Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, PR China; Affiliated Hospital of Guizhou Medical University, Guiyang 550000, PR China.
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, PR China; College of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
J Pharm Biomed Anal. 2022 Feb 5;209:114468. doi: 10.1016/j.jpba.2021.114468. Epub 2021 Nov 11.
In China, Wang Bi Granule (WBG), composed of 16 herbal and 1 animal-based compounds, is used for clinical treatment of the "Wang Bi" syndrome, commonly referred to as later rheumatoid arthritis (RA) in modern medicine. It is also used in the treatment of ankylosing spondylitis, tuberculous arthritis, and Kashin-Beck disease, which are characterized by joint pain and swelling deformation. However, its pharmacological mechanisms remain unknown. We aimed to characterize the chemical components in WBG and examine the underlying mechanism for RA treatment using integrative pharmacological strategy, including chemical composition detection, efficacy evaluation, and mechanism exploration. We employed UPLC-QTOF-MS/MS to describe the chemical profile of WBG. TNF-α-stimulated RAW264.7 cells were used to simulate the inflammatory processes in RA and evaluate the anti-inflammatory effects of WBG. Network pharmacology was used to determine the mechanism underlying WBG action in RA. A total of 278 chemical components were identified or tentatively characterized. The water extract of WBG improved the imbalance in inflammation in TNF-α-stimulated RAW264.7 cells by regulating 179 differential genes. 55 key active constituents were obtained based on the interactions among "components" targets, RA-related genes, and differential genes (WBG vs TNF-α group) which may ameliorate RA by regulating 161 hub genes primarily involved in inflammation-related pathways. The present study, for the first time, employed integrative pharmacology to characterize the chemical profile of WBG and elucidate its mechanism of action against RA through an inflammation-immune regulatory system.
在中国，王氏保赤丸（WBG）由 16 种草药和 1 种动物化合物组成，用于临床治疗“王氏保赤”综合征，现代医学通常称为类风湿关节炎（RA）。它还用于治疗强直性脊柱炎、结核性关节炎和大骨节病，这些疾病的特征是关节疼痛和肿胀变形。然而，其药理机制尚不清楚。我们旨在通过综合药理学策略，包括化学成分检测、功效评估和机制探索，来描述 WBG 的化学成分并研究其治疗 RA 的潜在机制。我们采用 UPLC-QTOF-MS/MS 来描述 WBG 的化学成分。我们采用 TNF-α 刺激的 RAW264.7 细胞来模拟 RA 中的炎症过程，并评估 WBG 的抗炎作用。网络药理学用于确定 WBG 在 RA 中的作用机制。共鉴定或推测出 278 种化学成分。WBG 水提物通过调节 179 个差异基因改善了 TNF-α 刺激的 RAW264.7 细胞中炎症的失衡。基于“成分”靶点、RA 相关基因和差异基因（WBG 与 TNF-α 组）之间的相互作用，获得了 55 个关键活性成分，这些成分可能通过调节主要涉及炎症相关途径的 161 个枢纽基因来改善 RA。本研究首次采用综合药理学方法来描述 WBG 的化学成分，并通过炎症免疫调节系统阐明其治疗 RA 的作用机制。
