treatment of RA, which may help to illustrate the mechanisms involved in the action of and may provide a better understanding of the relationship between and RA. This study provides novel insights into the development of new drugs and utilization of Mongolian traditional Chinese medicine resources.
地锦草具有清热、解毒、祛风、利湿的功效。在本研究中，采用超高效液相色谱-质谱联用（UPLC-MS/MS）结合网络药理学方法研究了地锦草潜在的抗炎化合物，并在脂多糖激活的RAW 264.7巨噬细胞模型上进一步验证。使用现代先进的分离纯化方法从活性部位制备单体化合物。采用UPLC-Q-Exactive高分辨质谱鉴定地锦草活性部位的化学成分。首次从地锦草中分离出D-甘露醇、京尼平苷酸、红景天苷、山栀苷甲酯、刺五加苷B、栀子苷、7,8-二羟基香豆素、栀子苷甲酯、紫景天苷、香草酸、对羟基肉桂酸、黑麦草内酯、丁香树脂醇、小麦黄素和香叶木素。基于现有文献建立了地锦草化合物数据库，以预测其治疗类风湿性关节炎的作用机制。结果表明，PI3K-Akt信号通路介导了地锦草的作用，在类风湿性关节炎治疗中值得更多关注。最后，通过脂多糖处理的RAW 264.7巨噬细胞中NO、TNF-α、IL-6和IL-1水平的降低，验证了四种目标化合物的抗类风湿性关节炎作用。本研究探索了地锦草治疗类风湿性关节炎的潜在靶点和信号通路，有助于阐明其作用机制，加深对其与类风湿性关节炎关系的理解。本研究为新药开发和蒙药资源利用提供了新的见解。
